BRAF targets in melanoma. Biological mechanisms, resistance, and drug discovery. Cancer drug discovery and development. Volume 82. Ed. Ryan J. Sullivan. Springer (2015)
Trametinib, the only currently approved MEK inhibitor, is an active therapy and is superior to cytotoxic chemotherapy. The single agent activity appears to be somewhat inferior to vemurafenib or dabrafenib with a lower response rate and lower median PFS (although no direct comparison has been performed). Trametinib has minimal benefit following progression on BRAF inhibitors and is not used widely as monotherapy currently except in patients with contraindications to vemurafenib and dabrafenib. Its role in combination therapy, however, may be much more significant. Binimetinib and other experimental MEK inhibitors may also have clinical utility in the future.
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