Avutometinib

Avutometinib (INN; codenamed RO-5126766, CH-5126766, CKI-27, R-7304, RG-7304, and VS-6766 at various stages of its development) is an inhibitor of Ras-Raf-MEK-ERK signaling being developed as a potential treatment for cancer.

Avutometinib

Skeletal formula and ball-and-stick model of avutometinib
Clinical data
Other names	RO-5126766; CH-5126766; CKI-27; R-7304; RG-7304
Pharmacokinetic data
Elimination half-life	60 h (45.8–93.7 h)
Identifiers
IUPAC name 3-[[3-fluoro-2-(methylsulfamoylamino)pyridin-4-yl]methyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one
CAS Number	946128-88-7
PubChem CID	16719221
DrugBank	DB15254
ChemSpider	17623621
UNII	D0D4252V97
KEGG	D12515
ChEBI	CHEBI:78825
ChEMBL	ChEMBL3264002
PDB ligand	CHU (PDBe, RCSB PDB)
Chemical and physical data
Formula	C21H18FN5O5S
Molar mass	471.46 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=C(C(=O)OC2=C1C=CC(=C2)OC3=NC=CC=N3)CC4=C(C(=NC=C4)NS(=O)(=O)NC)F
InChI InChI=1S/C21H18FN5O5S/c1-12-15-5-4-14(31-21-25-7-3-8-26-21)11-17(15)32-20(28)16(12)10-13-6-9-24-19(18(13)22)27-33(29,30)23-2/h3-9,11,23H,10H2,1-2H3,(H,24,27) Key:LMMJFBMMJUMSJS-UHFFFAOYSA-N

It was discovered by Chugai Pharmaceutical Co. (a subsidiary of Roche) through derivatization of a hit compound identified by high-throughput screening.^[1] It was licensed by Verastem Oncology in 2020 for clinical trials.^[2][3]

The co-packaged medication avutometinib/defactinib was approved for medical use in the United States in May 2025.^[4][5]