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PDGFR alpha/KIT Mutant-specific Inhibitor BLU-285

Known as: BLU-285 
An orally bioavailable inhibitor of specific mutated forms of platelet-derived growth factor receptor alpha (PDGFR alpha; PDGFRa) and mast/stem cell… Expand
National Institutes of Health

Papers overview

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2020
2020
Systemic mastocytosis (SM) has greatly benefited from the broad application of precision medicine techniques to hematolymphoid… Expand
Review
2018
Review
2018
Gastrointestinal stromal tumors (GISTs) originate from interstitial cells of Cajal and account for over 5,000 newly diagnosed… Expand
2018
2018
  • Cancer discovery
  • 2018
  • Corpus ID: 46803714
In a phase I trial of avapritinib (formerly BLU-285), which targets D816V mutant KIT, for the treatment of advanced systemic… Expand
Highly Cited
2017
Highly Cited
2017
BLU-285 is a selective and potent mutant KIT and PDGFRA inhibitor active in both preclinical and clinical settings. Treatment… Expand
2017
2017
11011Background: Oncogenic mutations in KIT or PDGFRα drive > 85% of GIST. However, primary and acquired mutations in the… Expand
2017
2017
Background: The KIT D816V mutant is a key oncogenic driver found in ~90% of AdvSM, a group of poor prognosis mast cell (MC… Expand
2017
2017
  • Cancer discovery
  • 2017
  • Corpus ID: 12802010
Tyrosine kinase inhibitors may initially control gastrointestinal stromal tumors, but most patients eventually experience disease… Expand
Review
2016
Review
2016
Background: Aggressive Systemic Mastocytosis (ASM) and the related disorders, SM with associated hematologic non-mast cell… Expand
2015
2015
The advent of imatinib therapy in gastrointestinal stromal tumor (GIST) has been transformative, altering the treatment of… Expand
2015
2015
KIT exon 17 mutants conferring ligand-independent constitutive kinase activity are known drivers of disease in both solid tumors… Expand