Kopczynski C C, Heah T
Aerie Pharmaceuticals, Inc., Durham, North Carolina, USA.
Aerie Pharmaceuticals, Inc., Bedminster, New Jersey, USA.
Drugs Today (Barc). 2018 Aug;54(8):467-478. doi: 10.1358/dot.2018.54.8.2849627.
Once-daily (p.m.) netarsudil ophthalmic solution 0.02% (Rhopressa) is approved in the United States for lowering elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. Netarsudil, a Rho kinase (ROCK) inhibitor that lowers IOP primarily by increasing trabecular outflow, produces statistically and clinically significant reductions in mean IOP from baseline, with comparable effects on nocturnal and diurnal IOP. In three phase III trials of patients with elevated IOP, the ocular hypotensive efficacy of once-daily netarsudil 0.02% met the criteria for noninferiority to twice-daily timolol 0.5% at all time points over 3 months in patients with baseline IOP less than 25 mmHg. The most frequent adverse event (AE) was generally mild conjunctival hyperemia, the severity of which did not increase with continued dosing. Netarsudil was associated with minimal treatment-related serious or systemic AEs, likely due to the lack of systemic exposure. This report summarizes the available preclinical and clinical data on netarsudil.
0.02%奈他地尔滴眼液（Rhopressa）每日一次（下午使用）已在美国获批，用于降低开角型青光眼或高眼压症患者的眼压升高。奈他地尔是一种Rho激酶（ROCK）抑制剂，主要通过增加小梁网房水外流来降低眼压，与基线相比，可使平均眼压在统计学和临床上显著降低，对夜间和日间眼压的影响相当。在三项针对眼压升高患者的III期试验中，对于基线眼压低于25 mmHg的患者，0.02%奈他地尔每日一次的降眼压疗效在3个月的所有时间点均达到非劣效于0.5%噻吗洛尔每日两次的标准。最常见的不良事件（AE）通常为轻度结膜充血，其严重程度不会随着持续用药而增加。奈他地尔与最少的治疗相关严重或全身性AE相关，这可能是由于缺乏全身暴露。本报告总结了奈他地尔现有的临床前和临床数据。
