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Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Properties of Taranabant, a Novel Selective Cannabinoid-1 Receptor Inverse Agonist, for the Treatment of Obesity: Results From a Double-Blind, Placebo-Controlled, Single Oral Dose Study in Healthy Volunteers

From Merck Research Laboratories, Boston, Massachusetts (Dr Addy); Merck Research Laboratories, West Point, Pennsylvania (Dr Li, Dr Agrawal, Dr Stone, Dr Majumdar, Dr Zhong, Mr Li); Merck Research Laboratories, Rahway, New Jersey (Dr Yuan, Dr Maes, Dr Rothenberg, Ms Cote, Ms Rosko, Dr Gottesdiener, Dr Stoch, Dr Wagner); Merck Research Laboratories, Harlow, Essex, United Kingdom (Dr Cummings); and Hammersmith Medicines Research, Central Middlesex Hospital, Park Royal, London, United Kingdom (Dr Warrington, Dr Boyce). Dr Rothenberg's current affiliation is Johnson & Johnson, Raritan, New Jersey.

Taranabant is a novel cannabinoid CB-1 receptor (CB1R) inverse agonist in clinical development for the treatment of obesity. This double-blind, randomized, placebo-controlled, single oral dose study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of taranabant (0.5-600 mg) in 24 healthy male volunteers. Single-dose AUC_0- and C_max values for taranabant increased approximately linearly with dose up to 200 mg, with slightly less than dose-proportional increases in AUC_0- and C_max values for doses >200 mg. Plasma taranabant had a biphasic disposition, with a median t_max of 1 to 2.5 hours and a terminal elimination t of 38 to 69 hours. Coadministration of taranabant with a high-fat meal led to a 14% increase in C_max and a 74% increase in AUC_0-. Clinical adverse experiences associated with single doses of taranabant were generally mild and transient. Of the 198 clinical adverse experiences reported, the most common drug-related ones were nausea (36), headache (22), drowsiness (14), abdominal discomfort/abdominal pain/stomachache (14), hiccups (9), dizziness (8), decreased appetite (7), increased bowel movement (7), mood change (6), tiredness (4), vomiting (4), and sweating increased (4). Taranabant has pharmacokinetic characteristics suitable for a once-daily dosing regimen.

Key Words: MK-0364 • taranabant • cannabinoid-1 receptor inverse agonist • obesity • appetite • satiety

Address for correspondence: Carol Addy, MD, MMSc, Director, Clinical Pharmacology, Merck Research Laboratories, 33 Avenue Louis Pasteur, HB3-429, Boston, MA 02115; e-mail: carol_addy{at}merck.com.

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