INTRODUCTION: Metastatic melanoma is an aggressive disease resistant to 
chemotherapy. Recent clinical trials have reported improved survival for two 
novel agents; ipilimumab, a humanized, IgG1 monoclonal antibody that blocks 
cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) and vemurafenib , a BRAF 
(v-raf murine sarcoma viral oncogene homolog B1) inhibitor targeting an 
activating mutation in the serine-threonine-protein kinase BRAF gene.
AREAS COVERED: The authors reviewed preclinical and clinical data examining the 
safety of vemurafenib in melanoma. MEDLINE and EMBASE were searched using the 
medical subject heading 'vemurafenib' and the following text terms: melanoma, 
BRAF inhibition, vemurafenib. This review provides the reader with an overview 
of current data examining the efficacy and safety of vemurafenib in metastatic 
melanoma.
EXPERT OPINION: Vemurafenib is an oral agent licensed for patients with BRAF 
V600E mutation-positive inoperable and metastatic melanoma. The most common 
adverse effects observed in Phase III clinical trials were dermatological 
events, arthralgia and fatigue. Specific dermatological toxicities included 
development of cutaneous squamous cell cancers and keratoacanthomas. 
Prolongation of the QT interval was also reported. Regular dermatological 
assessments and electrocardiograms are recommended. Ongoing trials are examining 
vemurafenib in both the adjuvant setting and metastatic setting in combination 
with ipilimumab and MEK inhibitors (mitogen-activated protein 
kinase/extracellular signal-regulated kinase). Understanding and overcoming 
mechanisms of resistance to BRAF inhibitors is the focus of ongoing research.