General Information of This Linker
Linker ID
LIN0UQJNN
Linker Name
Amide-based linker
Linker Type
Flexible reactive (amino) linker
Antibody-Linker Relation
Uncleavable
Structure
Formula
C6H13NO
Isosmiles
CC(C)CCC(N)=O
InChI
InChI=1S/C6H13NO/c1-5(2)3-4-6(7)8/h5H,3-4H2,1-2H3,(H2,7,8)
InChIKey
ACMPWZQOUILVFB-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
115.176
Polar area
43.09
Complexity
8
xlogp Value
0.9079
Heavy Count
8
Rot Bonds
3
Hbond acc
1
Hbond Donor
1
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
CMB-401 [Terminated in phase 2]
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
Platinum-sensitive EOC (recurrence >6 months after completion of an initial platinumcontaining chemotherapy regimen).
Administration Dosage
Initial infusion of 35 mg/m2 of hCTM01 (anti-PEM antibody not conjugated to calicheamicin) over a period of 15 min, followed 45 min later (60 min from the start of the initial infusion) by an infusion of 16 mg/m2 of CMB-401 over an additional 60 min, up to 7 cycles, with 4 weeks between cycles.
Experiment 2 Reporting the Activity Date of This ADC [2]
Patients Enrolled
EOC refractory to or unsuitable for platinum/standard therapy; with a WHO performance status of 0-2; life expectancy of more than three months and fulfilling other standard eligibility criteria.
Administration Dosage
Up to four cycles of a dual infusion of 35.00 mg/m2 hCTMO1 'predose' followed by doses of CMB-401 which were increased for each cohort, CMB-401 dosing commenced at 2 mg/m2 and progressed via seven cohorts to 16.00 mg/m2.
References
Ref 1 A phase 2 study of the cytotoxic immunoconjugate CMB-401 (hCTM01-calicheamicin) in patients with platinum-sensitive recurrent epithelial ovarian carcinoma. Cancer Immunol Immunother. 2003 Apr;52(4):243-8.
Ref 2 Phase I open study of the effects of ascending doses of the cytotoxic immunoconjugate CMB-401 (hCTMO1-calicheamicin) in patients with epithelial ovarian cancer. Ann Oncol. 2000 Jun;11(6):735-41.

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