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Olverembatinib is an orally administered **small-molecule tyrosine kinase inhibitor** developed by Ascentage Pharma. It was designed as a third-generation BCR-ABL1 inhibitor and has broader multikinase activity that includes **KIT, platelet-derived growth factor receptor alpha, fibroblast growth factor receptor, and SRC family kinases**, supporting development beyond leukemia into solid tumors such as gastrointestinal stromal tumor. In the GIST setting, olverembatinib has been studied in a Phase 1 trial in patients with unresectable or metastatic GIST and other solid tumors, including SDH-deficient GIST after prior tyrosine kinase inhibitor therapy. The drug is already approved in China for certain chronic myeloid leukemia indications, while in GIST it remains an investigational targeted anticancer therapy.
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