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奈他舒地尔滴眼液 0.02%:全球首次获批。

Netarsudil Ophthalmic Solution 0.02%: First Global Approval.

机构信息

Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Drugs. 2018 Mar;78(3):389-396. doi: 10.1007/s40265-018-0877-7.

DOI:10.1007/s40265-018-0877-7
PMID:29453668
Abstract

Netarsudil ophthalmic solution 0.02% (hereafter referred to as netarsudil 0.02%) [Rhopressa] is a Rho-associated protein kinase inhibitor that is thought to lower intraocular pressure (IOP) by increasing aqueous humour outflow through the trabecular meshwork. It has been developed by Aerie Pharmaceuticals and was recently approved in the USA for the reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension. The recommended dosage is one drop in the affected eye(s) once daily in the evening. Phase III development in the EU and phase II development in Japan are underway for this indication. This article summarizes the milestones in the development of netarsudil 0.02% leading to this first approval for the reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension.

摘要

盐酸奈甲唑啉滴眼液 0.02%(以下简称奈甲唑啉 0.02%)[Rhopressa]是一种 Rho 相关蛋白激酶抑制剂,据认为通过增加房水通过小梁网流出来降低眼内压(IOP)。它由 Aerie 制药公司开发,最近在美国获得批准,用于降低开角型青光眼或高眼压症患者的升高的 IOP。推荐剂量为每晚一次,每次一滴滴入受影响的眼睛。该适应症在欧盟的 III 期开发和日本的 II 期开发正在进行中。本文总结了奈甲唑啉 0.02% 的开发里程碑,最终首次批准该药物用于降低开角型青光眼或高眼压症患者的升高的 IOP。

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Netarsudil Ophthalmic Solution 0.02%: First Global Approval.奈他舒地尔滴眼液 0.02%:全球首次获批。
Drugs. 2018 Mar;78(3):389-396. doi: 10.1007/s40265-018-0877-7.
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Netarsudil ophthalmic solution 0.02% for the treatment of patients with open-angle glaucoma or ocular hypertension.0.02%奈他地尔眼药水用于治疗开角型青光眼或高眼压症患者。
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Fixed-Dose Combination of Netarsudil and Latanoprost in Ocular Hypertension and Open-Angle Glaucoma: Pooled Efficacy/Safety Analysis of Phase 3 MERCURY-1 and -2.固定剂量组合奈他舒地尔和拉坦前列素治疗眼高压和开角型青光眼:3 期 MERCURY-1 和 -2 的汇总疗效/安全性分析。
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Two Phase 3 Clinical Trials Comparing the Safety and Efficacy of Netarsudil to Timolol in Patients With Elevated Intraocular Pressure: Rho Kinase Elevated IOP Treatment Trial 1 and 2 (ROCKET-1 and ROCKET-2).两项比较奈立定(netarsudil)和噻吗洛尔(timolol)安全性和疗效的 3 期临床试验: Rho 激酶升高的眼压治疗试验 1 和 2(ROCKET-1 和 ROCKET-2)。
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Netarsudil/Latanoprost Fixed-Dose Combination for Elevated Intraocular Pressure: Three-Month Data from a Randomized Phase 3 Trial.奈他舒地尔/拉坦前列素固定剂量复方制剂治疗高眼压:一项随机 3 期临床试验的 3 个月数据。
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Netarsudil/latanoprost fixed-dose combination for the treatment of open-angle glaucoma or ocular hypertension.奈他地尔/拉坦前列素固定剂量组合用于治疗开角型青光眼或高眼压症。
Drugs Today (Barc). 2019 Sep;55(9):563-574. doi: 10.1358/dot.2019.55.9.3039670.

