Active Ingredient History
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
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Mastocytosis (approved 2020)
Breast Neoplasms (Phase 2)
Central Nervous System Neoplasms (Phase 1)
Colorectal Neoplasms (Phase 2)
Esophageal Neoplasms (Phase 2)
Gastrointestinal Stromal Tumors (Phase 1)
Leukemia, Mast-Cell (Phase 1)
Leukemia, Myeloid, Acute (Phase 2)
Lung Neoplasms (Phase 2)
Mastocytosis (Phase 2)
Mastocytosis, Systemic (Phase 1)
Melanoma (Phase 2)
Neoplasm Metastasis (Phase 2)
Neoplasms (Phase 2)
Sarcoma (Phase 2)
| Trial | Phase | Start Date | Organizations | Indications |
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