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Avutometinib

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Chemical compound Pharmaceutical compound
Avutometinib
Skeletal formula and ball-and-stick model of 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
IUPAC name
  • 3-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
3D model (JSmol)
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


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. It was licensed by Verastem Oncology in 2020 for clinical trials.

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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