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Resistance to RAF Inhibitors Revisited
Journal article   Open access   Peer reviewed

Resistance to RAF Inhibitors Revisited

Edward Hartsough, Yongping Shao and Andrew E. Aplin
Journal of investigative dermatology, v 134(2), pp 319-325
01 Feb 2014
PMID: 24108405
url
https://doi.org/10.1038/jid.2013.358View
Published, Version of Record (VoR) Open

Abstract

Dermatology Life Sciences & Biomedicine Science & Technology
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.

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Dermatology
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