barzolvolimab   Click here for help

GtoPdb Ligand ID: 11607

Synonyms: CDX-0159
Compound class: Antibody
Comment: Barzolvolimab (CDX-0159) is a clinical stage humanized anti-KIT IgG1 monoclonal antibody that was developed by Celldex Therapeutics (as claimed in their patent US10781267B2) [1]. CDX-0159 is a variant of CDX-0158 (a.k.a. KTN0158 [2]) that was re-engineered to improve its safety profile and increase its serum half-life. CDX-0158 was originally designed for potential to treat GIST and other KIT-dependent tumours. This original version of the antibody inhibits mutant and wild type KIT phosphorylation, reduces mast cell degranulation and mast cell numbers, and shrinks tumours in a preclinical canine model of spontaneous mast cell tumour development [2].
Bioactivity Comments
As of July 2021, we had been unable to identify a quantitative binding affinity value for the CDX-0159-KIT interaction. Affinity values for several humanised mAb constructs are presented in US10781267B2 (in the pM range), but we cannot conclusively ascertain which (if any) of these is CDX-0159.
Selectivity at catalytic receptors
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Target
Sp.
Type
Action
Reference
KIT proto-oncogene, receptor tyrosine kinase Hs Antibody Binding - - - 1
⤷ [1]