Avapritinib

DescriptionBLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively). It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.

UsesAvapritinib is a medication used for the treatment of tumors due to one specific rare mutation. Avapritinib is a potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor.

General DescriptionClass: receptor tyrosine kinase; Treatment: GIST, SM; Other name: BLU-285; Elimination half-life = 32–57 h; Protein binding = 98.8%