imatinib mesilate at a glance
Medicine class
BCR-ABL tyrosine kinase inhibitor
Main roles
Selected leukaemias, gastrointestinal stromal tumours and other uncommon cancers linked to susceptible kinases
Administration
Take with a meal and a large glass of water to reduce stomach irritation
Monitoring
Regular blood counts and liver and kidney function checks are important
What is imatinib mesilate used for?
Eligibility depends on the diagnosis, disease stage and molecular or cell-marker results.
Philadelphia chromosome-positive chronic myeloid leukaemia in adults and children
Philadelphia chromosome-positive acute lymphoblastic leukaemia in adults and children, including alongside chemotherapy in newly diagnosed disease
PDGFR-rearranged myelodysplastic or myeloproliferative diseases in adults
FIP1L1-PDGFRα-rearranged advanced hypereosinophilic syndrome or chronic eosinophilic leukaemia in adults
KIT-positive gastrointestinal stromal tumours in adults, including unresectable or metastatic disease and selected patients with a significant recurrence risk following surgery
Unresectable, recurrent or metastatic dermatofibrosarcoma protuberans in adults who are not eligible for surgery
How does imatinib mesilate work?
Imatinib blocks tyrosine kinases including BCR-ABL, KIT and PDGFR. When abnormally active, these proteins send continuous growth signals. Blocking them can slow abnormal cell multiplication and promote cell death.
imatinib mesilate preparations and strengths
Capsule
Route: Oral
Strengths: 100 mg, 400 mg
Tablet
Route: Oral
Strengths: 100 mg, 400 mg, 600 mg
How to take imatinib mesilate
Follow the specialist team’s instructions and do not stop treatment without speaking to them.
Take with a meal and a large glass of water.
Swallow capsules whole where possible. If swallowing is difficult, the selected capsule contents may be dispersed in still water or apple juice.
The selected film-coated tablet may be dispersed in still water or apple juice and taken immediately after it has fully broken up.
Avoid inhaling or touching capsule contents and avoid eye contact; wash hands immediately afterwards.
Use caution when driving or using machinery if dizziness, drowsiness or blurred vision occurs.
imatinib mesilate side effects
Common or expected effects
- Nausea, vomiting, diarrhoea, indigestion or abdominal pain
- Headache or fatigue
- Muscle cramps and muscle, joint or bone pain
- Rash or itching
- Swelling around the eyes or ankles and weight gain
Get urgent medical advice
- Fever, severe chills, sore throat or mouth ulcers suggesting infection
- Unexpected bleeding or bruising
- Rapid weight gain, breathlessness or extensive swelling suggesting significant fluid retention
- Yellow skin or eyes, dark urine or severe loss of appetite suggesting liver injury
- Severe abdominal pain, vomiting blood, black stools or blood in stools
- Severe rash, blistering or peeling skin, including the mouth or eyes
- Seizures, reduced consciousness, sudden weakness or difficulty speaking
- Markedly reduced urine, unusual bleeding with confusion, or severe pallor and breathlessness
imatinib mesilate in pregnancy
Imatinib is generally avoided during pregnancy unless a specialist considers it clearly necessary. Congenital anomalies and pregnancy losses have been reported, although human information is limited. Discuss planned or suspected pregnancy promptly with the specialist team and do not stop treatment independently. Effective contraception is advised during treatment and for a short period afterwards.
imatinib mesilate while breastfeeding
Imatinib and its active metabolite enter breast milk, and the effect of ongoing exposure on an infant is unknown. The selected product information advises against breastfeeding during treatment and for a short period after stopping. Seek specialist advice when planning feeding.
imatinib mesilate interactions
Check all prescribed, non-prescription and herbal products with the specialist team or pharmacist.
Rifampicin, carbamazepine, phenytoin, phenobarbital and other strong CYP3A4 inducers
They can substantially lower imatinib exposure and risk loss of treatment effect, so concurrent use should generally be avoided.
St John’s wort
It can lower imatinib exposure and should be avoided.
Common questions about imatinib mesilate
Answers are fully visible for fast scanning and source review.
Is imatinib mesilate chemotherapy?
It is a targeted anticancer treatment rather than traditional cytotoxic chemotherapy. It may be used alongside chemotherapy for some Philadelphia chromosome-positive acute lymphoblastic leukaemia.
Why should it be taken with food?
Taking it with a meal and plenty of water helps reduce irritation of the stomach and digestive tract.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.