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Current and emerging strategies for the management of imatinib-refractory advanced gastrointestinal stromal tumors.


ABSTRACT: Since its approval by the US Food and Drug Administration in February 2002, the tyrosine kinase inhibitor, imatinib, has become the standard of care for patients with metastatic or unresectable KIT-positive gastrointestinal stromal tumors (GISTs). Imatinib functions by blocking the adenosine triphosphate binding site of the constitutively activated mutant KIT or platelet-derived growth factor receptor α, effectively shutting down the oncogenic signal that drives up to 90% of these tumors. In doing so, it has transformed the management of a condition previously refractory to systemic treatments and established GIST as a model for the use of targeted therapies and oncogene addiction in solid tumors. However, while more than 80% of patients will receive clinical benefit from imatinib monother

SUBMITTER: Kee D 

PROVIDER: S-EPMC3424497 | biostudies-literature | 2012 Sep

REPOSITORIES: biostudies-literature

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