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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.

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。

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