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Drugs. 2018 May;78(7):773-780. doi: 10.1007/s40265-018-0914-6.
Latanoprostene bunod ophthalmic solution 0.024% (hereafter referred to as latanoprostene bunod 0.024%) [Vyzulta™] is a nitric oxide (NO)-donating prostaglandin F analogue approved in the USA for the reduction of intraocular pressure (IOP) in patients with open-angle glaucoma (OAG) or ocular hypertension. It is thought to lower IOP by increasing aqueous humour outflow through the uveoscleral pathway (mediated by latanoprost acid) and increasing the facility of aqueous humour outflow through the trabecular meshwork pathway (mediated by NO). Results from two multinational, phase III studies (APOLLO and LUNAR) and a pooled analysis of these studies demonstrated the noninferiority of latanoprostene bunod 0.024% to timolol ophthalmic solution 0.5% (hereafter referred to as timolol 0.5%) in terms of IOP-lowering efficacy over 3 months in patients with OAG or ocular hypertension, with the superiority of latanoprostene bunod 0.024% over timolol 0.5% subsequently demonstrated in APOLLO and the pooled analysis. Moreover, there was no apparent loss of IOP-lowering effect in subsequent safety extension periods of up to 9 months. The IOP-lowering efficacy seen in APOLLO and LUNAR was confirmed in a phase III study (JUPITER) in Japanese patients, with IOP reductions observed early (week 4) and maintained over the longer-term (12 months). Latanoprostene bunod 0.024% was well tolerated over up to 12 months in these studies, with most ocular treatment-emergent adverse events (TEAEs) being mild to moderate in severity. Thus, current evidence indicates once-daily latanoprostene bunod 0.024% is an effective and well tolerated treatment option for the reduction of IOP in adults with OAG or ocular hypertension.
拉坦前列素苯丁胺滴眼剂 0.024%(以下简称拉坦前列素苯丁胺 0.024%)[Vyzulta™]是一种一氧化氮(NO)供体前列腺素 F 类似物,在美国被批准用于降低开角型青光眼(OAG)或高眼压症患者的眼内压(IOP)。它被认为通过增加房水通过葡萄膜巩膜途径的流出(由拉坦前列素酸介导)以及通过小梁网途径增加房水流出的便利性(由 NO 介导)来降低 IOP。两项多中心 III 期研究(APOLLO 和 LUNAR)和这些研究的汇总分析结果表明,在 3 个月内,拉坦前列素苯丁胺 0.024%在降低 OAG 或高眼压症患者的 IOP 疗效方面不劣于噻吗洛尔滴眼剂 0.5%(以下简称噻吗洛尔 0.5%),随后在 APOLLO 和汇总分析中证明了拉坦前列素苯丁胺 0.024%优于噻吗洛尔 0.5%。此外,在长达 9 个月的后续安全性延长期间,没有明显的 IOP 降低效果丧失。在日本患者的一项 III 期研究(JUPITER)中证实了 APOLLO 和 LUNAR 中观察到的 IOP 降低效果,在早期(第 4 周)观察到 IOP 降低,并在较长时间内维持(12 个月)。在这些研究中,拉坦前列素苯丁胺 0.024%在长达 12 个月的时间内得到了良好的耐受,大多数眼部治疗中出现的不良事件(TEAEs)的严重程度为轻度至中度。因此,目前的证据表明,每日一次的拉坦前列素苯丁胺 0.024%是降低 OAG 或高眼压症成人 IOP 的有效且耐受良好的治疗选择。