General Information of This Antibody
Antibody ID
ANI0INHAA
Antibody Name
Sacituzumab
Organization
Immunomedics, Inc.
Indication
Neoplasms
Synonyms
hRS7
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized IgG1-kappa
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
 Antigen Info 
ChEMBI ID
CHEMBL3707405
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
QVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTY
TDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVS
SASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQS
SGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLG
GPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQY
NSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRE
EMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSR
WQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Heavy Chain Varible Domain
QVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTY
TDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVS
S
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Heavy Chain Constant Domain 1
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRV
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Heavy Chain Constant Domain 2
APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK
PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK
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Heavy Chain Constant Domain 3
GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS
DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Heavy Chain Hinge Region
EPKSCDKTHTCPPCP
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Heavy Chain CDR 1
GYTFTNYG
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Heavy Chain CDR 2
INTYTGEP
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Heavy Chain CDR 3
ARGGFGSSYWYFDV
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Light Chain Sequence
DIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPD
RFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Light Chain Varible Domain
DIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPD
RFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIK
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Light Chain Constant Domain
RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD
SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Light Chain CDR 1
QDVSIA
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Light Chain CDR 2
SAS
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Light Chain CDR 3
QQHYITPLT
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Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
Sacituzumab tirumotecan [Apprpved in 2024]
Identified from the Human Clinical Data
Click To Hide/Show 32 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Patients Enrolled
Adults (18-75) with histologically confirmed metastatic/locally advanced TNBC (HER2 IHC 0/1+ or FISH-negative; ER/PR <1%)
Administration Dosage
5 mg/kg, IV (in the vein) on day 1 and Day 15 of each 28 day cycle.
Related Clinical Trial
NCT Number NCT05347134  Clinical Status PHASE3
Clinical Description
A Randomized, Controlled, Open-label, Multi-center Phase III Clinical Trial of SKB264 for Injection Versus Investigator Selected Regimens in Patients with Unresectable Locally Advanced, Recurrent or Metastatic Triple-negative Breast Cancer Who Have Failed Second-line or Above Prior Standard of Care
Primary Endpoint
Primary endpoint is progression-free survival (PFS) assessed by Independent Review Committee per RECIST 1.1 [Time Frame: up to 24 months].
Other Endpoint
Secondary endpoints include investigator-assessed PFS, objective response rate (ORR), disease control rate (DCR), duration of response (DoR), and overall survival (OS) - all evaluated per RECIST 1.1 with 24-month timeframe.
Experiment 2 Reporting the Activity Date of This ADC [2]
Patients Enrolled
Adults (18-75) with confirmed TNBC/HR+/HER2- BC (no prior systemic chemo for metastatic disease)
Administration Dosage
SKB264 will be administered as an intravenous (IV) infusion every 2 weeks on Day 1 of each 14-day cycle
Related Clinical Trial
NCT Number NCT05445908  Clinical Status PHASE2
Clinical Description
A Phase 2 Clinical Study of SKB264 With/Without KL-A167 in Patients With Unresectable Locally Advanced, Recurrent or Metastatic HER2-negative Breast Cancer Who Have Not Received Prior Systemic Therapy
Primary Endpoint
Primary endpoints: Incidence/severity of AEs (CTCAE v5.0) [Time Frame: Baseline to 30 days post-last dose, up to 24 months]; ORR (CR+PR per RECIST 1.1) [Time Frame: Baseline to first response, up to 24 months].
Other Endpoint
Secondary endpoints: PFS (baseline to PD/death) [24 months]; DOR (first response to PD/death) [24 months]; DCR (CR+PR+SD) [24 months]; PK (Cmax/Cmin of SKB264-ADC, SKB264-TAB, KL610023, KL-A167) [Cycles 1-3,5,7,9,11, q6 cycles from Cycle 17]; ADA for SKB264/KL-A167 [Same as PK].
Experiment 3 Reporting the Activity Date of This ADC [3]
Patients Enrolled
Adults (18-75) with confirmed HR+/HER2- BC
Administration Dosage
IV infusion on day 1 and Day 15 of each 28 day cycle
Related Clinical Trial
NCT Number NCT06081959  Clinical Status PHASE3
Clinical Description
A Randomized, Open-label, Multicenter Phase 3 Study of SKB264 Versus Treatment of Physician's Choice (TPC) in Patients with Unresectable Locally Advanced, Recurrent or Metastatic HR+/HER2- Breast Cancer Who Had Failed At Least One Line of Chemotherapy
Primary Endpoint
Primary endpoint: PFS assessed by BIRC per RECIST 1.1 (time from randomization to PD/death) [Time Frame: up to 24 months].
Other Endpoint
Secondary endpoints: OS (randomization to death) [24 months]; investigator-assessed PFS [24 months]; ORR (CR+PR by BIRC/investigators) [24 months]; DCR (CR+PR+SD) [24 months]; DoR (first response to PD/death) [24 months]; EORTC QLQ-C30 for QoL [2 years]; AE/SAE incidence (CTCAE 5.0) [ICF signing to 30 days post-last dose].
Experiment 4 Reporting the Activity Date of This ADC [4]
Patients Enrolled
Confirmed TNBC (de novo metastatic or relapsed &ge;6 months post-curative therapy); no prior systemic therapy for metastatic disease
Administration Dosage
Participants will receive SKB264 on Day 1 and Day 15 of each 4-week cycle
Related Clinical Trial
NCT Number NCT06279364  Clinical Status PHASE3
Clinical Description
A Randomized, Open-Label, Multicenter Phase 3 Study of SKB264 Versus Investigator's Choice Chemotherapy as First-Line Treatment in Patients With Unresectable Recurrent or Metastatic Triple-Negative Breast Cancer
Primary Endpoint
Primary endpoints: OS (randomization to death) [~40 months]; PFS by BICR (randomization to PD/death per RECIST 1.1) [~28 months].
Other Endpoint
Secondary endpoints: ORR (CR+PR by BICR/investigator) [~28 months]; DoR (first response to PD/death) [~28 months]; investigator-assessed PFS [~28 months]; DCR (CR+PR+SD) [~28 months]; TTR (randomization to first response) [~28 months]; AE/SAE incidence (ICF signing to 30 days post-last dose).
Experiment 5 Reporting the Activity Date of This ADC [5]
Related Clinical Trial
NCT Number NCT06849492  Clinical Status PHASE2
Clinical Description
An Open, Multicenter Study on the Treatment of Recurrent and Metastatic Triple-negative Breast Cancer Guided by Cell Surface Protein Typing (HIM) in Triple-negative Breast Cancer
Experiment 6 Reporting the Activity Date of This ADC [6]
Patients Enrolled
Histologically confirmed cervical cancer (squamous/adenosquamous/adenocarcinoma); recurrent/metastatic disease progressing after 1 prior platinum-based chemo (+/- bevacizumab) with prior anti-PD-1/PD-L1
Administration Dosage
Participants will receive 4 mg/kg of sacituzumab tirumotecan once every 2 weeks (Q2W) via intravenous (IV) infusion until progressive disease or discontinuation.
Related Clinical Trial
NCT Number NCT06459180  Clinical Status PHASE3
Clinical Description
A Phase 3 Randomized, Active-controlled, Open-label, Multicenter Study to Compare the Efficacy and Safety of MK-2870 Monotherapy Versus Treatment of Physician's Choice as Second-line Treatment for Participants With Recurrent or Metastatic Cervical Cancer (TroFuse-020/GOG-3101/ENGOT-cx20)
Primary Endpoint
Sacituzumab Tirumotecan Run-in phase endpoints: ORR (CR+PR per RECIST 1.1 by BICR) [~51 months]; AE incidence [~51 months]; treatment discontinuation due to AEs [~51 months]. Phase 3 primary endpoints: OS (randomization to death) [~43 months]; PFS by BICR (randomization to PD/death per RECIST 1.1) [~43 months].
Other Endpoint
Phase 3 secondary endpoints: ORR (CR+PR by BICR) [~43 months]; DOR (first response to PD/death) [~43 months]; AE incidence [~51 months]; treatment discontinuation due to AEs [~51 months]; EORTC QLQ-C30 outcomes (TTD, score changes in GHS/QoL, physical/role functioning) [~51 months].
Experiment 7 Reporting the Activity Date of This ADC [7]
Patients Enrolled
Unresectable/metastatic colorectal cancer, PDAC or BTC; prior cancer therapy completed with recovery from treatment-related toxicities.
Administration Dosage
Participants will receive sacituzumab tirumotecan in one of two dose levels and chemotherapy by intravenous (IV) infusion, every 2 weeks. Participants will continue to receive the treatment until the cancer gets worse or they don't tolerate treatment.
Related Clinical Trial
NCT Number NCT06428409  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2 Study to Evaluate the Safety and Efficacy of MK-2870 Monotherapy or in Combination With Other Anticancer Agents in Gastrointestinal Cancers
Primary Endpoint
Primary endpoints: DLT incidence (Cycle 1, first 4 weeks); AE incidence [~53 months]; treatment discontinuation due to AEs [~53 months]; ORR by BICR (CR+PR per RECIST 1.1) [~53 months].
Other Endpoint
Secondary endpoints: DOR by BICR (first response to PD/death) [~53 months]; PFS by BICR (treatment start to PD/death) [~53 months]; OS (treatment start to death) [~53 months].
Experiment 8 Reporting the Activity Date of This ADC [8]
Patients Enrolled
Histologically confirmed endometrial carcinoma/carcinosarcoma; measurable disease per RECIST 1.1 (BICR-assessed); prior platinum-based chemo and anti-PD-1/PD-L1 therapy (sequential/combined).
Administration Dosage
Participants will receive 4 mg/kg of sacituzumab tirumotecan via intravenous (IV) infusion on Day 1 of each 14-day cycle.
Related Clinical Trial
NCT Number NCT06132958  Clinical Status PHASE3
Clinical Description
A Phase 3, Randomized, Active-controlled, Open-label, Multicenter Study to Compare the Efficacy and Safety of MK-2870 Monotherapy Versus Treatment of Physician's Choice in Participants With Endometrial Cancer Who Have Received Prior Platinum-based Chemotherapy and Immunotherapy (MK-2870-005/ENGOT-en23/GOG-3095)
Primary Endpoint
Primary endpoints: PFS by BICR per RECIST 1.1 (randomization to progression/death) [~4 years]; OS (randomization to death) [~4 years].
Other Endpoint
Secondary endpoints: ORR by BICR (CR+PR) [~4 years]; DOR (response to progression/death) [~4 years]; AE incidence and treatment discontinuation due to AEs [~4 years]; EORTC QLQ-C30 GHS/QoL score change [baseline to ~4 years].
Experiment 9 Reporting the Activity Date of This ADC [9]
Patients Enrolled
Age 18-75; locally advanced/metastatic epithelial cancers (breast/ovarian/NSCLC/gastric/SCLC/urothelial); measurable disease; refractory to standard therapy; adequate hematologic/organ function
Administration Dosage
Five dose levels have been selected for evaluation in the Phase I part of the study: 2, 4, 6, 9, and 12 mg/kg of SKB264
Related Clinical Trial
NCT Number NCT04152499  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase I-II, First-in-Human Study of SKB264 in Patients With Locally Advanced Unresectable /Metastatic Solid Tumors Who Are Refractory to Available Standard Therapies
Primary Endpoint
Phase I primary: MTD/RDE determination [12 months]; Phase II primary: ORR (CR+PR per RECIST 1.1) [12 months].
Other Endpoint
Phase I secondary: DLTs [28 days]; safety profile (AEs/SAEs ≥Grade 3 per CTCAE v5.0) [treatment+30 days]; preliminary efficacy (ORR/DOR/PFS/OS) [12 months]; ADA formation [6 cycles]; PK parameters (SKB264-ADC/TAB/free payload) [6 cycles]. Phase II secondary: safety profile; efficacy (DOR/PFS/OS) [12 months]; ADA formation; PK parameters; TROP2 expression correlation [screening to EOT].

