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Imatinib Mechanism Of Action

imatinib mechanism of action

Imatinib is a small molecule kinase inhibitor used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia) as its mesylate salt, imatinib mesilate (INN). It is occasionally referred to as CGP57148B or STI571 (especially in older publications). It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies.

It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non-specifically inhibiting rapidly dividing cells.

Imatinib (Glivec)

Find out what imatinib is, how you have it and other important information about taking imatinib.

Imatinib is a targeted cancer drug (biological therapy) and is also known by its brand name Glivec (pronounced glee-vec).

It is a treatment for many different types of cancer.

How it works

Imatinib is a type of biological therapy called a tyrosine kinase inhibitor (TKI). Tyrosine kinases are proteins that cells use to signal to each other to grow. They act as chemical messengers. There are a number of different tyrosine kinases and blocking them stops the cancer cells growing.

Imatinib targets different tyrosine kinases, depending on the type of cancer.

How you have it

You have imatinib as a tablet that you swallow whole, with a glass of water after food. If you can’t swallow the tablets, you can dissolve them in a glass of mineral water or apple juice. Drop the whole tablets into the fluid, and stir with a spoon until the tablets have broken up completely. Then drink the whole glassful.

Medical uses

Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies.

Chronic myelogenous leukemia

The U.S. Food and Drug Administration (FDA) has approved imatinib as first-line treatment for Philadelphia chromosome-positive CML, both in adults and children. The drug is approved in multiple contexts of Philadelphia chromosome-positive CML, including after stem cell transplant, in blast crisis, and newly diagnosed.[7]

Side effects

bcr-abl kinase (green), which causes CML, inhibited by imatinib (red; small molecule).

The most common side effects include nausea, vomiting, diarrhea, headaches, leg aches/cramps, fluid retention, visual disturbances, itchy rash, lowered resistance to infection, bruising or bleeding, loss of appetite;[17] weight gain, reduced number of blood cells (neutropenia, thrombocytopenia, anemia), and edema.[18] Although rare, restoration of hair color has been reported as well.[19][20] Severe congestive cardiac failure is an uncommon but recognized side effect of imatinib and mice treated with large doses of imatinib show toxic damage to their myocardium.

If imatinib is used in prepubescent children, it can delay normal growth, although a proportion will experience catch-up growth during puberty.[2

Precautions

Before taking imatinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: bleeding problems, heart problems (such as heart failure), kidney disease, liver disease, removal of thyroid gland.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Storage

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets

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