The open-label study was conducted to determine the potential pharmacokinetic interaction of itraconazole (200 mg), an antifungal agent that strongly inhibits CYP3A4, on the pharmacokinetics of LIVALO (4 mg). The secondary objective assessed the safety of LIVALO 4 mg with the addition of itraconazole. Eighteen healthy males (aged 18 to 55 years) received LIVALO 4 mg once daily on days 1 and 8, and itraconazole 200 mg once daily on days 5 to 9. The results of this study showed that itraconazole did not increase plasma concentrations of LIVALO or its main metabolite pitavastatin lactone, potentially reducing the incidence of adverse events.

Additionally, LIVALO was shown to be well tolerated both as monotherapy and when combined with itraconazole and was not associated with any moderate or severe adverse events or clinically relevant changes in laboratory, vital or physical signs or ECG. No subjects withdrew from the study.

"This study suggests that, compared with other commonly prescribed statins, LIVALO's metabolic route may offer a favorable tolerability profile when administered with drugs that inhibit CYP3A4," said Roger E. Morgan, M.D., Chief Medical Officer, Kowa Research Institute. "Combined with LIVALO's safety and efficacy profile, the low incidence of drug-drug interactions represents a benefit in the long-term treatment of patients with dyslipidemia."

These results support previous LIVALO studies showing that grapefruit juice did not have a significant effect on plasma concentrations (<15%).( )

Source: kowapharma