NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, University of Florence , Florence , Italy.
Expert Opin Ther Pat. 2019 Oct;29(10):793-803. doi: 10.1080/13543776.2019.1661992. Epub 2019 Sep 4.
: Elevated intraocular pressure (IOP) is the most prevalent risk factor for glaucoma. Prostaglandin analogs are a first-line therapy for glaucoma due to their ability to reduce IOP, once-daily dosing, efficacy, and minimal side-effect profile. Many compounds targeting different PG receptors have been developed in the last years, some of them being in clinical use. Latanoprost, Bimatoprost, Travoprost, and Tafluprost are clinically used as antiglaucoma drugs and act as agonists of the PGF2α receptor. The inability to fully understand the mechanism of action of clinically used PGF2α analogs is thus a strong driver for additional research into the mechanism of action of ocular hypotensive drugs belonging to this class of pharmacological agents. : This review explores the last 5 years (2013-2018), where many patents describing new compounds acting on different prostaglandin receptors, and mainly targeting EP1-4 and FP receptors, were released. : To date, there has been a growing awareness over recent years of the therapeutic use of novel derivatives as new antiglaucoma pharmaceutical products. Patents involved in discovering new approaches and new molecules for the treatment of glaucoma diseases encouraged the scientific community to increase the variety of drugs available for the treatment of ocular diseases.
眼压升高(IOP)是青光眼最常见的危险因素。前列腺素类似物是治疗青光眼的一线药物,因为它们具有降低眼压、每日一次给药、疗效和最小的副作用特征。近年来,已经开发出许多针对不同 PG 受体的化合物,其中一些已在临床应用。拉坦前列素、比马前列素、曲伏前列素和他氟前列素作为青光眼药物在临床上使用,作用于 PGF2α 受体激动剂。因此,无法完全了解临床使用的 PGF2α 类似物的作用机制是对属于该类药物的眼部降压药物作用机制进行额外研究的强大动力。
本文综述了过去 5 年(2013-2018 年)发布的许多专利,这些专利描述了作用于不同前列腺素受体的新型化合物,主要针对 EP1-4 和 FP 受体。
近年来,人们越来越意识到新型衍生物在治疗青光眼等疾病方面的治疗用途。涉及发现治疗青光眼疾病的新方法和新分子的专利鼓励科学界增加可用于治疗眼部疾病的药物种类。