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  • Title: [Strategy for patients with GIST after failure of imatinib].
    Author: Abe S, Kubota T.
    Journal: Gan To Kagaku Ryoho; 2009 Apr; 36(4):540-3. PubMed ID: 19381023.
    Abstract:
    Sunitinib malate(SU11248)is an oral multitargeted receptor tyrosine kinase inhibitor(MTI)that has antitumor activities for patients with gastrointestinal stromal tumor; GIST after failure of Imatinib. Sunitinib has demonstrated significant clinical benefits, including PFS, RR and OS in the USA and Japan. However, cis-mutations in the activation loop of the KIT gene tend to develop Sunitinib-resistant GIST. Two clinical trials revealed that new multitargeted receptor tyrosine kinase inhibitors, Sorafenib and Nilotinib, had antitumor activities for Sunitinib-resistant GIST with longer PFS and a different spectrum. Now, clinical trials of several new MTIs are ongoing in Western countries. Inhibition of the KIT gene cis-mutations and antiangiogenesis activities may be essential for the strategy for Imatinib/Sunitinibresistant GIST.
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