monlunabant

Monlunabant is a peripherally selective small molecule inverse agonist of the cannabinoid receptor 1 (CB1), originally discovered as a β-arrestin–2-biased CB1 antagonist. It was developed for weight loss and metabolic disorders by Inversago Pharma and later acquired by Novo Nordisk. Monlunabant acts primarily on peripheral CB1 receptors, which play key roles in metabolism, appetite regulation, and cardiometabolic pathways in tissues such as adipose tissue, gastrointestinal tract, kidneys, liver, pancreas, muscles, and lungs. Despite its design to minimize central nervous system effects compared to earlier CB1 antagonists like rimonabant (Acomplia), clinical trials have reported mild to moderate neuropsychiatric side effects including anxiety and sleep disturbances. Monlunabant has been evaluated in Phase 2 trials for obesity and diabetic kidney disease; while it showed statistically significant weight loss at lower doses compared to placebo in obesity studies, efficacy was modest with limited additional benefit at higher doses. The drug failed to meet primary endpoints in diabetic kidney disease trials[1][3][5][8].

Other names

monlunabantINV-202INV202INV 202MRI-1891MRI1891MRI 1891S-MRI-1891S-MRI1891S-MRI 1891