Verosudil (AR-12286) 是一种有效的 Rho 激酶 (ROCK) 抑制剂，对 ROCK1 和 ROCK2 的 Ki 分别为 2 和 2 nM。AR-12286 主要通过增加眼房水通过小梁网流出来降低眼压。
Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork[1][2].
[1]. Lin CW, Sherman B, Moore LA, et al. Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma. J Ocul Pharmacol Ther. 2018;34(1-2):40‐51.
[2]. Kopczynski C, Novack GD, Swearingen D, van Haarlem T. Ocular hypotensive efficacy, safety and systemic absorption of AR-12286 ophthalmic solution in normal volunteers. Br J Ophthalmol. 2013;97(5):567‐572.
动态评分
0.0