Pronunciation:

i-ma-TIN-ib

Brand Names:

• Gleevec

Dosage Forms:

• Tablet
• Capsule

Classifications:

Therapeutic—

Antineoplastic Agent

Pharmacologic—

Tyrosine Kinase Inhibitor

Uses of This Medicine:

Imatinib is a new type of medication that prevents and stops the growth of cancer cells. It helps your body fight against a type of cancer called Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) or gastrointestinal stromal tumors (GIST). CML is a disease in which your body makes too many abnormal white blood cells, which can cause you to become sick more often and to feel weak or tired. Imatinib helps your body stop making these abnormal white blood cells. GIST is a group of cancer cells that start growing in the wall of the stomach, intestines, or rectum. Imatinib helps your body stop making these abnormal cells .

Imatinib is also used to treat other conditions such as Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL), myelodysplastic syndrome (MDS) or myeloproliferative diseases (MPD), aggressive systemic mastocytosis (ASM), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), and dermatofibrosarcoma protuberans (DFSP) .

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

This medicine is available only with your doctor's prescription .

Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for 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, newly diagnosed, as part of combination chemotherapy .

Before Using This Medicine:

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

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of imatinib in children below 2 years of age. Safety and efficacy have not been established .

Older adults—

Appropriate studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of imatinib in the elderly. However, serious side effects such as swelling of the face, hands, fingers, feet, and/or lower legs, and unusual weight gain may be more likely to occur in elderly patients, who may be more sensitive than younger adults to the effects of imatinib .

Pregnancy—

	Pregnancy Category	Explanation
All Trimesters	D	Studies in pregnant women have demonstrated a risk to the fetus. However, the benefits of therapy in a life threatening situation or a serious disease, may outweigh the potential risk.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Aprepitant
• Carbamazepine
• Dexamethasone
• Fosaprepitant
• Phenobarbital
• Phenytoin
• Rifampin
• St John's Wort
• Warfarin

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Anemia or
• Platelet problems or
• White blood cell problems—May worsen and affect the decision to continue therapy .

• Chickenpox (including recent exposure) or
• Herpes zoster (shingles)—Risk of severe disease affecting other parts of the body .

• Infection—Imatinib may decrease your body's ability to fight infection .

• Liver disease—Drug effects may be increased because of slower removal of imatinib from the body .

• Heart disease—Patients with this condition should be monitored closely when using imatinib .

Proper Use of This Medicine:

Take imatinib only as directed by your doctor. Do not use more or less of it, and do not use it more often than your doctor ordered. The exact amount of medicine you need has been carefully worked out. Taking too much may increase the 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 to help prevent stomach irritation .

If you cannot swallow the tablet, you may dissolve the tablet in a glass of water or apple juice. If you are taking the 100 mg tablet, dissolve it in 2 ounces (1/4 cup) of water or juice. If you are taking the 400 mg tablet, dissolve it in 7 ounces (about 1 cup) of water or juice. Stir with a spoon and drink immediately after the tablet has dissolved .

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablet):
  • For the treatment of ALL:
    • Adults—600 milligrams (mg) once a day.
    • Children—Use and dose must be determined by your doctor .
  • For the treatment of ASM:
    • Adults—400 milligrams (mg) once a day.
    • Children—Use and dose must be determined by your doctor .
  • For the treatment of DFSP:
    • Adults—800 milligrams (mg) per day.
    • Children—Use and dose must be determined by your doctor .
  • For the treatment of HES or CEL:
    • Adults—400 milligrams (mg) once a day.
    • Children—Use and dose must be determined by your doctor .
  • For the treatment of CML:
    • Adults—400 milligrams (mg) or 600 mg per day, as determined by your doctor. Dosage may be increased as needed.
    • Children—Use and dose must be determined by your doctor .
  • For the treatment of GIST:
    • Adults—400 milligrams (mg) or 600 mg per day, as determined by your doctor.
    • Children—Use and dose must be determined by your doctor .
  • For the treatment of MDS or MPD:
    • Adults—400 milligrams (mg) once a day.
    • Children—Use and dose must be determined by your doctor .

Missed dose—

If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage—

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly and to check for unwanted effects .

Using this medicine while you are pregnant can harm your unborn baby. If you think you have become pregnant while using the medicine, tell your doctor right away .

