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ARD-101 is an oral, first-in-class small molecule developed by Aardvark Therapeutics. It acts as a pan-agonist of bitter taste receptors (TAS2Rs), primarily targeting the gastrointestinal tract. By activating these receptors on enteroendocrine cells, ARD-101 stimulates the release of gut peptide hormones such as GLP-1, GLP-2, and cholecystokinin (CCK), which regulate appetite and metabolism. The drug is designed to be gut-restricted with minimal systemic exposure, aiming to reduce hunger and body fat without common side effects like nausea seen in other anti-obesity drugs. Its primary indication is Prader-Willi syndrome (PWS), where it has shown efficacy in reducing hyperphagia and improving body composition. Development for general obesity and weight gain has been discontinued[2][5][6][7][8].
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