CB1 antagonists for obesity--what lessons have we learned from rimonabant? 2009

Vincenzo Di Marzo, and Jean-Pierre Després
Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, Pozzuoli, Italy. vdimarzo@icmib.na.cnr.it

When compared with other modifiable cardiovascular risk factors, such as hypertension, dyslipidemia and smoking, obesity remains a surprisingly puzzling condition to prevent and treat. The history of the development of anti-obesity drugs has known more defeats than even partial victories. With very few drugs on the market, and bad publicity related to adverse events, obesity remains an almost completely unmet challenge for the pharmaceutical industry. In light of past experience with endocannabinoid-system antagonists, such as rimonabant, we propose that a major paradigm shift in clinical practice might be necessary to justify the use of pharmacotherapy for obesity. Furthermore, we suggest that the criteria currently used by regulatory authorities to evaluate and approve anti-obesity drugs should be rigorously re-examined. Finally, we discuss how pharmacological approaches that aim to counteract overactivity of the endocannabinoid system should be revisited in the future to treat visceral (intra-abdominal) obesity and its metabolic consequences.

UI MeSH Term Description Entries
D009765 Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).
D010880 Piperidines A family of hexahydropyridines.
D011720 Pyrazoles Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077285 Rimonabant A pyrazole and piperidine derivative that acts as a selective cannabinoid type-1 receptor (CB1 RECEPTOR) antagonist. It inhibits the proliferation and maturation of ADIPOCYTES, improves lipid and glucose metabolism, and regulates food intake and energy balance. It is used in the management of OBESITY. Acomplia,N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride,Rimonabant Hydrochloride,SR 141716,SR 141716A,SR-141716A,SR141716,SR141716A,Zimulti
D043884 Receptor, Cannabinoid, CB1 A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release. Cannabinoid Receptor CB1,CB1 Receptor,Receptor CB1, Cannabinoid,Receptor, CB1
D019440 Anti-Obesity Agents Agents that increase energy expenditure and weight loss by neural and metabolic regulation. Anti-Obesity Agent,Anti-Obesity Drug,Antiobesity Agent,Antiobesity Drug,Weight-Loss Agents,Weight-Loss Drug,Anti-Obesity Drugs,Antiobesity Agents,Antiobesity Drugs,Weight-Loss Drugs,Agent, Anti-Obesity,Agent, Antiobesity,Agents, Anti-Obesity,Agents, Antiobesity,Agents, Weight-Loss,Anti Obesity Agent,Anti Obesity Agents,Anti Obesity Drug,Anti Obesity Drugs,Drug, Anti-Obesity,Drug, Antiobesity,Drug, Weight-Loss,Drugs, Anti-Obesity,Drugs, Antiobesity,Drugs, Weight-Loss,Weight Loss Agents,Weight Loss Drug,Weight Loss Drugs
D063385 Cannabinoid Receptor Modulators Compounds that interact with and modulate the activity of CANNABINOID RECEPTORS. Modulators, Cannabinoid Receptor,Receptor Modulators, Cannabinoid

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