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Glaucoma - Rho kinase (ROCK) inhibitors

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Background

 

Rho kinase (ROCK) inhibitors (increase outflow):

Overview

  1. Efficacy of Rhokinase inhibitors slightly more than latanoprost.
  2. Novel class of topical agents for the topical treatment of glaucoma
  3. Also available as a combination product - combined with latanoprost: Rocklatan®
  4. Drops are instilled once daily.
  5. Rho Kinase Inhibitors increase drainage of intraocular fluid by improving outflow of the trabecular meshwork.

 

Side Effects

Side effects can include eye redness, corneal deposits, stinging, and small bleeds on the white of the eye.



Netarsudil 0.02% (Rhopressa®)

Netarsudil 0.02% (Rhopressa®)  top of page

Pharmacology:   Netarsudil is a rho kinase inhibitor, which is believed to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork. The exact mechanism is unknown. After topical ocular dosing, netarsudil is metabolized by esterases in the eye.

Dosing: One drop into the affected eye(s) once daily in the evening.

Side effects: The most common adverse reaction is conjunctival hyperemia (53%). Other common adverse reactions, approximately 20% include: corneal verticillata, instillation site pain, and conjunctival hemorrhage.

Efficacy: RHOPRESSA 0.02% was evaluated in three randomized and controlled clinical trials, namely AR-13324-CS301 (NCT 02207491, referred to as Study 301), AR-13324-CS302 (NCT 02207621, referred to as Study 302), and AR-13324-CS304 (NCT 02558374, referred to as Study 304), in patients with open-angle glaucoma or ocular hypertension. Studies 301 and 302 enrolled subjects with baseline IOP lower than 27 mmHg and Study 304 enrolled subjects with baseline IOP lower than 30 mmHg. The treatment duration was 3 months in Study 301, 12 months in Study 302, and 6 months in Study 304.

The three studies demonstrated up to 5 mmHg reductions in IOP for subjects treated with RHOPRESSA 0.02% once daily in the evening. For patients with baseline IOP < 25 mmHg, the IOP reductions with RHOPRESSA 0.02% dosed once daily were similar to those with timolol 0.5% dosed twice daily (see Table 1). For patients with baseline IOP equal to or above 25 mmHg, however, RHOPRESSA 0.02% resulted in smaller mean IOP reductions at the morning time points than timolol 0.5% for study visits on Days 43 and 90; the difference in mean IOP reduction between the two treatment groups was as high as 3 mmHg, favoring timolol.

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here.

Rho kinase (ROCK) inhibitors Ophthalmology