Advantages and disadvantages of using Rho kinase inhibitors to reduce intraocular pressure

Abstract

ABSTRACT Introduction Rho kinase (ROCK) inhibitors (RKIs) have been available commercially as topical ocular hypotensive agents for approximately a decade. RKIs have promise as their presumed mechanism of action is increased trabecular meshwork (TM) outflow, the presumed primary site of pathology in open-angle glaucoma. Areas covered We reviewed recent literature on netarsudil, ripasudil, H-1337, and VVN539 as monotherapy and in combination with other topical ocular hypotensive agents. Expert opinion With a unique primary mechanism of increase in trabecular outflow, these agents target the glaucomatous pathology in aqueous humor dynamics. The ocular hypotensive efficacy of netarsudil, once-daily (q.d.), is in the range of non-cardioselective beta-adrenoceptor antagonists. Ripasudil, given twice-daily (b.i.d.), is somewhat less effective. H-1337 and VVN539, at an early development stage, both seem to have efficacy in the range of netarsudil. Conjunctival hyperemia is an adverse event common to all RKIs tested to date. The greater adoption of RKIs in therapy may be limited by financial considerations, at least in the U.S. Search strategy We searched PubMed for the keywords netarsudil (AR13324), ripasudil (K-115), H-1337, and VVN539 as of November 2023. We found 349 citations which we reviewed for consideration in this review. Herein we summarize primary research reports, excluding news stories or meeting abstracts. We also searched www.clinicaltrials.gov to find new trials of interest.