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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
Author(s) -
Addy Carol,
Li Susie,
Agrawal Nancy,
Stone Julie,
Majumdar Anup,
Zhong Ling,
Li Hankun,
Yuan Jinyu,
Maes Andrea,
Rothenberg Paul,
Cote Josee,
Rosko Kim,
Cummings Corinne,
Warrington Steven,
Boyce Malcolm,
Gottesdiener Keith,
Stoch Aubrey,
Wagner John
Publication year - 2008
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 - 10.1177/0091270008314467
Subject(s) - pharmacokinetics , tolerability , medicine , pharmacodynamics , nausea , adverse effect , pharmacology , placebo , rimonabant , vomiting , anesthesia , agonist , cannabinoid receptor , receptor , alternative medicine , pathology
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 ith 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 l/2 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 ssociated 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.