IMATINIB (Systemic)

Some commonly used brand names are:

In the U.S.?

• Gleevec

In Canada?

• Gleevec

Category

• Antineoplastic

Description

Imatinib (i-MAT-in-ib)is a new type of medication that prevents andstops the growth of cancer cells. It helps your body fight against a typeof cancer called chronic myeloid leukemia (CML) or gastrointestinal stromaltumor (GIST). CML is a disease in which your body makes too many abnormalwhite blood cells which can cause you to become sick more often and also tofeel weak or tired. Imatinib helps your body to stop making these abnormalwhite blood cells. GIST is a group of cancer cells that started growing inthe wall of the stomach, intestines, or rectum. Imatinib helps your body tostop making these abnormal cells.

Before you begin treatment with imatinib, you and your doctor should talkabout the good this medicine will do as well as the risks of using it.

This medicine is available only with your doctor's prescription, in thefollowing dosage form:

Oral
• Capsules (Canada)
• Tablets (U.S. and Canada)

Before Using This Medicine

In deciding to use a medicine,the risks of taking the medicine must be weighed against the good it willdo. This is a decision you and your doctor will make. For imatinib, the followingshould be considered:

Allergies?Tell your doctor if you have ever had any unusualor allergic reaction to imatinib. Also tell your health care professionalif you are allergic to any other substances, such as foods, preservatives,or dyes.

Pregnancy?Imatinib has not been studied in pregnant women.However, studies in animals have shown that imatinib causes birth defectsand other problems with pregnancy. Before taking this medicine, make sureyour doctor knows if you are pregnant or if you may become pregnant. Thismedicine may be needed in serious diseases or other situations that threatenthe mother's life. Be sure you have discussed this with your doctor.

Breast-feeding?It is not known whether imatinib passes intohuman breast milk. However, imatinib is not recommended during breast-feeding,because it may cause unwanted effects in nursing babies.

Children?Studies on this medicine have been done only inchildren over 3 years of age with Ph+ chronic phase CML and adult patients,and there is no specific information comparing use of imatinib to treat otherconditions in children with use in other age groups. Safety and effectivenesshave not been established in these children

Older adults?This medicine has been tested and has not beenshown to cause different side effects or problems in older people than itdoes in younger adults. Fluid retention may be more likely to occur in elderlypatients, who may be more sensitive than younger adults to the effects ofimatinib.

Other medicines?Although certain medicines should not be usedtogether at all, in other cases two different medicines may be used togethereven if an interaction might occur. In these cases, your doctor may want tochange the dose, or other precautions may be necessary. When you are takingimatinib, it is especially important that your doctor and pharmacist knowif you are taking any of the following:

• Acetaminophen (e.g., Tylenol)? imatinib may increase the amountof acetaminophen in your body when you take them together.

• Amphotericin B by injection (e.g., Fungizone) or
• Antineoplastics (cancer medicines) or
• Antithyroid agents (medicine for overactive thyroid) or
• Azathioprine (e.g., Imuran) or
• Chloramphenicol (e.g., Chloromycetin) or
• Colchicine or
• Cyclophosphamide (e.g., Cytoxan) or
• Flucytosine (e.g., Ancobon) or
• Ganciclovir (e.g., Cytovene) or
• Interferon (e.g., Intron A, Roferon-A) or
• Mercaptopurine (e.g., Purinethol) or
• Methotrexate (e.g., Rheumatrex) or
• Plicamycin (e.g., Mithracin) or
• Zidovudine (e.g., AZT, Retrovir)?Concurrent use of these medicineswith imatinib increases the risk of infection.

• If you have ever been treated with x-rays or other cancer medicines?Imatinibmay increase the effects of these medicines or radiation therapy on the blood.

• Carbamazepine (e.g., Tegretol) or
• Dexamethasone (e.g., Decadron) or
• Phenobarbital (e.g., Luminal) or
• Phenytoin (e.g., Dilantin) or
• Rifampicin (e.g., Rifampin) or
• St. John's Wort?These medications may decrease the amount ofimatinib in your body.

• Clarithromycin (e.g., Biaxin) or
• Erythromycin (e.g., E-Mycin, Erythrocin) or
• Itraconazole (e.g., Sporanox) or
• Ketoconazole (e.g., Nizoral)?These medications may increasethe amount of imatinib in your body.

• Cyclosporine (e.g., Sandimmune) or
• Pimozide (e.g., Orap)?Imatinib may increase the amount of thesemedications in your blood to possibly harmful levels.

• Warfarin (e.g., Coumadin)?Imatinib may interfere with the metabolismof warfarin, which can cause clotting problems.

• Grapefruit or
• Grapefruit juice or
• Grapefruit-containing food or vitamin?These foods or vitaminsmay increase the amount of imatinib in your body. This may increase the chanceof side effects.

Other medical problems?The presence of other medicalproblems may affect the use of imatinib. Make sure you tell your doctor ifyou have any other medical problems, especially:

• Anemia or
• Platelet problems or
• White blood cell problems?May worsen and affect the decisionto continue therapy

• Chickenpox (including recent exposure) or
• Herpes zoster (shingles)?Risk of severe disease affecting otherparts of the body

• Liver disease?Effects may be increased because of slower removalof imatinib from the body

• Infection?Imatinib may decrease your body's ability to fightinfection

Proper Use of This Medicine

Take imatinib only as directed by your doctor. Do not use more or lessof it, and do not use it more often than your doctor ordered. The exact amountof medicine you need has been carefully worked out. Taking too much may increasethe chance of side effects, while taking too little may not improve your condition.

