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Tolerability, Pharmacokinetics, and Neuroendocrine Effects of PRX‐00023, a Novel 5‐HT1A Agonist, in Healthy Subjects
Author(s) -
Iyer Ganesh R.,
Jr John F. Reinhard,
Oshana Scott,
Kauffman Michael,
Donahue Stephen
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 - 10.1177/0091270007300953
Subject(s) - tolerability , pharmacokinetics , medicine , pharmacology , agonist , pharmacodynamics , physiology , adverse effect , receptor
PRX‐00023 is a novel, nonazapirone 5‐HT1A agonist in clinical development for treatment of affective disorders. The objectives of the initial clinical phase I studies (a single ascending dose study and multiple dose‐ascending and high‐dose titration studies) were to measure the pharmacokinetics, pharmacodynamic (neuroendocrine) effects, and tolerability of PRX‐00023 in healthy subjects. The studies evaluated 10‐mg to 150‐mg doses of PRX‐00023 in up to 112 healthy male and female subjects aged 18 to 54 years. Single and multiple oral doses of PRX‐00023 were found to be safe and well tolerated in healthy subjects. PRX‐00023 was absorbed relatively rapidly, with a t max of 0.5 to 2 hours, and eliminated with a half‐life of approximately 12 hours. PRX‐00023 treatment transiently increased blood prolactin levels 2 to 3 hours after administration, consistent with its mechanism as a 5‐HT1A agonist.