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RV-202 is a novel, orally bioavailable small molecule mitochondrial uncoupler (MU) being developed by Rivus Pharmaceuticals for the treatment of obesity and associated cardiometabolic diseases. It functions by increasing the mitochondrial oxygen consumption rate (OCR) and energy expenditure through the uncoupling of mitochondrial respiration, a process primarily mediated via the adenine nucleotide translocase (ANT). Preclinical studies in diet-induced obese (DIO) mouse models have demonstrated that RV-202 induces significant, fat-selective weight loss and fat mass reduction while preserving lean muscle mass. Additionally, RV-202 has shown potential for synergistic efficacy when combined with GLP-1 receptor agonists such as semaglutide, where it enhances weight loss durability and prevents weight rebound following treatment cessation.
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