Antibody ID	ANI0INHAA
Antibody Name	Sacituzumab
Organization	Immunomedics, Inc.
Indication	Neoplasms
Synonyms	hRS7    Click to Show/Hide
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     Click to Show/Hide
Heavy Chain Varible Domain	QVQLQQSGSELKKPGASVKVSCKASGYTFTNYGMNWVKQAPGQGLKWMGWINTYTGEPTY TDDFKGRFAFSLDTSVSTAYLQISSLKADDTAVYFCARGGFGSSYWYFDVWGQGSLVTVS S     Click to Show/Hide
Heavy Chain Constant Domain 1	ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRV     Click to Show/Hide
Heavy Chain Constant Domain 2	APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK     Click to Show/Hide
Heavy Chain Constant Domain 3	GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK     Click to Show/Hide
Heavy Chain Hinge Region	EPKSCDKTHTCPPCP     Click to Show/Hide
Heavy Chain CDR 1	GYTFTNYG     Click to Show/Hide
Heavy Chain CDR 2	INTYTGEP     Click to Show/Hide
Heavy Chain CDR 3	ARGGFGSSYWYFDV     Click to Show/Hide
Light Chain Sequence	DIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPD RFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain Varible Domain	DIQLTQSPSSLSASVGDRVSITCKASQDVSIAVAWYQQKPGKAPKLLIYSASYRYTGVPD RFSGSGSGTDFTLTISSLQPEDFAVYYCQQHYITPLTFGAGTKVEIK     Click to Show/Hide
Light Chain Constant Domain	RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain CDR 1	QDVSIA     Click to Show/Hide
Light Chain CDR 2	SAS     Click to Show/Hide
Light Chain CDR 3	QQHYITPLT     Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Objective Response Rate (ORR)	21.00%
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.    Click to Show/Hide
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	medium PFS=5.50 months.
Other Endpoint	medium OS=13.90 months.
Experiment 2 Reporting the Activity Date of This ADC					[2]
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.    Click to Show/Hide
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					[3]
Efficacy Data	Objective Response Rate (ORR)	35.00%
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.    Click to Show/Hide
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					[4]
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					[5]
Efficacy Data	Objective Response Rate (ORR)	14.00%
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.    Click to Show/Hide
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					[6]
Efficacy Data	Objective Response Rate (ORR)	17.70% (small-cell lung cancer) 22.20% (endometrial cancer) 9.10% (castrate-resistant prostate cancer)
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.    Click to Show/Hide
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					[7]
Efficacy Data	Objective Response Rate (ORR)	19.00%
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.    Click to Show/Hide
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					[8]
Efficacy Data	Objective Response Rate (ORR)	30.00%
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.    Click to Show/Hide
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					[9]
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					[10]
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.

Experiment 1 Reporting the Activity Date of This ADC					[11]
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)

Experiment 1 Reporting the Activity Date of This ADC					[12]
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					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.60 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					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.02 nM
Method Description	Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	COLO 205 cells		CVCL_0218
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.44 nM
Method Description	Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.86 nM
Method Description	Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 6 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.50 nM
Method Description	Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 7 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.90 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					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.19 nM
Method Description	Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 9 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.61 nM
Method Description	Briefly, cells were plated into 96-well clear, flat-bottomed plates. The immunoconjugate reconstituted in media was diluted with media to a final concentration of range of 0.004 to 250 nM in the wells. Plates were incubated in humidified chamber for 96 h 37°C/5% CO2. Growth inhibition was measured as a percent of growth relative to untreated cells.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630

Experiment 1 Reporting the Activity Date of This ADC					[16]
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 2 Reporting the Activity Date of This ADC					[17]
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 3 Reporting the Activity Date of This ADC					[18]
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.
Experiment 4 Reporting the Activity Date of This ADC					[19]
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 5 Reporting the Activity Date of This ADC					[20]
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 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	< 30.00% (Day 21)	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 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	< 30.00% (Day 21)	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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 38.40% (Day 21)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.90% (Day 21)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	44.00% (Day 24)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	< 50.00% (Day 21)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.70% (Day 21)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.60% (Day 24)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 21)	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 10 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 21)	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 11 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 21)	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 12 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 21)	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 13 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 21)	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 14 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 21)	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 15 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 24)	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)

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	51.20% (Day 24)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	75.60% (Day 24)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	78.40% (Day 24)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98.50% (Day 24)	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					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 24)	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
Experiment 6 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 24)	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 1 Reporting the Activity Date of This ADC					[21]
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					[21]
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					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.70 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					[21]
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					[21]
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

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Objective Response Rate (ORR)	36.40%
Patients Enrolled	Patients (pts) aged 18 years with locally advanced/metastatic solid tumors refractory to/relapsed.
Administration Dosage	Treated with 1 dose of ESG401 during escalation at doses of 2-20 mg/kg once Q3W (Regimen A), or 12-16 mg/kg D1,8,15 in a 4-week cycle (Regimen B).
Related Clinical Trial
NCT Number	NCT04892342	Clinical Status	Phase 1/2
Clinical Description	An open-label, multiple dose, dose escalation and cohort expansion phase 1/2 study to investigate the safety, tolerability, pharmacokinetics and antitumor activities of ESG401 in Subjects with locally advanced/metastatic solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[23]
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					[23]
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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.50% (Day 26)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.70% (Day 26)	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					[23]
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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	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 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	77.60 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					[23]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	393.90 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

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.00% (Day 26)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	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 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.00% (Day 26)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	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 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	120.80 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					[23]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	447.50 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

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.00% (Day 26)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.80% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	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 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 29)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	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					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	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 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 32)	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

Experiment 1 Reporting the Activity Date of This ADC					[24]
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					[24]
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					[24]
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

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.00 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					[25]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	38.50 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					[25]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	56.20 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

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.40 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					[26]
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

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Half Maximal Effective Concentration (EC50)	21.00 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					[26]
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

Ref 1	Sacituzumab Govitecan in Hormone Receptor-Positive/Human Epidermal Growth Factor Receptor 2-Negative Metastatic Breast Cancer. J Clin Oncol. 2022 Oct 10;40(29):3365-3376.
Ref 2	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 3	Sacituzumab Govitecan in Metastatic Triple-Negative Breast Cancer. N Engl J Med. 2021 Apr 22;384(16):1529-1541.
Ref 4	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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