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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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2019
2019
The frequent occurrence of multidrug resistance (MDR) conferred by the overexpression of ATP-binding cassette (ABC) transporters… Expand
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2019
2019
Mutations in two type-3 receptor tyrosine kinases (RTKs), KIT and FLT3, are common in both acute myeloid leukaemia (AML) and… Expand
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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
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2017
2017
BLU-285 is a selective and potent mutant KIT and PDGFRA inhibitor active in both preclinical and clinical settings. Treatment… Expand
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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
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2017
2017
11011Background: Oncogenic mutations in KIT or PDGFRα drive > 85% of GIST. However, primary and acquired mutations in the… Expand
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2017
2017
  • Cancer discovery
  • 2017
  • Corpus ID: 12802010
Tyrosine kinase inhibitors may initially control gastrointestinal stromal tumors, but most patients eventually experience disease… Expand
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2015
2015
The advent of imatinib therapy in gastrointestinal stromal tumor (GIST) has been transformative, altering the treatment of… Expand
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2015
2015
KIT exon 17 mutants conferring ligand-independent constitutive kinase activity are known drivers of disease in both solid tumors… Expand
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