December 2, 2008


By Anonymous User

Class: Chemotherapy

Generic Name: Imatinib mesylate (eye-MAT-in-ib mez-I-late)
Trade Name: Gleevec®, Glivec®

How is this drug used? Imatinib mesylate is FDA approved for the treatment of all phases of Philadelphia chromosome-positive chronic myelogenous leukemia and it is also approved for the treatment of c-Kit positive gastrointestinal stromal tumors (GIST). It is important for patients to remember that physicians have the ability to prescribe medication for conditions other than those for which the drug has been approved by the FDA. Patients who have received a prescription of this drug for a condition other than which it is approved may wish to discuss this issue with their physician.

What is the mechanism of action? Imatinib mesylate is a tyrosine kinase inhibitor. A genetic abnormality, referred to as the Philadelphia-chromosome, leads to continually active growth signaling to cancer cells in the majority of cases of chronic myeloid leukemia. Imatinib mesylate inhibits the growth signaling processes, suppressing replication and ultimately causing death of Philadelphia-chromosome positive chronic myeloid leukemia cells. Imatinib mesylate also appears to have growth inhibitory effects in some diseases such as GIST that is c-Kit positive.

How is imatinib mesylate given (administered)? Imatinib mesylate is administered orally, in the form of a capsule, and the dose depends on several factors, including the condition being treated, the size of the patient, the particular regimen being used, and the overall health of the patient. It should be taken with food and a large glass of water to minimize gastrointestinal irritation.

How are patients monitored? Patients will usually have scheduled meetings with their healthcare provider while they are being treated with imatinib mesylate.  Typically, blood will be drawn to check levels of blood cells and to monitor functions of some organ systems, such as the kidneys or liver.  Patients may also undergo physical examinations, scans or other measures to assess side effects and response to therapy.

What are the common (occur in 30% or more of patients) side effects of treatment with imatinib mesylate?

• Low white blood cell levels – increases risk of infection
• Low red blood cell levels – increases risk of anemia
• Low platelet levels – increases risk of bleeding
• Nausea and vomiting
• Fluid retention resulting in swelling of the feet, hands or face
• Diarrhea
• Bleeding (hemorrhage)
• Rash
• Fever
• Muscle cramps
• Bone pain

What are the less common (occur in 10% to 29% of patients) side effects of treatment with imatinib mesylate?

• Night sweats
• Nose bleeds
• Shortness of breath
• Weight gain
• Loss of appetite
• Headache
• Dizziness
• Insomnia
• Generalized fatigue
• Heartburn
• Abdominal pain
• Cough
• Constipation
• Joint or muscle pain
• Throat pain or inflammation
• Change in liver function tests, liver damage

This is not a complete list of side effects. Some patients may experience other side effects that are not listed here. Patients may wish to discuss with their physician the other less common side effects of this drug, some of which may be serious.

Some side effects may require medical attention. Other side effects do not require medical attention and may go away during treatment. Patients should check with their physician about any side effects that continue or are bothersome.
What can patients do to help alleviate or prevent discomfort and side effects?

• Pay careful attention to the physician’s instructions and inform the physician of any side effects.
• Maintain adequate rest and nutrition.
• Wear sunscreen and protective clothing and try to minimize sun exposure.
• Drink plenty of fluids. (Patients should ask their physician about the amount of liquid to consume during a day.)
• If possible, avoid large crowds or people who are sick or not feeling well, as this drug may leave some patients susceptible to infection.
• Wash hands often to reduce the risk of infection.
• Eat small meals frequently to help alleviate nausea.
• Avoid activities that may cause injury or bruising.
• Use a soft toothbrush and an electric razor to prevent cuts on the mouth or skin.

Are there any special precautions patients should be aware of before starting treatment?

• Patients should inform their physician if they are pregnant, breastfeeding or planning a family in the near future. This drug may cause birth defects. It is important to use some kind of birth control while undergoing treatment. Also, patients may want to talk to their physician if they are considering having children in the future, since some drugs may cause fertility problems.
• It is important that patients inform their physician of any pre-existing conditions (chicken pox, heart disease, kidney disease, liver disease, lung disease, etc.) as they may worsen with this drug.
• Patients should inform their physician of any other medication they are taking (whether prescription or over-the-counter, including vitamins, herbs, etc.) as they may interfere with treatment.
• Patients should inform their physician if taking the blood thinner, warfarin, as they may require extra monitoring and dose adjustment.
• Patients should check with their physician before starting any new drug or nutritional supplement.
• Patients should inform their physician of any known drug or food allergies or any reactions to medications they have experienced in the past.
• Patients should use caution when driving or completing tasks that require mental alertness until effects of the drug are known

When should patients notify their physician?

• Bleeding from nose, mouth, vagina or rectum; bruising, black tarry stools, blood in the urine
• Shortness of breath, difficulty breathing, cough
• Swelling of ankles, hands or face
• Sudden weight gain
• Little or no urine output
• Yellowing of skin or eyes
• Chest pain or palpitations
• Fainting
• Swelling, pain or redness in only one extremity
• Flu or cold-like symptoms - fever, chills, sore throat, cough
• Signs of infection – redness, swelling, pus, tenderness, painful urination
• Persistent or severe fatigue
• Muscle or bone pain
• Tremors or cramping
• Skin rash

What is a package insert?
A package insert is required by the FDA and contains a summary of the essential scientific information needed for the safe and effective use of the drug for healthcare providers and consumers.  A package insert typically includes information regarding specific indications, administration schedules, dosing, side effects, contraindications, results from some clinical trials, chemical structure, pharmacokinetics and metabolism of the specific drug. By carefully reviewing the package insert, you will get the most complete and current information about how to safely use this drug. If you do not have the package insert for the drug you are using, your pharmacist or physician may be able to provide you with a copy.

Copyright © 2010 CancerConnect Last updated 07/10.

Important Limitations of Use

The information provided above on the drug you have selected is provided for your information only and is not a substitute for consultation with an appropriate medical doctor. We are providing this information solely as a courtesy and, as such, it is in no way a recommendation as to the safety, efficacy or appropriateness of any particular drug, regimen, dosing schedule for any particular cancer, condition or patient nor is it in any way to be considered medical advice. Patients should discuss the appropriateness of a particular drug or chemotherapy regimen with their physician.

As with any printed reference, the use of particular drugs, regimens and drug dosages may become out-of-date over time, since new information may have been published and become generally accepted after the latest update to this printed information. Please keep in mind that health care professionals are fully responsible for practicing within current standards, avoiding use of outdated regimens, employing good clinical judgment in selecting drugs and/or regimens, in calculating doses for individual patients, and verifying all dosage calculations.



The prescribing physician is solely responsible for making all decisions relating to appropriate patient care including, but not limited to, drugs, regimens, dose, schedule, and any supportive care.

Tags: Chemotherapy, G