Linker Information

General Information of This Linker
Linker ID
LIN0YXWRQ
Linker Name
Mal-Val-Cit
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C20H32N6O7
Isosmiles
CCC(NCCNC(=O)CCCN1C(=O)C=CC1=O)C(=O)NC(CCCNC(N)=O)C(=O)O
InChI
InChI=1S/C20H32N6O7/c1-2-13(18(30)25-14(19(31)32)5-3-9-24-20(21)33)22-10-11-23-15(27)6-4-12-26-16(28)7-8-17(26)29/h7-8,13-14,22H,2-6,9-12H2,1H3,(H,23,27)(H,25,30)(H,31,32)(H3,21,24,33)
InChIKey
VOSBZJYYHPWAPI-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
468.511
Polar area
200.03
Complexity
33
xlogp Value
-1.8061
Heavy Count
33
Rot Bonds
16
Hbond acc
7
Hbond Donor
6
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
MDX-1203 [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 [1]
Patients Enrolled
Advanced or recurrent clear cell renal cell carcinoma (ccRCC) or relapsed or refractory B-non Hodgkin lymphoma (NHL), life expectancy of 12 weeks; ECOG performance status of 0-2; measurable disease by RECIST 1.1 criteria for ccRCC and by IWG 2007 criteria for B-NHL as well as adequate hematologic, renal and liver function parameters.
Administration Dosage
0.50, 1.00, 2.00, 4.00, 8.00, 15.00 mg/kg administered every 21 days in a 42 day cycle for a maximum of 17 cycles, IV.
Related Clinical Trial
NCT Number NCT00944905  Clinical Status Phase 1
Clinical Description
A phase 1, multicenter, open-label, dose-escalation, multidose study of MDX-1203 in subjects with advanced/recurrent clear cell renal cell carcinoma or relapsed/refractory B-cell non Hodgkin's lymphoma.
Primary Endpoint
The highest best tolerated dose and the recommended dose for future studies was 8 mg/kg dose.There was no MTD determined during the acute toxicity assessment window according to protocol-defined DLT according to protocol-defined DLT. There was disease stabilization in 18 of 26 patients (69.23%) without correlation with received dose.
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT00944905  Clinical Status Phase 1
Clinical Description
A phase 1, multicenter, open-label, dose-escalation, multidose study of MDX-1203 in subjects with advanced/recurrent clear cell renal cell carcinoma or relapsed/refractory B-cell non Hodgkin's lymphoma.
References
Ref 1 First-in-human multicenter phase I study of BMS-936561 (MDX-1203), an antibody-drug conjugate targeting CD70. Cancer Chemother Pharmacol. 2016 Jan;77(1):155-62.
Ref 2 A Phase I, Multicenter, Open-Label, Dose-Escalation, Multidose Study of MDX-1203 in Subjects With Advanced/Recurrent Clear Cell Renal Cell Carcinoma or Relapsed/Refractory B-Cell Non Hodgkin's Lymphoma

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