Efficacy and safety of netarsudil 0.02% ophthalmic solution in patients with open-angle glaucoma and ocular hypertension

ABSTRACT

Introduction: Currently, the only modifiable risk factor to slow or halt the progression of glaucoma is the lowering of intraocular pressure (IOP). Netarsudil 0.02% is a new medication that was approved by the U.S. FDA in 2017 for reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

Areas covered: We reviewed recent literature on the efficacy and safety of netarsudil both alone and in combination. We included recently published manuscripts from both human and animal studies.

Expert opinion: Netarsudil functions by inhibiting rho-associated protein kinases, making it the first IOP lowering medication to directly target the trabecular meshwork. Although the efficacy of the medication in lowering intraocular pressure has been substantiated in numerous studies, the ocular hypotensive effect of netarsudil is in the range of timolol, and less than latanoprost in most studies. The safety profile of netarsudil differs from other currently approved topical ocular hypotensive agents, and at least half of the patients using it are expected to have adverse events – although they may be mild and transient. A fixed-dose combination of netarsudil with latanoprost was approved in March 2019, which has greater ocular hypotensive efficacy than either netarsudil or latanoprost alone.

KEYWORDS:

• Netarsudil
• latanoprost
• intraocular pressure
• Rhopressa®
• Rocklatan®
• ROCK
• glaucoma

Article highlights

• Netarsudil 0.02% is a new medication that was approved by the U.S. FDA in 2017 for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

• Netarsudil functions by targeting rho-associated kinase protein (ROCK) to relax the trabecular meshwork and increase aqueous outflow. It is credited with being the first IOP lowering medication to directly target the trabecular meshwork.

• Numerous controlled studies have shown netarsudil to be effective in lowering intraocular pressure in patients.

• In pivotal controlled clinical studies, netarsudil 0.02% q.d. had an ocular hypotensive efficacy in the same range as timolol.

• The most commonly observed adverse event is conjunctival hyperemia, which occurs in roughly half of all patients. Less common adverse events include corneal verticillata, instillation site pain, and corneal endothelial changes. In the studied patient population, the incidence and nature of adverse events are both more frequent and different than latanoprost and timolol.

• A FDC of netarsudil/latanoprost is a more effective ocular hypotensive than either component alone. This agent (Rocklatan™) is also now FDA approved.

Declaration of interest

J Berryman has no relevant financial interests to disclose. G Novack serves as a consultant to the following firms3E BioAdvisors, LLC; Aerie Pharmaceuticals, Inc.; Aerpio Therapeutics; CalypsoQ; Graybug; Jenivision, Inc.; Nicox; Ocular Theraputix; Ocuphire Pharma, Inc.; pH Pharma; PolyActiva; RHMM Inc.; and Sylentis. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

A reviewer of this manuscript declares being a paid speaker for Aerie Pharmaceuticals. Peer reviewers on this manuscript have no other relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.