Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XCWMD
ADC Name
Cantuzumab ravtansine
Synonyms
C242 DM4 immunoconjugate; C242 maytansinoid-4 conjugate; Maytasinoid DM4-conjugated humanised monoclonal antibody huC242; Monoclonal antibody C-242 DM4 conjugate; IMGN-242; huC242-DM4; C-242 DM4
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Organization
ImmunoGen, Inc.
Drug Status
Terminated in phase 2
Indication
In total 1 Indication(s)
Gastric cancer [ICD11:2B72]
Terminated in phase 2
Drug-to-Antibody Ratio
3.5
Structure
Antibody Name
Cantuzumab
  Antibody Info 
Antigen Name
Syndecan-1 (SDC1)
  Antigen Info 
Payload Name
Mertansine DM4
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
N-succinimidyl 4-(2-pyridyldithio) butanoate (SPDB)
  Linker Info 
Conjugate Type
Random conjugation through nucleophilic lysines.
Combination Type
Ravtansine
Puchem SID
472423076 , 381125618 , 404770028 , 476262823 , 160677286 , 172232547 , 476269508
Drugbank ID
DB05594
ChEBI ID
CHEMBL1742998
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
Undisclosed  NCT00620607
Phase 2
A phase 2, open label, multiple center study of HUC242-DM4 given as an intravenous infusion once every three weeks to patients with metastatic gastric or gastroesophageal junction carcinomas.
Undisclosed  NCT00352131
Phase 1
A phase 1 study to assess the safety and pharmacokinetics of huC242-DM4 administered as a single intravenous infusion once every three weeks to subjects with solid tumors.
Undisclosed  NCT00352131
Phase 1
A phase 1 study to assess the safety and pharmacokinetics of huC242-DM4 administered as a single intravenous infusion once every three weeks to subjects with solid tumors.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 48.85
%
MOLP-8 cells
Plasma cell myeloma
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]
Related Clinical Trial
NCT Number NCT00620607  Clinical Status Phase 2
Clinical Description A phase 2, open label, multiple center study of HUC242-DM4 given as an intravenous infusion once every three weeks to patients with metastatic gastric or gastroesophageal junction carcinomas.
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT00352131  Clinical Status Phase 1
Clinical Description A phase 1 study to assess the safety and pharmacokinetics of huC242-DM4 administered as a single intravenous infusion once every three weeks to subjects with solid tumors.
Experiment 3 Reporting the Activity Date of This ADC [3]
Patients Enrolled
Metastatic or inoperable colorectal, pancreatic, and other CanAg-expressing tumors who have failed standard therapy (about 95% of pts. had received = 4 prior chemotherapy regimens).
Administration Dosage
A single intravenous (IV) infusion once every three weeks, 18, 36, 60, 90, 126, 168, 223, and 297 mg/m2.
Related Clinical Trial
NCT Number NCT00352131  Clinical Status Phase 1
Clinical Description A phase 1 study to assess the safety and pharmacokinetics of huC242-DM4 administered as a single intravenous infusion once every three weeks to subjects with solid tumors.
Primary Endpoint
HuC242-DM4 was well tolerated at the 168 mg/m2 dose level. The MTD is not yet defined.
Other Endpoint
No clinically significant myelosuppression and no formation of antibody to humanized antibody (HAHA) or drug (HADA).
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 [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 48.85% (Day 20) Positive CD138 expression (CD138 +++/++)
Method Description
MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model MOLP-8 CDX model
In Vitro Model Plasma cell myeloma MOLP-8 cells CVCL_2124
References
Ref 1 A Phase II, Open Label, Multiple Center Study of huC242-DM4 Given as an Intravenous Infusion Once Every Three Weeks to Patients With Metastatic Gastric or Gastroesophageal Junction Carcinomas, NCT00620607
Ref 2 A Phase I Study to Assess the Safety and Pharmacokinetics of huC242-DM4 Administered as a Single Intravenous Infusion Once Every Three Weeks to Subjects With Solid Tumors, NCT00352131
Ref 3 A phase I study of a CanAg-targeted immunoconjugate, huC242-DM4, in patients with Can Ag-expressing solid tumors. Journal of Clinical Oncology 25, no. 18_suppl (June 20, 2007) 3062-3062.
Ref 4 Immunoconjugates targeting cd138 and uses thereof; 2009-07-02.

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