Pharmacokinetics, safety, and tolerability of phentermine in healthy participants receiving taranabant, a novel cannabinoid-1 receptor (CB1R) inverse agonist

J Clin Pharmacol. 2009 Oct;49(10):1228-38. doi: 10.1177/0091270009341651.

Abstract

This study assessed the potential pharmacokinetic interaction and safety/tolerability of taranabant and phentermine coadministration. This was a randomized, double-blind, 3-panel, fixed-sequence study in healthy participants. Panels A, B, and C evaluated the safety/tolerability of phentermine 15 mg coadministered with taranabant 0.5, 1, and 2 mg for 7 days (panel A) and 28 days (panels B and C). In panels A and C, phentermine 15 mg was administered both with (7 days, panel A; 28 days, panel C) and without (7 days) taranabant 0.5 mg or 2 mg to evaluate pharmacokinetics. The primary endpoint was phentermine AUC(0-24 h) in panels A and C. Secondary endpoints were changes from baseline in blood pressure and heart rate for all panels. The geometric mean ratios and 90% confidence intervals for phentermine AUC(0-24 h) in the presence/absence of taranabant 0.5 mg and 2 mg were 1.08 (0.99, 1.17) and 1.04 (0.98, 1.10), respectively. No significant differences in blood pressure and heart rate were observed with any treatment versus placebo. Coadministration of taranabant 0.5 mg, 1 mg, and 2 mg with phentermine was well tolerated with no pharmacokinetic interaction and did not result in meaningful changes in blood pressure or heart rate versus placebo.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Amides / administration & dosage
  • Amides / adverse effects*
  • Anti-Obesity Agents / adverse effects
  • Anti-Obesity Agents / pharmacokinetics*
  • Blood Pressure / drug effects
  • Drug Administration Schedule
  • Drug Interactions
  • Drug Inverse Agonism*
  • Drug Therapy, Combination
  • Female
  • Heart Rate / drug effects
  • Humans
  • Male
  • Middle Aged
  • Phentermine / administration & dosage
  • Phentermine / adverse effects*
  • Phentermine / pharmacokinetics*
  • Pyridines / administration & dosage
  • Pyridines / adverse effects*
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors*

Substances

  • Amides
  • Anti-Obesity Agents
  • Pyridines
  • Receptor, Cannabinoid, CB1
  • Phentermine
  • N-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide