RV201

RV201 is an oral small molecule Controlled Metabolic Accelerator (CMA) being developed by Rivus Pharmaceuticals for the treatment of obesity and associated cardiometabolic diseases. As a mitochondrial uncoupler, RV201 works by increasing resting energy expenditure through the dissipation of the mitochondrial proton gradient, a process that promotes the oxidation of fatty acids to generate heat rather than ATP. This mechanism is designed to drive fat-specific weight loss and improve insulin sensitivity while preserving lean muscle mass. Preclinical data presented at ObesityWeek 2025 demonstrated that RV201, both as a monotherapy and in combination with GLP-1 receptor agonists like semaglutide, effectively increases energy expenditure without causing significant elevations in body temperature, representing a potential new class of oral weight-loss medications.