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Drugs Today (Barc). 2019 Apr;55(4):247-264. doi: 10.1358/dot.2019.55.4.2958476.

Encorafenib and binimetinib for the treatment of BRAF V600E/K-mutated melanoma.

Author information

1
Department of Medicine, Division of Medical Oncology, University of Toronto, Toronto, Ontario, Canada. april.rose@uhn.ca.

Abstract

BRAF is a constituent of the mitogen-activated protein kinase (MAPK) signaling pathway, which serves to activate downstream MEK, and is one of the most commonly mutated oncogenes in human tumors. Indeed, BRAF V600 mutations are present in approximately 40% of metastatic melanoma tumors. Encorafenib (LGX-818, Braftovi) and binimetinib (MEK-162, Mektovi) are small-molecule inhibitors of BRAF and MEK, respectively. BRAF and MEK inhibitors have been shown to improve overall and progression-free survival among patients with metastatic melanoma. Of these inhibitors, encorafenib and binimetinib are the newest combination, which received approval by the Food and Drug Administration (FDA) for the treatment of BRAF V600E/K-mutated melanoma in June 2018. This review will focus on the preclinical pharmacology, pharmacokinetics and clinical utility of encorafenib and binimetinib in BRAF V600-mutated melanoma.

KEYWORDS:

BRAF V600 mutation; BRAF inhibitors; Binimetinib; Encorafenib; MEK inhibitors; Melanoma

PMID:
31050693
DOI:
10.1358/dot.2019.55.4.2958476
[Indexed for MEDLINE]

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