Binimetinib binimetinib

Drug Class

MEK inhibitor

Mechanism

Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2, blocking the MAPK pathway in BRAF-mutant cancer cells.

Approved Indication

Treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with encorafenib.

What This Means For Patients

Binimetinib is a targeted MEK inhibitor approved for use in combination with encorafenib to treat patients with advanced melanoma carrying BRAF V600 mutations. It works by blocking signaling proteins that promote cancer cell division. Although not fully approved by NMPA in China (under review as of early 2025), it can be accessed by eligible patients in the Boao Lecheng pilot zone.

Regulatory Approvals

• FDA — approved (2018) — label
• EMA — approved (2018) — source

Pivotal Clinical Evidence

• COLUMBUS — Dummer et al., Lancet Oncol 2018 (NCT01909453) — DOI

Sources

• https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210498s000lbl.pdf
• https://www.ema.europa.eu/en/medicines/human/EPAR/mektovi
• https://doi.org/10.1016/S1470-2045(18)30142-6