Pronunciation:

i-ma-TIN-ib

Brand Names:

• Gleevec

Dosage Forms:

• Tablet

Classifications:

Therapeutic—

Antineoplastic Agent

Pharmacologic—

Tyrosine Kinase Inhibitor

Uses of This Medicine:

Imatinib is used alone or together with other medicines to treat different types of cancer or bone marrow conditions. It prevents or stops the growth of cancer cells and is called an antineoplastic (cancer) agent. Imatinib is used for these conditions:

• Aggressive systemic mastocytosis (ASM)
• Chronic eosinophilic leukemia (CEL)
• Dermatofibrosarcoma protuberans (DFSP)
• Gastrointestinal stromal tumors (GIST)
• Hypereosinophilic syndrome (HES)
• Myelodysplastic syndrome (MDS)
• Myeloproliferative diseases (MPD)
• Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL)
• Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML)

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

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 to treat Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase and acute lymphoblastic leukemia (Ph+ ALL) in children younger than 1 year of age. Safety and efficacy have not been established.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of imatinib in the elderly. However, serious side effects (eg, 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.

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—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Eliglustat
• Flibanserin
• Lomitapide
• Measles Virus Vaccine, Live
• Mumps Virus Vaccine, Live
• Rotavirus Vaccine, Live
• Rubella Virus Vaccine, Live
• Varicella Virus Vaccine, Live
• Zoster Vaccine, Live

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.

• Abametapir
• Acalabrutinib
• Acetaminophen
• Adenovirus Vaccine
• Alfentanil
• Alprazolam
• Amiodarone
• Aprepitant
• Avapritinib
• Bacillus of Calmette and Guerin Vaccine, Live
• Benzhydrocodone
• Bosutinib
• Brexpiprazole
• Brigatinib
• Buprenorphine
• Carbamazepine
• Cholera Vaccine, Live
• Cilostazol
• Clozapine
• Cobimetinib
• Codeine
• Colchicine
• Daridorexant
• Deflazacort
• Dengue Tetravalent Vaccine, Live
• Dihydrocodeine
• Dihydroergotamine
• Domperidone
• Doxorubicin
• Doxorubicin Hydrochloride Liposome
• Elacestrant
• Elexacaftor
• Encorafenib
• Entrectinib
• Enzalutamide
• Eplerenone
• Ergotamine
• Fedratinib
• Fentanyl
• Fexinidazole
• Finerenone
• Fosaprepitant
• Fosnetupitant
• Fosphenytoin
• Gemfibrozil
• Gepirone
• Ginseng
• Hydrocodone
• Ibrutinib
• Ifosfamide
• Infigratinib
• Influenza Virus Vaccine, Live
• Itraconazole
• Ivabradine
• Ivacaftor
• Ivosidenib
• Ketoconazole
• Larotrectinib
• Lemborexant
• Levoketoconazole
• Lumacaftor
• Lumateperone
• Lurasidone
• Lurbinectedin
• Mavacamten
• Meperidine
• Methadone
• Methotrexate
• Midazolam
• Mitapivat
• Mitotane
• Mobocertinib
• Naloxegol
• Netupitant
• Olaparib
• Omaveloxolone
• Oxycodone
• Pacritinib
• Palovarotene
• Pemigatinib
• Pentazocine
• Pexidartinib
• Phenobarbital
• Phenytoin
• Pimozide
• Piperaquine
• Poliovirus Vaccine, Live
• Pralsetinib
• Primidone
• Rifampin
• Rimegepant
• Selpercatinib
• Selumetinib
• Simeprevir
• Sirolimus Protein-Bound
• Smallpox Vaccine
• Sonidegib
• Sparsentan
• St John's Wort
• Sufentanil
• Tacrolimus
• Tafamidis
• Tazemetostat
• Tezacaftor
• Tolvaptan
• Tramadol
• Typhoid Vaccine, Live
• Ubrogepant
• Venetoclax
• Venlafaxine
• Voclosporin
• Warfarin
• Yellow Fever Vaccine
• Zanubrutinib
• Zolpidem

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Eltrombopag
• Levothyroxine
• Suvorexant

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. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

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
• Ascites (fluid in the abdomen) or
• Bleeding problems or
• Congestive heart failure or
• Hypothyroidism (underactive thyroid) or
• Infection or
• Neutropenia (low white blood cells) or
• Pericardial effusion (fluid around the heart) or
• Pleural effusion (fluid around the lungs) or
• Pulmonary edema (fluid in the lungs) or
• Stomach bleeding or
• Stomach perforation (hole in the stomach) or
• Thrombocytopenia (low number of platelets)—Use with caution. May make these conditions worse.

• Kidney disease or
• Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of This Medicine:

Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. 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.

Swallow the tablet whole. Do not break or crush it.

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 is dissolved.

Do not eat grapefruit or drink grapefruit juice while you are using this medicine. Grapefruit and grapefruit juice may cause the blood levels of this medicine to be higher than normal.

