Netarsudil ophthalmic solution 0.02% (hereafter referred to as netarsudil 0.02%) [Rhopressa®] is a Rho-associated protein kinase inhibitor that is thought to lower intraocular pressure (IOP) by increasing aqueous humour outflow through the trabecular meshwork. It has been developed by Aerie Pharmaceuticals and was recently approved in the USA for the reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension. The recommended dosage is one drop in the affected eye(s) once daily in the evening. Phase III development in the EU and phase II development in Japan are underway for this indication. This article summarizes the milestones in the development of netarsudil 0.02% leading to this first approval for the reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension.
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Abu-Hassan DW, Acott TS, Kelley MJ. The trabecular meshwork: a basic review of form and function. J Ocul Biol. 2014;2(1).
Aptel F, Chiquet C, Romanet JP. Intraocular pressure-lowering combination therapies with prostaglandin analogues. Drugs. 2012;72(10):1355–71.
Donegan RK, Lieberman RL. Discovery of molecular therapeutics for glaucoma: challenges, successes, and promising directions. J Med Chem. 2016;59(3):788–809.
Lin CW, Sherman B, Moore LA, et al. Discovery and preclinical development of netarsudil, a novel ocular hypotensive agent for the treatment of glaucoma. J Ocul Pharmacol Ther. 2017:1–12.
Aerie Pharmaceuticals Inc. RHOPRESSA® (netarsudil ophthalmic solution) 0.02%, for topical ophthalmic use: US prescribing information. 2017. https://www.fda.gov/. Accessed 16 Jan 2018.
Aerie Pharmaceuticals Inc. Aerie Pharmaceuticals announces U.S. FDA approval of Rhopressa® (netarsudil ophthalmic solution) 0.02% for the lowering of elevated IOP in patients with open-angle glaucoma or ocular hypertension. 2017. http://aeriepharma.com/. Accessed 16 Jan 2018.
Aerie Pharmaceuticals Inc. Aerie Pharmaceuticals reports positive Rocket 4 six-month topline safety and efficacy results for RhopressaTM (netarsudil ophthalmic solution) 0.02%. 2017. http://aeriepharma.com/. Accessed 16 Jan 2018.
Aerie Pharmaceuticals Inc. Aerie Pharmaceuticals initiates netarsudil ophthalmic solution phase 2 clinical trial designed to meet requirements of regulatory filing in Japan. 2017. http://aeriepharma.com/. Accessed 16 Jan
Aerie Pharmaceuticals Inc. Aerie Pharmaceuticals submits New Drug Application to U.S. Food and Drug Administration for Rhopressa(TM) (netarsudil ophthalmic solution) 0.02%. 2016. http://aeriepharma.com/. Accessed 16 Jan 2018.
Aerie Pharmaceuticals Inc. Aerie Pharmaceuticals enters into collaboration agreement with DSM focused on technology to potentially deliver Aerie compounds to treat retinal diseases such as wet AMD. 2017. http://aeriepharma.com/. Accessed 8 Feb 2018.
Aerie Pharmaceuticals Inc. Aerie Pharmaceuticals announces drug delivery asset acquisition to further advance its retinal disease program. 2017. http://aeriepharma.com/. Accessed 8 Feb 2018.
Li G, Mukherjee D, Navarro I, et al. Visualization of conventional outflow tissue responses to netarsudil in living mouse eyes. Eur J Pharmacol. 2016;787:20–31.
Wang RF, Williamson JE, Kopczynski C, et al. Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes. J Glaucoma. 2015;24(1):51–4.
Ren R, Li G, Le TD, et al. Outflow facility in human eyes through multiple mechanisms. Invest Ophthalmol Vis Sci. 2016;57(14):6197–209.
Kiel JW, Kopczynski CC. Effect of AR-13324 on episcleral venous pressure in Dutch belted rabbits. J Ocul Pharmacol Ther. 2015;31(3):146–51.
Wu K, Ren R, Li G, et al. Netarsudil increases size of giant vacuoles in Schlemm’s canal of perfused human eyes [abstract]. Invest Ophthalmol Vis Sci. 2017;58(8):1074.
Stamer WD, Li G, Agrahari V, et al. Rapid reversal of corticosteroid-induced ocular hypertension by netarsudil [abstract]. Invest Ophthalmol Vis Sci. 2017;58(8):3404.
Levy B, Ramirez N, Novack GD, et al. Ocular hypotensive safety and systemic absorption of AR-13324 ophthalmic solution in normal volunteers. Am J Ophthalmol. 2015;159(5):980–5.e1.
Sit A. Aqueous humor dynamics of netarsudil ophthalmic solution in humans [abstract no. FP-GLA-080]. In: European Society of Ophthalmology Congress (SOE). 2017.
Weiss M, Levy B, Kopczynski C, et al. Evaluation of AR-13324, a novel dual mechanism agent, in lowering of IOP in glaucoma and ocular hypertension. Investig Ophthalmol Vis Sci. 2013;54(15):754.
Peace J, Kopczynski C, Heah T. Ocular hypotensive efficacy of netarsudil ophthalmic solution 0.02% over a 24-hour period: a pilot study [abstract]. Invest Ophthalmol Vis Sci. 2017;58(8):2460.
Bacharach J, Dubiner HB, Levy B, et al. Double-masked, randomized, dose-response study of AR-13324 versus latanoprost in patients with elevated intraocular pressure. Ophthalmology. 2015;122(2):302–7.
Serle JB, Katz LJ, McLaurin E, et al. Two Phase 3 clinical trials comparing the safety and efficacy of netarsudil to timolol in patients with elevated intraocular pressure. Am J Ophthalmol. 2017. https://doi.org/10.1016/j.ajo.2017.11.019.
Khouri AS, Heah T, Kopczynski C, et al. A double-masked, randomized, parallel study of netarsudil ophthalmic solution, 0.02% QD compared to timolol maleate ophthalmic solution, 0.5% BID in patients with elevated intraocular pressure (ROCKET-4) [abstract]. Invest Ophthalmol Vis Sci. 2017;58(8):2461.
The preparation of this review was not supported by any external funding.
Conflicts of interest
During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. Sheridan Hoy is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.
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Hoy, S.M. Netarsudil Ophthalmic Solution 0.02%: First Global Approval. Drugs 78, 389–396 (2018). https://doi.org/10.1007/s40265-018-0877-7