BRAF targets in melanoma. Biological mechanisms, resistance, and drug discovery. Cancer drug discovery and development. Volume 82. Ed. Ryan J. Sullivan. Springer (2015)
Binimetinib (MEK162; Novartis) is an experimental small molecule inhibitor of MEK1/2 with a recently completed phase II study. The response rate in the BRAF V600 mutant group was 23% with a median PFS of 3.6 months. In contrast to other MEK inhibitors, binimetinib induced responses in NRAS mutant melanoma (response rate 20%). Clinical development for this agent as monotherapy has largely focused on the 15–20% of melanomas harboring NRAS mutations. However, trials in combination with encorafenib are also ongoing for patients with BRAF mutant melanoma.