- Synonyms: STI-571
- Imatinib, sold under the brand name Gleevec, is a tyrosine kinase inhibitor (TKI) primarily used to treat chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GISTs).
- It was the first FDA-approved targeted therapy, revolutionizing the treatment of kinase-driven cancers.
- This inhibitor specifically targets BCR-ABL, an abnormal tyrosine kinase responsible for uncontrolled cell growth in CML.
- By binding to its ATP-binding site, imatinib blocks phosphorylation signals that drive cancer cell proliferation.
- Beyond BCR-ABL, imatinib also inhibits other tyrosine kinases, including c-KIT and PDGFR (platelet-derived growth factor receptor), both of which play critical roles in GISTs and other malignancies.
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