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imatinib (Gleevec, Imkeldi)
Tyrosine Kinase Inhibitors

How it is administered

Imatinib is taken by mouth as a tablet or oral solution. Tablets are available in 100 mg and 400 mg strengths, and the oral solution contains 80 mg per mL. All doses should be taken with a meal and a large glass of water to reduce stomach upset. For patients who have difficulty swallowing tablets, the tablets can be dissolved in water or apple juice. The oral solution should be measured with an accurate measuring device, not a household spoon.

How it works

Imatinib is a type of medication called a tyrosine kinase inhibitor. It works by blocking the activity of certain abnormal proteins (kinases) in cancer cells, particularly the BCR-ABL protein produced by the Philadelphia chromosome abnormality found in some types of leukemia, including Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). By blocking this protein, imatinib stops the cancer cells from growing and dividing, and can lead to their death.

Imatinib also inhibits other proteins involved in cancer growth, such as c-Kit and PDGF receptors. This broad activity helps control the spread and progression of certain blood cancers. In Ph+ ALL, imatinib is often used in combination with chemotherapy to improve outcomes. Its effectiveness is due to its ability to specifically target cancer cells with these abnormal proteins, while having less effect on normal, healthy cells.

Common side effects

  • Edema (swelling, especially around the eyes or in the legs)
  • Nausea and vomiting
  • Muscle cramps
  • Musculoskeletal pain
  • Diarrhea
  • Rash
  • Fatigue
  • Abdominal pain

Other possible side effects include headache, joint pain, weight gain, and changes in blood counts (such as low white blood cells, red blood cells, or platelets). Serious side effects can include liver problems, heart failure, severe fluid retention, and bleeding. Your doctor will monitor you with regular blood tests and check-ups to watch for these effects.

Who Should take it

Imatinib is prescribed for adults and children with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). In adults, it is used for those with relapsed or refractory Ph+ ALL. In children, it is used in combination with chemotherapy for newly diagnosed Ph+ ALL.

Imatinib is also used for other blood cancers, such as chronic myeloid leukemia (CML), and for certain rare tumors. For Ph+ ALL, it is an important part of treatment because it specifically targets the abnormal protein driving the leukemia. Your doctor will decide if imatinib is right for you based on your diagnosis, age, and overall health.

Who should not take it

There are no absolute contraindications listed for imatinib. However, it should be used with caution in certain situations. People with severe liver or kidney impairment may need dose adjustments or careful monitoring. Women who are pregnant or may become pregnant should avoid imatinib, as it can harm an unborn baby. Women should use effective contraception during treatment and for 14 days after stopping imatinib.

People who are breastfeeding should not use imatinib, as it can pass into breast milk and may harm a nursing baby. If you have a history of heart problems, fluid retention, or liver disease, your doctor will monitor you closely during treatment. Always tell your healthcare provider about all your medical conditions and medications before starting imatinib.

Commonly used with

For Ph+ ALL, imatinib is commonly used together with chemotherapy. In children, it is specifically given in combination with intensive chemotherapy regimens. In adults, it may be used alone or with other treatments, depending on the stage and response of the disease.

Imatinib may also be used with supportive medications to manage side effects, such as anti-nausea drugs or diuretics for fluid retention. Your healthcare team will tailor your treatment plan to your specific needs.

Commonly tested with

Imatinib has been studied in combination with various chemotherapy regimens for Ph+ ALL, especially in pediatric populations. It has also been compared to other tyrosine kinase inhibitors, such as nilotinib, in clinical trials for related blood cancers.

In clinical studies, imatinib is often tested alongside standard chemotherapy protocols to determine the best timing and duration of combined therapy. Your doctor may also monitor your response to imatinib with regular blood and bone marrow tests.

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