Cobimetinib

Definition

An orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. Cobimetinib 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. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases.

Also known as COBIMETINIB, Cotellic, GDC 0973, GDC-0973, GDC0973, MEK Inhibitor GDC-0973, XL 518, XL-518, XL518 — per NCIT

Also identified as

• ATC L01EE02 per RXNORM
• NCIT NCIT:C68923 per NCIT
• SCTID 715257001 per RXNORM
• SCTID 715741000 per RXNORM
• UNII ER29L26N1X per RXNORM

Indications