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本文引用的文献

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Two Phase 3 Clinical Trials Comparing the Safety and Efficacy of Netarsudil to Timolol in Patients With Elevated Intraocular Pressure: Rho Kinase Elevated IOP Treatment Trial 1 and 2 (ROCKET-1 and ROCKET-2).两项比较奈立定(netarsudil)和噻吗洛尔(timolol)安全性和疗效的 3 期临床试验: Rho 激酶升高的眼压治疗试验 1 和 2(ROCKET-1 和 ROCKET-2)。
Am J Ophthalmol. 2018 Feb;186:116-127. doi: 10.1016/j.ajo.2017.11.019. Epub 2017 Dec 1.
2
Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma.发现和临床前开发新型眼部降眼压剂奈他舒地尔治疗青光眼。
J Ocul Pharmacol Ther. 2018 Jan/Feb;34(1-2):40-51. doi: 10.1089/jop.2017.0023. Epub 2017 Jun 13.
3
ROCK抑制剂的药物和细胞类型特异性效应作为网状角膜上皮水肿的潜在原因
Cells. 2025 Feb 11;14(4):258. doi: 10.3390/cells14040258.
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The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif.具有1,2 - 二硫杂环戊烷 - 3 - 基 motif的ROCK2抑制剂的合成与生物活性
RSC Med Chem. 2024 Aug 1;15(10):3576-96. doi: 10.1039/d4md00438h.
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Engineered sensor actuator modulator as aqueous humor outflow actuator for gene therapy of primary open-angle glaucoma.工程传感器执行器调制器作为房水流出执行器用于原发性开角型青光眼的基因治疗。
J Transl Med. 2024 Aug 28;22(1):791. doi: 10.1186/s12967-024-05581-1.
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Efficacy and Safety of Rho Kinase Inhibitors vs. Beta-Blockers in Primary Open-Angle Glaucoma: A Systematic Review with Meta-Analysis.Rho激酶抑制剂与β受体阻滞剂治疗原发性开角型青光眼的疗效和安全性:一项系统评价与荟萃分析
J Clin Med. 2024 Mar 18;13(6):1747. doi: 10.3390/jcm13061747.
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Therapeutic Potential of Antioxidants and Hybrid TEMPOL Derivatives in Ocular Neurodegenerative Diseases: A Glimpse into the Future.抗氧化剂和杂化TEMPOL衍生物在眼部神经退行性疾病中的治疗潜力:展望未来
Biomedicines. 2023 Nov 1;11(11):2959. doi: 10.3390/biomedicines11112959.
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Connective tissue growth factor: Role in trabecular meshwork remodeling and intraocular pressure lowering.结缔组织生长因子:在小梁网重塑和眼压降低中的作用。
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Clin Ophthalmol. 2023 Oct 17;17:3063-3076. doi: 10.2147/OPTH.S420932. eCollection 2023.
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Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms.
奈他地尔通过多种机制增加人眼的房水流出率。
Invest Ophthalmol Vis Sci. 2016 Nov 1;57(14):6197-6209. doi: 10.1167/iovs.16-20189.
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Visualization of conventional outflow tissue responses to netarsudil in living mouse eyes.活体小鼠眼中传统房水流出组织对奈他地尔反应的可视化。
Eur J Pharmacol. 2016 Sep 15;787:20-31. doi: 10.1016/j.ejphar.2016.04.002. Epub 2016 Apr 13.
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Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.青光眼分子疗法的发现:挑战、成功与前景方向
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Ocular hypotensive safety and systemic absorption of AR-13324 ophthalmic solution in normal volunteers.AR-13324眼药水在正常志愿者中的眼内降压安全性及全身吸收情况。
Am J Ophthalmol. 2015 May;159(5):980-5.e1. doi: 10.1016/j.ajo.2015.01.026. Epub 2015 Jan 28.
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Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes.0.04% AR-13324(一种ROCK和去甲肾上腺素转运体抑制剂)对正常血压猴眼房水动力学的影响。
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The Trabecular Meshwork: A Basic Review of Form and Function.小梁网:形态与功能的基础综述
J Ocul Biol. 2014 May;2(1). doi: 10.13188/2334-2838.1000017.
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Double-masked, randomized, dose-response study of AR-13324 versus latanoprost in patients with elevated intraocular pressure.双盲、随机、剂量反应研究 AR-13324 与拉坦前列素在眼压升高患者中的疗效比较。
Ophthalmology. 2015 Feb;122(2):302-7. doi: 10.1016/j.ophtha.2014.08.022. Epub 2014 Sep 27.