What is imatinib, 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?
Gleevec
Is imatinib available as a generic drug?
No
Do I need a prescription for imatinib?
Yes
What are the side effects of imatinib?
Common side effects include:
- fluid retention,
- headache,
- diarrhea,
- loss of appetite,
- weakness,
- nausea and vomiting,
- abdominal distention,
- swelling of arms and legs,
- rash,
- itching,
- fever,
- dizziness, and
- muscle pain.
Serious side effects include:
- fever associated with reduced white blood cells,
- reduced platelets
- reduced red blood cell counts,
- infection,
- stomach or intestinal bleeding,
- bleeding in the brain,
- heart failure,
- reduced liver function, and
- fluid in the lungs.
What is the dosage for imatinib?
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?
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.
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Is imatinib 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?
What preparations of imatinib are available?
Tablets: 100, and 400 mg
How should I keep imatinib stored?
Imatinib should be stored at room temperature between 15 C – 30 C (59 F – 86 F).