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

被引：16

作者：

Bernabe, Reyes ^{[1
,2
]}

Patrao, Ana ^{[1
]}

Carter, Louise ^{[1
]}

Blackhall, Fiona ^{[1
,3
]}

Dean, Emma ^{[1
,3
]}

机构：

[1] Christie NHS Fdn Trust, Manchester, Lancs, England

[2] Hosp Valme, Seville, Spain

[3] Univ Manchester, Manchester, Lancs, England

来源：

FUTURE ONCOLOGY | 2016年 / 12卷 / 22期

关键词：

MEK inhibitor; non-small-cell lung cancer; selumetinib; PHASE-II TRIAL; ORAL MEK INHIBITOR; KRAS-MUTANT; OPEN-LABEL; AZD6244; ARRY-142886; CLINICAL-TRIAL; PLUS DOCETAXEL; MULTICENTER; EFFICACY; CHEMOTHERAPY;

D O I：

10.2217/fon-2016-0132

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

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.

引用

页码：2545 / 2560

页数：16

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