Resistance to RAF Inhibitors Revisited

被引：63

作者：

Hartsough, Edward ^{[1
]}

Shao, Yongping ^{[1
]}

Aplin, Andrew E. ^{[1
,2
]}

机构：

[1] Thomas Jefferson Univ, Dept Canc Biol, Philadelphia, PA 19107 USA

[2] Thomas Jefferson Univ, Dept Dermatol & Cutaneous Biol, Philadelphia, PA 19107 USA

来源：

JOURNAL OF INVESTIGATIVE DERMATOLOGY | 2014年 / 134卷 / 02期

关键词：

ACQUIRED-RESISTANCE; FEEDBACK INHIBITION; DRIVEN RESISTANCE; IMPROVED SURVIVAL; ADVANCED MELANOMA; BRAF INHIBITION; MEK INHIBITION; OPEN-LABEL; PHASE-II; VEMURAFENIB;

D O I：

10.1038/jid.2013.358

中图分类号：

R75 [皮肤病学与性病学];

学科分类号：

100206 ;

摘要：

In early 2011, we reviewed the initial success of the RAF inhibitor vemurafenib in mutant V600 BRAF melanoma patients. It was soon evident that the response to RAF inhibitor is heterogeneous and that the short-term benefits are burdened by the development of resistance. The field has progressed rapidly with the Food and Drug Administration approval of vemurafenib and the development of other RAF and MEK (mitogen-activated protein kinase/extracellular signal-regulated kinase) inhibitors. Despite these advances, the issue of RAF inhibitor resistance remains. Here, we review recent clinical advances in the field, the growing number of resistance mechanisms, preclinical evidence for combinatorial trials using RAF inhibitors as the building blocks, and the new challenges that are arising.

引用

页码：319 / 325

页数：7

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