GDC-0973 Cobimetinib

Cobimetinib, also known as GDC-0973 and XL-518 , is an orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. MEK inhibitor GDC-0973 specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types.

MEK Inhibitor Related Products:

Selumetinib; Mirdametinib (PD0325901); Trametinib; PD184352 (CI-1040); PD98059; BIX02189; U0126-EtOH; Pimasertib; BIX02188; TAK-733; Binimetinib (MEK162); SL327; Refametinib; GDC-0623; RO5126766 (CH5126766); APS-2-79 hydrochloride; AZD8330

[1]. Hoeflich KP, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72(1):210-9.

[2]. Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43.