BRAF inhibitors: encorafenib (LGX818)

BRAF targets in melanoma. Biological mechanisms, resistance, and drug discovery. Cancer drug discovery and development. Volume 82. Ed. Ryan J. Sullivan. Springer (2015)


Encorafenib (LGX818; Novartis) is a selective BRAF inhibitor currently undergoing phase II and III testing. This agent has a longer dissociation time compared to available BRAF inhibitors which may confer additional activity. In a phase I trial, 16 of 24 (67%) BRAF inhibitor naпve patients experienced partial responses [13]. Among patients pre-treated with other BRAF inhibitors, the response rate was < 10%. Toxicities were similar to vemurafenib and dabrafenib although palmar-plantar erythrodysesthesia was observed more frequently and only two patients developed cSCCs. Ongoing development is focused on monotherapy across malignancies harboring BRAF mutations and on combination therapy with other agents in advanced melanoma.

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