Pharmacokinetics, tolerability, and safety of ACP-103 following single or multiple oral dose administration in healthy volunteers

• Published in: Journal of clinical pharmacology Vol. 47; no. 6; p. 704
• Main Authors: Vanover, Kimberly E, Robbins-Weilert, Doris, Wilbraham, Darren G, Mant, Timothy G K, van Kammen, Daniel P, Davis, Robert E, Weiner, David M
• Format: Journal Article
• Language: English
• Published: England 01.06.2007
• Subjects: Adolescent; Adult; Area Under Curve; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Half-Life; Humans; Male; Middle Aged; Piperidines - administration & dosage; Piperidines - adverse effects; Piperidines - pharmacokinetics; Serotonin 5-HT2 Receptor Agonists; Urea - administration & dosage; Urea - adverse effects; Urea - analogs & derivatives; Urea - pharmacokinetics
• ISSN: 0091-2700
• DOI: 10.1177/0091270007299431

The pharmacokinetics, safety, and tolerability of ACP-103, a selective serotonin 5-HT(2A) receptor inverse agonist, were evaluated in 2 double-blind, placebo-controlled, dose escalation studies in healthy male volunteers. Pharmacokinetic sampling was measured up to 216 hours after single oral/nasogastric doses of ACP-103 and after the last dose of once-daily oral administration of ACP-103 for 14 days. Single doses of ACP-103 (20-300 mg) resulted in dose-proportionate mean C(max) values (9-152 ng/mL) and AUC(0-infinity) (706-10 798 h x ng/mL), and multiple doses (50-150 mg) resulted in dose-proportionate mean C(max,ss) (93-248 ng/mL) and AUC(0-infinity,ss) (1839-4680 h x ng/mL). The half-life of ACP-103 was approximately 55 hours, with a t(max) at 6 hours. ACP-103 was well tolerated at single doses up to and including 300 mg and multiple doses up to 100 mg once daily for 14 days.