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Pharmacokinetics and Safety of Fosf luconazole after Single Intravenous Bolus Injection in Healthy Male Japanese Volunteers

From Pfizer Global R&D, Tokyo Laboratories, Pfizer Japan, Inc., Tokyo, Japan (S. Sobue, Dr. Sekiguchi, K. Shimatani) and Clinical Sciences, Pfizer Global R&D, Sandwich, Kent, United Kingdom (Dr. Tan).

This was a single blind, placebo-controlled, escalating single-dose, three-period crossover study using two subject cohorts to investigate the safety, tolerability, and pharmacokinetics in healthy male Japanese subjects after intravenous bolus injection of fosfluconazole 50 to 2000 mg, a phosphate prodrug of fluconazole (FLCZ). Fosfluconazole was rapidly converted to FLCZ with only minor amounts excreted in the urine (less than 4% of the dose). Fosfluconazole had a volume of distribution at the higher doses, which was similar to the extracellular volume in man (0.2 L/kg) and was eliminated with a terminal half-life of 1.5 to 2.5 hours. There was apparent dose proportionality in FLCZ pharmacokinetics. C_max and AUC of FLCZ appeared to increase proportionally with increasing doses of fosfluconazole. There were no apparent dose-dependent trends in t_max, t_1/2, or mean residence time (MRT) of FLCZ. Bolus injection of fosfluconazole was well tolerated at doses of up to 2000 mg in healthy Japanese subjects.

Key Words: Fosfluconazole • fluconazole • antifungal drug • pharmacokinetics • safety

Address for reprints: Satoshi Sobue, Department of Clinical Pharmacology, Pfizer Global R&D, Tokyo Laboratories, Pfizer Japan, Inc., Shinjuku Bunka Quint Bldg. 3-22-7, Yoyogi, Shibuya-ku, Tokyo 151-8589, Japan.

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