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Gleevec is the trade name for the generic drug name Imatinib Mesylate. STI-571 is another name for Imatinib Mesylate. In some cases, health care professionals may use the trade name Gleevec or other name STI-571 when referring to the generic drug name Imatinib Mesylate.

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Imatinib Mesylate is a targeted therapy. Imatinib Mesylate is classified as a signal transduction inhibitor – protein-tyrosine kinase inhibitor.

Targeted therapy is the result of about 100 years of research dedicated to understanding the differences between cancer cells and normal cells.  To date, cancer treatment has focused primarily on killing rapidly dividing cells because one feature of cancer cells is that divide rapidly.  Unfortunately, some of our normal cells divide rapidly too, causing multiple side effects.

Targeted therapy is about identifying other features of cancer cells.  Scientists look for specific differences in the cancer cells and the normal cells.  This information is used to create a targeted therapy to attack the cancer cells without damaging the normal cells, thus leading to fewer side effects.  Each type of targeted therapy works a little bit differently but all interfere with the ability of the cancer cell to grow, divide, repair and/or communicate with other cells.

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There are different types of targeted therapies, defined in three broad categories.  Some targeted therapies focus on the internal components and function of the cancer cell.  The targeted therapies use small molecules that can get into the cell and disrupt the function of the cells, causing them to die.  There are several types of targeted therapy that focus on the inner parts of the cells.   Other targeted therapies target receptors that are on the outside of the cell.   Therapies that target receptors are also known as monoclonal antibodies.  Antiangiogenesis inhibitors target the blood vessels that supply oxygen to the cells, ultimately causing the cells to starve.

Research continues to identify which cancers may be best treated with targeted therapies and to identify additional targets for more types of cancer.

Imatinib mesylate belongs to the signal transduction inhibitor category of targeted therapies.  It is particularly a protein-tyrosine kinase inhibitor.

• Imatinib mesylate is a pill, taken by mouth, once or twice daily.
• Imatinib mesylate should be taken with a large glass of water, after a meal.
• The amount of Imatinib mesylate that you will receive depends on many factors, including your general health or other health problems, and the type of cancer or condition being treated.  Your doctor will determine your dose and schedule.

Important things to remember about the side effects of Imatinib mesylate:

• Most people do not experience all of the side effects listed.
• Side effects are often predictable in terms of their onset and duration.
• Side effects are almost always reversible and will go away after treatment is complete.
• There are many options to help minimize or prevent side effects.
• There is no relationship between the presence or severity of side effects and the effectiveness of the medication.
• The side effects of Imatinib mesylate and their severity depend on how much of the drug is given.  In other words, high doses may produce more severe side effects.

The following side effects are common (occurring in greater than 30%) for patients taking Imatinib mesylate:

• Low blood counts.  Your white and red blood cells and platelets may temporarily decrease.  This can put you at increased risk for infection, anemia and/or bleeding.
• Nausea and vomiting
• Edema (swelling of the face, feet, hands)
• Muscle cramps and bone pain
• Diarrhea
• Hemorrhage (see bleeding problems)
• Skin rash (see skin reactions)
• Fever

These side effects are less common side effects (occurring in about 10-29%) of patients receiving Imatinib mesylate:

• Headache
• Fatigue
• Joint pain
• Indigestion (see heartburn)
• Abdominal pain
• Cough
• Shortness of breath
• Poor appetite
• Constipation
• Night sweats (see skin reactions)
• Nose bleeds (see bleeding problems)
• Weakness
• Your fertility, meaning your ability to conceive or father a child, may be affected by Imatinib mesylate.  Please discuss this issue with your health care provider.

A rare, but potentially serious side effect of Imatinib mesylate is liver toxicity.  There may be elevations in transaminase, bilirubin, and lactate dehydrogenase.

Not all side effects are listed above. Some that are rare (occurring in less than 10% of patients) are not listed here.  However, you should always inform your health care provider if you experience any unusual symptoms.