Defactinib is an inhibitor of FAK used alongside a MEK1/RAF inhibitor for the treatment of recurrent low-grade serous ovarian cancer. Defactinib is a small molecule kinase inhibitor targeted against focal adhesion kinase (FAK) and proline-rich tyrosine kinase-2 (Pyk2), the two members of the FAK family of nonreceptor tyrosine kinases.
- Mechanism
- Curator reviewed · 5 references
The tyrosine kinase FAK, a signal transducer for integrins, is normally activated by binding to integrins in the extracellular matrix but may be upregulated and constitutively activated in various tumor cell types. The upregulation of FAK is a key resistance mechanism in the context of therapies that target the RAS/RAF/MEK/ERK (MAPK) pathway.
Defactinib is an inhibitor of FAK used alongside avutometinib, a RAF/MEK1 inhibitor. It prevents the integrin-mediated activation of several downstream signal transduction pathways, including those involving RAS/MEK/ERK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation, survival, and tumor angiogenesis.
- Primary indication
- Defactinib is indicated in combination with avutometinib for the treatment of adult patients with KRAS-mutated recurrent low-grade serous ovarian cancer (LGSOC) who have received prior systemic therapy.Curator reviewed · 1 structured indication
- Formula / weight
- C20H21F3N8O3S · 510.5 g/mol (avg)
- First approval
- United States, 2025
- Also known as
- N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide
- Code names
- PF-04554878 · VS-6063
- Brand names
Resolves to
FWLMVFUGMHIOAA-UHFFFAOYSA-NSMILESCNC(=O)C1=CC=C(NC2=NC=C(C(NCC3=C(N=CC=N3)N(C)S(C)(=O)=O)=N2)C(F)(F)F)C=C1What you can answer from here — as of September 12, 2026
Which drugs share a target with Defactinib, and which of those have an active Phase 3 trial?
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