Radell J E, Serle J B
Icahn School of Medicine at Mount Sinai, New York, New York, USA.
Drugs Today (Barc). 2019 Sep;55(9):563-574. doi: 10.1358/dot.2019.55.9.3039670.
The fixed-dose combination (FDC) of netarsudil 0.02%/ latanoprost 0.005% was approved by the United States Food and Drug Administration (FDA) on March 12, 2019, for the reduction of intraocular pressure (IOP) in patients with open-angle glaucoma (OAG) and ocular hypertension (OHT). Netarsudil is a Rho kinase (ROCK) inhibitor and latanoprost is a prostaglandin analogue (PGA). Once-daily administration of this FDC reduces IOP by enhancing aqueous outflow through both the trabecular pathways (ROCK inhibition) and uveoscleral pathways (PGA). Two phase III clinical trials, MERCURY-1 and MERCURY-2, confirmed significantly greater efficacy of the FDC than the individual components, with IOP reductions of 30% or greater observed in 59-65% of subjects treated with FDC compared with 29-37% of subjects treated with latanoprost alone and 21-29% of subjects treated with netarsudil alone. The FDC was well tolerated with mostly mild ocular side effects and limited systemic side effects. This paper will review the work leading to FDA approval and the clinical indications for the use of this combination.
奈他地尔0.02%/拉坦前列素0.005%的固定剂量复方制剂（FDC）于2019年3月12日获得美国食品药品监督管理局（FDA）批准，用于降低开角型青光眼（OAG）和高眼压症（OHT）患者的眼压（IOP）。奈他地尔是一种Rho激酶（ROCK）抑制剂，拉坦前列素是一种前列腺素类似物（PGA）。每日一次服用该FDC可通过小梁途径（ROCK抑制）和葡萄膜巩膜途径（PGA）增强房水流出，从而降低眼压。两项III期临床试验MERCURY-1和MERCURY-2证实，FDC的疗效明显优于单一成分，接受FDC治疗的受试者中有59%-65%的眼压降低30%或更多，而单独使用拉坦前列素治疗的受试者中这一比例为29%-37%，单独使用奈他地尔治疗的受试者中这一比例为21%-29%。该FDC耐受性良好，主要为轻度眼部副作用，全身副作用有限。本文将回顾促成FDA批准该药物的相关工作以及使用该复方制剂的临床适应症。