Be careful not to handle crushed or broken tablets. If you have contact with broken or crushed tablets, wash your skin with soap and water right away.

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 (tablets):
  • For the treatment of aggressive systemic mastocytosis (ASM):
    • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
    • Children—Use and dose must be determined by your doctor.
  • For the treatment of chronic eosinophilic leukemia (CEL) or hypereosinophilic syndrome (HES):
    • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
    • Children—Use and dose must be determined by your doctor.
  • For the treatment of dermatofibrosarcoma protuberans (DFSP):
    • Adults—800 milligrams (mg) per day as a single dose or divided and given as 400 mg 2 times per day.
    • Children—Use and dose must be determined by your doctor.
  • For the treatment of gastrointestinal stromal tumors (GIST):
    • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 800 mg per day.
    • Children—Use and dose must be determined by your doctor.
  • For the treatment of myelodysplastic syndrome (MDS) or myeloproliferative diseases (MPD):
    • Adults—400 milligrams (mg) once a day.
    • Children—Use and dose must be determined by your doctor.
  • For the treatment of Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL):
    • Adults—600 milligrams (mg) once a day.
    • Children 1 year of age and older—Dose is based on body size and must be determined by your doctor. The dose is usually 340 milligrams per square meter (mg/m[2]) per day. The dose may be taken once a day or the dose may be divided into two small doses (once in the morning and once in the evening). However, the dose is usually not more than 600 mg per day.
    • Children younger than 1 year of age—Use and dose must be determined by your doctor.
  • For the treatment of Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML):
    • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 800 mg per day.
    • Children 1 year of age and older—Dose is based on body size and must be determined by your doctor. The dose is usually 340 milligrams per square meter (mg/m[2]) per day. The dose may be taken once a day or divided into 2 small doses (once in the morning and once in the evening). However, the dose is usually not more than 600 mg per day.
    • Children younger than 1 year of age—Use and dose must be determined by your doctor.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, 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.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

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

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. Blood tests may be needed to check for unwanted effects. Be sure to keep all appointments.

Using this medicine while you are pregnant can harm your unborn baby. Use a highly effective form of birth control (especially if you are a sexually active female patient) during treatment and for 14 days after your last dose to keep from getting pregnant. 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 blistering, peeling, or loosening of the skin, red skin lesions, severe acne or skin rash, sores or ulcers on the skin, or fever or chills while you are using this medicine.

Some serious side effects such as black, tarry stools, severe stomach pain, or vomiting of blood or material that looks like coffee grounds 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 the 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.

If you are rapidly gaining weight, having chest pain or discomfort, extreme tiredness or weakness, difficulty with breathing, uneven heartbeat, or excessive swelling of the hands, wrist, ankles, or feet, check with your doctor immediately. These may be symptoms of heart problems or your body keeping too much water.

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, unusual tiredness or weakness, or yellow eyes or skin. These could be symptoms of a serious liver problem.

This medicine may cause slow growth. If your child is using this medicine, the doctor will need to keep track of your child's height and weight to make sure that your child is growing properly.

This medicine may cause a serious type of reaction called tumor lysis syndrome. Your doctor may give you a medicine to help prevent this. Call your doctor right away if you have a decrease or change in urine amount, joint pain, stiffness, or swelling, lower back, side, or stomach pain, a rapid weight gain, swelling of the feet or lower legs, or unusual tiredness or weakness.

This medicine may cause dizziness, drowsiness, or trouble in seeing clearly. Make sure you know how you react to this medicine before you drive, use machines, or do other jobs that require you to be alert or able to see well.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

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 or stomach pain, cramping, burning, or tenderness

bleeding from wound after surgery

bleeding gums

bleeding problems

bloating or swelling of the face, hands, lower legs, 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 the 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 or skin rash

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

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

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 or leg on one side of the body, sudden and severe

yellow eyes or skin

Incidence not known

Anxiety

blistering, peeling, or loosening of the skin

change in vision not present before treatment

chest pain, possibly moving to the left arm, neck, or shoulder

confusion

delayed or slow growth in children

irregular, fast or slow, or shallow breathing

nausea, heartburn, or indigestion, severe and continuing

pain in the bones

red, irritated eyes

red skin lesions, often with a purple center

seeing floaters, veil, or curtain appearing across part of vision

severe abdominal or stomach pain, cramping, or burning

severe constipation

severe vomiting

tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over affected area

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

difficulty having a bowel movement (stool)

difficulty with moving

discouragement

excess air or gas in the stomach or intestines

fear or nervousness

feeling sad or empty

feeling unusually cold

full or bloated feeling

increased bowel movements

irritability

lack or loss of strength

loose stools

loss of interest or pleasure

muscle stiffness

night sweats

passing gas

stomach discomfort, upset, or pain

swollen joints

trouble concentrating

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.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.