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.


Allikas: https://en.wikipedia.org/wiki/Avutometinib
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