GENERAL NEWS – ENZALUTAMIDE (ANTINEOPLASTIC AGENT) ADDED TO FUNGAL PHARMACOLOGY

Significant interaction with itraconazole, posaconazole, fluconazole and voriconazole

24/12/2015 - A new interacting agent has been added to Fungal Pharmacology: enzalutamide (antineoplastic agent: clinically significant interactions with itraconazole, posaconazole, fluconazole and voriconazole).

One drug-drug interaction study with a parallel-treatment design (n = 41) evaluated the effects of itraconazole (200 mg once daily) on the pharmacokinetics of enzalutamide and its active metabolite N-desmethyl enzalutamide after a single dose of enzalutamide (160 mg). Coadministration of itraconazole increased the composite AUC(0-inf) by 1.3-fold. A single-sequence crossover design (n = 14) was used to determine the effects of enzalutamide 160 mg/day on the pharmacokinetics of a single oral dose of sensitive substrates for CYP2C8 (pioglitazone 30 mg), CYP2C9 (warfarin 10 mg), CYP2C19 (omeprazole 20 mg), or CYP3A4 (midazolam 2 mg). Enzalutamide reduced the AUC(0-inf) of oral S-warfarin, omeprazole, and midazolam by 56, 70, and 86 %, respectively; therefore, enzalutamide is a moderate inducer of CYP2C9 and CYP2C19 and a strong inducer of CYP3A4.

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