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Pharmacokinetics, Tolerability, and Safety of ACP‐103 Following Single or Multiple Oral Dose Administration in Healthy Volunteers
Author(s) -
Vanover Kimberly E.,
RobbinsWeilert Doris,
Wilbraham Darren G.,
Mant Timothy G. K.,
Kammen Daniel P.,
Davis Robert E.,
Weiner David M.
Publication year - 2007
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270007299431
Subject(s) - pharmacokinetics , tolerability , medicine , pharmacology , oral administration , placebo , bioavailability , adverse effect , alternative medicine , pathology
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–∞ (706–10 798 h·ng/mL), and multiple doses (50–150 mg) resulted in dose‐proportionate mean C max, ss (93–248 ng/mL) and AUC 0–∞,ss (1839–4680 h·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.