PDGFR alpha/KIT Mutant-specific Inhibitor BLU-285
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Systemic mastocytosis (SM) has greatly benefited from the broad application of precision medicine techniques to hematolymphoid… Expand Gastrointestinal stromal tumors (GISTs) originate from interstitial cells of Cajal and account for over 5,000 newly diagnosed… Expand In a phase I trial of avapritinib (formerly BLU-285), which targets D816V mutant KIT, for the treatment of advanced systemic… Expand BLU-285 is a selective and potent mutant KIT and PDGFRA inhibitor active in both preclinical and clinical settings. Treatment… Expand 11011Background: Oncogenic mutations in KIT or PDGFRα drive > 85% of GIST. However, primary and acquired mutations in the… Expand Background: The KIT D816V mutant is a key oncogenic driver found in ~90% of AdvSM, a group of poor prognosis mast cell (MC… Expand Tyrosine kinase inhibitors may initially control gastrointestinal stromal tumors, but most patients eventually experience disease… Expand Background: Aggressive Systemic Mastocytosis (ASM) and the related disorders, SM with associated hematologic non-mast cell… Expand The advent of imatinib therapy in gastrointestinal stromal tumor (GIST) has been transformative, altering the treatment of… Expand KIT exon 17 mutants conferring ligand-independent constitutive kinase activity are known drivers of disease in both solid tumors… Expand