Drug intelligence / Profile preview

ritobegron + bisoprolol

Development stage
Discontinued
Lead developer
Kissei Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

**ritobegron + bisoprolol** is an experimental combination of two small molecule drugs: ritobegron, a selective β3-adrenergic receptor agonist, and bisoprolol, a β1-adrenergic receptor antagonist (beta-blocker). Ritobegron is developed as a treatment for overactive bladder by relaxing detrusor smooth muscle via β3-adrenergic receptor activation, while bisoprolol is a cardioselective beta-blocker used to manage hypertension and heart disease by antagonizing β1-adrenergic receptors. This combination has been investigated to determine if bisoprolol can mitigate the cardiovascular side effects associated with β3-agonists like ritobegron, particularly increases in heart rate and blood pressure. The addition of bisoprolol has been shown in clinical studies to blunt both the adverse cardiovascular effects and the desired activation of brown adipose tissue thermogenesis as observed with similar β3-agonists. The combination is not an approved therapy and appears primarily used in clinical research settings for mechanistic and safety studies[1][2][4].

02

Targets

ADRB3 (β3)ADRB2 (β2)ADRB1 (β1)

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