Background: The cornea is transparent tissue that serves as the window of the eye, allowing light to
enter from the outer environment. The corneal endothelium maintains corneal transparency; thus, its dysfunction
results in corneal haziness and causes severe vision loss. The only available therapeutic choice for treating corneal
endothelial dysfunction has been transplantation using donor corneas; consequently, researchers have been
pressed to develop new therapeutic options.
Methods: The goal of the review is to provide an overview of the research into Rho kinase (ROCK) inhibitors in
the field of corneal endothelium therapy and the potential for clinical use of ROCK inhibitors.
Results: We reported that ROCK inhibitor enhances wound healing in the corneal endothelium. We further proposed
the development of ROCK inhibitors as drugs that suppress the incidence of bullous keratopathy following
severe corneal endothelial damage, especially that occurring during cataract surgery, one of the leading causes of
corneal transplantation. We also proposed the use of ROCK inhibitors as adjunct drugs for cell-based therapeutic
treatment of corneal endothelial dysfunction. ROCK inhibitors promote the engraftment of injected cultured corneal
endothelial cells to the recipient cornea, thereby enabling the regeneration of corneal endothelium. Of note,
we have initiated clinical research into cell injection therapy using a ROCK inhibitor as an adjunct drug.
Conclusion: This review documents the potency of ROCK inhibitors in clinical use, both as eye drops and as
adjunct drugs for cell-based therapy for the treatment of corneal endothelial dysfunction.