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Resistance to Raf inhibition in cancer.

ABSTRACT: The use of small molecule BRAF inhibitors has revolutionized the treatment of advanced melanoma. Despite this, resistance is commonplace and associated with a median progression-free survival of >5 months. Major resistance mechanisms include reactivation of the MAPK pathway and increased PI3K/AKT signaling. Here we review some of the combination therapeutic strategies currently undergoing evaluation for the management of acquired drug resistance in melanoma.

SUBMITTER: Haarberg HE 

PROVIDER: S-EPMC4031441 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature

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Resistance to Raf inhibition in cancer.

Haarberg H Eirik HE   Smalley Keiran S M KS  

Drug discovery today. Technologies 20140301

The use of small molecule BRAF inhibitors has revolutionized the treatment of advanced melanoma. Despite this, resistance is commonplace and associated with a median progression-free survival of >5 months. Major resistance mechanisms include reactivation of the MAPK pathway and increased PI3K/AKT signaling. Here we review some of the combination therapeutic strategies currently undergoing evaluation for the management of acquired drug resistance in melanoma. ...[more]