Drug intelligence / Profile preview

adaprolol

Development stage
Discontinued
Lead developer
Pharmos
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Adaprolol is a "soft" beta-adrenergic antagonist specifically designed for the treatment of glaucoma. Developed using the soft drug design principle, it is engineered to be metabolically labile, undergoing rapid transformation into an inactive metabolite once it enters the systemic circulation. This design aims to provide the potent ocular hypotensive benefits of beta-blockers while avoiding systemic side effects such as bradycardia and bronchoconstriction. Studies have shown that while both enantiomers effectively lower intraocular pressure, the R-enantiomer possesses a more favorable safety profile with negligible cardiac activity compared to the S-enantiomer.

Other names
adaprolol maleate(±)-adaprololR(-)-adaprololS(+)-adaprolol
02

Targets

ADRB1 (β1)

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