refametinib

Refametinib is an orally bioavailable, highly potent, and selective small molecule inhibitor of mitogen‑activated protein kinase kinases 1 and 2 (MEK1/2). It acts as a non‑ATP competitive, allosteric inhibitor by binding to an allosteric pocket adjacent to the ATP binding site on MEK1/2, locking the enzyme in a catalytically inactive conformation. This inhibition disrupts the MAPK/ERK signaling pathway, leading to reduced tumor cell proliferation and cell cycle arrest. Refametinib has demonstrated antineoplastic activity in preclinical models and was investigated for use in various solid tumors including liver cancer (hepatocellular carcinoma), pancreatic cancer, biliary cancer, and other solid tumors. The drug was originally developed by Valeant Pharmaceuticals International and further developed by Ardea Biosciences (a subsidiary of AstraZeneca) and Bayer HealthCare[1][3][5][6].

Other names

refametinib