Pimasertib hydrochloride

Direct inhibition of mitogen-activated protein kinase (MAPK) kinase (MEK) is a promising strategy in the development of cancer therapeutics to control tumor growth which depends upon aberrant MAPK signaling pathway, such as RAS and BRAF mutant cancer models. Most of the MEK inhibitors that are currently in early clinical development are selective for MEK1 and/or MEK2. Pimasertib (MSC-1936369B, AS-703026) is a highly selective, small-molecule inhibitor of the protein kinase MEK1/2. Several clinical trials are investigating its role, as single agent or in combination, in solid tumors and hematologic malignancies. This review will describe the preclinical and clinical activity of pimasertib