AR00426032

AR00426032 is the N-demethylated active metabolite of **binimetinib**, formed primarily by the action of the cytochrome P450 enzymes CYP1A2 and CYP2C19. It is considered pharmacologically active and has been observed in plasma following the oral administration of binimetinib. Like binimetinib, AR00426032 acts as a selective, reversible, ATP-uncompetitive inhibitor of the serine/threonine kinases mitogen-activated protein kinase kinase 1 and 2 (**MEK1** and **MEK2**), important components in the MAPK/ERK signaling pathway, which is commonly dysregulated in cancers such as melanoma. The presence and relative activity of AR00426032 has been confirmed in both human plasma and preclinical metabolic studies.[1]

Other names

N-demethylated binimetinib