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Experiment 10 Reporting the Activity Date of This ADC [10]
Patients Enrolled
Histologically confirmed 2L gastric/GEJ/esophageal adenocarcinoma (non-HER2+); metastatic/unresectable disease; progression on 1L platinum/fluoropyrimidine&plusmn;immunotherapy; available tumor tissue; ECOG 0-1; resolved toxicities (&le;Grade 1); life expectancy &ge;3 months; controlled HBV/HCV/HIV permitted.
Administration Dosage
Participants will receive ramucirumab at 8mg/kg via intravenous (IV) infusion on days 1 and 15 of each 4-week cycle for up to ~60 weeks plus paclitaxel at 80 mg/M^2 via IV infusion on Days 1, 8, and 15 of each 4-week cycle (3 weeks on and 1 week off) for up to ~60 weeks.
Related Clinical Trial
NCT Number NCT06445972  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2 Open-Label, Umbrella Platform Design Study to Evaluate the Safety and Efficacy of MK-2870 Plus Paclitaxel as the Second-Line Treatment of Participants With Advanced/Metastatic Gastroesophageal Adenocarcinoma: Substudy 06D
Primary Endpoint
Primary endpoints: DLT incidence (NCI CTCAE v5.0) [~28 days]; AE incidence [~60 days]; treatment discontinuation due to AEs [~28 days]; ORR (CR+PR per RECIST 1.1 by BICR) [~30 months].
Other Endpoint
Secondary endpoints: PFS by BICR (randomization to PD/death) [~52 months]; DOR by BICR (response to PD/death) [~52 months]; OS (randomization to death) [~52 months]; AE incidence and treatment discontinuation during efficacy phase [~52 months]; MK-2870 ADA formation [~52 months].
Experiment 11 Reporting the Activity Date of This ADC [11]
Patients Enrolled
Inclusion: Histologically confirmed untreated 1L unresectable/metastatic gastroesophageal adenocarcinoma (non-HER2+); no prior systemic therapy for metastatic disease; measurable disease per RECIST 1.1; recovered toxicities (<Grade 1); ECOG 0-1; life expectancy &ge;6 months; adequate organ function; controlled HBV/HCV/HIV permitted.
Administration Dosage
Participants will receive pembrolizumab 400 mg via intravenous (IV) injection on day 1 of every 6 week cycle for up to 18 cycles (up to ~2 years)
Related Clinical Trial
NCT Number NCT06469944  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2 Open-Label, Umbrella Platform Design Study of MK-2870 With Pembrolizumab (MK-3475) and Chemotherapy in Participants With 1L Locally Advanced Unresectable/Metastatic Gastroesophageal Adenocarcinoma (Gastric Adenocarcinoma, Gastroesophageal Junction Adenocarcinoma, and Esophageal Adenocarcinoma): Substudy 06C
Primary Endpoint
Primary endpoints: DLT incidence (NCI CTCAE v5.0) [~28 days]; AE incidence and treatment discontinuation due to AEs [~28 days]; ORR (CR+PR per RECIST 1.1 by BICR) [~28 months].
Other Endpoint
Secondary endpoints: PFS by BICR (randomization to PD/death) [~55 months]; DOR by BICR (response to PD/death) [~55 months]; OS (randomization to death) [~55 months]; AE incidence and treatment discontinuation [~55 months]; ADA formation against sac-TMT (MK-2870) [up to Cycle 5].
Experiment 12 Reporting the Activity Date of This ADC [12]
Patients Enrolled
Inclusion: Histologically confirmed metastatic/unresectable ESCC; progressed on prior platinum+anti-PD1/PD-L1 therapy; evaluable tumor sample; controlled BP; recovered toxicities (&le;Grade 1, &le;Grade 2 neuropathy permitted); endocrine AEs with stable hormone replacement eligible.
Administration Dosage
Participants receive paclitaxel 80-100 mg/m^2 intravenously (IV) on days 1, 8, and 15 every 28-day cycle until progressive disease (PD) or discontinuation
Related Clinical Trial
NCT Number NCT05319730  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2 Open-Label, Umbrella Platform Design Study of Investigational Agents With or Without Pembrolizumab (MK-3475) and/or Chemotherapy in Participants With Advanced Esophageal Cancer Previously Exposed to PD-1/PD-L1 Treatment (KEYMAKER-U06): Substudy 06B
Primary Endpoint
Primary endpoints: DLT incidence (NCI CTCAE v5.0) [~3 weeks]; AE incidence and treatment discontinuation due to AEs [~3 weeks]; ORR (CR+PR per RECIST 1.1 by BICR) [~92 weeks].
Other Endpoint
Secondary endpoints: PFS by BICR (allocation to PD/death) [~189 weeks]; DOR by BICR (response to PD/death) [~189 weeks]; OS (allocation to death) [~189 weeks]; AE incidence and treatment discontinuation during efficacy phase [~189 weeks].
Experiment 13 Reporting the Activity Date of This ADC [13]
Patients Enrolled
Histologically confirmed advanced/metastatic gastric/GEJ/esophageal adenocarcinoma; measurable disease per RECIST 1.1; progressed on &ge;2 prior regimens; HER2 status-independent (HER2+ must have prior trastuzumab); adequate organ function; tumor tissue for TROP2 assessment; recovered toxicities (&le;Grade 1); ECOG 0-1; controlled HIV/HBV/HCV permitted; oral medication ability.

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Administration Dosage
Participants will receive sacituzumab tirumotecan at a dose of 4mg/kg by intravenous (IV) infusion on days 1, 15, and 29 of every 42-day cycle.
Related Clinical Trial
NCT Number NCT06356311  Clinical Status PHASE3
Clinical Description
A Phase 3, Multicenter, Open-label, Randomized Study to Compare the Efficacy and Safety of MK-2870 Versus Treatment of Physician's Choice in 3L+ Advanced/Metastatic Gastroesophageal Adenocarcinoma (Gastric Adenocarcinoma, Gastroesophageal Junction Adenocarcinoma, and Esophageal Adenocarcinoma)
Primary Endpoint
OS (randomization to death) [~31 months].
Other Endpoint
PFS by BICR per RECIST 1.1 (randomization to PD/death) [~25 months]; ORR (CR+PR) by BICR [~25 months]; DOR by BICR (response to PD/death) [~48 months]; AE incidence and treatment discontinuation due to AEs [~48 months].
Experiment 14 Reporting the Activity Date of This ADC [14]
Patients Enrolled
Eligible participants had histologically confirmed advanced/metastatic non-squamous NSCLC with specific mutations, RECIST 1.1 progression after prior therapy (EGFR TKI + platinum-based therapy for mutated cases), measurable disease, and available tumor tissue. Required criteria: recovery from prior therapy AEs (Grade &le;1), controlled HBV/HIV if applicable, and ECOG performance status 0-1 within 3 days pre-randomization.

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Administration Dosage
Participants will receive 4 mg/kg of sacituzumab tirumotecan via intravenous (IV) infusion on Days 1, 15 and 29 of each 6-week cycle.
Related Clinical Trial
NCT Number NCT06074588  Clinical Status PHASE3
Clinical Description
A Randomized, Open-label, Phase 3 Study of MK-2870 vs Chemotherapy (Docetaxel or Pemetrexed) in Previously Treated Advanced or Metastatic Nonsquamous Non-small Cell Lung Cancer (NSCLC) With EGFR Mutations or Other Genomic Alterations
Primary Endpoint
Progression-free Survival (PFS) in NSCLC patients with EGFR mutations was assessed up to 35 months, defined as time from randomization to first disease progression per RECIST 1.1 (BICR) or death. Overall Survival (OS) in this cohort was measured up to 41 months as time from randomization to death. For all NSCLC participants, PFS (up to 35 months) and OS (up to 41 months) were similarly defined. Objective Response Rate (ORR) in EGFR-mutated NSCLC (up to 35 months) and all NSCLC participants (up to 35 months) was the percentage achieving Complete Response (CR: disappearance of target lesions) or Partial Response (PR: ≥30% decrease in target lesion diameters) per RECIST 1.1 (BICR). Duration of Response (DOR) in all NSCLC participants (up to 6 years) was time from first CR/PR to progression/death.

