Selective α1a‐adrenoreceptor antagonists are effective agents for treatment of benign prostatic hyperplasia, a disorder occurring in middle‐aged and elderly males. The objective of this study was to determine the single‐ and multiple‐dose pharmacokinetics of fiduxosin, a novel, selective α1a‐adrenoreceptor antagonist. This was a Phase I, randomized, double‐blind, placebo‐controlled, parallel‐group, single and multiple oral dose study of fiduxosin. Single daily oral doses of 30, 60, or 90 mg of fiduxosin or placebo were administered to healthy adult male subjects (N = 36; 8 active and 4 placebo per dosing group) on Day 1 and Days 5 to 11 (7 consecutive days) after a high‐fat breakfast. Fiduxosin plasma concentration‐time profiles for Days 1 and 11 were used to assess fiduxosin pharmacokinetics. Fiduxosin single‐dose and steady‐state pharmacokinetics were dose independent after oral administration under nonfasting conditions. Steady state was achieved after 4 days of qd dosing. Approximately 28% of the oral dose was eliminated by the fecal route as unchanged drug. Less than 1% of the unchanged drug was recovered in the urine after oral administration.

01 May 2002·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

Multiple dose pharmacokinetics of fiduxosin under fasting conditions in healthy elderly male subjects

Q3 · MEDICINE

Article

Author: Dutta, Sandeep ; Zhang, Yiming ; Daszkowski, Daniel J ; Verlinden, Marleen ; Granneman, G Richard

AbstractSelective α1a-adrenoceptor antagonists are effective agents for treatment of benign prostatic hyperplasia, a disorder occurring in middle-aged and elderly males. The objective of this study was to determine the pharmacokinetics of fiduxosin, a novel α1a-adrenoceptor antagonist, following multiple dose administration. This was carried out in a Phase I, randomized, double-blind, placebo-controlled, parallel group, multiple oral dose study of fiduxosin. Single once-daily oral doses of 30, 60, 90 or 120 mg of fiduxosin or placebo were administered to healthy elderly male subjects (n = 48; 8 active and 4 placebo per dosing group) for 14 consecutive days. Fiduxosin plasma concentration-versus-time prof les for days 1, 7 and 14 were used to assess fiduxosin pharmacokinetics. Steady state was achieved by day 7. At steady-state mean Tmax (time to maximum plasma concentration), CL/F (apparent oral clearance) and Vβ/F (apparent volume of distribution) ranges were 1.8-7.8h, 27.3–47.2 L h−1 and 846-1399L, respectively. Tmax and Vβ/F were independent of dose. Cmax (maximum plasma concentration), Cmin (minimum plasma concentration) and AUC24 (area under plasma concentration vs time curve from 0 to 24 h) for days 7 and 14 were linearly proportional with dose over the 30–120 mg/day dose range and were unchanged from day 7 to day 14. It was concluded that fiduxosin multiple-dose pharmacokinetics were dose-independent and time-invariant over the 30–120 mg/day dose range under fasting conditions.

01 Mar 2002·European Journal of Drug Metabolism and PharmacokineticsQ4 · MEDICINE

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

Q4 · MEDICINE

Article

Author: Sandeep Dutta ; G. Richard Granneman ; Marleen Verlinden ; Yiming Zhang

The effect of food on the pharmacokinetics of fiduxosin, a novel selective alpha1a-receptor antagonist, was determined in healthy male subjects. This was a Phase I, 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 Cmax, Tmax, AUC(infinity), CL/F and Vbeta/F values under fasting and nonfasting conditions were 34.3 and 150 ng/mL, 5.4 and 5.4 h, 822 and 1940 ng x 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 Cmax central value was more than 4-fold and the AUC(infinity) central value more than 2-fold the central value of the fasting regimen. Tmax was not significantly different between fasting and nonfasting regimens. Food also decreased fiduxosin oral clearance (CL/F) by 60% and volume of distribution (Vbeta/F) by 75%.

100 Deals associated with Fiduxosin Hydrochloride

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Indication	Highest Phase	Country/Location	Organization	Date
Prostatic Hyperplasia	Phase 2	US	Abbott Laboratories	-

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