[PDF][PDF] Activation of human brown adipose tissue by a β3-adrenergic receptor agonist

AM Cypess, LS Weiner, C Roberts-Toler, EF Elía… - Cell metabolism, 2015 - cell.com
AM Cypess, LS Weiner, C Roberts-Toler, EF Elía, SH Kessler, PA Kahn, J English…
Cell metabolism, 2015cell.com
Increasing energy expenditure through activation of endogenous brown adipose tissue
(BAT) is a potential approach to treat obesity and diabetes. The class of β3-adrenergic
receptor (AR) agonists stimulates rodent BAT, but this activity has never been demonstrated
in humans. Here we determined the ability of 200 mg oral mirabegron (Myrbetriq, Astellas
Pharma, Inc.), a β3-AR agonist currently approved to treat overactive bladder, to stimulate
BAT as compared to placebo. Mirabegron led to higher BAT metabolic activity as measured …
Summary
Increasing energy expenditure through activation of endogenous brown adipose tissue (BAT) is a potential approach to treat obesity and diabetes. The class of β3-adrenergic receptor (AR) agonists stimulates rodent BAT, but this activity has never been demonstrated in humans. Here we determined the ability of 200 mg oral mirabegron (Myrbetriq, Astellas Pharma, Inc.), a β3-AR agonist currently approved to treat overactive bladder, to stimulate BAT as compared to placebo. Mirabegron led to higher BAT metabolic activity as measured via 18F-fluorodeoxyglucose (18F-FDG) using positron emission tomography (PET) combined with computed tomography (CT) in all twelve healthy male subjects (p = 0.001), and it increased resting metabolic rate (RMR) by 203 ± 40 kcal/day (+13%; p = 0.001). BAT metabolic activity was also a significant predictor of the changes in RMR (p = 0.006). Therefore, a β3-AR agonist can stimulate human BAT thermogenesis and may be a promising treatment for metabolic disease.
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