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Other Endpoint
Quality of Life metrics included changes from baseline in EORTC QLQ-C30 scores (Global Health Status/QoL [Items 29-30], Dyspnea [Item 8]) and QLQ-LC13 scores (Cough [Item 31], Chest Pain [Item 40]) up to 48 weeks, with higher scores indicating better QoL for Global Health but worse symptoms for others. Time to Deterioration (TTD) was defined as first ≥10-point score decline (confirmed by subsequent ≥10-point drop) in Global Health Status/QoL, Dyspnea, Cough, and Chest Pain scores up to 48 weeks. Safety outcomes included number of participants with ≥1 Adverse Event (AE) (up to 6 years) and treatment discontinuations due to AEs (up to 4 years).

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Experiment 15 Reporting the Activity Date of This ADC [15]
Patients Enrolled
Inclusion criteria: Histologically/cytologically confirmed NSCLC (squamous/nonsquamous) without EGFR/ALK/ROS1 targets, PD-L1 &ge;50% (central IHC), ECOG 0-1, life expectancy &ge;3 months, and controlled HIV on ART if applicable.
Administration Dosage
Participants receive sacituzumab tirumotecan via intravenous (IV) infusion on Days 1, 15 and 29 of each 6-week cycle + 400 mg Pembrolizumab every 6 weeks (q6w) via IV infusion on Day 1 of each 6-week cycle for 18 cycles.
Related Clinical Trial
NCT Number NCT06170788  Clinical Status PHASE3
Clinical Description
A Randomized, Open-label, Phase 3 Study of MK-2870 in Combination With Pembrolizumab Compared to Pembrolizumab Monotherapy in the First-line Treatment of Participants With Metastatic Non-small Cell Lung Cancer With PD-L1 TPS Greater Than or Equal to 50% (TroFuse-007)
Primary Endpoint
Overall Survival (OS) was defined as time from randomization to death from any cause (up to 48 months).
Other Endpoint
Progression-free survival (PFS) was defined as time from randomization to first documented disease progression per RECIST 1.1 (BICR) or death (up to 48 months). Objective Response (OR) required confirmed CR/PR per RECIST 1.1 (BICR), with Duration of Response (DOR) measuring time from first CR/PR to progression/death. Quality of Life assessments included EORTC QLQ-C30 (Items 29/30: 7-point scale for GHS/QOL; Item 8: 4-point dyspnea scale) and QLQ-LC13 (Items 31/40: 4-point scales for cough/chest pain), with Time to Deterioration (TTD) analyzed for each (baseline to 24 months). Safety outcomes covered AE rates (27 months) and treatment discontinuations due to AEs (24 months).

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Experiment 16 Reporting the Activity Date of This ADC [16]
Patients Enrolled
Inclusion criteria: Histologically/cytologically confirmed advanced nonsquamous NSCLC; recovered from prior treatment AEs (Grade <1); controlled HBV/HCV/HIV if applicable; life expectancy &ge;3 months.
Administration Dosage
Participants receive 4 mg/kg sacituzumab tirumotecan via intravenous (IV) infusion every 2 weeks (Days 1, 15, and 29 of every 6-week cycle) until discontinuation criteria is met.
Related Clinical Trial
NCT Number NCT06305754  Clinical Status PHASE3
Clinical Description
A Randomized, Open-label, Phase 3 Study of MK-2870 vs. Platinum Doublets in Participants With EGFR-mutated, Advanced Nonsquamous Non-small Cell Lung Cancer (NSCLC) Who Have Progressed on Prior EGFR Tyrosine Kinase Inhibitors
Primary Endpoint
Progression-Free Survival (PFS) was defined as time from randomization to first documented disease progression per RECIST 1.1 (BICR) or death (up to 51 months). Overall Survival (OS) was defined as time from randomization to death from any cause (up to 51 months). Both PFS and OS will be reported for all randomized participants.
Other Endpoint
Objective Response Rate (ORR) required confirmed CR (disappearance of all target lesions) or PR (≥30% decrease in sum of target lesion diameters) per RECIST 1.1 (BICR). Duration of Response (DOR) measured time from first CR/PR to progression/death. Quality of Life assessments included EORTC QLQ-C30 (Items 29/30: 7-point GHS/QOL scale; Item 8: 4-point dyspnea scale) and QLQ-LC13 (Items 31/40: 4-point scales for cough/chest pain), with Time to Deterioration (TTD) defined as ≥10-point score decrease (baseline to 6 years). Safety outcomes covered AE incidence and treatment discontinuations (up to 6 years).

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Experiment 17 Reporting the Activity Date of This ADC [17]
Patients Enrolled
Histologically/cytologically confirmed resectable Stage II-IIIB (N2) NSCLC; eligible for neoadjuvant pembrolizumab+chemotherapy and surgery; post-surgery without pCR; disease-free on imaging; recovered AEs (Grade&le;1); controlled HIV/HBV/HCV if applicable. Required tumor tissue for central PD-L1/TROP2 testing.
Administration Dosage
Participants will receive pembrolizumab 200 mg intravenous (IV) infusion every 3 weeks (Q3W) for up to 12 weeks + double-platinum chemotherapy per neoplasm histology classification at the investigator's discretion as neoadjuvant therapy prior to surgery; followed by sacituzumab tirumotecan 4 mg/kg IV infusion every 2 weeks (Q2W) for up to 12 doses (~24 weeks) with pembrolizumab monotherapy 200 mg IV infusion every 6 weeks (Q6W) for up to 7 cycles (~42 weeks).

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Related Clinical Trial
NCT Number NCT06312137  Clinical Status PHASE3
Clinical Description
A Phase 3 Randomized Open-Label Study of Adjuvant Pembrolizumab With or Without MK-2870 in Participants With Resectable Stage II to IIIB (N2) NSCLC Not Achieving pCR After Receiving Neoadjuvant Pembrolizumab With Platinum-based Doublet Chemotherapy Followed by Surgery
Primary Endpoint
Disease-Free Survival (DFS) was assessed by Blinded Independent Central Review (BICR) as time from randomization to any recurrence (local/locoregional/regional/distant), new primary NSCLC, or death (up to 93 months).
Other Endpoint
Overall Survival (OS) measured time to death (up to 118 months). Secondary endpoints included Distant Metastasis-Free Survival (DMFS; time to first distant metastasis/death), investigator-assessed DFS, and Lung Cancer-Specific Survival (LCSS). Safety outcomes covered AE incidence and treatment discontinuations. Quality of Life was evaluated via EORTC QLQ-C30 (GHS/QoL, physical/role functioning, dyspnea) and QLQ-LC24 (cough, chest pain) scales (0-100; higher scores indicate better function except symptom scales).

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Experiment 18 Reporting the Activity Date of This ADC [18]
Patients Enrolled
Eligible participants must have previously untreated, resectable Stage II-IIIB (N2) NSCLC confirmed as EGFR wild-type, demonstrate ECOG performance status 0-1, provide tumor tissue samples, and meet criteria for both neoadjuvant therapy and subsequent surgical intervention.
Related Clinical Trial
NCT Number NCT06788912  Clinical Status PHASE2
Clinical Description
KEYMAKER-U01 Substudy 01E: A Phase 2 Umbrella Study With Rolling Arms of Investigational Agents With or Without Chemotherapy in Combination With Pembrolizumab in Treatment of Participants With Newly Diagnosed Resectable Stages II-IIIB (N2) Non-small Cell Lung Cancer (NSCLC)
Primary Endpoint
The primary endpoints focus on pathological response, including Pathological Complete Response (pCR) defined as no residual viable tumor in resected specimens and Percent Residual Viable Tumor (%RVT) quantifying remaining tumor cells in the tumor bed, both evaluated within approximately 20 weeks after neoadjuvant therapy.
Other Endpoint
Secondary endpoints encompass safety outcomes (adverse event incidence over 5 years, treatment discontinuations within 1 year, and perioperative complications within 20 weeks), efficacy measures (event-free survival, overall survival, and distant metastasis-free survival over 5 years, plus objective response rate at 12 weeks), and surgical parameters (hospitalization duration, readmission rates, operative time, and transfusion requirements within 20 weeks).

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Experiment 19 Reporting the Activity Date of This ADC [19]
Patients Enrolled
Eligible participants must be aged 18-75 with histologically confirmed NSCLC, stratified into three cohorts: Cohort 1 (EGFR/ALK wild-type, &le;1 prior chemotherapy line), Cohort 2 (EGFR/ALK wild-type, treatment-na&iuml;ve), and Cohort 3 (EGFR-mutant, EGFR-TKI failures). Additional criteria include provision of tumor tissue for biomarker analysis, &ge;1 measurable lesion (excluding skin/bone-only disease), ECOG 0-1, life expectancy &ge;12 weeks, adequate organ function, and agreement to use contraception during and for 6 months post-treatment. All patients must provide informed consent and comply with protocol requirements.

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Administration Dosage
SKB264 will be administered as an intravenous (IV) infusion every 3 weeks on Day 1 of each 21-day cycle (5mg/kg)
Related Clinical Trial
NCT Number NCT05351788  Clinical Status PHASE2
Clinical Description
A Phase II Clinical Study of Combination Therapy of SKB264 in Patients With Advanced or Metastatic Non-small Cell Lung Cancer
Primary Endpoint
The primary endpoints include safety evaluation through incidence and severity of adverse events (AEs) graded by CTCAE v5.0, assessed from baseline up to 30 days after the last dose or until initiation of new anti-cancer therapy (up to 24 months), as well as efficacy measured by Objective Response Rate (ORR), defined as the percentage of participants achieving Complete Response (CR) or Partial Response (PR) per RECIST v1.1 criteria, evaluated from baseline to the first documented response (up to 24 months).