This medicine should be taken with a tall glass of water and a meal.

Do not take imatinib with grapefruit, grapefruit juice, or grapefruit-containingfoods or supplements.

Dosing?The dose of imatinib will be different fordifferent patients. The dose that is used may depend on a number of things,how you are responding to the medicine and whether or not it is affectingyour blood cells. If you are taking imatinib at home,follow your doctor's orders or the directions on the label. If youhave any questions about the proper dose of imatinib, ask your doctor.

Missed dose?If you miss a dose of this medicine, do not takethe missed dose at all and do not double the next one. Instead, go back toyour regular dosing schedule and check with your doctor.

Storage?To store this medicine:

• Keep out of the reach of children.
• Store away from heat and direct light.
• Do not store in the bathroom, near the kitchen sink, or in otherdamp places. Heat or moisture may cause the medicine to break down.
• Do not keep outdated medicine or medicine no longer needed. Be surethat any discarded medicine is out of the reach of children.

Precautions While Using This Medicine

It is very important that your doctor check your progress atregular visits to make sure that this medicine is working properlyand to check for unwanted effects.

While you are being treated with imatinib, and after you stop treatmentwith it, do not have any immunizations (vaccinations)without your doctor's approval. Imatinib may lower your body's resistanceand there is a chance you might get the infection the immunization is meantto prevent. In addition, other persons living in your household should nottake oral polio vaccine since there is a chance they could pass the poliovirus on to you. Also, avoid persons who have recently taken oral polio vaccine.Do not get close to them and do not stay in the same room with them for verylong. If you cannot take these precautions, you should consider wearing aprotective face mask that covers the nose and mouth.

Imatinib can temporarily lower the number of white blood cells in yourblood, increasing the chance of getting an infection. It can also lower thenumber of platelets, which are necessary for proper blood clotting. If thisoccurs, there are certain precautions you can take, especially when your bloodcount is low, to reduce the risk of infection or bleeding:

• If you can, avoid people with infections. Checkwith your doctor immediately if you think you are getting an infectionor if you get a fever or chills, cough or hoarseness, lower back or side pain,or painful or difficult urination.
• Check with your doctor immediately ifyou notice any unusual bleeding or bruising; black, tarry stools; blood inurine or stools; or pinpoint red spots on your skin.
• Be careful when using a regular toothbrush, dental floss, or toothpick.Your medical doctor, dentist, or nurse may recommend other ways to clean yourteeth and gums. Check with your medical doctor before having any dental workdone.
• Do not touch your eyes or the inside of your nose unless you havejust washed your hands and have not touched anything else in the meantime.
• Be careful not to cut yourself when you are using sharp objects suchas a safety razor or fingernail or toenail cutters.
• Avoid contact sports or other situations where bruising or injurycould occur.

Side Effects of This Medicine

Along with its needed effects, a medicinemay cause some unwanted effects. Although not all of these side effects mayoccur, if they do occur they may need medical attention.

Check with your doctoras soon as possible if any of the following side effects occur:

More common

Black, tarry stools; bleeding problems; bloating or swelling of face, hands, lower legs,and/or feet; chest pain; chills; cough; decreasedurination; fever; painfulor difficult urination; pale skin; rapid weight gain; shortness of breath; sore throat; sores, ulcers, or whitespots on lips or in mouth; swollen glands; trouble breathing, exertional; unusualbleeding or bruising; unusual tiredness or weakness

Less common

Body aches or pain; convulsions (seizures); dry mouth; ear congestion; general feeling of discomfort or illness; headache sudden and severe; increasedthirst; irregular heartbeat; loss of appetite; loss of voice; mood changes; muscle pain or cramps; nausea and vomiting; numbness or tinglingin hands, feet, or lips; runny nose; shivering; small red or purple spotson skin; sneezing; stuffynose; sweating; tightnessin chest; wheezing

Rare

Bloody stools; blurred vision; inability to speak; slurred speech; temporary blindness; vomiting of bloodor material that looks like coffee grounds; weaknessin arm and/or leg on one side of the body, sudden and severe

Otherside effects may occur that usually do not need medical attention. These sideeffects may go away during treatment as your body adjusts to the medicine.However, check with your doctor if any of the following side effects continueor are bothersome.

More common

Bone pain; increased bowel movements; joint pain; loose stools; skin rash; stomach pain

Less common

Acid indigestion; back pain; bad unusual or unpleasant (after)taste; bloated full feeling; bloody nose; change in taste; difficulty having a bowel movement(stool); dizziness; excessair or gas in stomach or intestines; headache; itching skin; lack or loss of strength; large, flat, blue or purplish patches in the skin; loss of appetite; nightsweats; passing gas; sleeplessness; trouble sleeping; unableto sleep; upset stomach; watering of eyes; weight loss

Other side effects not listed abovemay also occur in some patients. If you notice any other effects, check withyour doctor.

Additional Information

Once a medicine has been approvedfor marketing for a certain use, experience may show that it is also usefulfor other medical problems. Although this use is not included in product labeling,imatinib is used in certain patients with the following medical condition:

• Acute lymphoblastic leukemia, Philadelphia chromosome-positive, newlydiagnosed, as part of combination chemotherapy

Other than the above information, there is no additional information relatingto proper use, precautions, or side effects for this use.