Imatinib Mesylate
It is a protein-tyrosine kinase inhibitor that inhibits Bcr-Abl tyrosine kinase. It is also an inhibitor of the receptor tyrosine kinases for platelet derived growth factor and stem cell factor, C-kit, and inhibits their mediated cellular events.Philadelphia chromosome positive chronic myeloid leukemia (CML). Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST).
To be administered orally with a meal and a large glass of water. Range of dosage to be adjusted according to therapeutic response and adverse effects. Chronic Phase CML: 400mg-600mg/day. Accelerated Phase or blast crisis CML : 600mg-800mg/day (400mg twice daily). Unresectable and/or metastatic malignant GIST: 400mg-600mg/day.
Hypersensitivity.
Dose adjustment/reduction or treatment interruption is recommended if a severe adverse effect develops. Paediatric : Safety and efficacy have not been established under the age of 18-years of age. Pregnancy : Safety is not established. Lactation : Safety is not established. Elderly : Safe
Nausea, vomiting, diarrhoea, abdominal pain, rash, edema, and muscle cramps. Local or generalised fluid, retention and rapid weight gain. Cytopenias. Hepatotoxicity.
Ketoconazole, itraconazole, erythromycin, and clarithromycin may increase plasma concentration of imatinib, while dexamethasone, phenytoin, carbamazepine, rifampicin, phenobarbital may decrease the plasma concentration of imatinib. It will increase plasma concentration of triazolo-benzodiazepines, dihydropyridine, calcium channel blcokers, certain HMG-CoA reductase inhibitors etc. Warferin.
