Avutometinib is an inhibitor of MEK1 and RAF used alongside a FAK inhibitor for the treatment of recurrent low-grade serous ovarian cancer. Avutometinib is a small molecule kinase inhibitor targeted against RAF/MEK1, key regulators of the RAS/RAF/MEK/ERK (MAPK) pathway.
- Mechanism
- Curator reviewed · 2 references
The RAS/RAF/MEK/extracellular signal-regulated kinase (ERK) signaling pathway is often dysregulated in human cancers and plays a key role in tumor cell proliferation, differentiation and survival.
Upon oral administration, avutometinib specifically targets, binds to, and inhibits the kinase activities of Raf and MEK, resulting in the inhibition of Raf/MEK-mediated signal transduction pathways. Treatment of cancer cells with avutometinib increases the level of phosphorylated focal adhesion kinase (FAK), so it is used in conjunction with defactinib, an inhibitor of FAK.
- Primary indication
- Avutometinib is indicated in combination with defactinib 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
- C21H18FN5O5S · 471.46 g/mol (avg)
- First approval
- United States, 2025
- Also known as
- RO-5126766 free base
- Code names
- CH-5126766 · CKI-27 · R-7304 · RG-7304 · RO-5126766 · VS-6766
- Brand names
Resolves to
LMMJFBMMJUMSJS-UHFFFAOYSA-NSMILESCNS(=O)(=O)NC1=C(F)C(CC2=C(C)C3=C(OC2=O)C=C(OC2=NC=CC=N2)C=C3)=CC=N1What you can answer from here — as of September 13, 2026
Which drugs share a target with Avutometinib, and which of those have an active Phase 3 trial?
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