2009•Chinese Journal of Gastroenterology and HepatologyRequires access

The present and future of gastrointestinal stromal tumors' drug therapy

Jie Zhong

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Abstract

Gastrointestinal stromal tumors(GISTs) are the most common mesenchymal tumors of the gastrointestinal tract.The research on GISTs' molecular tumorgenesis has greatly promoted the development of the therapy,especially treatment with molecular targeted therapeutic drugs.Gleevec(Imatinib) inhibits several tyrosine kinases including kit and PDGFR-α and-β,and it is the first-line treatment for unresectable or metastatic GISTs.However,certain specific mutations of the kit gene result in GISTs which are relatively unresponsive to the Gleevec treatment.New therapeutic agents like sunitinib which inhibits multiple tyrosine kinases including kit,PDGFR,FLT3 and VEGFR have been approved for the treatment of imatinibresistant or intolerant GISTs.Also,there are some new tyrosine kinases inhibitors in the process of preclinical or clinical study,which are administered alone or with Gleevec.

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What this paper is about

Gastrointestinal stromal tumors(GISTs) are the most common mesenchymal tumors of the gastrointestinal tract.The research on GISTs' molecular tumorgenesis has greatly promoted the development of the therapy,especially treatment with molecular targeted therapeutic drugs.Gleevec(Imatinib) inhibits several tyrosine kinases including kit and PDGFR-α and-β,and it is the first-line treatment for unresectable or metastatic GISTs.However,certain specific mutations of the kit gene result in GISTs which are relatively unresponsive to the Gleevec treatment.New therapeutic agents like sunitinib which inhibits multiple tyrosine kinases including kit,PDGFR,FLT3 and VEGFR have been approved for the treatment of imatinibresistant or intolerant GISTs.Also,there are some new tyrosine kinases inhibitors in the process of preclinical or clinical study,which are administered alone or with Gleevec.

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Available abstract

Gastrointestinal stromal tumors(GISTs) are the most common mesenchymal tumors of the gastrointestinal tract.The research on GISTs' molecular tumorgenesis has greatly promoted the development of the therapy,especially treatment with molecular targeted therapeutic drugs.Gleevec(Imatinib) inhibits several tyrosine kinases including kit and PDGFR-α and-β,and it is the first-line treatment for unresectable or metastatic GISTs.However,certain specific mutations of the kit gene result in GISTs which are relatively unresponsive to the Gleevec treatment.New therapeutic agents like sunitinib which inhibits multiple tyrosine kinases including kit,PDGFR,FLT3 and VEGFR have been approved for the treatment of imatinibresistant or intolerant GISTs.Also,there are some new tyrosine kinases inhibitors in the process of preclinical or clinical study,which are administered alone or with Gleevec.

Key concepts: Sunitinib, Imatinib, Tyrosine kinase, GiST, Medicine, Tyrosine-kinase inhibitor, Cancer research, Targeted therapy

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