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

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.

History of changes in PMDA indication

2019-01-08: New approval for the treatment of unresectable melanoma with BRAF gene mutation.
2020-11-27: New indication and a new dosage for the treatment of unresectable, advanced or recurrent BRAF mutation-positive colorectal cancer that has progressed after cancer chemotherapy.

Also known as

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