Avutometinib
Clinical data
Other namesRO-5126766; CH-5126766; CKI-27; R-7304; RG-7304
Pharmacokinetic data
Elimination half-life60 h (45.8–93.7 h)
Identifiers
  • 3-[[3-fluoro-2-(methylsulfamoylamino)pyridin-4-yl]methyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
Chemical and physical data
FormulaC21H18FN5O5S
Molar mass471.46 g·mol−1
3D model (JSmol)
  • CC1=C(C(=O)OC2=C1C=CC(=C2)OC3=NC=CC=N3)CC4=C(C(=NC=C4)NS(=O)(=O)NC)F
  • 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


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.

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]

References

  1. Ishii N, Harada N, Joseph EW, Ohara K, Miura T, Sakamoto H, Matsuda Y, Tomii Y, Tachibana-Kondo Y, Iikura H, Aoki T, Shimma N, Arisawa M, Sowa Y, Poulikakos PI, Rosen N, Aoki Y, Sakai T (July 2013). "Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity". Cancer Res. 73 (13): 4050–4060. doi:10.1158/0008-5472.CAN-12-3937. PMC 4115369. PMID 23667175.
  2. Adams, Ben (2020-01-08). "Verastem pens KRAS-focused drug licensing deal with Chugai". Fierce Biotech. Retrieved 2022-06-05.
  3. "Drug Profile: Avutometinib" (PDF). AdisInsight. 2022-05-23. Retrieved 2022-06-05.


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