Avapritinib in the treatment of PDGFRA exon 18 mutated gastrointestinal stromal tumors.
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Embargo End Date
ICR Authors
Authors
Smrke, A
Gennatas, S
Huang, P
Jones, RL
Gennatas, S
Huang, P
Jones, RL
Document Type
Journal Article
Date
2020-08-01
Date Accepted
Abstract
Gastrointestinal stromal tumors (GIST) can be molecularly classified based on different subtypes including mutations in KIT and PDGFRA. Patients with PDGFRA mutations are an important subgroup that commonly arise in the stomach and are associated with a more indolent disease course. Importantly, the most common PDGFRA molecular subtype, the D842V mutation in exon 18 of the gene which alters the activation loop, is imatinib insensitive in in vitro studies. Poor responses to imatinib have been seen clinically compared with PDGFRA exon 18 non-D842V-mutated GIST. Avapritinib (BLU-285) is a potent KIT and PDGFRA-specific tyrosine kinase inhibitor which has shown >90% response rates in patients with PDGFRA 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 PDGFRA exon 18 D842V-mutated GIST.
Citation
Future oncology (London, England), 2020, 16 (22), pp. 1639 - 1646
Source Title
Publisher
TAYLOR & FRANCIS LTD
ISSN
1479-6694
eISSN
1744-8301
Collections
Research Team
Molecular and Systems Oncology