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HOME >> API >> API List 2 >> Imatinib Mesylate >> Interaction

Imatinib Mesylate CAS Registry Number 220127-57-1

INTERACTION
Imatinib Mesylate

Pretreatment of healthy volunteers with multiple doses of rifampin followed by a single dose of , increased  oral-dose clearance by 3.8-fold, which significantly (p < 0.05) decreased mean Cmax and AUC. If alternative treatment cannot be administered
Agents Inhibiting CYP3A Metabolism

There was a significant increase in exposure to imatinib (mean Cmax and AUC increased by 26% and 40%, respectively) in healthy subjects when  was co-administered with a single dose of ketoconazole (a CYP3A4 inhibitor). Caution is recommended when administering  with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, and voriconazole). Grapefruit juice may also increase plasma concentrations of imatinib and should be avoided. Substances that inhibit the cytochrome P450 isoenzyme (CYP3A4) activity may decrease metabolism and increase imatinib concentrations.
Interactions with Drugs Metabolized by CYP3A4.

 increases the mean Cmax and AUC of simvastatin (CYP3A4 substrate) 2- and 3.5-fold, respectively, suggesting an inhibition of the CYP3A4 by . Particular caution is recommended when administering

with CYP3A4 substrates that have a narrow therapeutic window (e.g., alfentanil, cyclosporine, diergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus or tacrolimus).
Interactions with Drugs Metabolized by CYP2D6

In vitro,  inhibits the cytochrome P450 isoenzyme CYP2D6 activity at similar concentrations that affect CYP3A4 activity. Systemic exposure to substrates of CYP2D6 is expected to be increased when coadministered with . No specific studies have been performed and caution is recommended.
Interaction with Acetaminophen

In vitro,  inhibits acetaminophen O-glucuronidation (Ki value of 58.5 µM) at therapeutic levels.

Systemic exposure to acetaminophen is expected to be increased when co-administered with . No specific studies in humans have been performed and caution is recommended.

Information Associated with Product:
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