What is imatinib used for?

Imatinib is used to treat various cancers, including chronic myeloid leukemia (CML), certain types of acute lymphoblastic leukemia (ALL), and gastrointestinal stromal tumors (GIST).

How should I take imatinib?

You should take imatinib tablets orally with a meal and a large glass of water.

Can I take imatinib if I am pregnant?

No, imatinib can cause fetal harm and birth defects; women should avoid pregnancy while using this medication.

Is it safe to breastfeed while on imatinib?

It is advised not to breastfeed during treatment and for one month after your last dose because the drug passes into breast milk.

What are the most common side effects of imatinib?

The most frequent side effects are swelling, nausea, vomiting, muscle cramps, diarrhea, rash, and fatigue.

Should I avoid grapefruit juice while taking imatinib?

Yes, you should avoid grapefruit juice because it can increase the levels of imatinib in your body.

Can imatinib cause heart problems?

Yes, severe heart failure and heart dysfunction have been reported in some patients.

Does imatinib affect my liver?

Yes, severe liver toxicity can occur, so your liver function should be checked monthly.

Imatinib | CAS 152459-95-5 | KTUFNOKKBVMGRW

Loading compound...

Kinase inhibitor

Imatinib (brand name Gleevec) is a small molecule kinase inhibitor used to treat several types of blood cancers and specific tumor types. It works by blocking specific proteins that help cancer cells grow and survive.

How it worksImatinib works by blocking certain proteins, such as the BCR-ABL tyrosine kinase, that act like 'on switches' for cancer cell growth. By turning these switches off, the drug helps stop cancer cells from multiplying and can cause them to die.

Brand names:GLEEVEC

Used for

Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in adults and childrenChronic myeloid leukemia in blast crisis, accelerated phase, or chronic phase after interferon-alpha therapy failedRelapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in adultsNewly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in children (used with chemotherapy)Myelodysplastic/myeloproliferative diseases (MDS/MPD) linked to PDGF gene changesAggressive systemic mastocytosis (ASM)Hypereosinophilic syndrome (HES) and chronic eosinophilic leukemia (CEL)Dermatofibrosarcoma protuberans (DFSP)Gastrointestinal stromal tumors (GIST)

Conditions

Ph+ CMLPh+ ALLMDS/MPDASMHES/CELDFSPGIST

Class

Kinase InhibitorSmall MoleculeAntineoplasticKinase inhibitorHematologicCardiovascularHepaticGastrointestinalIntegumentaryEndocrineRenal

How to take

Forms100 mg film-coated tablets, 400 mg film-coated tablets

RoutesOral

Doses vary widely based on the specific condition being treated, ranging from 100 mg to 800 mg per day. For example, adults with Ph+ CML in the chronic phase typically take 400 mg once daily.

Tablets should be taken with a meal and a large glass of water. If you have trouble swallowing, tablets can be dissolved in water or apple juice. If a daily dose of 800 mg is prescribed, it should be taken as 400 mg twice a day.

Key warnings

·Monitor for sudden weight gain or swelling, which may indicate fluid retention.
·Regular blood counts are necessary to check for low red blood cells, white blood cells, or platelets.
·Liver function should be checked before starting treatment and monthly thereafter.
·Watch for signs of heart problems, especially if you have existing heart risk factors.
·Be aware of the risk of serious bleeding or holes in the digestive tract.

Do not use if

·None listed

Side effects

Common

Edema (swelling)NauseaVomitingMuscle crampsMuscle or musculoskeletal painDiarrheaRashFatigueAbdominal pain

Serious

·Severe fluid retention and swelling
·Low blood counts (anemia, neutropenia, or thrombocytopenia)
·Heart failure or heart dysfunction
·Severe liver problems (hepatotoxicity)
·Severe bleeding (hemorrhage)
·Gastrointestinal perforation (holes in the stomach or intestines)
·High eosinophil levels causing heart toxicity
·Skin reactions (bullous dermatologic reactions)
·Thyroid issues (hypothyroidism)
·Growth retardation in children
·Tumor lysis syndrome
·Kidney toxicity

Seek help if

·Severe swelling
·Shortness of breath
·Signs of bleeding
·Yellowing of skin or eyes (jaundice)
·Severe stomach pain

Interactions

·Strong CYP3A4 inducers may make imatinib less effective.
·Strong CYP3A4 inhibitors may increase the amount of imatinib in your body.
·Grapefruit juice can increase imatinib levels; it should be avoided.
·Imatinib may increase the levels of other drugs that use the CYP3A4 or CYP2D6 pathways.
·High doses of methotrexate may stay in the body longer when taken with imatinib.
·Patients needing blood thinners should use heparin rather than warfarin.

FoodTake imatinib with a meal and a large glass of water. Avoid grapefruit juice.

Special populations

PregnancyImatinib can cause serious harm to an unborn baby. Animal studies have shown it can cause birth defects. Women should avoid pregnancy while taking this medication.

BreastfeedingImatinib and its active forms pass into breast milk. It is advised that women do not breastfeed while taking this drug and for at least 1 month after the last dose.

PediatricImatinib is used in children for certain types of leukemia, but there is no safety data available for children under 1 year of age.

GeriatricIn studies, older patients (over 65) experienced higher rates of swelling (edema) compared to younger patients, though the drug worked similarly well.

Talk to your doctor

Monitor

·Weight (for fluid retention)
·Blood counts (anemia, neutropenia, thrombocytopenia)
·Liver function
·Heart health/cardiac symptoms
·Signs of bleeding

Questions to ask

·How often will my blood counts and liver function be checked?
·What should I do if I experience sudden swelling or weight gain?
·Are there specific foods or drinks I must avoid?
·How should I manage nausea or diarrhea if they occur?

Pharmacokinetics

OnsetC max achieved within 2 to 4 hours post-dose

Bioavailability98%

Protein bindingClinically relevant concentrations result in binding to plasma proteins

MetabolismMetabolized by CYP3A4 and CYP2D6

Practical

OverdoseIf an overdose occurs, the patient should be monitored and given supportive care. Symptoms of overdose can include nausea, vomiting, diarrhea, rash, swelling, fatigue, muscle spasms, and low blood counts.

Ingredients

Inactive

colloidal silicon dioxidecrosspovidonemagnesium stearateferric oxide redferric oxide yellowhypromellosehydroxypropyl cellulosepolyethylene glycol

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.