Linker Information

General Information of This Linker
Linker ID
LIN0YDWRB
Linker Name
Maleimido-caproyl based linker
Linker Type
Flexible reactive (thiol) linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C16H25N3O5
Isosmiles
NCCCCC(NC(=O)CCCCCN1C(=O)C=CC1=O)C(=O)O
InChI
InChI=1S/C16H25N3O5/c17-10-4-3-6-12(16(23)24)18-13(20)7-2-1-5-11-19-14(21)8-9-15(19)22/h8-9,12H,1-7,10-11,17H2,(H,18,20)(H,23,24)
InChIKey
OQMSUSITQGKAEJ-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
339.392
Polar area
129.8
Complexity
24
xlogp Value
0.1702
Heavy Count
24
Rot Bonds
12
Hbond acc
5
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
MEDI4276 [Phase 1/2 (discontinued)]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Patients Enrolled
Eligibility requires HER2+ advanced breast/gastric cancer patients (age&ge;18) with prior HER2-targeted therapy and measurable disease (RECIST 1.1), excluding recent anticancer treatment (<28 days), excessive anthracycline exposure, or active brain metastases.
Administration Dosage
Participants received IV dose of 0.05 mg/kg MEDI4276 every three weeks (Q3W) for 2 years.
Related Clinical Trial
NCT Number NCT02576548  Clinical Status PHASE1
Clinical Description
A Phase 1/2 Multicenter, Open-label, Dose-escalation, and Dose-expansion Study to Evaluate the Safety, Pharmacokinetics, Immunogencity, and Antitumor Activity of MEDI4276 in Subjects With Select HER2-expressing Advanced Solid Tumors
Primary Endpoint
Primary endpoints include safety assessment (AEs/SAEs/DLTs) to determine MTD, with monitoring through 90 days post-MEDI4276 dose, covering lab tests, vital signs, and ECGs for comprehensive safety profile evaluation.
Other Endpoint
Secondary objectives evaluate efficacy (ORR/PFS/OS over 3 years) and PK/immunogenicity (Cmax/AUC/ADA incidence within 30 days post-treatment), measuring tumor response and drug exposure while tracking antibody development.
References
Ref 1 A Phase 1/2 Study of MEDI4276 in Adults Subjects With Select HER2-expressing Advanced Solid Tumors.