Dabrafenib: A narrative drug review

Abstract

Activating mutations in the BRAF gene lead to an unregulated downstream signaling of the MAPK/extracellular-signal-regulated kinase pathway. This pathway is implicated in a range of solid tumors, and BRAF inhibitors are an attractive option in the treatment of these cancers. At present, three BRAF inhibitors have received the Food and Drug Administration approval for the treatment of cancer, namely, dabrafenib, vemurafenib, and encorafenib. Dabrafenib is approved for the treatment of advanced melanomas, anaplastic thyroid cancers, non-small cell lung cancers, and for the adjuvant treatment of melanomas harboring the BRAF V600E/K mutation. This review of dabrafenib describes its chemistry, pharmacokinetics, interactions, clinical indications, and safety profile. We identified and included studies from the PubMed database using search terms “dabrafenib”, “trametinib” or “pharmacology” for qualitative synthesis.

Keywords

• anaplastic thyroid cancer
• braf
• dabrafenib
• melanoma
• non-small cell lung cancer