Drug intelligence / Profile preview

avutometinib

Development stage
Phase 3
Lead developer
Verastem Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

Avutometinib is an oral small molecule kinase inhibitor that targets both MEK1 and RAF kinases. It is used 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. Avutometinib’s unique mechanism blocks both MEK kinase activity and the ability of RAF to phosphorylate MEK, thereby inhibiting the MAPK pathway without compensatory activation that can limit efficacy in other inhibitors. The drug was developed by Chugai Pharmaceutical and further developed by Amgen, Eli Lilly and Company, and Verastem Oncology[4][6][9]. It received accelerated FDA approval in May 2025 as part of a co-packaged regimen (Avmapki Fakzynja Co-Pack) with defactinib[1][2][5].

Brand names
Avmapki Fakzynja Co-Pack
Other names
avutometinib potassium
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)RAF1 (c-Raf-1 (Y340D/Y341D))MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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