Single- and multiple-dose pharmacokinetics of fiduxosin under nonfasting conditions in healthy male subjects.
Selective alpha1a-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 alpha1a-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.
Dutta
Sandeep
S
Clinical Pharmacokinetics, Abbott Laboratories, Abbott Park, IL 60064-6104, USA.
Zhang
Yiming
Y
Daszkowski
Daniel J
DJ
Granneman
G Richard
GR
Verlinden
Marleen
M
D000284:Administration, Oral; D000368:Aged; D019540:Area Under Curve; D004041:Dietary Fats / Q000008:administration & dosage / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005215:Fasting; D005243:Feces / Q000737:chemistry; D018565:Food-Drug Interactions; D006262:Health; D006575:Heterocyclic Compounds, 3-Ring / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D006801:Humans; D008297:Male; D008875:Middle Aged; D011744:Pyrimidinones / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine
D004041:Dietary Fats; D006575:Heterocyclic Compounds, 3-Ring; D011744:Pyrimidinones; C447622:fiduxosin