Effect of food on the pharmacokinetics of fiduxosin in healthy male subjects

The effect of food on the pharmacokinetics of fiduxosin, a novel selective alpha(1a)-receptor antagonist, was determined in healthy male subjects. This was a Phase 1, open-label, single-center, randomized, two-period, crossover, single oral dose study of fiduxosin. Healthy male subjects (N=14) were administered single oral doses of 30 mg of fiduxosin under fasting or nonfasting (1026 Kcal, 54 g fat, 46% calories from fat) conditions in each period. Fiduxosin plasma concentration profiles were used to assess fiduxosin Pharmacokinetics. The mean C-max, T-max, AUC(infinity), CL/F and V-beta/F values under fasting and nonfasting conditions were 34.3 and 150 ng/mL, 5.4 and 5.4 h, 822 and 1940 ng.h/mL, 42.5 and 17.2 L/h, and 924 and 235 L, respectively, The harmonic mean t(1/2) under fasting and nonfasting conditions were 13.9 and 9.28 h, respectively. Food significantly increased the bioavailability of fiduxosin. Under the nonfasting regimen, the C-max central value was more than 4-fold and the AUC(infinity) central value more than 2-fold the central value of the fasting regimen. T-max was not significantly different between fasting and nonfasting regimens. Food also decreased fiduxosin oral clearance (CL/F) by 60% and volume of distribution (V-beta/F) by 75%.