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Other Endpoint
Secondary endpoints comprise Progression-Free Survival (PFS), defined as time from baseline to disease progression or death (up to 24 months); Duration of Response (DOR), measuring time from first response to progression or death in responders only (up to 24 months); Disease Control Rate (DCR), combining CR, PR, and Stable Disease (SD) rates per RECIST v1.1 (up to 24 months); pharmacokinetic parameters (Cmax and Cmin) for SKB264-ADC, SKB264-TAB, free KL610023, and KL-A167, assessed during Cycles 1-8 and every 4 cycles thereafter (up to 24 months); and Anti-Drug Antibodies (ADA) for SKB264 and KL-A167, evaluated similarly.

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Experiment 20 Reporting the Activity Date of This ADC [20]
Patients Enrolled
Eligible subjects must be &ge;18 years with histologically confirmed locally advanced/metastatic NSCLC, either EGFR wild-type/ALK-negative (treatment-na&iuml;ve or with &le;1 prior therapy) or EGFR-mutant (TKI-na&iuml;ve or TKI-resistant), able to provide tumor samples, have &ge;1 measurable lesion per RECIST v1.1, ECOG 0-1, &ge;3-month life expectancy, adequate organ function, recovery from prior treatment toxicities, compliance with contraceptive requirements, and willingness to sign informed consent and adhere to protocol procedures.

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Administration Dosage
intravenous (IV) infusion (Q2W or Q3W)
Related Clinical Trial
NCT Number NCT05816252  Clinical Status PHASE2
Clinical Description
A Phase II Study of SKB264 as Monotherapy or as Combination Therapy in Subjects With Advanced or Metastatic Non-small Cell Lung Cancer
Primary Endpoint
The study evaluates safety and tolerability through dose-limiting toxicity (DLT), incidence/severity of adverse events (AEs), and treatment discontinuation due to AEs, assessed from informed consent until 30 days post-treatment (up to 36 months), while efficacy is measured by objective response rate (ORR) per RECIST v1.1, defined as the proportion of subjects achieving complete (CR) or partial response (PR) during the study period (up to 36 months).

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Other Endpoint
Key secondary endpoints include duration of response (DOR) for responders (time from first CR/PR to progression/death), progression-free survival (PFS) (time from treatment initiation to progression/death), and overall survival (OS) (time from treatment start to death from any cause), all evaluated over approximately 36 months using radiographic assessments and clinical follow-up.

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Experiment 21 Reporting the Activity Date of This ADC [21]
Patients Enrolled
Eligible participants must be 18-75 years old with histologically confirmed stage IIIB/IIIC/IV non-squamous NSCLC harboring EGFR-sensitive mutations after EGFR-TKI failure, have &ge;1 measurable lesion per RECIST 1.1, ECOG 0-1, &ge;12-week life expectancy, adequate organ function, use effective contraception, and voluntarily comply with study procedures through signed informed consent.

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Administration Dosage
SKB264 by IV infusion on Days 1 and 15 of each 4-week cycle;
Related Clinical Trial
NCT Number NCT05870319  Clinical Status PHASE3
Clinical Description
A Randomized, Open-Label, Multicenter Phase 3 Study to Evaluate SKB264 Monotherapy Versus Pemetrexed in Combination with Platinum in Patients with Locally Advanced or Metastatic Non-squamous Non-small Cell Lung Cancer with EGFR Mutation Who Have Failed to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor (EGFR-TKI) Therapy
Primary Endpoint
The study evaluates efficacy through progression-free survival (PFS) assessed by both blinded independent review committee (BIRC) and investigators per RECIST 1.1, measured from baseline until disease progression or death (up to 36 months), along with overall survival (OS) from randomization to death (up to 2 years), objective response rate (ORR), disease control rate (DCR), duration of response (DOR), and time to response (TTR) - all assessed by investigators and BIRC per RECIST 1.1 within 2 years.

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Other Endpoint
Safety assessments include incidence/severity of adverse events (AEs) and serious adverse events (SAEs) per CTCAE 5.0 from informed consent until 30 days post-treatment, while quality of life is measured through changes in EORTC QLQ-C30 and QLQ-LC13 questionnaires over 2 years to evaluate disease-related symptoms and health-related quality of life impact.

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Experiment 22 Reporting the Activity Date of This ADC [22]
Patients Enrolled
Eligible patients must have untreated, PD-L1 TPS &ge;1% stage IIIB/IIIC/IV NSCLC ineligible for radical therapy, &ge;1 measurable lesion per RECIST 1.1, ECOG 0-1 performance status, &ge;12-week life expectancy, and adequate organ function.
Administration Dosage
Participants will receive SKB264 on Day 1, Day 15 and Day 29 of each 6-week cycle,Pembrolizumab on Day1 of each 6-week cycle.
Related Clinical Trial
NCT Number NCT06448312  Clinical Status PHASE3
Clinical Description
A Randomized, Open-Label, Multicenter Phase III Clinical Study of SKB264 in Combination With Pembrolizumab Versus Pembrolizumab as First-Line Treatment for PD-L1 Positive Patients With Locally Advanced or Metastatic Non-Small Cell Lung Cancer
Primary Endpoint
The primary efficacy endpoint is Progression-Free Survival (PFS) assessed by Blinded Independent Central Review (BICR) per RECIST 1.1, measuring time from randomization to first documented disease progression or death (up to 22 months).
Other Endpoint
Secondary endpoints include Overall Survival (OS) from randomization to death (up to 40 months), investigator-assessed PFS (up to 22 months), Objective Response Rate (ORR), Disease Control Rate (DCR), Duration of Response (DoR), and Time to Response (TTR) - all evaluated by both BICR and investigators per RECIST 1.1 within 22 months.
Experiment 23 Reporting the Activity Date of This ADC [23]
Patients Enrolled
Eligible participants must be aged 18-75 with histologically confirmed treatment-na&iuml;ve stage IIIB-IV non-squamous NSCLC harboring EGFR-sensitive mutations, have &ge;1 measurable lesion per RECIST v1.1, ECOG PS 0-1, &ge;12-week life expectancy, available tumor samples, and adequate organ function, ensuring a well-defined patient population for this clinical investigation.

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Administration Dosage
Participants will receive SKB264 on Day 1 and Day 15 of each 4-week cycle, Osimertinib once-daily for each 4-week cycle.
Related Clinical Trial
NCT Number NCT06670196  Clinical Status PHASE3
Clinical Description
A Randomized, Open-Label, Multicenter, Phase III Clinical Study of SKB264 in Combination with Osimertinib Versus Osimertinib Alone As First-Line Treatment for Patients with Epidermal Growth Factor Receptor (EGFR) Mutations, Locally Advanced or Metastatic Non-Squamous Non-Small Cell Lung Cancer
Primary Endpoint
The primary efficacy endpoint is progression-free survival (PFS) assessed by blinded independent central review (BICR) per RECIST 1.1 criteria, measuring time from randomization to first documented disease progression or death from any cause, with evaluation continuing for approximately 36 months.
Other Endpoint
Secondary endpoints include overall survival (OS) assessed up to 49 months, investigator-evaluated PFS (36 months), objective response rate (ORR), disease control rate (DCR), duration of response (DoR), and time to response (TTR) - all measured by both BICR and investigators per RECIST 1.1 standards over 36 months, providing comprehensive efficacy evaluation across multiple dimensions.

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Experiment 24 Reporting the Activity Date of This ADC [24]
Patients Enrolled
Eligible patients (18-75 years) must have histologically confirmed NSCLC (with specific EGFR/ALK status requirements per cohort) or nasopharyngeal carcinoma, disease progression after prior therapies (including EGFR-TKIs, platinum chemotherapy, or PD-1/L1 inhibitors where applicable), &ge;1 measurable lesion, ECOG 0-1, &ge;12-week life expectancy, adequate organ function, and willingness to provide tumor tissue samples and comply with contraceptive requirements during and for 6 months post-treatment.

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Administration Dosage
SKB264 will be administered as an intravenous (IV) infusion on Day 1 and Day 15 of each 28-day cycle
Related Clinical Trial
NCT Number NCT05631262  Clinical Status PHASE2
Clinical Description
A Multicenter, Open-label, Phase 2 Study to Evaluate the Efficacy and Safety of SKB264 Monotherapy in Selected Subjects with Advanced Solid Tumors
Primary Endpoint
The primary efficacy endpoint is objective response rate (ORR), defined as the proportion of patients achieving complete response (CR) or partial response (PR) per RECIST 1.1 criteria, assessed from baseline until disease progression or death (up to 21 months). Safety will be evaluated through incidence and severity of adverse events (graded by CTCAE v5.0) monitored from informed consent through 30 days post-treatment.

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Other Endpoint
Secondary endpoints include progression-free survival (PFS), duration of response (DOR), and disease control rate (DCR) - all assessed per RECIST 1.1 over 21 months - along with overall survival (OS) until death. Pharmacokinetic parameters (Cmax/Cmin of SKB264-ADC, SKB264-TAB and free KL610023) and immunogenicity (anti-drug antibodies) will be evaluated for 12 months post-enrollment to characterize drug exposure and potential immune responses.

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Experiment 25 Reporting the Activity Date of This ADC [25]
Patients Enrolled
Eligible participants must have ECOG performance status 0-1, &ge;3 month life expectancy, and measurable disease per RECIST 1.1 across five cancer cohorts: recurrent/metastatic cervical cancer (Cohort A), advanced urothelial carcinoma (Cohort B), recurrent ovarian cancer (Cohort C), metastatic prostate cancer (Cohort D), and advanced endometrial cancer (Cohort E). Additional requirements include providing tumor samples for biomarker analysis, adequate organ function, recovery from prior treatment toxicities (excluding non-safety concerns), compliance with contraception guidelines, and ability to provide informed consent.

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Administration Dosage
be administrated as an intravenous (IV) infusion on Day 1,15, 29 of each 42-day cycle;
Related Clinical Trial
NCT Number NCT05642780  Clinical Status PHASE2
Clinical Description
A Multicenter, Open-label, Phase 2, Basket Study to Evaluate the Efficacy and Safety of SKB264 in Combination With Pembrolizumab in Subjects With Selected Solid Tumors
Primary Endpoint
The study evaluates safety through dose-limiting toxicities (DLTs) and adverse events (AEs) graded by CTCAE v5.0 from informed consent through 30 days post-treatment, while efficacy is assessed via objective response rate (ORR) per RECIST 1.1 (confirmed CR/PR) and, for prostate cancer patients (Cohort D), PSA response rate (≥50% decrease confirmed ≥3 weeks apart), both measured from baseline until progression/death (up to 21 months).

