imatinib, Gleevec

  • Pharmacy Author:
    Omudhome Ogbru, PharmD

    Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

  • Medical and Pharmacy Editor: Jay W. Marks, MD
    Jay W. Marks, MD

    Jay W. Marks, MD

    Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

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What is imatinib-oral, and how does it work (mechanism of action)?

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.

What brand names are available for imatinib-oral?

Gleevec

Is imatinib-oral available as a generic drug?

GENERIC AVAILABLE: No

Do I need a prescription for imatinib-oral?

Yes

What are the side effects of imatinib-oral?

Common side effects include:

Serious side effects include:

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What is the dosage for imatinib-oral?

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.

Which drugs or supplements interact with imatinib-oral?

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.

Is imatinib-oral safe to take if I'm pregnant or breastfeeding?

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

Imatinib is excreted in human milk; therefore, nursing mothers should either discontinue imatinib or stop breastfeeding.

What else should I know about imatinib-oral?

What preparations of imatinib-oral are available?

Tablets: 100, and 400 mg

How should I keep imatinib-oral stored?

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

REFERENCE: FDA Prescribing Information

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Reviewed on 5/18/2015
References
REFERENCE: FDA Prescribing Information

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