Linker Information

General Information of This Linker
Linker ID
LIN0ZHZRH
Linker Name
DBCO-Val-Cit-PABA
Antibody-Linker Relation
Cleavable
Structure
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Luveltamab tazevibulin [Phase 2/3 (discontinued)]
 ADC Info 
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
15%
Negative FOLR1 expression (FOLR1-)
In Vivo Model STRO-002 monotherapy PDX model (PDX:PDX model 5)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
53%
Low FOLR1 expression (FOLR1+)
In Vivo Model PDX model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
70%
Moderate FOLR1 expression (FOLR1++)
In Vivo Model PDX model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
80%
High FOLR1 expression (FOLR1+++)
In Vivo Model PDX model
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
High FOLR1 expression (FOLR1+++)
In Vivo Model PDX model
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
High FOLR1 expression (FOLR1+++)
In Vivo Model PDX model
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 26 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.24 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Lung squamous cell carcinoma NCI-H1703 cells CVCL_1490
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.74 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.84 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Lung non-small cell carcinoma NCI-H2110 cells CVCL_1530
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.4 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.42 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.7 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.8 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Amelanotic melanoma MDA-MB-435 cells CVCL_0417
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.2 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.29 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Amelanotic melanoma MDA-MB-435 cells CVCL_0417
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.42 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Plasma cell myeloma OPM-2 cells CVCL_1625
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.18 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.59 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
7.9 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
9.18 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Colon carcinoma HCT 116 cells CVCL_0291
Experiment 15 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
9.2 nM
Low FOLR1 expression (FOLR1+)
In Vitro Model Lung adenocarcinoma NCI-H1651 cells CVCL_1484
Experiment 16 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.07 ng/mL
Moderate FOLR1 expression (FOLR1++)
Method Description
STRO-002 in lgrov1 cell.
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 17 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.35 ng/mL
High FOLR1 expression (FOLR1+++)
Method Description
STRO-002 in KB cell.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 18 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.42 ng/mL
Low FOLR1 expression (FOLR1+)
In Vitro Model Diffuse large B-cell lymphoma SU-DHL-6 cells CVCL_2206
Experiment 19 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.6 ng/mL
Low FOLR1 expression (FOLR1+)
In Vitro Model Endometrial adenocarcinoma Ishikawa cells CVCL_2529
Experiment 20 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.1 ng/mL
Low FOLR1 expression (FOLR1+)
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 21 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.2 ng/mL
Moderate FOLR1 expression (FOLR1++)
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 22 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.8 ng/mL
Low FOLR1 expression (FOLR1+)
In Vitro Model High grade ovarian serous adenocarcinoma OVKATE cells CVCL_3110
Experiment 23 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.6 ng/mL
Moderate FOLR1 expression (FOLR1++)
Method Description
SC209 in lgrov1 cell.
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 24 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.9 ng/mL
High FOLR1 expression (FOLR1+++)
Method Description
SC209 in KB cell.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 25 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
291 ng/mL
Moderate FOLR1 expression (FOLR1++)
Method Description
SC239 in lgrov1 cell.
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 26 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
400 ng/mL
High FOLR1 expression (FOLR1+++)
Method Description
SC239 in KB cell.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Identified from the Human Clinical Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
37.50%
Patients Enrolled
Eligible patients (≥18 years, ECOG 0-1, measurable disease) include platinum-resistant (1-3 prior regimens) or sensitive ovarian cancers (Cohorts A/C) and endometrial cancers progressing post-platinum/immunotherapy (Cohort B, ≤3 regimens). Exclusions: low-grade/rare histologies, prior FolRalpha-targeting therapies, CNS metastasis, >3 prior lines, or severe comorbidities. Tumor tissue submission is mandatory.

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Administration Dosage
Enrollment has been completed with 39 pts treated at 9 dose levels (0.5 to 6.4 mg/kg). Data cut-off is Jan 30, 2021.
Related Clinical Trial
NCT Number NCT03748186  Clinical Status PHASE1
Clinical Description
A Phase 1 Open-Label, Safety, Pharmacokinetic and Preliminary Efficacy Study of STRO-002, an Anti-Folate Receptor Alpha (FolRalpha) Antibody-Drug Conjugate (ADC), in Patients With Advanced Epithelial Ovarian Cancer (Including Fallopian Tube or Primary Peritoneal Cancers) and Endometrial Cancers
Primary Endpoint
The study evaluates STRO-002's safety and defines its recommended/maximum tolerated doses (RP2D/MTD) via dose-limiting toxicity assessments over 18 months. Preliminary efficacy in ovarian/Fallopian/primary peritoneal and endometrial cancers is measured by RECIST 1.1 ORR over 24 months.
Other Endpoint
Pharmacokinetic analysis (18-24 months) includes Cmax, t1/2, AUCinf, CL, and Vss measurements, with anti-drug antibody monitoring. Expansion cohorts assess safety through AE incidence, DOR, PFS (RECIST 1.1), CA-125 changes (GCIG criteria), and repeat PK evaluations.
Experiment 2 Reporting the Activity Date of This ADC [3]
Patients Enrolled
Eligible patients are adults (≥18, ECOG 0-1) with FOLR1-positive, platinum-resistant high-grade serous ovarian/fallopian/primary peritoneal cancer (1-3 prior regimens). Prior bevacizumab is required unless contraindicated. Exclusions: rare histologies, prior FOLR1-targeting ADCs/tubulin inhibitors, platinum-refractory disease, severe comorbidities, CNS involvement, or ongoing trials. Measurable disease per RECIST v1.1 and adequate organ function are required.

