imatinib mesilate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
imatinib mesilate: clinical details
Prescribing considerations
- Initiation and supervision by clinicians experienced in haematological malignancies or malignant sarcomas.
- Confirm the relevant molecular or cellular target and licensed disease context.
- Review hepatic, renal and cardiac disease, fluid status, bleeding risk, interactions and pregnancy potential.
- Correct clinically important dehydration and hyperuricaemia where tumour lysis is a concern.
- Assess photosensitivity risk and advise sun protection.
Contraindications and cautions
- Hypersensitivity to imatinib or a formulation excipient.
- Exercise particular caution with hepatic or renal impairment, cardiac dysfunction, previous hepatitis B infection and conditions carrying a high bleeding risk.
Monitoring
- Full blood count and liver function regularly.
- Renal function before treatment and during long-term therapy.
- Weight and evidence of fluid retention or cardiac or renal failure.
- Hepatitis B screening before initiation and ongoing surveillance in carriers.
- Thyroid-stimulating hormone in thyroidectomised patients receiving levothyroxine.
- Growth in children and adolescents.
- Disease-specific haematological, cytogenetic or molecular response.
Clinical pharmacology
An orally absorbed small-molecule inhibitor of BCR-ABL, KIT, PDGFR and several other receptor tyrosine kinases. It is highly protein-bound, principally metabolised through CYP3A4 and has an active N-demethylated metabolite.
Formulation and product differences
- The selected film-coated tablet is scored and may be dispersed in still water or apple juice if swallowing is difficult.
- The selected hard capsule contains lactose. Its contents may be dispersed if swallowing is difficult, but opening requires precautions to avoid inhalation and skin or eye contact.
imatinib mesilate preparations and strengths
Capsule
Route: Oral
Strengths: 100 mg, 400 mg
Tablet
Route: Oral
Strengths: 100 mg, 400 mg, 600 mg
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.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.