Tolerability, pharmacokinetics, and neuroendocrine effects of PRX-00023, a novel 5-HT1A agonist, in healthy subjects.

Abstract

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 tmax 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.

• Authors: Ganesh R Iyer, John F Reinhard Jr, Scott Oshana, Michael Kauffman, Stephen Donahue
• Journal: Journal of clinical pharmacology (J Clin Pharmacol) Vol. 47 Issue 7 Pg. 817-24 (Jul 2007) ISSN: 0091-2700 [Print] England
• PMID: 17495280 (Publication Type: Clinical Trial, Phase I, Journal Article)

Chemical References

• Antidepressive Agents
• Piperazines
• Serotonin 5-HT1 Receptor Agonists
• Sulfonamides
• Prolactin
• naluzotan

Topics

• Adolescent
• Adult
• Antidepressive Agents (administration & dosage, adverse effects, pharmacokinetics, pharmacology)
• Cohort Studies
• Double-Blind Method
• Female
• Half-Life
• Humans
• Male
• Middle Aged
• Piperazines (administration & dosage, adverse effects, pharmacokinetics, pharmacology)
• Prolactin (blood)
• Serotonin 5-HT1 Receptor Agonists
• Sulfonamides (administration & dosage, adverse effects, pharmacokinetics, pharmacology)