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Discovery to Launch of Anti-allergy (Emadine; Patanol/Pataday/Pazeo) and Anti-glaucoma (Travatan; Simbrinza) Ocular Drugs, and Generation of Novel Pharmacological Tools Such as AL-8810.抗过敏(依美斯汀;帕坦洛/帕迪特/帕泽奥)和抗青光眼(曲伏前列素;辛布林扎)眼科药物的研发至上市,以及新型药理学工具如AL - 8810的产生。
ACS Pharmacol Transl Sci. 2020 Nov 5;3(6):1391-1421. doi: 10.1021/acsptsci.0c00137. eCollection 2020 Dec 11.
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Prostaglandin F receptor antagonist attenuates LPS-induced systemic inflammatory response in mice.前列腺素 F 受体拮抗剂可减轻 LPS 诱导的小鼠全身炎症反应。
FASEB J. 2020 Nov;34(11):15197-15207. doi: 10.1096/fj.202001481R. Epub 2020 Sep 28.
2
Improvement in inner retinal function in glaucoma with nicotinamide (vitamin B3) supplementation: A crossover randomized clinical trial.尼可酰胺(维生素 B3)补充治疗对青光眼患者内层视网膜功能的改善作用:一项交叉随机临床试验。
Clin Exp Ophthalmol. 2020 Sep;48(7):903-914. doi: 10.1111/ceo.13818. Epub 2020 Jul 28.
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Unaltered Perception of Suprathreshold Contrast in Early Glaucoma Despite Sensitivity Loss.尽管敏感性降低,早期青光眼仍存在未改变的阈上对比度知觉。
Invest Ophthalmol Vis Sci. 2020 Jul 1;61(8):23. doi: 10.1167/iovs.61.8.23.
4
Stanniocalcin-1 (STC-1), a downstream effector molecule in latanoprost signaling, acts independent of the FP receptor for intraocular pressure reduction.斯钙素-1(STC-1)是拉坦前列素信号通路中的下游效应分子,其降低眼内压的作用不依赖于 FP 受体。
PLoS One. 2020 May 4;15(5):e0232591. doi: 10.1371/journal.pone.0232591. eCollection 2020.
5
The Diagnosis and Treatment of Glaucoma.青光眼的诊断与治疗。
Dtsch Arztebl Int. 2020 Mar 27;117(13):225-234. doi: 10.3238/arztebl.2020.0225.
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Matrix Metalloproteinases and Glaucoma Treatment.基质金属蛋白酶与青光眼治疗。
J Ocul Pharmacol Ther. 2020 May;36(4):208-228. doi: 10.1089/jop.2019.0146. Epub 2020 Apr 1.
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The antagonism of prostaglandin FP receptors inhibits the evolution of spreading depolarization in an experimental model of global forebrain ischemia.前列腺素 FP 受体拮抗剂抑制全脑缺血实验模型中扩散性去极化的进展。
Neurobiol Dis. 2020 Apr;137:104780. doi: 10.1016/j.nbd.2020.104780. Epub 2020 Jan 25.
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Ab externo implantation of the MicroShunt, a poly (styrene--isobutylene--styrene) surgical device for the treatment of primary open-angle glaucoma: a review.用于治疗原发性开角型青光眼的聚(苯乙烯-异丁烯-苯乙烯)手术装置MicroShunt的外部植入:综述
Eye Vis (Lond). 2019 Nov 15;6:36. doi: 10.1186/s40662-019-0162-1. eCollection 2019.
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ICON: Diagnosis and management of allergic conjunctivitis.ICON:过敏性结膜炎的诊断与管理。
Ann Allergy Asthma Immunol. 2020 Feb;124(2):118-134. doi: 10.1016/j.anai.2019.11.014. Epub 2019 Nov 21.
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Efficacy and safety of prostaglandin analogues in primary open-angle glaucoma or ocular hypertension patients: A meta-analysis.前列腺素类似物在原发性开角型青光眼或高眼压症患者中的疗效与安全性:一项荟萃分析。
Medicine (Baltimore). 2019 Jul;98(30):e16597. doi: 10.1097/MD.0000000000016597.

抗过敏(依美斯汀;帕坦洛/帕迪特/帕泽奥)和抗青光眼(曲伏前列素;辛布林扎)眼科药物的研发至上市,以及新型药理学工具如AL - 8810的产生。

Discovery to Launch of Anti-allergy (Emadine; Patanol/Pataday/Pazeo) and Anti-glaucoma (Travatan; Simbrinza) Ocular Drugs, and Generation of Novel Pharmacological Tools Such as AL-8810.

作者信息

Sharif Najam A

机构信息

Department of Pharmacology & Neuroscience University of North Texas Health Science Center, Fort Worth, Texas 76107, United States.

出版信息

ACS Pharmacol Transl Sci. 2020 Nov 5;3(6):1391-1421. doi: 10.1021/acsptsci.0c00137. eCollection 2020 Dec 11.

DOI:10.1021/acsptsci.0c00137
PMID:33344909
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7737327/
Abstract

The eye and eyesight are exquistly designed and are precious, and yet we often take them for granted. Good vision is critical for our long-term survival and for humanity's enduring progress. Unfortunately, since ocular diseases do not culminate in life-and-death scenarios, awareness of the plight of millions of people suffering from such eye ailments is not publicized as other diseases. However, losing eyesight or falling victim to visual impairment is a frightening outlook for most people. Glaucoma, a collection of chronic optic neuropathies, of which the most prevalent form, primary open-angle glaucoma (POAG), is the second leading cause of irreversible blindness. POAG currently afflicts >70 million people worldwide and is an insidious, progressive, silent thief of sight that is asymptomatic. On the other hand, allergic conjunctivitis (AC), and the associated rhinitis ("hay-fever"), frequently victimizes a huge number of people worldwide, especially during seasonal changes. While not life-threatening, sufferers of AC soon learn the value of drugs to treat their signs and symptoms of AC as they desire rapid relief to overcome the ocular itching/pain, redness, and tearing AC causes. Herein, I will describe the collective efforts of many researchers whose industrious, diligent, and dedicated team work resulted in the discovery, biochemical/pharmacological characterization, development and eventual launch of drugs to treat AC (e.g., olopatadine [Patanol/Pataday/Pazeo] and emedastine [Emedine]), and for treating ocular hypertension and POAG (e.g., travoprost [Travatan ] and Simbrinza). This represents a personal perspective.

摘要

眼睛及其视力的设计极其精巧且十分珍贵,但我们却常常对其视而不见。良好的视力对于我们的长期生存以及人类的持续进步至关重要。不幸的是,由于眼部疾病不会导致生死攸关的情况,数百万患有此类眼疾的人的困境不像其他疾病那样得到广泛宣传。然而,对大多数人来说,失明或成为视力障碍的受害者是一个可怕的前景。青光眼是一组慢性视神经病变,其中最常见的形式——原发性开角型青光眼(POAG)是不可逆失明的第二大主要原因。目前,POAG在全球折磨着超过7000万人,它是一种隐匿、渐进、无声的视力窃贼,且没有症状。另一方面,过敏性结膜炎(AC)以及相关的鼻炎(“花粉症”)在全球范围内经常使大量的人患病,尤其是在季节变化期间。虽然不会危及生命,但AC患者很快就会认识到药物对于治疗其AC症状的价值,因为他们渴望迅速缓解以克服AC所引起的眼部瘙痒/疼痛、发红和流泪。在此,我将描述众多研究人员的共同努力,他们勤奋、勤勉且专注的团队合作促成了用于治疗AC(例如奥洛他定[帕坦洛/帕他迪/帕佐]和依美斯汀[埃美丁])以及治疗高眼压和POAG(例如曲伏前列素[适利达]和布林佐胺噻吗洛尔[ Simbrinza])的药物的发现、生化/药理学特性研究、开发及最终上市。这代表了一种个人观点。