Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0DIWSF
ADC Name	Cantuzumab mertansine
Synonyms	C242 maytansinoid conjugate; huC242 maytansinoid conjugate; Monoclonal antibody C-242 DM1 conjugate; Monoclonal antibody C-242 May conjugate; Monoclonal antibody huC242-May conjugate; huC242-DM1; SB-408075; C-242 May; C-242 DM1 Click to Show/Hide
Organization	ImmunoGen, Inc.
Drug Status	Terminated in phase 1
Indication	In total 1 Indication(s) Solid tumors [ICD11:2A00-2A0Z\|2B50-2F9Z] Terminated in phase 1
Drug-to-Antibody Ratio	4
Structure
	3D MOL	2D MOL
Antibody Name	Cantuzumab		Antibody Info
Antigen Name	Syndecan-1 (SDC1)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	N-succinimidyl 4-(2-pyridyldithio) pentanoate (SPP)		Linker Info
Conjugate Type	Random conjugation through nucleophilic lysines.
Combination Type	Mertansine
Puchem SID	472397977 , 135315063 , 476269507 , 476262822 , 17397513 , 480408953 , 160687954
Drugbank ID	DB17239
TTD ID	D0N3JT
ChEBI ID	CHEMBL1742997

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. Click to Show/Hide
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. Click to Show/Hide

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			[1]
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			[2]
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 in a three-times a week schedule: a phase I and pharmacokinetic study. Cancer Chemother Pharmacol. 2008 Oct;62(5):911-9.
Ref 2	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.