INTRODUCTION: The development of selective BRAF inhibitors in patients with 
metastatic BRAF V600 mutant melanoma has proven to be an effective therapeutic 
strategy. While vemurafenib was the first approved BRAF inhibitor for this 
indication, another selective BRAF inhibitor, dabrafenib, has demonstrated 
efficacy in patients with BRAF mutant melanoma, including those with active 
brain metastases and other malignancies.
AREAS COVERED: This review covers the current role of BRAF inhibitors in 
patients with metastatic melanoma and the clinical development of dabrafenib. 
The pharmacological, safety and efficacy data are discussed from the Phases I, 
II and III studies of dabrafenib. In addition, the results of the Phase II study 
of dabrafenib in melanoma patients with active brain metastases (BREAK-MB) and 
the Phase I/II study of dabrafenib/trametinib are examined.
EXPERT OPINION: While dabrafenib has demonstrated comparable efficacy to 
vemurafenib in BRAF V600E mutant melanoma patients, the BREAK-MB and 
dabrafenib/trametinib studies have taken BRAF inhibitor strategies further with 
evidence of disease activity in patients with metastatic melanoma brain 
metastases and potential abrogation of BRAF inhibitor resistance.