imatinib, Gleevec

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GENERIC NAME: imatinib


DRUG CLASS AND MECHANISM: Imatinib is an oral medication used for treating chronic myeloid leukemia and acute lymphoblastic leukemia. It is classified as a kinase inhibitor. Kinase inhibitors include dasatinib (Sprycel), erlotinib (Tarceva), gefitinib (Iressa), nilotinib (Tasigna), pazopanib (Votrient), sunitinib (Sutent), and vandetanib (Caprelsa). Kinase inhibitors prevent tumors from growing by reducing the action of proteins that control cell division, growth and survival. These proteins are usually present in larger quantities or are more active in cancer cells. By reducing the activity of these proteins, growth and survival of cancer cells are reduced. The FDA approved imatinib in April 2003.



PREPARATIONS: Tablets: 100, and 400 mg

STORAGE: Imatinib should be stored at room temperature between 15-30 C (59-86 F).

PRESCRIBED FOR: Imatinib is used for the treatment of adult and pediatric patients with newly diagnosed Philadelphia chromosome positive, chronic myeloid leukemia (Ph+ CML); treatment of Ph+ CML after failure of interferon-alpha therapy; adults with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL); adults with myeloproliferative or myelodysplastic diseases; mastocytosis; hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL); dermatofibrosarcoma protuberans; and gastrointestinal stromal tumors (GIST)

DOSING: The recommended dose range is 300-800 mg orally daily depending on the condition being treated. All doses should be administered with a meal and a large glass of water. A dose of 800 mg should be administered as 400 mg twice daily. Doses less than 800 mg may be administered once daily. It can be dissolved in apple juice or water for those with difficulty swallowing.

DRUG INTERACTIONS: The blood concentration of imatinib may be increased by several drugs that reduce its break down by the liver. Examples include ketoconazole, itraconazole (Sporanox), clarithromycin (Biaxin), atazanavir (Reyataz), indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir), saquinavir (Invirase), telithromycin (Ketek), voriconazole (Vfend), and grapefruit juice. Increased blood concentrations of imatinib may increase the occurrence of adverse effects.

Certain drugs decrease the blood concentration of imatinib resulting in decreased blood levels and possibly reduced effect. Examples include carbamazepine, phenobarbital, rifampin, phenytoin, fosphenytoin, primidone, and St John's Wort.

Imatinib increases the blood concentration of simvastatin (Zocor) by reducing the activity of enzymes that break down simvastatin in the liver. This may increase the side effects of simvastatin. Imatinib may interact with other drugs that are broken down in a similar way as simvastatin.

PREGNANCY: Imatinib is harmful to the fetus and should not be used during pregnancy.

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