Cell Metabolism
Volume 21, Issue 1, 6 January 2015, Pages 33-38
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Article
Activation of Human Brown Adipose Tissue by a β3-Adrenergic Receptor Agonist

https://doi.org/10.1016/j.cmet.2014.12.009Get rights and content
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Highlights

  • The β3-AR agonist mirabegron acutely activates human BAT glucose uptake

  • The β3-AR agonist mirabegron acutely activates human WAT lipolysis

  • Mirabegron stimulates brown/beige fat in multiple depots.

  • Mirabegron-induced BAT activity is a predictor of whole-body thermogenesis

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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