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Temuterkib (LY3214996) is an orally available, highly selective small molecule inhibitor of extracellular signal-regulated kinase 1 and 2 (ERK1/2). It acts by inhibiting ERK1/2, thereby blocking the activation of the mitogen-activated protein kinase (MAPK)/ERK signaling pathway, which is frequently dysregulated in cancers with mutations in BRAF, RAS, MAP2K1/2, or NF1. This inhibition disrupts cell proliferation and survival signals that drive tumor growth. Temuterkib has demonstrated antitumor activity in preclinical models and is being evaluated clinically for advanced cancers harboring MAPK pathway alterations. The drug was developed by Eli Lilly.
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