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Verosudil (AR-12286) is a potent and selective small molecule Rho-associated protein kinase (ROCK) inhibitor developed by Aerie Pharmaceuticals for the treatment of glaucoma and ocular hypertension. It belongs to the water-soluble amino-isoquinoline amide class and exhibits high selectivity for both ROCK1 and ROCK2 isoforms. Verosudil lowers intraocular pressure (IOP) primarily by increasing aqueous humor outflow through the trabecular meshwork. The drug was evaluated in Phase 2 and Phase 2b/3 clinical trials as an ophthalmic solution at concentrations ranging from 0.05% to 0.7%. Although clinical studies demonstrated statistically significant IOP reductions, Aerie Pharmaceuticals discontinued its development in 2017, replacing it with the next-generation compound netarsudil (AR-13324), which showed superior efficacy.
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