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Experiment 26 Reporting the Activity Date of This ADC [26]
Patients Enrolled
Eligible participants must have histologically confirmed locally advanced/metastatic urothelial carcinoma (la/mUC) with evaluable tumor tissue. Part 1 requires prior platinum chemotherapy (&le;2 lines; avelumab maintenance counts as one line), while Part 2 excludes prior systemic therapy for la/mUC. All subjects must have recovered from prior treatment toxicities (&le;Grade 1) and meet standard organ function requirements.

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Administration Dosage
Participants will receive sacituzumab tirumotecan as an intravenous (IV) infusion and EV as an IV infusion on Days 1 and 8 of every 3-week cycle until disease progression, intolerable toxicity, or investigator decision.
Related Clinical Trial
NCT Number NCT06483334  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2 Randomized, Umbrella Study to Evaluate the Efficacy and Safety of MK-2870 Plus Enfortumab Vedotin (EV) With and Without Pembrolizumab, as Treatment for Participants With Advanced Urothelial Carcinoma (KEYMAKER-U04): Substudy 04C
Primary Endpoint
The study evaluates safety through dose-limiting toxicities (DLTs) and adverse events (AEs) graded by CTCAE v5.0 in both Part 1 (up to 3 years) and Part 2 (up to 2 years), including treatment discontinuations due to AEs. Efficacy is assessed via objective response rate (ORR) per RECIST 1.1 (confirmed CR/PR) in Part 2 (up to 3 years), with DLTs specifically monitored during the first 21 days of each part.

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Other Endpoint
Secondary endpoints include pharmacokinetic parameters (Cmax/Ctrough of sacituzumab tirumotecan-ADC, free payload, enfortumab vedotin-ADC, and pembrolizumab-ADC) measured through serial blood sampling across treatment cycles (up to Cycle 35), along with immunogenicity (antidrug antibody incidence) for all study drugs. Part 1 additionally evaluates ORR, while Part 2 assesses duration of response (DOR) from first CR/PR to progression/death per RECIST 1.1.

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Experiment 27 Reporting the Activity Date of This ADC [27]
Patients Enrolled
Eligible participants must have recurrent low-grade Ta NMIBC with visible tumors on recent cystoscopy, meeting intermediate-risk criteria (multiple/recurrent tumors >3cm or treatment failure), with ECOG 0-2 performance status confirmed within 14 days prior to treatment initiation.
Administration Dosage
Participants receive intravesical Sacituzumab Tirumotecan for 6 weeks
Related Clinical Trial
NCT Number NCT06637423  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2 Open-label Clinical Study to Evaluate the Safety and Efficacy of Intravesical Sacituzumab Tirumotecan (Sac-TMT, MK-2870) in Participants With Intermediate-risk Nonmuscle Invasive Bladder Cancer (NMIBC)
Primary Endpoint
The study evaluates safety through dose-limiting toxicities (DLTs) during the first 7 weeks using NCI CTCAE v5.0 criteria, while monitoring all adverse events (AEs) - defined as any unfavorable medical occurrence temporally associated with treatment - for up to 10 weeks, including treatment discontinuations due to AEs within approximately 6 weeks.
Other Endpoint
Pharmacokinetic analysis of sacituzumab tirumotecan (sac-TMT) includes serum/plasma measurements (AUC, Cmax, Cmin, half-life) for both ADC and free payload over 6 weeks, with efficacy endpoints assessing complete response rate (CRR) by cystoscopy/cytology within 6 months and duration of response (DCR) tracking recurrence-free survival up to 24 months.

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Experiment 28 Reporting the Activity Date of This ADC [37]
Related Clinical Trial
NCT Number NCT05347134  Clinical Status Phase 3
Clinical Description
A randomized, controlled, open-label, multi-center phase 3 clinical trial of SKB264 for injection versus investigator selected regimens in patients with unresectable locally advanced, recurrent or metastatic triple-negative breast cancer who have failed second-line or above prior standard of care.
Experiment 29 Reporting the Activity Date of This ADC [38]
Related Clinical Trial
NCT Number NCT05642780  Clinical Status Phase 2
Clinical Description
Amulticenter, open-label, phase 2, basket study to evaluate the efficacy and safety of SKB264 in combination with pembrolizumab in subjects with selected solid tumors.
Experiment 30 Reporting the Activity Date of This ADC [39]
Related Clinical Trial
NCT Number NCT05351788  Clinical Status Phase 2
Clinical Description
A phase 2 clinical study of combination therapy of SKB264 in patients with advanced or metastatic non-small cell lung cancer.
Experiment 31 Reporting the Activity Date of This ADC [40]
Related Clinical Trial
NCT Number NCT05445908  Clinical Status Phase 2
Clinical Description
A phase 2 clinical study of SKB264 with/without KL-A167 in patients with unresectable locally advanced, recurrent or metastatic triple-negative breast cancer (TNBC) who have not received prior systemic therapy.
Experiment 32 Reporting the Activity Date of This ADC [41]
Related Clinical Trial
NCT Number NCT05631262  Clinical Status Phase 2
Clinical Description
A multicenter, open-label, phase 2 study to evaluate the efficacy and safety of SKB264 monotherapy in selected subjects with advanced solid tumors.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 15 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI) < 30% Negative TROP2 expression (TROP2-)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 3 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX model (PDX: A11068)
Experiment 2 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI) < 30% Negative TROP2 expression (TROP2-)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX model (PDX: A11068)
Experiment 3 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 38.40% Moderate TROP2 expression (TROP2++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX model (PDX: A11068)
Experiment 4 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 42.90% Low TROP2 expression (TROP2+)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX models (PDX: 0501116)
Experiment 5 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
44%
High TROP2 expression (TROP2+++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 0.5 mg/kg for BR1282 PDX models twice a week for six times.
In Vivo Model Breast cancer PDX model (PDX: BR1282)
Experiment 6 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI) < 50% Negative TROP2 expression (TROP2-)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 10 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX model (PDX: A11068)
Experiment 7 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 66.70% High TROP2 expression (TROP2+++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX models (PDX: 406022)
Experiment 8 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
92.60%
High TROP2 expression (TROP2+++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1.5 mg/kg for BR1282 PDX models twice a week for six times.
In Vivo Model Breast cancer PDX model (PDX: BR1282)
Experiment 9 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
Low TROP2 expression (TROP2+)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 10 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX models (PDX: 0501116)
Experiment 10 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
Low TROP2 expression (TROP2+)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 3 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX models (PDX: 0501116)
Experiment 11 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
Moderate TROP2 expression (TROP2++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 10 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX model (PDX: A11068)
Experiment 12 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
Moderate TROP2 expression (TROP2++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 3 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX model (PDX: A11068)
Experiment 13 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
High TROP2 expression (TROP2+++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 10 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX models (PDX: 406022)
Experiment 14 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
High TROP2 expression (TROP2+++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 3 mg/kg for gastric cancer PDX models twice a week for six times.
In Vivo Model Gastric cancer PDX models (PDX: 406022)
Experiment 15 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
High TROP2 expression (TROP2+++)
Method Description
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 5 mg/kg for BR1282 PDX models twice a week for six times.
In Vivo Model Breast cancer PDX model (PDX: BR1282)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
51.20%
High TROP2 expression (TROP2+++)
Method Description
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 3 mg/kg in the NCI-N87.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
75.60%
High TROP2 expression (TROP2+++)
Method Description
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 1 mg/kg in the HCC1806.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 3 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
78.40%
High TROP2 expression (TROP2+++)
Method Description
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 0.3 mg/kg in the NCI-N87.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
98.50%
High TROP2 expression (TROP2+++)
Method Description
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 3 mg/kg in the HCC1806.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 5 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
High TROP2 expression (TROP2+++)
Method Description
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 1 mg/kg in the NCI-N87.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC [43]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
High TROP2 expression (TROP2+++)
Method Description
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 10 mg/kg in the HCC1806.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.28 nM
High TROP2 expression (TROP2+++)
Method Description
Tumor cells were seeded on 96-well plates at the following concentrations:Calu-3 (8,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
In Vitro Model Lung adenocarcinoma Calu-3 cells CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.24 nM
High TROP2 expression (TROP2+++)
Method Description
Tumor cells were seeded on 96-well plates at the following concentrations: NCI-N87 (5,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.41 nM
High TROP2 expression (TROP2+++)
Method Description
Tumor cells were seeded on 96-well plates at the following concentrations: NCI-H23 (TROP2+, 3,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
In Vitro Model Lung adenocarcinoma NCI-H23 cells CVCL_1547
Experiment 4 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.7 nM
High TROP2 expression (TROP2+++)
Method Description
Tumor cells were seeded on 96-well plates at the following concentrations: HCC1806 (3,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 5 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.03 nM
High TROP2 expression (TROP2+++)
Method Description
Tumor cells were seeded on 96-well plates at the following concentrations: BxPC-3 (2,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
18.83 nM
Negative TROP2 expression (TROP2-)
Method Description
Tumor cells were seeded on 96-well plates at the following concentrations: NCIH23 (parental, 3,000 cells per well).After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
In Vitro Model Lung adenocarcinoma NCI-H23 cells CVCL_1547
Sacituzumab govitecan [Approved in 2020]
Identified from the Human Clinical Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [28]
Efficacy Data Objective Response Rate (ORR)
21%
Patients Enrolled
Patients had histologically locally confirmed measurable HR+/HER2 MBC and 2-4 prior systemic chemotherapy regimens for metastatic disease. (Neo)adjuvant therapy for early-stage disease qualified as one of the required prior chemotherapy regimens if the development of unresectable, locally advanced, or metastatic disease occurred within 12 months of therapy (early relapse). Patients must have previously received at least one taxane, at least one anticancer hormonal treatment, and at least one CDK4/6i.

