[Strategy for patients with GIST after failure of imatinib].
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.
Abe
Sadanori
S
Center for Comprehensive and Advanced Medicine, Keio University Hospital, Tokyo, Japan.
Kubota
Tetsuro
T
D000970:Antineoplastic Agents / Q000627:therapeutic use*; D001549:Benzamides; D002986:Clinical Trials as Topic; D019008:Drug Resistance, Neoplasm / Q000187:drug effects*; D046152:Gastrointestinal Stromal Tumors / Q000188:drug therapy* / Q000201:enzymology / Q000601:surgery; D006801:Humans; D000068877:Imatinib Mesylate; D010879:Piperazines / Q000627:therapeutic use*; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use; D011743:Pyrimidines / Q000627:therapeutic use*; D017211:Treatment Failure
D000970:Antineoplastic Agents; D001549:Benzamides; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D000068877:Imatinib Mesylate