A Report On Gleevec ( Imatinib Mesylate )

1126 WordsDec 7, 20165 Pages
Gleevec (imatinib mesylate) Antineoplastic MW = 589.7 g/mol pKa = 5.5 Chemical Formula = C29H31N7O ● CH4SO3 IUPAC name: N-(4-methyl-3-{[4-(pyridine-3-yl) pyrimidin-2-yl]amino}phenyl)-4-((4-methylpiperazin-1-yl) methyl]benzamide Description Imatinib mesylate is a protein tyrosine kinase (RTK) inhibitor that exhibits high specificity and potency for ABL, c-kit, and PDGF receptors, which often harbor activating mutations and are typically mutually exclusive of each other and within specific cancer types.2 The compound has been approved as a targeted chemotherapy for Philadelphia chromosome positive chronic and acute myeloid leukemia (Ph+ CML and AML), Ph+ acute lymphoblastic leukemia (ALL), platelet-derived growth factor receptor (PDGFR) aberrancy-related myelodysplastic or myeloproliferative pathologies, kit+ expressing advanced gastrointestinal stromal tumors (GIST), and for FIP1L1-PDGFRα gene fusion expressing hypereosinophilic syndrome (HES) or chronic eosinophilic leukemia (CEL).1 Imatinib is available in 100 mg and 400 mg tablets for case-dependent single agent or adjunct therapy1. Therapeutic doses range from 100 mg to 800 mg/day, depending on diagnosis, age, and hepatic function.1 The drug exhibits pH-dependent solubility in aqueous solutions (soluble at pH ≤ 5.5), varying solubility in polar protic solvents, and is immiscible in polar aprotic liquids.1 Mechanism of Action Imatinib is a competitive antagonist that exhibits specific activity for ABL, c-kit, and PDGFR

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