Imatinib, a selective tyrosine kinase inhibitor, is currently the standard of care first-line treatment for unresectable or metastatic gastrointestinal stromal tumour (GIST), improving survival time and delaying disease progression in many patients. Nevertheless, primary and secondary (acquired) resistance to imatinib is a substantial problem in routine clinical practice. Sunitinib is an oral, multitargeted tyrosine kinase inhibitor that was approved for the treatment of imatinib-resistant or -intolerant GIST. In the pivotal phase III study, sunitinib provided substantial clinical benefits including disease control and superior survival versus placebo as second-line treatment. Treatment with sunitinib was reasonably well tolerated. The availability of sunitinib represents an important clinical advance in GIST management, providing physicians and patients with an effective therapy when resistance to imatinib develops.
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