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Ibipinabant is a potent and selective cannabinoid receptor 1 (CB1) inverse agonist that was developed for the treatment of obesity and type 2 diabetes. Originally discovered by Bristol Myers Squibb and co-developed with Solvay, the compound works by blocking endocannabinoid signaling at CB1 receptors located in the central nervous system and peripheral tissues such as the liver and adipose tissue. This mechanism aims to reduce appetite and improve metabolic parameters, including glycemic control and lipid profiles. Clinical development reached Phase IIb, where the drug demonstrated efficacy in weight reduction and HbA1c lowering in overweight and obese patients. However, development was terminated in 2008 following the withdrawal of rimonabant (the first-in-class CB1 antagonist) from the European market due to significant psychiatric side effects, including depression and anxiety, which were deemed a class-wide risk for centrally acting CB1 blockers.
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