Dr. Adham Abu Taha Presented by: Raya M.Walid Salah Sprecyl Introduction Mechanism of action Pharmacokinetic Side effects Contraindications Major drug-drug interactions Sprycel Generic name: Dasatinib Brand name: Sprycel Company: Bristol-Myers Squibb Indication: Philadelphia chromosome positive chronic myeloid leukemia Approval date: October, 2010 Chronic Myeloid Leukemia It is a form of leukemia characterized by the increased and unregulated growth of myeloid cells in the bone marrow and the accumulation of these cells in the blood. Caused by a translocation between chromosome 9 and chromosome 22, which produces the kinase BCR-Abl. Mechanism of Action Sprycel is a kinase inhibitor that binds to the ATP site of the active conformation of BCR-Abl. Pharmacokinetic Oral bioavailability: 20% Binds extensively to plasma proteins (96%) Metabolized in the liver by CYP3A4, eliminated mainly by the feces. Plasma half-life: 3-5 hours. Dosage: 100 mg once daily. Side Effects Low blood cell count: anemia, neutropenia and thrombocytopenia. Bleeding Fluid retention Heart problems GI problems: nausea, vomiting, diarrhea. Tiredness, weakness, fever and fatigue. Contraindications Pregnancy Breast-feeding Patients under 18 years old Drug Interactions CYP3A4 inhibitors: Ketoconazole, Ritonavir, Indinavir, Erythromycin, Clarithromycin. CYP3A4 inducers: Dexamethasone, Phenytoin, Rifampin, Phenobarbital. Drugs that reduce stomach acidity. Thank You