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Administration Dosage
10 mg/kg intravenously once weekly on day 1 and day 8 every 21 days.
Related Clinical Trial
NCT Number NCT03901339  Clinical Status Phase 3
Clinical Description
Phase 3 study of sacituzumab govitecan (IMMU-132) versus treatment of physician's choice (tpc) in subjects with hormonal receptor-positive (hr+) human epidermal growth factor receptor 2 (HER2) negative metastatic breast cancer (MBC) who have failed at least two prior chemotherapy regimens.
Primary Endpoint
PFS=5.50 months.
Other Endpoint
OS=13.90 months.
Experiment 2 Reporting the Activity Date of This ADC [29]
Efficacy Data Objective Response Rate (ORR)
31.43%
Patients Enrolled
Patients had metastatic triple-negative breast cancer (mTNBC) that had progressed following 2 prior standard chemotherapy regimens (no upper limit) for unresectable, locally advanced, or metastatic disease, and included a taxane (any setting). Per protocol, patients were also eligible after only one prior regimen in the metastatic setting if their disease recurred within 12 months of completing (neo)adjuvant therapy.

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Administration Dosage
10 mg/kg on days 1 and 8 of 21-day cycles; until progression, unacceptable toxicity, study withdrawal, or death.
Related Clinical Trial
NCT Number NCT02574455  Clinical Status Phase 3
Clinical Description
Analysis of patients without and with an initial triple-negative breast cancer diagnosis in the phase 3 randomized ASCENT study of sacituzumab govitecan in metastatic triple-negative breast cancer.
Primary Endpoint
PFS=4.60 months for patients without TNBC at initial diagnosis PFS=5.70 months for patients with TNBC at initial diagnosis.
Other Endpoint
ORR=31.43%.
Experiment 3 Reporting the Activity Date of This ADC [30]
Efficacy Data Objective Response Rate (ORR)
35%
Patients Enrolled
Patients with metastatic triple-negative breast cancer that was relapsed or refractory to two or more previous standard chemotherapy regimens (no upper limit) for unresectable, locally advanced or metastatic disease; previous therapy had to include a taxane (for any indication). Patients had to have triple-negative breast cancer according to standard American Society of Clinical OncologyCollege of American Pathologists criteria.

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Administration Dosage
Sacituzumab govitecan at a dose of 10 mg per kilogram of body weight intravenously on days 1 and 8 of each 21-day cycle.
Related Clinical Trial
NCT Number NCT02574455  Clinical Status Phase 3
Clinical Description
An international, multi-center, open-label, randomized, phase 3 trial of sacituzumab govitecan versus treatment of physician choice in patients with metastatic triple-negative breast cancer who received at least two prior treatments.
Primary Endpoint
Progression-free survival=5.60 months,(95% CI, 4.30-6.30) with sacituzumab govitecan and 1.70 months (95% CI,1.50 to 2.60) with chemotherapy (hazard ratio for disease progression or death, 0.41; 95% CI, 0.32-0.52).
Other Endpoint
The percentage of patients with an objective response was 35.00% with sacituzumab govitecan and 5.00% with chemotherapy.
Experiment 4 Reporting the Activity Date of This ADC [31]
Efficacy Data Objective Response Rate (ORR)
38.80%
High TROP2 expression (TROP2+++)
Patients Enrolled
Histologically or cytologically confirmed metastatic triple negative breast cancer (mTNBC); refractory or relapsing after 2 prior standard chemotherapy for unresectable, locally advanced, or metastatic disease, including a taxane (any setting).
Administration Dosage
10 mg/kg intravenously on Days 1 and 8 of each 21-day treatment cycle.
Related Clinical Trial
NCT Number NCT04454437  Clinical Status Phase 2
Clinical Description
A phase IIb, single arm, multicenter trial of sacituzumab govitecan in chinese patients with metastatic triple-negative breast cancer who received at least two prior treatments.
Primary Endpoint
Objective response rate=38.80% (95% CI 28.06-50.30), clinical benefit rate=43.80% (95% CI 32.68-55.30).
Other Endpoint
Median PFS=5.55 months (95% CI 4.14-N/A).
Experiment 5 Reporting the Activity Date of This ADC [32]
Efficacy Data Objective Response Rate (ORR)
14%
Patients Enrolled
Patients 18 years of age with mSCLC who had relapsed or were refractory to at least one prior standard line of therapy for metastatic disease, and with measurable tumors by CT, were enrolled. They were required to have Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1, adequate bone marrow, hepatic and renal function, and other eligibility as described in the phase I trial (25). Previous therapy had to be completed at least 2 weeks before enrollment.

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Administration Dosage
Either 8 or 10 mg/kg i.v. on days 1 and 8 of 21-day cycles.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
OrR=14.00% (17.00% for 10 mg/kg group).
Other Endpoint
The median response duration=5.70 months; the clinical benefit rate (CBR>4 months), 34.00%; median PFS=3.70 months; median OS=7.50 months.
Experiment 6 Reporting the Activity Date of This ADC [33]
Efficacy Data Objective Response Rate (ORR)
17.70
22.20
9.10 %
Patients Enrolled
Patients were >18 years of age with metastatic cancer [cervical, clear-cell renal, CRC, epithelial ovarian, endometrial, esophageal, gastric, hepatocellular, CRPC, pancreatic ductal adenocarcinoma, squamous cell head and neck, thyroid, urothelial (UC) cancer; glioblastoma multiforme; mTNBC or non-mTNBC; and SCLC or NSCLC] who had relapsed after or were refractory to at least one prior standard therapeutic regimen.

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Administration Dosage
Intravenous 8, 10, 12, or 18 mg/kg on days 1 and 8 of 21-day cycles until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
Safety and pharmacokinetic parameters with investigator-evaluated objective response rate.
Other Endpoint
Efficacy endpoints included: ORR, which included both confirmed partial response (PR) and complete response (CR).
Experiment 7 Reporting the Activity Date of This ADC [34]
Efficacy Data Objective Response Rate (ORR)
19%
Patients Enrolled
Patients 18 years with mNSCLC who had measurable disease and progressed after at least one line of therapy for stage IV disease were enrolled. Requirements included Eastern Cooperative Oncology Group performance status 0 or 1, adequate bone marrow and hepatic and renal function, and other eligibility criteria as described in the phase I trial. Prior systemic therapy had to be completed at least 4 weeks before enrollment.

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Administration Dosage
Doses of 8 or 10 mg/kg were given on days 1 and 8 of 21-day cycles; intravenously.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
Safety and objective response rate (ORR).
Other Endpoint
Progression-free survival and overall survival.
Experiment 8 Reporting the Activity Date of This ADC [35]
Efficacy Data Objective Response Rate (ORR)
30%
Patients Enrolled
Patients 18 years of age who had mTNBC refractory to or relapsed after at least one standard line of therapy since diagnosis and measurable disease by computed tomography scan (or magnetic resonance imaging). patients had an Eastern Cooperative Oncology Group performance status of 0 or 1, adequate bone marrow, hepatic and renal function, and prior toxicities at study entry of grade 1 by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 4.03. Patients with brain metastasis were excluded, unless treated and without progression, and were not receiving high-dose corticosteroids for at least 4 weeks.

