Antibody Information

General Information of This Antibody
Antibody ID
ANI0KQQRV
Antibody Name
Cantuzumab
Organization
ImmunoGen, Inc.
Indication
Solid tumors
Synonyms
huC242
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized IgG1-kappa
Antigen Name
Syndecan-1 (SDC1)
  Antigen Info 
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
QVQLVQSGAEVKKPGETVKISCKASDYTFTYYGMNWVKQAPGQGLKWMGWIDTTTGEPTY
AQKFQGRIAFSLETSASTAYLQIKSLKSEDTATYFCARRGPYNWYFDVWGQGTTVTVSSA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDEL
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Light Chain Sequence
DIVMTQSPLSVPVTPGEPVSISCRSSKSLLHSNGNTYLYWFLQRPGQSPQLLIYRMSNLV
SGVPDRFSGSGSGTAFTLRISRVEAEDVGVYYCLQHLEYPFTFGPGTKLELKRTVAAPSV
FIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSL
SSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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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
B-B4-DM1 [Investigative]
 ADC Info 
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 [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.90% Positive CD138 expression (CD138+++/++)
Method Description
The in vivo antitumor activity of B-B4-DM1 was evaluated in a CD138 positive OPM1 and OPM2 MM cells xenograft models. CB-17 SCID mice were inoculated subcutaneously in the interscapular area with 5x106 OPM1 (A-B) or OPM2 (C-D) MM cells. Animals were treated daily intravenously for 3 consecutive days with either vehicle alone (PBS; n = 5), unconjugated B-B4 (13.3 ug/kg; n = 5), B-B4DM1 (150 ug DM1/kg; n = 5), or control huC242-DM1 (150 ug DM1/kg; n = 5).

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In Vivo Model Multiple myeloma PDX model (PDX: OPM2)
In Vitro Model Multiple myeloma Multiple myeloma cells Homo sapiens
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 [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 27.30% Positive CD138 expression (CD138+++/++)
Method Description
The in vivo antitumor activity of B-B4-DM1 was evaluated in a CD138 positive OPM1 and OPM2 MM cells xenograft models. CB-17 SCID mice were inoculated subcutaneously in the interscapular area with 5x106 OPM1 (A-B) or OPM2 (C-D) MM cells. Animals were treated daily intravenously for 3 consecutive days with either vehicle alone (PBS; n = 5), unconjugated B-B4 (13.3 ug/kg; n = 5), B-B4DM1 (150 ug DM1/kg; n = 5), or control huC242-DM1 (150 ug DM1/kg; n = 5).

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In Vivo Model CD138-expressing OPM1 MM cells xenograft model
In Vitro Model Multiple myeloma Multiple myeloma cells Homo sapiens
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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
25.00 nM
Positive CD138 expression (CD138+++/++)
Method Description
The inhibitory activity of B-B4-DM1 against cancer cell growth was compared with B-B4 and DM1 against cancer cell growth in vitro. The cells were treated with B-B4-DM1, B-B4 and DM1 for 96 hours.
In Vitro Model Plasma cell myeloma MM1.R cells CVCL_8794
Cantuzumab ravtansine [Terminated in phase 2]
 ADC Info 
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 [2]
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 [3]
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 [4]
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 [5]
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
Cantuzumab mertansine [Terminated in phase 1]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Objective Response Rate (ORR)
0.00%
Patients Enrolled
Histological documentation of advanced or metastatic epithelial solid tumor which were likely to express the CanAg antigen, that were refractory or resistant to standard chemotherapy, or for which no effective standard therapy exists.
Administration Dosage
IV infusion at an initial dose of 30 mg/m2, three times per week for three consecutive weeks for a total of nine doses.
Experiment 2 Reporting the Activity Date of This ADC [7]
Patients Enrolled
Solid malignancies refractory to standard therapy or for whom no standard therapy existed.
Administration Dosage
IV cantuzumab mertansine was administered at a rate of 1 mg/min for 30 minutes and then increased to 3 mg/min if hypersensitivity phenomena were not observed. Treatment courses were repeated every 3 weeks.
References
Ref 1 Cytotoxic activity of the maytansinoid immunoconjugate B-B4-DM1 against CD138+ multiple myeloma cells. Blood. 2004 Dec 1;104(12):3688-96.
Ref 2 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 3 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 4 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 5 Immunoconjugates targeting cd138 and uses thereof; 2009-07-02.
Ref 6 Cantuzumab mertansine in a three-times a week schedule: a phase I and pharmacokinetic study. Cancer Chemother Pharmacol. 2008 Oct;62(5):911-9.
Ref 7 Cantuzumab mertansine, a maytansinoid immunoconjugate directed to the CanAg antigen: a phase I, pharmacokinetic, and biologic correlative study. J Clin Oncol. 2003 Jan 15;21(2):211-22.

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