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Gastrointestinal Stromal Tumor Resource Center

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The mechanisms of imatinib resistance in gastrointestinal stromal tumours: Theoretical basis and therapeutic aspect

Last Updated: Monday, December 1, 2025

Imatinib, a small molecule inhibiting KIT and PDGFRA, was approved in 2002 for advanced GISTs. However, resistance develops, causing 50% of patients to relapse within 2–5 years. This review summarizes resistance mechanisms, including alterations in signaling pathways and disrupted autophagy/glycolysis. It also explores strategies to overcome resistance, such as the role of microRNAs, immunotherapy, and combination therapies, examining clinical trials to enhance the prognosis for advanced GIST patients. 

Journal of Cellular and Molecular Medicine
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