School of Pharmacy, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei 11031, Taiwan.
Department of Pharmacy, Taipei Municipal Wanfang Hospital, Taipei Medical University, No. 111, Section 3, Xing-Long Road, Taipei 11696, Taiwan.
J Med Chem. 2020 Oct 8;63(19):10533-10593. doi: 10.1021/acs.jmedchem.9b01033. Epub 2020 Jun 2.
The ocular drug discovery field has evidenced significant advancement in the past decade. The FDA approvals of Rhopressa, Vyzulta, and Roclatan for glaucoma, Brolucizumab for wet age-related macular degeneration (wet AMD), Luxturna for retinitis pigmentosa, Dextenza (0.4 mg dexamethasone intracanalicular insert) for ocular inflammation, ReSure sealant to seal corneal incisions, and Lifitegrast for dry eye represent some of the major developments in the field of ocular therapeutics. A literature survey also indicates that gene therapy, stem cell therapy, and target discovery through genomic research represent significant promise as potential strategies to achieve tissue repair or regeneration and to attain therapeutic benefits in ocular diseases. Overall, the emergence of new technologies coupled with first-in-class entries in ophthalmology are highly anticipated to restructure and boost the future trends in the field of ophthalmic drug discovery. This perspective focuses on various aspects of ocular drug discovery and the recent advances therein. Recent medicinal chemistry campaigns along with a brief overview of the structure-activity relationships of the diverse chemical classes and developments in ocular drug delivery (ODD) are presented.
在过去的十年中，眼科药物发现领域取得了重大进展。FDA 批准了 Rhopressa、Vyzulta 和 Roclatan 用于治疗青光眼，Brolucizumab 用于湿性年龄相关性黄斑变性（湿性 AMD），Luxturna 用于治疗色素性视网膜炎，Dextenza（0.4mg 地塞米松管内植入物）用于眼部炎症，Resure 密封剂用于密封角膜切口，以及 Lifitegrast 用于治疗干眼症，这些都代表了眼科治疗领域的一些重大进展。文献调查还表明，基因治疗、干细胞治疗以及通过基因组研究发现靶点，都代表着实现组织修复或再生以及在眼部疾病中获得治疗益处的潜在策略，具有重要意义。总的来说，新技术的出现以及眼科领域的首创产品，有望重塑和推动眼科药物发现领域的未来发展趋势。本文着眼于眼科药物发现的各个方面及其最新进展。本文介绍了近期的药物化学研究进展，并简要概述了不同化学类别药物的构效关系以及眼科药物传递（ODD）的发展情况。
