Selumetinib in the Treatment of Non-Small-Cell Lung Cancer | Zendy

Reyes Bernabé | Zendy; Ana Sofia Patrão | Zendy; Louise Carter | Zendy; Fiona Blackhall | Zendy; Emma Dean | Zendy

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Selumetinib in the Treatment of Non-Small-Cell Lung Cancer

Author(s) -

Reyes Bernabé,

Ana Sofia Patrão,

Louise Carter,

Fiona Blackhall,

Emma Dean

Publication year - 2016

Publication title -

future oncology

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.857

H-Index - 72

eISSN - 1744-8301

pISSN - 1479-6694

DOI - 10.2217/fon-2016-0132

Subject(s) - selumetinib , medicine , kras , tolerability , lung cancer , docetaxel , oncology , mek inhibitor , chemotherapy , targeted therapy , mapk/erk pathway , cancer , pharmacodynamics , cancer research , pharmacology , pharmacokinetics , kinase , adverse effect , colorectal cancer , biology , microbiology and biotechnology

The 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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