Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0RHAZG
ADC Name
Ladiratuzumab vedotin
Synonyms
MK-6440; SGN-LIV1A
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Organization
Seagen Inc.; F. Hoffmann-La Roche Ltd.; Merck Sharp & Dohme Corp.
Drug Status
Phase 2
Indication
In total 11 Indication(s)
Adenocarcinoma [ICD11:2D40]
Phase 2
Breast cancer [ICD11:2C60-2C65]
Phase 2
Esophageal squamous cell carcinoma [ICD11:2B71]
Phase 2
Gastric cancer [ICD11:2B72]
Phase 2
Head and neck squamous carcinoma [ICD11:2C31]
Phase 2
Melanoma [ICD11:2C30]
Phase 2
Non-small cell lung cancer [ICD11:2C25]
Phase 2
Prostate cancer [ICD11:2C82]
Phase 2
Small cell lung cancer [ICD11:2C25]
Phase 2
Solid tumors [ICD11:2A00-2A0Z|2B50-2F9Z]
Phase 2
Triple negative breast cancer [ICD11:2C60-2C65]
Phase 2
Drug-to-Antibody Ratio
4
Structure
Antibody Name
Ladiratuzumab
  Antibody Info 
Antigen Name
Zinc transporter ZIP6 (SLC39A6)
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Mc-Val-Cit-PABC
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Vedotin
Puchem SID
472418926 , 381127804 , 404772836 , 404720278
Drugbank ID
DB15409
TTD ID
D0VQ8Q
ChEBI ID
CHEMBL4298101
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Objective Response Rate (ORR)  NCT03310957
Phase 1/2
Single arm, open label phase 1b/2 study of SGN-LIV1A in combination with pembrolizumab for first-line treatment of patients with unresectable locally-advanced or metastatic triple-negative breast cancer.

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Objective Response Rate (ORR)  NCT01969643
Phase 1
A phase 1, open-label, dose-escalation study to evaluate the safety and tolerability of SGN-LIV1A in patients with metastatic breast cancer.
Undisclosed  NCT04032704
Phase 2
Open-label phase 2 study of ladiratuzumab vedotin (LV) for unresectable locally advanced or metastatic solid tumors.
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Effective Concentration (EC50) 
6.3
ng/mL
MCF-7 cells
Invasive breast carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Objective Response Rate (ORR)
35.00%
Patients Enrolled
Unresectable locally advanced or metastatic triple-negative breast cancer (mTNBC). Patients must have measureable disease per RECIST v1.1, an ECOG score of 0 or 1, and no prior cytotoxic or anti-PD-L1 treatment for advanced disease.
Administration Dosage
LV 2.50 mg/kg + pembrolizumab 200 mg intravenously every three weeks.
Related Clinical Trial
NCT Number NCT03310957  Clinical Status Phase 1/2
Clinical Description Single arm, open label phase 1b/2 study of SGN-LIV1A in combination with pembrolizumab for first-line treatment of patients with unresectable locally-advanced or metastatic triple-negative breast cancer.
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
32.00%
Patients Enrolled
Women with LIV-1-positive, unresectable, locally advanced or metastatic breast cancer (LA/MBC).
Administration Dosage
Received a median of 3 cycles (range, 112) of SGN-LIV1A at doses of 0.50-2.80 mg/kg.
Related Clinical Trial
NCT Number NCT01969643  Clinical Status Phase 1
Clinical Description A phase 1, open-label, dose-escalation study to evaluate the safety and tolerability of SGN-LIV1A in patients with metastatic breast cancer.
Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT04032704  Clinical Status Phase 2
Clinical Description Open-label phase 2 study of ladiratuzumab vedotin (LV) for unresectable locally advanced or metastatic solid tumors.
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
6.30 ng/mL
Method Description
The inhibitory activity of SGN-LIV1A against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Phase 1 study of the antibody-drug conjugate SGN-LIV1A in patients with heavily pretreated triple-negative metastatic breast cancer. Cancer Res (2018) 78 (4_Supplement): PD3-14.
Ref 2 Ladiratuzumab vedotin for metastatic triple negative cancer: preliminary results, key challenges, and clinical potential. Expert Opin Investig Drugs. 2022 Jun;31(6):495-498. doi: 10.1080/13543784.2022.2042252.
Ref 3 Open-Label Phase 2 Study of Ladiratuzumab Vedotin (LV) for Unresectable Locally Advanced or Metastatic Solid Tumors, NCT04032704
Ref 4 SGN-LIV1A: a novel antibody-drug conjugate targeting LIV-1 for the treatment of metastatic breast cancer. Mol Cancer Ther. 2014 Dec;13(12):2991-3000.

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