Jill Sturdivant, Stuart S Williams, Maria Ina, Meredith Weksler, Alan McDougal, Daphne Clancy, Mitchell A deLong, Natalie Girouard, Maria Zaretskaia, Karen Brennan, Angela Glendenning, Briana Foley, Cheng-Wen Lin, Jeffrey C White, Casey Kopczynski, Curtis R Kelly
Purpose: A new class of ocular steroids designed to mitigate steroid-induced intraocular pressure (IOP) elevation while maintaining anti-inflammatory activity was developed. Herein is described the discovery and preclinical characterization of ROCK'Ster compound 1 . Methods: Codrugs consisting of a Rho kinase inhibitor (ROCKi) and a corticosteroid were synthesized. Compounds were initially screened in vitro for ROCKi activity and anti-inflammatory activity against the proinflammatory interleukin 23 and bacterial lipopolysaccharide (LPS) pathways...
January 4, 2023: Journal of Ocular Pharmacology and Therapeutics