Vemurafenib for the treatment of melanoma.

Hdl Handle:
http://hdl.handle.net/10147/296022
Title:
Vemurafenib for the treatment of melanoma.
Authors:
Jordan, Emmet John; Kelly, Catherine M
Affiliation:
Waterford Regional Hospital, Department of Medical Oncology, Dunmore Road, Waterford, Ireland.
Citation:
Vemurafenib for the treatment of melanoma. 2012, 13 (17):2533-43 Expert Opin Pharmacother
Journal:
Expert opinion on pharmacotherapy
Issue Date:
Dec-2012
URI:
http://hdl.handle.net/10147/296022
DOI:
10.1517/14656566.2012.737780
PubMed ID:
23094782
Abstract:
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.
Item Type:
Article
Language:
en
MeSH:
Antineoplastic Agents; Drug Resistance, Neoplasm; Humans; Indoles; Melanoma; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; Sulfonamides
ISSN:
1744-7666

Full metadata record

DC FieldValue Language
dc.contributor.authorJordan, Emmet Johnen_GB
dc.contributor.authorKelly, Catherine Men_GB
dc.date.accessioned2013-07-15T12:53:48Z-
dc.date.available2013-07-15T12:53:48Z-
dc.date.issued2012-12-
dc.identifier.citationVemurafenib for the treatment of melanoma. 2012, 13 (17):2533-43 Expert Opin Pharmacotheren_GB
dc.identifier.issn1744-7666-
dc.identifier.pmid23094782-
dc.identifier.doi10.1517/14656566.2012.737780-
dc.identifier.urihttp://hdl.handle.net/10147/296022-
dc.description.abstractMetastatic 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.en_GB
dc.language.isoenen
dc.rightsArchived with thanks to Expert opinion on pharmacotherapyen_GB
dc.subject.meshAntineoplastic Agents-
dc.subject.meshDrug Resistance, Neoplasm-
dc.subject.meshHumans-
dc.subject.meshIndoles-
dc.subject.meshMelanoma-
dc.subject.meshProtein Kinase Inhibitors-
dc.subject.meshProto-Oncogene Proteins B-raf-
dc.subject.meshSulfonamides-
dc.titleVemurafenib for the treatment of melanoma.en_GB
dc.typeArticleen
dc.contributor.departmentWaterford Regional Hospital, Department of Medical Oncology, Dunmore Road, Waterford, Ireland.en_GB
dc.identifier.journalExpert opinion on pharmacotherapyen_GB
dc.description.fundingNo fundingen
dc.description.provinceMunsteren
dc.description.peer-reviewpeer-reviewen

Related articles on PubMed

All Items in Lenus, The Irish Health Repository are protected by copyright, with all rights reserved, unless otherwise indicated.