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Administration Dosage
10 mg/kg starting dose on days 1 and 8 of 21-day repeated cycles; intravenously; eight cycles.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
Safety and objective response rate.
Other Endpoint
Progression-free survival and overall survival.
Experiment 9 Reporting the Activity Date of This ADC [36]
Efficacy Data Objective Response Rate (ORR)
33.30%
Patients Enrolled
Metastatic triple-negative breast cancer.
Administration Dosage
10 mg per kilogram intravenously on days 1 and 8 of each 21-day cycle until disease progression or unacceptable toxic effects.
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Primary Endpoint
Objective response rate=33.3% (95% confidence interval [CI].
Other Endpoint
The median duration of response=7.70 months (95% CI, 4.90 to 10.08),clinical benefit rate = 45.40%.
Experiment 10 Reporting the Activity Date of This ADC [42]
Related Clinical Trial
NCT Number NCT01631552  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of IMMU-132 (hRS7-SN38 antibody drug conjugate) in patients with epithelial cancer.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [44]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.14 nM
Method Description
Antibody-dependent cell cytotoxicity (ADCC) against Trop-2-positive and Trop-2-negative EC cell lines was measured in vitro,compared to control ADC (P = 0.014 and P = 0.005).
In Vivo Model Endometrioma PDX model (PDX: END(K)265)
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [45]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.18-0.26 nM
Method Description
Two Trop-2 positive (CVX-8, ADX-3), and one Trop-2 negative (ADX-2) cell lines were used. A cell line with a strong Trop-2 expression (CVX-8) was used to test in vivo antitumor activity in xenografts models,in vitro experiments.
In Vitro Model Primary cervical cancer Primary cervical cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [46]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.6 nM
Method Description
The inhibitory activity of sacituzumab govitecan govitecan against USC with heterogeneous Trop-2 expression was tested by admixing ARK2 USC cells (i.e., high Trop-2 expression) compared to control ADC (p< 0.05),in vitro.
In Vitro Model Endometrial serous adenocarcinoma USPC-ARK-2 cells CVCL_IV73
Experiment 3 Reporting the Activity Date of This ADC [47]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.02 nM
Method Description
The hRS7 conjugates of the two SN-38 derivatives,using 0.4 mg or 0.2 mg/kg SN-38 twice weekly* 4 weeks,were equivalent in drug substitution (~6),cell binding (Kd =1.2 nmol/L), cytotoxicity (IC50=2.2 nmol/L), and serum stability in vitro (t/1/2= 20hours).
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 4 Reporting the Activity Date of This ADC [47]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.44 nM
Method Description
The hRS7 conjugates of the two SN-38 derivatives,using 0.4 mg or 0.2 mg/kg SN-38 twice weekly* 4 weeks,were equivalent in drug substitution (~6),cell binding (Kd =1.2 nmol/L), cytotoxicity (IC50=2.2 nmol/L), and serum stability in vitro (t/1/2= 20hours).
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC [47]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.86 nM
Method Description
The hRS7 conjugates of the two SN-38 derivatives,using 0.4 mg or 0.2 mg/kg SN-38 twice weekly* 4 weeks,were equivalent in drug substitution (~6),cell binding (Kd =1.2 nmol/L), cytotoxicity (IC50=2.2 nmol/L), and serum stability in vitro (t/1/2= 20hours).
In Vitro Model Prostate carcinoma PC-3 cells CVCL_0035
Experiment 6 Reporting the Activity Date of This ADC [47]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.5 nM
Method Description
The hRS7 conjugates of the two SN-38 derivatives,using 0.4 mg or 0.2 mg/kg SN-38 twice weekly* 4 weeks,were equivalent in drug substitution (~6),cell binding (Kd =1.2 nmol/L), cytotoxicity (IC50=2.2 nmol/L), and serum stability in vitro (t/1/2= 20hours).
In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
Experiment 7 Reporting the Activity Date of This ADC [48]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.9 nM
Method Description
The inhibitory activity of sacituzumab govitecan govitecan against USC with heterogeneous Trop-2 expression was tested by admixing ARK2 USC cells (i.e., high Trop-2 expression) compared to control ADC (p< 0.05),in vitro.
In Vitro Model Endometrial serous adenocarcinoma USPC-ARK-2 cells CVCL_IV73
Experiment 8 Reporting the Activity Date of This ADC [47]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.19 nM
Method Description
The hRS7 conjugates of the two SN-38 derivatives,using 0.4 mg or 0.2 mg/kg SN-38 twice weekly* 4 weeks,were equivalent in drug substitution (~6),cell binding (Kd =1.2 nmol/L), cytotoxicity (IC50=2.2 nmol/L), and serum stability in vitro (t/1/2= 20hours).
In Vitro Model Lung adenocarcinoma Calu-3 cells CVCL_0609
Experiment 9 Reporting the Activity Date of This ADC [47]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.61 nM
Method Description
The hRS7 conjugates of the two SN-38 derivatives,using 0.4 mg or 0.2 mg/kg SN-38 twice weekly* 4 weeks,were equivalent in drug substitution (~6),cell binding (Kd =1.2 nmol/L), cytotoxicity (IC50=2.2 nmol/L), and serum stability in vitro (t/1/2= 20hours).
In Vitro Model Lung squamous cell carcinoma SK-MES-1 cells CVCL_0630
ADC-III-28 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 58.01% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model SK-OV-3 CDX model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.18% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model SK-OV-3 CDX model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.50% High TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model Colo205 CDX model
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 4 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.70% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 6 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.84% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model Colo205 CDX model
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 7 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 8 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [49]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
77.6 nM
High TROP2 expression (TROP2+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 2 Reporting the Activity Date of This ADC [49]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
393.9 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
ADC-II-53 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 72% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
ADC-II-11-a [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 82% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [49]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
120.8 nM
High TROP2 expression (TROP2+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 2 Reporting the Activity Date of This ADC [49]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
447.5 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
ADC-II-57 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.80% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
ADC-II-11-b [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99% High HER2 expression (HER2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC [49]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive TROP2 expression (TROP2+++/++)
Method Description
Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model FaDu CDX model
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
WO2022228495A1 ADC-76 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [50]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive TROP2 expression (TROP2+++/++)
Method Description
To establish squamous carcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 5 mg/kg.
In Vivo Model NCI-H2170 CDX model
In Vitro Model Lung squamous cell carcinoma NCI-H2170 cells CVCL_1535
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [50]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
41.56 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the NCI-H2170 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Lung squamous cell carcinoma NCI-H2170 cells CVCL_1535
Experiment 2 Reporting the Activity Date of This ADC [50]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
91.85 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the MDA-MB-231 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC [50]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
346.96 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the LK-2 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Lung squamous cell carcinoma LK-2 cells CVCL_1377
Sacituzumab-Compound (Ia) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [51]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
23 pM
Positive TROP2 expression (TROP2+++/++)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model Bladder carcinoma KMBC-2 cells CVCL_2977
Experiment 2 Reporting the Activity Date of This ADC [51]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
38.5 pM
Positive TROP2 expression (TROP2+++/++)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model Bladder carcinoma SW780 cells CVCL_1728
Experiment 3 Reporting the Activity Date of This ADC [51]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
56.2 pM
Positive TROP2 expression (TROP2+++/++)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model Breast ductal carcinoma HCC2157 cells CVCL_1261
Trop2-ADC-05 (DAR8) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [52]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.4 nM
Positive TROP2 expression (TROP2 +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC [52]
Efficacy Data Half Maximal Effective Concentration (EC50)
10000 nM
Negative TROP2 expression (TROP2 -)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Lung adenocarcinoma NCI-H23 cells CVCL_1547
Trop2-ADC-01 (DAR8) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [52]
Efficacy Data Half Maximal Effective Concentration (EC50)
21 nM
Positive TROP2 expression (TROP2 +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC [52]
Efficacy Data Half Maximal Effective Concentration (EC50)
10000 nM
Negative TROP2 expression (TROP2 -)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Lung adenocarcinoma NCI-H23 cells CVCL_1547
ZA202500415A-ADC Example 3 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [53]
Efficacy Data Tumor Growth lnhibition value (TGl)
74.76%
Method Description
Cell line-derived xenograft models were established in female NOD/SCID mice, by subcutaneous injection of 5x106 (JIMT-1) tumor cells, and treatmen with 2.5mg/kg ADC (Qw&#422) after tumor volume about 160.66mm3. Determined tumor volume after the experiment, measured at day 27.
In Vivo Model JIMT-1 Breast cancer xenograft model
Experiment 2 Reporting the Activity Date of This ADC [53]
Efficacy Data Tumor Growth lnhibition value (TGl)
121.55%
Method Description
Cell line-derived xenograft models were established in female NOD/SCID mice, by subcutaneous injection of 5x106 (JIMT-1) tumor cells, and treatmen with 10mg/kg ADC (Qw&#422) after tumor volume about 160.66mm3. Determined tumor volume after the experiment, measured at day 27.
In Vivo Model JIMT-1 Breast cancer xenograft model
Experiment 3 Reporting the Activity Date of This ADC [53]
Efficacy Data Tumor Growth lnhibition value (TGl)
122.04%
Method Description
Cell line-derived xenograft models were established in female NOD/SCID mice, by subcutaneous injection of 5x106 (JIMT-1) tumor cells, and treatmen with 5mg/kg ADC (Qw&#422) after tumor volume about 160.66mm3. Determined tumor volume after the experiment, measured at day 27.
In Vivo Model JIMT-1 Breast cancer xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [53]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.423 uM
Method Description
IM95-m Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Gastric adenocarcinoma IM95-m cells CVCL_2962
Experiment 2 Reporting the Activity Date of This ADC [53]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.486 uM
Positive her2 expression (her2+++/++)
Method Description
JIMT 1 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [53]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.544 uM
Method Description
NCI H292 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 4 Reporting the Activity Date of This ADC [53]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3.999 uM
Positive her2 expression (her2+++/++)
Method Description
NCI N87 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [53]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
51.61 uM
Method Description
NCI H2170 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

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In Vitro Model Lung squamous cell carcinoma NCI-H2170 cells CVCL_1535
40151029 ADC 2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.085 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.182 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Lung papillary adenocarcinoma NCI-H441 cells CVCL_1561
Experiment 3 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.265 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.418 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.945 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Breast acantholytic squamous cell carcinoma HCC-1806 cells CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Negative TROP2 expression (TROP2-)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Lung adenocarcinoma Calu-6 cells CVCL_0236
40151029 ADC 1 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.144 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.224 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Lung papillary adenocarcinoma NCI-H441 cells CVCL_1561
Experiment 3 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.338 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.683 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.027 nM
Positive TROP2 expression (TROP2+++/++)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Breast acantholytic squamous cell carcinoma HCC-1806 cells CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC [54]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Negative TROP2 expression (TROP2-)
Method Description
Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.

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In Vitro Model Lung adenocarcinoma Calu-6 cells CVCL_0236
SA-7-49 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [55]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
28.28 nM
High TROP2 expression (TROP2 +++)
Method Description
Panc 08.13, Panc 10.05, A375 and HCT116 cells were seeded in 96-well plate at a density of 5000 cells per well. After overnight adherence at 37 °C in a humidified incubator with 5 % CO2, drugs were added to the cells in a specific concentration gradient. After incubated at 37 °C, 5 % CO2 for 72h, cell viability was detected using the Cell Counting Kit-8 kit (Shandong Sparkjade Biotechnology Co., Ltd.), and the absorbance optical density (OD) values at 450 nm were read by a microplate reader (SpectraMax i3, MD, USA). The cell viability rate was calculated according to the following equation: viability % = (ODadministration - ODblank)/ (ODcontrol - ODblank) × 100 %. Olaparib and Adavosertib were purchased from MedChemExpress. KU-60019, Rabusertib, ML323, Berzosertib, RI-1 and AZD7648 were purchased from Selleck.

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In Vitro Model Pancreatic ductal adenocarcinoma Panc 10.05 cells CVCL_1639
Experiment 2 Reporting the Activity Date of This ADC [55]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
31.59 nM
High TROP2 expression (TROP2 +++)
Method Description
Panc 08.13, Panc 10.05, A375 and HCT116 cells were seeded in 96-well plate at a density of 5000 cells per well. After overnight adherence at 37 °C in a humidified incubator with 5 % CO2, drugs were added to the cells in a specific concentration gradient. After incubated at 37 °C, 5 % CO2 for 72h, cell viability was detected using the Cell Counting Kit-8 kit (Shandong Sparkjade Biotechnology Co., Ltd.), and the absorbance optical density (OD) values at 450 nm were read by a microplate reader (SpectraMax i3, MD, USA). The cell viability rate was calculated according to the following equation: viability % = (ODadministration - ODblank)/ (ODcontrol - ODblank) × 100 %. Olaparib and Adavosertib were purchased from MedChemExpress. KU-60019, Rabusertib, ML323, Berzosertib, RI-1 and AZD7648 were purchased from Selleck.

