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Selumetinib in the treatment of non-small-cell lung cancer.

dc.contributor.authorBernabé, Reyes
dc.contributor.authorPatrao, Ana
dc.contributor.authorCarter, Louise
dc.contributor.authorBlackhall, Fiona H
dc.contributor.authorDean, Emma J
dc.date.accessioned2016-10-12T13:08:21Z
dc.date.available2016-10-12T13:08:21Z
dc.date.issued2016-07-28
dc.identifier.citationSelumetinib in the treatment of non-small-cell lung cancer. 2016: Future Oncolen
dc.identifier.issn1744-8301
dc.identifier.pmid27467210
dc.identifier.doi10.2217/fon-2016-0132
dc.identifier.urihttp://hdl.handle.net/10541/619941
dc.description.abstractThe RAS-RAF-MEK-ERK pathway regulates processes involved in the proliferation and survival of cells. KRAS mutations, prevalent in approximately 30% of patients with non-small-cell lung cancer (NSCLC), result in constitutive activation of the pathway. Selumetinib (AZD6244, ARRY-142886) is a potent and selective inhibitor of MEK1/2 which has demonstrated significant efficacy in combination with docetaxel in patients with KRAS mutant pretreated advanced NSCLC. Several trials in combination with other chemotherapy and targeted therapy regimens in lung cancer are ongoing. We review the development of selumetinib in patients with NSCLC, summarize the pharmacodynamic, pharmacokinetic and tolerability characteristics, and the available clinical trial data to understand the role of selumetinib in the treatment of NSCLC.
dc.languageENG
dc.language.isoenen
dc.rightsArchived with thanks to Future oncology (London, England)en
dc.titleSelumetinib in the treatment of non-small-cell lung cancer.en
dc.typeArticleen
dc.contributor.departmentThe Christie NHS Foundation Trust, Manchester, UKen
dc.identifier.journalFuture Oncologyen
html.description.abstractThe RAS-RAF-MEK-ERK pathway regulates processes involved in the proliferation and survival of cells. KRAS mutations, prevalent in approximately 30% of patients with non-small-cell lung cancer (NSCLC), result in constitutive activation of the pathway. Selumetinib (AZD6244, ARRY-142886) is a potent and selective inhibitor of MEK1/2 which has demonstrated significant efficacy in combination with docetaxel in patients with KRAS mutant pretreated advanced NSCLC. Several trials in combination with other chemotherapy and targeted therapy regimens in lung cancer are ongoing. We review the development of selumetinib in patients with NSCLC, summarize the pharmacodynamic, pharmacokinetic and tolerability characteristics, and the available clinical trial data to understand the role of selumetinib in the treatment of NSCLC.


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