Marketing Authorisation Holder
Sites are permitted to use any brand/generic of Imatinib.
Dosing regime
800mg loading dose, followed by a dose of 400mg enteral imatinib once daily for 9 days (total of 10 days therapy). Patients not able to swallow can receive imatinib as a suspension via a nasogastric tube if one has been placed as part of routine care.
Dose changes
Imatinib is a substrate for CYP3A4, and inhibits CYP3A4, CYP2D6 and CYP2C9. CYP3A4 inducers that may reduce imatinib levels: rifampicin, phenytoin, carbamazepine, and dexamethasone. Concomitant administration of these drugs should be avoided.
CYP3A4 inhibitors that may increase imatinib levels but no dose changes are required for azoles like ketoconazole, erythromycin, itraconazole.
Drugs that may have their plasma concentration increased by imatinib but no need for any dose change: cyclosporin, pimozide, statins, triazole-benzodiazepines, tacrolimus, sirolimus, ergotamine, diergotamine, fentanyl, alfentanil, terfenadine, bortezomib, docetaxel, quinidine, warfarin.
In general imatinib is relatively insensitive for CYP3A4 inhibition, as other routes may take over metabolism. Therefore, there is no need for adjustment, but registration of the following drugs is required: Lopinavir/ritonavir, and azole group of drugs
Date entered TRAITS
July 2023