Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ID: DRG0DIWSF)
ADC Name
Cantuzumab mertansine
Synonyms
cantuzumab mertansine; SB-408075; huC242-DM1; huC242-SPP-DM1
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Organization
ImmunoGen (Top20 MNC) (Originator);SmithKline Beecham (Top20 MNC)
Drug Status
Phase 1 (discontinued)
Drug-to-Antibody Ratio
3 to 4
Structure
Antibody Name
Cantuzumab
  Antibody Info 
Antigen Name
Mucin-1 (MUC1)
  Antigen Info 
Payload Name
DM1
  Payload Info 
Payload Target
Microtubule (MT)
  Target Info 
Linker Name
N-succinimidyl 4-(2-pyridyldithio) pentanoate (SPP)
  Linker Info 
Conjugate Type
Random Lysines
Combination Type
mertansine
2027 Update
The disease landscape of This ADC
2027 Update
The clinical trial pipelines of This ADC
Disease Name Phase 1 Phase 2 Phase 3 Approved
Unspecific solid tumor
1 Trials
Clinical trial identifier
https://pubmed.ncbi.nlm.nih.gov/15240523/
2027 Update
General Information of The ADMET Data Related to This ADC
Absorption
Click To Hide/Show 12 Absorption Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 216 mg·h/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 40 mg/m2.
 [2]
Maximum Observed Concentration (Cmax) 10.7 mg/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 40 mg/m2.
 [2]
Area Under the Concentration-Time Curve (AUC) 927 mg·h/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 60 mg/m2.
 [2]
Maximum Observed Concentration (Cmax) 34 mg/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 60 mg/m2.
 [2]
Area Under the Concentration-Time Curve (AUC) 1582 mg·h/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 80 mg/m2.
 [2]
Maximum Observed Concentration (Cmax) 43.5 mg/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 80 mg/m2.
 [2]
Area Under the Concentration-Time Curve (AUC) 1987 mg·h/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 96 mg/m2.
 [2]
Maximum Observed Concentration (Cmax) 51.22 mg/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 96 mg/m2.
 [2]
Area Under the Concentration-Time Curve (AUC) 2650 mg·h/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 115 mg/m2.
 [2]
Maximum Observed Concentration (Cmax) 73.5 mg/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 115 mg/m2.
 [2]
Area Under the Concentration-Time Curve (AUC) 3463 mg·h/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 138 mg/m2.
 [2]
Maximum Observed Concentration (Cmax) 80.8 mg/L
Patients received a total of 280 weekly infusions of huC242-DM1 at 138 mg/m2.
 [2]
Distribution
Click To Hide/Show 6 Distribution Data Related to This Level
Standard Type Value Units Description Reference
Volume of Distribution (Vd) 5.35 L
Patients received a total of 280 weekly infusions of huC242-DM1 at 40 mg/m2.
 [2]
Volume of Distribution (Vd) 4.04 L
Patients received a total of 280 weekly infusions of huC242-DM1 at 60 mg/m2.
 [2]
Volume of Distribution (Vd) 5.53 L
Patients received a total of 280 weekly infusions of huC242-DM1 at 80 mg/m2.
 [2]
Volume of Distribution (Vd) 4.85 L
Patients received a total of 280 weekly infusions of huC242-DM1 at 96 mg/m2.
 [2]
Volume of Distribution (Vd) 4.06 L
Patients received a total of 280 weekly infusions of huC242-DM1 at 115 mg/m2.
 [2]
Volume of Distribution (Vd) 4.58 L
Patients received a total of 280 weekly infusions of huC242-DM1 at 138 mg/m2.
 [2]
Excretion
Click To Hide/Show 8 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Clearance (CL) 39.5 mL/h/m2
Thirty-seven patients received 110 courses of cantuzumab mertansine at doses ranging from 22 to 295 mg/m2.
 [1]
Elimination Half-Life (t1/2) 41.1 h
Thirty-seven patients received 110 courses of cantuzumab mertansine at doses ranging from 22 to 295 mg/m2.
 [1]
Elimination Half-Life (t1/2) 13 h
Patients received a total of 280 weekly infusions of huC242-DM1 at 40 mg/m2.
 [2]
Elimination Half-Life (t1/2) 22 h
Patients received a total of 280 weekly infusions of huC242-DM1 at 60 mg/m2.
 [2]
Elimination Half-Life (t1/2) 39 h
Patients received a total of 280 weekly infusions of huC242-DM1 at 80 mg/m2.
 [2]
Elimination Half-Life (t1/2) 37 h
Patients received a total of 280 weekly infusions of huC242-DM1 at 96 mg/m2.
 [2]
Elimination Half-Life (t1/2) 40 h
Patients received a total of 280 weekly infusions of huC242-DM1 at 115 mg/m2.
 [2]
Elimination Half-Life (t1/2) 41 h
Patients received a total of 280 weekly infusions of huC242-DM1 at 138 mg/m2.
 [2]
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Objective Response Rate (ORR)  Undisclosed
Phase 1
A phase 1 study that patients with advanced solid tumors and documented CanAg expression were treated with escalating doses of cantuzumab mertansine IV administered three-times a week in a 3 out of 4 weeks schedule. Twenty patients (pts) with colon (11/20),rectal carcinomas (2/20),or other malignancies (7/20) were treated with doses ranging from 30 to 60 mg/m2 per day of cantuzumab mertansine IV three-times a week.

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Undisclosed  Undisclosed
Phase 1
Patients with CanAg-expressing solid malignancies were treated with escalating doses of cantuzumab mertansine administered IV every 3 weeks. Thirty-seven patients received 110 courses of cantuzumab mertansine at doses ranging from 22 to 295 mg/m2.

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Full List of Activity Data of This Antibody-drug Conjugate
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 [3]
Efficacy Data Objective Response Rate (ORR)
0%
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 [4]
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 Cantuzumab mertansine, a maytansinoid immunoconjugate directed to the CanAg antigen: a phase I, pharmacokinetic, and biologic correlative study
Ref 2 A phase I study of cantuzumab mertansine administered as a single intravenous infusion once weekly in patients with advanced solid tumors
Ref 3 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 4 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.