avapritinib (Ayvakit) Report issue

Small molecule Orphan Drug FDA Approved FDA Fast Track FDA Breakthrough Therapy FDA Priority Review FDA

Active Ingredient History

  • Now
Blu-285 is a potent and selective inhibitor for hematologic malignancies with KIT Exon 17 Mutations. BLU-285 has demonstrated biochemical in vitro activity on the KIT exon-17 mutant enzyme, KIT D816V. Cellular activity of BLU-285 on KIT D816 mutants was measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC50= 4 and 22 nM, respectively. In vivo BLU-285 was well tolerated and has demonstrated dose-dependent antitumor efficacy. Complete tumor growth inhibition and ≥ 75% KIT kinase inhibition was observed with 10 mg/kg once daily, oral dosing of BLU-285 in the aggressive KIT exon 17 mutant driven P815 mastocytoma model grown as a solid tumor allograft as well as in a disseminated model of the disease. BLU-285 was also well tolerated in this in vivo model and had no adverse effects on body weight at either dose.   NCATS

  • SMILES: CN1C=C(C=N1)C2=CN3N=CN=C(N4CCN(CC4)C5=NC=C(C=N5)[C@@](C)(N)C6=CC=C(F)C=C6)C3=C2
  • Mol. Mass: 498.558
  • ALogP: Missing data
  • ChEMBL Molecules: Missing data
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Drug Pricing (per unit)

United States

$798.4457 - $1050.5863
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Note: This drug pricing data is preliminary, incomplete, and may contain errors.


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