Avapritinib in the treatment of PDGFRA exon 18 mutated gastrointestinal stromal tumors

Gastrointestinal stromal tumors (GIST) can be molecularly classified based on different subtypes including mutations in and . Patients with mutations are an important subgroup that commonly arise in the stomach and are associated with a more indolent disease course. Importantly, the most common mole...

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Published inFuture oncology (London, England) Vol. 16; no. 22; pp. 1641 - 1648
Main Authors Smrke, Alannah, Gennatas, Spyridon, Huang, Paul, Jones, Robin L
Format Journal Article
LanguageEnglish
Published London Future Medicine Ltd 01.08.2020
Subjects
avapritinib
BLU-285
D842V
Gastrointestinal cancer
Gene expression
GIST
Kinases
Metastasis
Mutation
Patients
PDGFRA
Tumors
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Summary:Gastrointestinal stromal tumors (GIST) can be molecularly classified based on different subtypes including mutations in and . Patients with mutations are an important subgroup that commonly arise in the stomach and are associated with a more indolent disease course. Importantly, the most common molecular subtype, the D842V mutation in exon 18 of the gene which alters the activation loop, is imatinib insensitive in studies. Poor responses to imatinib have been seen clinically compared with exon 18 non-D842V-mutated GIST. Avapritinib (BLU-285) is a potent specific tyrosine kinase inhibitor which has shown >90% response rates in patients with exon 18 D842V-mutated GIST. Results from the Phase I trial of avapritinib have indicated that this drug should be the standard of care for patients with exon 18 D842V-mutated GIST.
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ISSN:1479-6694
1744-8301
DOI:10.2217/fon-2020-0348