Vemurafenib for the treatment of melanoma.

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Jordan EJ, Kelly CM

Vemurafenib for the treatment of melanoma.

Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24.

PubMed ID

23094782 [ View in PubMed

]

Abstract

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.

DrugBank Data that Cites this Article

Drugs

Vemurafenib

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Vemurafenib	Serine/threonine-protein kinase B-raf	Protein	Humans	Yes	Inhibitor	Details

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Vemurafenib	Cytochrome P450 1A2	Protein	Humans	Unknown	Inhibitor	Details
Vemurafenib	Cytochrome P450 2D6	Protein	Humans	Unknown	Inhibitor	Details
Vemurafenib	Cytochrome P450 3A4	Protein	Humans	Unknown	Substrate Inducer	Details

Drug Interactions

Drugs	Interaction
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