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In Vitro Model Pancreatic ductal adenocarcinoma Panc 08.13 cells CVCL_1638
References
Ref 1 SKB264 Injection Vs Investigator Selected Regimens to Treat Locally Advanced, Recurrent or Metastatic Triple-negative Breast Cancer
Ref 2 SKB264 +/- KL-A167 in Recurrent or Metastatic HER2-negative Breast Cancer
Ref 3 Study of SKB264 for Locally Advanced, Recurrent or Metastatic HR+/HER2- Breast Cancer
Ref 4 A Study of SKB264 Versus Investigator's Choice Chemotherapy in Patients With Unresectable Recurrent or Metastatic Triple-Negative Breast Cancer
Ref 5 HIM Typing Guides the Treatment of Advanced First-Line Triple-Negative Breast Cancer
Ref 6 A Study to Compare Sacituzumab Tirumotecan (MK-2870) Monotherapy Versus Treatment of Physician's Choice as Second-line Treatment for Participants With Recurrent or Metastatic Cervical Cancer (MK-2870-020/TroFuse-020/Gog-3101/ENGOT-cx20)
Ref 7 A Clinical Study of MK-2870 Alone or With Chemotherapy to Treat Gastrointestinal Cancers (MK-9999-02A)
Ref 8 Sacituzumab Tirumotecan (MK-2870) in Post Platinum and Post Immunotherapy Endometrial Cancer (MK-2870-005)
Ref 9 Phase I-II, FIH, TROP2 ADC, Advanced Unresectable/Metastatic Solid Tumors, Refractory to Standard Therapies
Ref 10 Substudy 06D: Combination Therapies in Second Line (2L) Gastroesophageal Adenocarcinoma (MK-3475-06D/Keymaker-U06)
Ref 11 Substudy 06C: A Study of Sacituzumab Tirumotecan (MK-2870) With Pembrolizumab (MK-3475) and Chemotherapy in Participants With First-Line Locally Advanced Unresectable/Metastatic Gastroesophageal Adenocarcinoma (MK-3475-06C/KEYMAKER-U06)
Ref 12 A Study to Evaluate Investigational Agents With or Without Pembrolizumab (MK-3475) in Participants With Advanced Esophageal Cancer Previously Exposed to Programmed Cell Death 1 Protein (PD-1)/ Programmed Cell Death Ligand 1 (PD-L1) Treatment (MK-3475-06B)
Ref 13 A Study to Evaluate Sacituzumab Tirumotecan (MK-2870) in Advanced/Metastatic Gastroesophageal Adenocarcinoma (MK-2870-015)
Ref 14 Sacituzumab Tirumotecan (MK-2870) Versus Chemotherapy in Previously Treated Advanced or Metastatic Nonsquamous Non-small Cell Lung Cancer (NSCLC) With EGFR Mutations or Other Genomic Alterations (MK-2870-004)
Ref 15 Sacituzumab Tirumotecan (MK-2870) in Combination With Pembrolizumab Versus Pembrolizumab Alone in Metastatic Non-small Cell Lung Cancer (NSCLC) With Programmed Cell Death Ligand 1 (PD-L1) Tumor Proportion Score (TPS) &ge; 50% (MK-2870-007)
Ref 16 Sacituzumab Tirumotecan (MK-2870) Versus Pemetrexed and Carboplatin Combination Therapy in Participants With Epidermal Growth Factor (EGFR)-Mutated, Advanced Nonsquamous Non-small Cell Lung Cancer (NSCLC) Who Have Progressed on Prior EGFR Tyrosine Kinase Inhibitors (MK-2870-009)
Ref 17 A Study to Assess Efficacy and Safety of Pembrolizumab With or Without Sacituzumab Tirumotecan (MK- 2870) in Adult Participants With Resectable Non Small Cell Lung Cancer (NSCLC) Not Achieving Pathological Complete Response (pCR) (MK-2870-019)
Ref 18 Pembrolizumab (MK-3475) Plus Investigational Agents in Resectable Non-small Cell Lung Cancer (NSCLC) (MK-3475-01E/KEYMAKER-U01)
Ref 19 SKB264 Combinatiton Therapy in Patients With Advanced or Metastatic Non-small Cell Lung Cancer.
Ref 20 A Study of SKB264 for the Treatment of Participants With Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC)
Ref 21 A Phase III Study of SKB264 for EGFR Mutant NSCLC Patients
Ref 22 A Study of SKB264 in Combination With Pembrolizumab Versus Pembrolizumab in Patients With Locally Advanced or Metastatic Non-Small Cell Lung Cancer
Ref 23 A Study of SKB264 in Combination with Osimertinib Versus Osimertinib in Patients with Epidermal Growth Factor Receptor (EGFR) Mutations, Locally Advanced or Metastatic Non-Squamous Non-Small Cell Lung Cancer
Ref 24 SKB264 Monotherapy in Selected Subjects with Advanced Solid Tumors
Ref 25 SKB264 in Combination With Pembrolizumab in Subjects With Selected Solid Tumors
Ref 26 A Study of Efficacy and Safety of Sacituzumab Tirumotecan (MK-2870) Plus Enfortumab Vedotin (EV) With and Without Pembrolizumab in Advanced Urothelial Carcinoma (MK-3475-04C/KEYMAKER-U04)
Ref 27 A Clinical Study of Sacituzumab Tirumotecan (MK-2870) in Patients With Bladder Cancer (MK-2870-027)
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Ref 29 Analysis of patients without and with an initial triple-negative breast cancer diagnosis in the phase 3 randomized ASCENT study of sacituzumab govitecan in metastatic triple-negative breast cancer. Breast Cancer Res Treat. 2022 Sep;195(2):127-139.
Ref 30 Sacituzumab Govitecan in Metastatic Triple-Negative Breast Cancer. N Engl J Med. 2021 Apr 22;384(16):1529-1541.
Ref 31 A Phase IIb, single arm, multicenter trial of sacituzumab govitecan in Chinese patients with metastatic triple-negative breast cancer who received at least two prior treatments. Int J Cancer. 2023 May 15;152(10):2134-2144. doi: 10.1002/ijc.34424. Epub 2023 Jan 30.
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Ref 33 Sacituzumab govitecan, a Trop-2-directed antibody-drug conjugate, for patients with epithelial cancer: final safety and efficacy results from the phase I/II IMMU-132-01 basket trial. Ann Oncol. 2021 Jun;32(6):746-756.
Ref 34 Therapy of Advanced Non-Small-Cell Lung Cancer With an SN-38-Anti-Trop-2 Drug Conjugate, Sacituzumab Govitecan. J Clin Oncol. 2017 Aug 20;35(24):2790-2797.
Ref 35 Efficacy and Safety of Anti-Trop-2 Antibody Drug Conjugate Sacituzumab Govitecan (IMMU-132) in Heavily Pretreated Patients With Metastatic Triple-Negative Breast Cancer. J Clin Oncol. 2017 Jul 1;35(19):2141-2148.
Ref 36 Sacituzumab Govitecan-hziy in Refractory Metastatic Triple-Negative Breast Cancer. N Engl J Med. 2019 Feb 21;380(8):741-751.
Ref 37 A Randomized, Controlled, Open-label, Multi-center Phase III Clinical Trial of SKB264 for Injection Versus Investigator Selected Regimens in Patients With Unresectable Locally Advanced, Recurrent or Metastatic Triple-negative Breast Cancer Who Have Failed Second-line or Above Prior Standard of Care, NCT05347134
Ref 38 A Multicenter, Open-label, Phase 2, Basket Study to Evaluate the Efficacy and Safety of SKB264 in Combination With Pembrolizumab in Subjects With Selected Solid Tumors, NCT05642780
Ref 39 A Phase Clinical Study of Combination Therapy of SKB264 in Patients With Advanced or Metastatic Non-small Cell Lung Cancer, NCT05351788
Ref 40 A Phase Clinical Study of SKB264 With/Without KL-A167 in Patients With Unresectable Locally Advanced, Recurrent or Metastatic Triple-negative Breast Cancer (TNBC) Who Have Not Received Prior Systemic Therapy, NCT05445908
Ref 41 A Multicenter, Open-label, Phase 2 Study to Evaluate the Efficacy and Safety of SKB264 Monotherapy in Selected Subjects With Advanced Solid Tumors, NCT05631262
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Ref 43 Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132. Front Oncol. 2022 Dec 23;12:951589.
Ref 44 Sacituzumab govitecan, an antibody-drug conjugate targeting trophoblast cell-surface antigen 2, shows cytotoxic activity against poorly differentiated endometrial adenocarcinomas invitro and invivo. Mol Oncol. 2020 Mar;14(3):645-656.
Ref 45 Cervical carcinomas that overexpress human trophoblast cell-surface marker (Trop-2) are highly sensitive to the antibody-drug conjugate sacituzumab govitecan. Sci Rep. 2020 Jan 22;10(1):973.
Ref 46 Clinicopathological features of women with epithelial ovarian cancer and double heterozygosity for BRCA1 and BRCA2: A systematic review and case report analysis. Gynecol Oncol. 2020 Feb;156(2):377-386.
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Ref 48 Invitro and invivo activity of sacituzumab govitecan, an antibody-drug conjugate targeting trophoblast cell-surface antigen 2 (Trop-2) in uterine serous carcinoma. Gynecol Oncol. 2020 Feb;156(2):430-438.
Ref 49 Antitumor compound, and preparation method therefor and use thereof; 2022-04-07.
Ref 50 Preparation method for antibody-drug conjugate, and application; 2022-11-03.
Ref 51 Neodegrader conjugates; 2021-10-07.
Ref 52 Bioactive substance conjugate, preparation method therefor and use thereof; 2022-08-18.
Ref 53 Antibody drug conjugate comprising NMT inhibitor and its use
Ref 54 Direct Preparation of Site-Specific Antibody-Drug Conjugates with Unpurified Antibodies in Culture Medium
Ref 55 Exploiting synthetic lethality in PDAC with antibody drug conjugates and ATR inhibition