Drug intelligence / Profile preview

oxymetazoline + pilocarpine

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

Overview

**Oxymetazoline + pilocarpine** is an ophthalmic combination therapy investigated for the pharmacological treatment of **presbyopia**, the age-related loss of near visual acuity. Pilocarpine is a muscarinic cholinergic receptor agonist that induces miosis (pupil constriction) and accommodation by stimulating the ciliary muscle, improving near vision. Oxymetazoline is a selective alpha1-adrenergic receptor agonist, primarily acting as a vasoconstrictor and, in the eye, can cause contraction of the dilator muscle, resulting in pupil dilation. In combination, oxymetazoline was hypothesized to modulate the duration and side effects of pilocarpine, potentially dampening peak miosis and lessening adverse events (e.g., headache). Phase 2 clinical studies found that pilocarpine increased near visual acuity in a dose-dependent manner, while oxymetazoline did not provide additional significant benefit in efficacy or headache mitigation. The most common adverse event was headache. The optimal pilocarpine concentration range was 1.16%–1.32%. Development for this fixed combination was discontinued in favor of pilocarpine monotherapy for presbyopia[1][2][3][4][5].

Brand names
AGN-190584 + AGN-199201
Other names
AGN-190584 + AGN-199201 combination
02

Targets

ADRA1A (α1A)ADRA2A (α2A)CHRM3 (M3)

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