Avutometinib Explained

Elimination Half-Life:60 h (45.8–93.7 h)
Cas Number:946128-88-7
Pubchem:16719221
Drugbank:DB15254
Chemspiderid:17623621
Unii:D0D4252V97
Kegg:D12515
Chebi:78825
Chembl:3264002
Pdb Ligand:CHU
Synonyms:RO-5126766; CH-5126766; CKI-27; R-7304; RG-7304
Iupac Name:3-3-fluoro-2-(methylsulfamoylamino)pyridin-4-ylmethyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one| C=21 | H=18 | F=1 | N=5 | O=5 | S=1| SMILES = CC1=C(C(=O)OC2=C1C=CC(=C2)OC3=NC=CC=N3)CC4=C(C(=NC=C4)NS(=O)(=O)NC)F| StdInChI = 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)| StdInChIKey = 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

}

Notes and 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 . 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 . July 2013 . 23667175 . 4115369 . 10.1158/0008-5472.CAN-12-3937.
  2. News: Adams . Ben . Verastem pens KRAS-focused drug licensing deal with Chugai . Fierce Biotech . 2020-01-08 . 2022-06-05.
  3. Web site: Drug Profile: Avutometinib . PDF . AdisInsight . 2022-05-23 . 2022-06-05 . subscription.