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Ritobegron + acipimox is a pharmacological combination consisting of a selective beta-3 adrenergic receptor agonist and a lipolysis inhibitor, primarily utilized in clinical research to investigate metabolic pathways. Ritobegron (KUL-7211), developed by Kissei Pharmaceutical, acts as a selective agonist of the beta-3 adrenergic receptor, which is involved in thermogenesis and bladder smooth muscle relaxation. Acipimox is a nicotinic acid derivative that acts as an agonist of the hydroxycarboxylic acid receptor 2 (HCAR2), effectively inhibiting the release of free fatty acids (FFAs) from adipose tissue. This combination has been specifically employed in physiological studies to determine whether the metabolic effects of beta-3 adrenergic stimulation, such as increased energy expenditure and lipid oxidation, are dependent on the systemic elevation of plasma FFAs. While ritobegron was initially developed for overactive bladder, its development was discontinued, and the combination remains a research tool rather than a commercial therapeutic product.
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