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Related Clinical Trial
NCT Number NCT05870748  Clinical Status PHASE2|||PHASE3
Clinical Description
REFRaME-O1: A Phase 2/3 Open-label Study Evaluating the Efficacy and Safety of Luveltamab Tazevibulin (STRO-002) Versus Investigator's Choice (IC) Chemotherapy in Women With Relapsed Platinum-resistant Epithelial Ovarian Cancer (Including Fallopian Tube or Primary Peritoneal Cancers) Expressing Folate Receptor Alpha (FOLR1)
Primary Endpoint
The study measures Progression-Free Survival (PFS) and Objective Response Rate (ORR) per RECIST 1.1 over up to 24 months, tracking the time from first dose to disease progression/death (PFS) and the best response of complete (CR) or partial response (PR).
Other Endpoint
Secondary endpoints include Overall Survival (OS), Duration of Response (DOR), and adverse event incidence/severity. Quality of life is evaluated using the QLQ-OV28 questionnaire, assessing abdominal symptoms, neuropathy, chemotherapy side effects, hormonal changes, body image, disease/treatment attitude, and sexual function over 24 months.
Experiment 3 Reporting the Activity Date of This ADC [4]
Patients Enrolled
Eligible patients must be ≥18 years with ECOG 0-1, high-grade serous EOC/fallopian tube/primary peritoneal cancer, measurable lesions (RECIST v1.1), and adequate organ function. Dose Escalation participants require specific platinum therapy history (1-4 prior regimens), while Expansion Cohort requires platinum-resistant disease (≤4 regimens). Key exclusions include non-serous histologies, prior tubulin-inhibitor ADCs, >4 regimens, contraindications to bevacizumab, active infections, significant comorbidities (cardiac/pulmonary/neurological), HIV/HBV/HCV (with exceptions), and concurrent trial participation. Pregnancy requires contraception through treatment and extended follow-up periods.

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Related Clinical Trial
NCT Number NCT05200364  Clinical Status PHASE1
Clinical Description
A Phase 1 Open-Label, Safety, Pharmacokinetic and Preliminary Efficacy Study of STRO-002, an Anti-Folate Receptor Alpha Antibody Drug Conjugate, in Combination With Bevacizumab in Patients With Advanced Epithelial Ovarian Cancer (Including Fallopian Tube or Primary Peritoneal Cancers)
Primary Endpoint
This study evaluates the safety and tolerability of STRO-002/bevacizumab combination therapy by assessing adverse events and clinical lab abnormalities across various dose levels, with DLT monitoring during initial treatment (Days 1-21). It also aims to establish the recommended Phase 2 dose (RP2D) by analyzing DLT frequency over approximately 24 months.

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Other Endpoint
Pharmacokinetic characterization of STRO-002 includes measurements of maximum plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC) throughout the study period. Additionally, the study assesses anti-drug antibody (ADA) formation against STRO-002 when administered with bevacizumab over the 24-month timeframe.
Experiment 4 Reporting the Activity Date of This ADC [5]
Patients Enrolled
Eligible patients must be <12 years with CBFA2T3::GLIS2-fusion AML (&ge;5% marrow blasts), refractory/relapsed, and adequate organ function (Lansky &ge;50). Exclusions: active CNS disease, corneal disorders, uncontrolled infections, prior FOLR1-targeting/tubulin-inhibitor ADCs, recent transplant (<84 days), or active GVHD requiring immunosuppression beyond low-dose steroids.

