Drug intelligence / Profile preview

pilocarpine + phentolamine

Development stage
Unknown
Lead developer
Opus Genetics
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

**Pilocarpine + phentolamine** is an ophthalmic fixed-dose combination developed as an eye drop formulation to address **presbyopia**. It contains pilocarpine, a muscarinic acetylcholine receptor agonist (miotic), and phentolamine, a reversible, non-selective alpha-1 and alpha-2 adrenergic receptor antagonist. Pilocarpine acts by constricting the pupil (miosis) through stimulation of muscarinic receptors, enhancing near vision in presbyopic patients. Phentolamine reduces pupillary diameter by blocking adrenergic receptors on the iris dilator muscle, further supporting improvement in near and intermediate visual acuity while potentially minimizing night vision disturbances. The combination has been studied, including in phase 3 clinical trials, for presbyopia and reversal of pharmacological mydriasis, and is under development by Opus Genetics (originator Ocuphire Pharma)[1][3][5][7][9].

Brand names
Nyxol + Low-Dose Pilocarpine Eye Drops
Other names
pilocarpine/phentolamineNyxol + pilocarpine
02

Targets

M1 (Muscarinic acetylcholine receptor M1)ADRA1A (α1A)CHRM3 (M3)ADRA2 (Alpha-2 adrenergic receptor family)CHRM2 (M2)

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