Serious skin reactions can occur during treatment with this medicine. Check with your doctor right away if you have any of the following symptoms while taking this medicine: blistering, peeling, loosening of skin, chills, cough, diarrhea, fever, itching, joint or muscle pain, red skin lesions, sore throat, sores, ulcers, white spots in mouth or on lips, or unusual tiredness or weakness .

Some serious side effects such as swelling of the face, hands, fingers, feet, and/or lower legs; severe stomach pain, black, tarry stools, and/or vomiting of blood or material that looks like coffee grounds; and unusual weight gain can occur during treatment with this medicine .

While you are being treated with imatinib, and after you stop treatment with it, do not have any immunizations (vaccinations) without your doctor's approval. Imatinib may lower your body's resistance and there is a chance you might get the infection the immunization is meant to prevent. In addition, other persons living in your household should not take oral polio vaccine since there is a chance they could pass the polio virus 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 very long. If you cannot take these precautions, you should consider wearing a protective face mask that covers the nose and mouth .

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

• If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or 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 if you notice any unusual bleeding or bruising; black, tarry stools; blood in urine 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 your teeth and gums. Check with your medical doctor before having any dental work done.
• Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
• Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.
• Avoid contact sports or other situations where bruising or injury could occur .

Check with your doctor right away if you have symptoms of jaundice (yellow skin or eyes) because these may be signs of a serious liver condition .

• This medicine may also cause serious heart conditions. Call your doctor right away if you start to have chest pain or discomfort; fast, irregular, or pounding heart beat; or shortness of breath .

Your doctor will need to check your blood at regular visits while you are using this medicine. Be sure to keep all appointments .

Side Effects of This Medicine:

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

Check with your doctor immediately if any of the following side effects occur:

More common

Abdominal pain, cramping, burning, or tenderness

bleeding from wound after surgery

bleeding gums

bleeding problems

bloating or swelling of face, hands, lower legs, and/or feet

blood in the urine

bloody eye

bloody nose

blue lips and fingernails

blurred vision

body aches or pain

chest pain or discomfort

chills

clay-colored stools

cough

coughing that sometimes produces a pink frothy sputum

coughing up blood

decrease in amount of urine

decreased appetite

decreased urination

diarrhea

difficult or labored breathing

difficulty with swallowing

dizziness

dry mouth

ear congestion

fever

general feeling of discomfort or illness

headache

inability to speak

increased menstrual flow or vaginal bleeding

increased thirst

irregular heartbeat

itching

joint pain

large, flat, blue or purplish patches on the skin

loss of appetite

loss of voice

mood changes

muscle aches and pain

muscle cramps

nasal congestion

nausea and vomiting

noisy, rattling breathing

nosebleed

numbness or tingling in the hands, feet, or lips

pain or tenderness around the eyes and cheekbones

painful or difficult urination

pale skin

prolonged bleeding from cuts

rapid weight gain

red, black, bloody, or tarry stools

red or dark brown urine

redness of the eye

seizures

shivering

shortness of breath

skin rash

slurred speech

small red or purple spots on the skin

sneezing

sore throat

sores, ulcers, or white spots on the lips or in the mouth

stuffy or runny nose

sweating

swelling in the legs and ankles

swollen glands

temporary blindness

tightness in the chest

trouble sleeping

troubled breathing at rest

troubled breathing when moving or walking

unusual bleeding or bruising

unusual tiredness or weakness

vomiting of blood or material that looks like coffee grounds

weakness in the arm and/or leg on one side of the body, sudden and severe

wheezing

yellow eyes or skin

Incidence not known

Blistering, peeling, or loosening of the skin

nausea, heartburn, and/or indigestion, severe and continuing

red, irritated eyes

red skin lesions, often with a purple center

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Acid or sour stomach

belching

bone pain

difficulty having a bowel movement (stool)

difficulty with moving

discouragement

excess air or gas in the stomach or intestines

fear, nervousness

feeling sad or empty

feeling unusually cold

full or bloated feeling

increased bowel movements

irritability

joint pain

lack or loss of strength

loose stools

loss of interest or pleasure

muscle stiffness

night sweats

passing gas

sleeplessness

stomach discomfort, upset, or pain

swollen joints

trouble concentrating

unable to sleep

weight loss

Less common

Back pain

bad, unusual or unpleasant (after) taste

change in taste

watering of the eyes

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.