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Administration Dosage
This trial has two parts, Part 1 will use a parallel model by assessing two luveltamab tazevibulin doses (3.5 and 4.3 mg/kg every 2 weeks). Two cohorts will be run in parallel. The transition from part 1 to part 2 is sequential, with part 2 testing the dose selected at the end of part 1.
Related Clinical Trial
NCT Number NCT06679582  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2, Open-label Study Evaluating the Efficacy, Safety, and Pharmacokinetics (PK) of Luveltamab Tazevibulin (STRO-002) in Infants and Children < 12 Years of Age with CBFA2T3::GLIS2 Acute Myeloid Leukemia (AML)
Primary Endpoint
The primary objective is to evaluate the efficacy of luveltamab tazevibulin monotherapy by assessing the complete remission (CR) rate within 12 weeks.
Other Endpoint
Secondary measures include long-term efficacy assessments (up to 2 years) such as duration of CR, response rate (CRh), EFS, RFS, and OS. Safety is monitored via AEs (CTCAE v5.0), while PK evaluates blood concentrations of luveltamab tazevibulin components (ADC, TAb, SC209). ADA incidence determines immunogenicity.
Experiment 5 Reporting the Activity Date of This ADC [6]
Patients Enrolled
Eligible patients (life expectancy >3 months, RECIST v1.1 measurable lesions, CTCAE v5.0 Grade &le;1 residual toxicity) require organ function adequacy and QTcF <500 msec. Cohort-specific criteria apply: ovarian (Cohorts A/B), endometrial (Cohort C), NSCLC (Cohort D), or TNBC (Cohort E) with 1-4 prior therapies. Exclusions: prior tubulin-inhibitor ADCs, FolRalpha-targeting agents, severe allergies, recent anticancer therapies (chemotherapy/immunotherapy/surgery/radiation), active ocular disorders, or folate supplement use. Ocular exclusions encompass corneal diseases, transplants, and conditions like uncontrolled glaucoma or diabetic retinopathy.

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Related Clinical Trial
NCT Number NCT06238687  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase I/IIa Study to Evaluate the Safety, Tolerability , Pharmacokinetics and Preliminary Efficacy of STRO-002 in Chinese Adults With Advanced Epithelial Ovarian Cancer, Endometrial Cancer, and Other Advanced Malignant Solid Tumors.
Primary Endpoint
This study investigates STRO-002's safety and efficacy, assessing DLTs (Days 1-21 post-dose), AE frequency, and key PK parameters (AUC, Cmax, t½) over 28 days post-treatment. ORR (RECIST v1.1) and RP2D determination are primary efficacy endpoints evaluated up to 24 months.
Other Endpoint
Secondary outcomes include ADA incidence, DOR, and PFS over 24 months, alongside tumor biomarker analysis (FolRalpha/CA-125) requiring ≥50% CA-125 reduction sustained for 28 days. These measures track immunogenicity, response durability, and disease progression post-STRO-002 administration.
Experiment 6 Reporting the Activity Date of This ADC [7]
Patients Enrolled
Eligible patients are adults (&ge;18 years, ECOG 0-1) with FOLR1-positive, unresectable Stage IIIb/c or IV NSCLC (non-squamous/adenosquamous), progressing after 2-4 systemic therapies and measurable lesions per RECIST 1.1. Exclusions: prior FOLR1/tubulin-inhibitor ADC treatment, untreated CNS metastases, immunosuppressive therapy (except for controlled brain metastases), severe allergies, ocular/cardiopulmonary disorders, organ transplants, or concurrent trial participation.

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Related Clinical Trial
NCT Number NCT06555263  Clinical Status PHASE2
Clinical Description
A Phase 2, Open-label Study Evaluating STRO-002, an Anti-folate Receptor Alpha (FOLR1) Antibody-Drug Conjugate, in Subjects with Previously Treated Advanced or Metastatic Non-small Cell Lung Cancer Expressing FOLR1
Primary Endpoint
The primary efficacy endpoint is Objective Response Rate (ORR), defined as the proportion of patients achieving CR or PR per RECIST 1.1 criteria, assessed over a 24-month timeframe.
Other Endpoint
Secondary endpoints include DOR (time from first response to progression/death), PFS (time from first dose to progression/death), and safety (AE incidence/lab abnormalities). PK analysis evaluates luveltamab tazevibulin via ADC concentration, total antibody, and cytotoxic warhead measurements over 24 months.
References
Ref 1 Discovery of STRO-002, a Novel Homogeneous ADC Targeting Folate Receptor Alpha, for the Treatment of Ovarian and Endometrial Cancers. Mol Cancer Ther. 2023 Feb 1;22(2):155-167.
Ref 2 Study of STRO-002, an Anti-Folate Receptor Alpha (FolR&alpha;) Antibody Drug Conjugate in Ovarian & Endometrial Cancers
Ref 3 REFRaME-O1: A Study to Investigate the Efficacy and Safety of Luveltamab Tazevibulin Versus Investigator's Choice (IC) Chemotherapy in Women With Ovarian Cancer (Including Fallopian Tube or Primary Peritoneal Cancers) Expressing FOLR1
Ref 4 A Study of STRO-002, an Anti-Folate Receptor Alpha Antibody Drug Conjugate, in Combination With Bevacizumab in Epithelial Ovarian Cancer
Ref 5 Luveltamab Tazevibulin (STRO-002) in Infants and Children < 12 Years of Age with Relapsed/Refractory CBFA2T3::GLIS2 AML
Ref 6 A Study of STRO-002 in Chinese Adults With Epithelial Ovarian Cancer and Other Advanced Malignant Solid Tumors
Ref 7 Study to Investigate Luveltamab Tazevibulin in Adults with Advanced or Metastatic Non-small Cell Lung Cancer