Avapritinib is a selective tyrosine kinase inhibitor being investigated for the treatment of multidrug resistant gastrointestinal tumors. It is one of the first medications available for the treatment of multidrug resistant cancers.
- Mechanism
- Curator reviewed · 3 references
Avapritinib has a negative modulating effect on the transporters ABCB1 and ABCG2, which mediate the multidrug resistance phenotype of some cancers. This modulation may be due to interactions of avapritinib with the drug binding pocket of these transporters. Negative modulation of these transporters, resensitizes cancerous cells to treatment with chemotherapeutic agents like paclitaxel.
- Primary indication
- Avapritinib is indicated for the treatment of adults with unresectable or metastatic GIST harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations.Curator reviewed · 7 structured indications
- Formula / weight
- C26H27FN10 · 498.57 g/mol (avg)
- First approval
- Canada, 2024 · United States, 2020 · European Union, 2020
- Code names
- 70C366 · BLU-285 · C-366 · CS3007 · X-720776
- Brand names
Resolves to
DWYRIWUZIJHQKQ-SANMLTNESA-NSMILESCN1C=C(C=N1)C1=CN2N=CN=C(N3CCN(CC3)C3=NC=C(C=N3)[C@@](C)(N)C3=CC=C(F)C=C3)C2=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Avapritinib, and which of those have an active Phase 3 trial?
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