Avapritinib: a new tyrosine kinase inhibitor for treatment of advanced gastrointestinal stromal tumors. The literature review and clinical case

• Main Authors: Daria A. Filonenko, Bela M. Medvedeva, Andrey A. Meshcheryakov
• Format: Article
• Language: Russian
• Published: IP Habib O.N. 2021-02-01
• Series: Современная онкология
• Subjects: gastrointestinal stromal tumors; pdgfra; avapritinib; blu-285; ayvakit
• Online Access: https://modernonco.orscience.ru/1815-1434/article/viewFile/61163/44252

We have three drugs for treatment of gastrointestinal stromal tumors (GIST): imatinib, sunitinib and regorafenib. Avapritinib (Ayvakit, BLU-285) is one more drug that was approved in January 2020. Avapritinib is a new selective tyrosine kinase inhibitor of PDGFRA and KIT mutations. Based on NAVIGATOR trial avapritinib was approved by FDA for treatment of PDGFRA exon 18 mutant GIST including D842V. Avapritinib was included in NCCN guidelines in the first line therapy PDGFRA D842V mutant GIST. There are only several cases describe imatinib and regorafenib efficacy in D842V mutation in the literature. Avapritinib is the first drug with high efficacy in D842V mutant GIST. Avapritinib has high efficacy against second mutations that explain its activity in 4 lines of treatment. This article summarizes the results of NAVIGATOR trial and describes a clinical case of the patient with advanced GIST who received avapritinib in 6th line of treatment. Partial response was achieved that lasted 9 months. The earliest side effects were periorbital edema and increased lacrimation. Three months later the dose of аvapritinib was reduced because of hematological toxicity.