Table 2.
Commonly known rho-kinase inhibitors and their usage.
| ROCK inhibitors | Clinical use | Main route of administration | Mechanism and pharmacodynamics | Side effects | Note |
|---|---|---|---|---|---|
| Y-27632 | Treatment of FECD | Topical (ophthalmic solution) | Corneal clearing and visual improvement | Symptomatic hypotension | • The first small molecule ROCK inhibitor • Approved for clinical use in the United States |
| Ripasudil (K-115) | Treatment of glaucoma and ocular hypertension | Topical (ophthalmic solution) | Reduce IOP | Mild conjunctival hyperemia | • A derivative of fasudil • The first ROCK inhibitor approved for clinical use • Approved for clinical use in Japan and the United States |
| Netarsudil (AR-13503) | Treatment of glaucoma and ocular hypertension, specifically in the United States | Topical (ophthalmic solution) | Reduce IOP | Conjunctival hyperemia and corneal verticillata, instillation site pain, and conjunctival hemorrhages | • Both an RKI and a norepinephrine transport inhibitor • Approved for clinical use in Japan and the United States |
| Fasudil | Treatment of vasospasms following subarachnoid hemorrhage, specifically in Japan | Intravenous infusion | Suppress cerebral vasospasm and associated cerebral ischemic symptoms | No severe side effects | Approved for clinical use in Japan and China |
| Belumosudil | Treatment of chronic graft versus host disease | Oral | Inhibit pro- and anti-inflammatory immune cell responses | Infections | Approved for clinical use in the United States |