Linker Information

General Information of This Linker
Linker ID
LIN0IUSXC
Linker Name
Caproyl acid
Antibody-Linker Relation
Uncleavable
Structure
Formula
C6H12O2
Isosmiles
CCCCCC(=O)O
InChI
InChI=1S/C6H12O2/c1-2-3-4-5-6(7)8/h2-5H2,1H3,(H,7,8)
InChIKey
FUZZWVXGSFPDMH-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
116.16
Polar area
37.3
Complexity
116.0837296
xlogp Value
1.6513
Heavy Count
8
Rot Bonds
4
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
Aprutumab ixadotin [Phase 1 (Terminated)]
 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
Advanced solid tumors from cancer indications known to be FGFR2-positive, which were refractory to any standard therapy or had no standard therapy available, patients were required to have measurable disease, Eastern Cooperative Oncology Group performance status (ECOG PS) of 0-1, an expected lifespan of at least 12 weeks.
Administration Dosage
The starting dose was 0.1 mg/kg body weight, with doses increased in two-fold increments up to 0.80 mg/kg, after which the dose was escalated in 0.50 mg/kg increments, intravenously on day 1 of every 21-day cycle.
Related Clinical Trial
NCT Number NCT02368951  Clinical Status Phase 1
Clinical Description
An open-label,phase 1, dose-escalation trial to evaluate the safety, tolerability, maximum tolerated dose, pharmacokinetic, and pharmacodynamics of the anti-FGFR2 antibody drug conjugate BAY1187982 in subjects with advanced solid tumors known to express FGFR2.
Primary Endpoint
Primary endpoints included safety, tolerability, and The MTD was determined to be 0.20 mg/kg.
Other Endpoint
Secondary endpoints were pharmacokinetic evaluation and tumor response to aprutumab ixadotin.
References
Ref 1 First-in-Human Phase I Study of Aprutumab Ixadotin, a Fibroblast Growth Factor Receptor 2 Antibody-Drug Conjugate (BAY 1187982) in Patients with Advanced Cancer. Target Oncol. 2019 Oct;14(5):591-601.