Title: The Acyclic CB1R Inverse Agonist Taranabant Mediates Weight Loss by Increasing Energy Expenditure and Decreasing Caloric Intake
Authors: Addy, Carol ×
Wright, Hamish
Van Laere, Koen
Gantz, Ira
Erondu, Ngozi
Musser, Bret J
Lu, Kaifeng
Yuan, Jinyu
Sanabria-Bohórquez, Sandra M
Stoch, Aubrey
Stevens, Cathy
Fong, Tung M
De Lepeleire, Inge
Cilissen, Caroline
Cote, Josee
Rosko, Kim
Gendrano, Isaias N
Nguyen, Allison Martin
Gumbiner, Barry
Rothenberg, Paul
de Hoon, Jan
Bormans, Guy
Depré, Marleen
Eng, Wai-Si
Ravussin, Eric
Klein, Samuel
Blundell, John
Herman, Gary A
Burns, H Donald
Hargreaves, Richard J
Wagner, John
Gottesdiener, Keith
Amatruda, John M
Heymsfield, Steven B #
Issue Date: Jan-2008
Publisher: Cell Press
Series Title: Cell Metabolism vol:7 issue:1 pages:68-78
Abstract: Cannabinoid 1 receptor (CB1R) inverse agonists are emerging as a potential obesity therapy. However, the physiological mechanisms by which these agents modulate human energy balance are incompletely elucidated. Here, we describe a comprehensive clinical research study of taranabant, a structurally novel acyclic CB1R inverse agonist. Positron emission tomography imaging using the selective CB1R tracer [(18)F]MK-9470 confirmed central nervous system receptor occupancy levels ( approximately 10%-40%) associated with energy balance/weight-loss effects in animals. In a 12-week weight-loss study, taranabant induced statistically significant weight loss compared to placebo in obese subjects over the entire range of evaluated doses (0.5, 2, 4, and 6 mg once per day) (p < 0.001). Taranabant treatment was associated with dose-related increased incidence of clinical adverse events, including mild to moderate gastrointestinal and psychiatric effects. Mechanism-of-action studies suggest that engagement of the CB1R by taranabant leads to weight loss by reducing food intake and increasing energy expenditure and fat oxidation.
ISSN: 1550-4131
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Nuclear Medicine & Molecular Imaging
Clinical Pharmacology Centre (-)
× corresponding author
# (joint) last author

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