Binimetinib (Mektovi)

Mechanism of action

From the NCI Drug Dictionary: An orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity. Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2.

Diseases for which it is used

• Colorectal cancer, BRAF-mutated
• BRAF-mutant melanoma
• NRAS-mutant melanoma

History of changes in FDA indication

• 2018-06-27: Initial FDA approval in combination with Encorafenib (Braftovi) for patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. (Based on Clinical Trial Registry COLUMBUS])

History of changes in EMA indication

• 2018-09-20: Initial authorization

History of changes in Health Canada indication

• 2021-03-02: Initial notice of compliance in combination with encorafenib for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600 mutation, as detected by a validated test.

Also known as

• Code names: ARRY-162, ARRY-438162, MEK162
• Brand names: Mektovi