他氟前列素滴眼液治疗青光眼的应用研究进展

Research progress of tafluprost eye drops in the treatment of glaucoma

他氟前列素是一种具有强前列腺素F受体亲和力的前列腺素类似物(prosaglandin analogues,PGA),2003年首次报告,2008年作为首个原研无防腐剂的PGA药剂上市,以显著的降眼压能力被用于治疗开角型青光眼和高眼压症的一线药物。其独特的双氟原子结构赋予其强代谢稳定性,使其以低于其他PGA滴眼液的药物浓度发挥同等的疗效。大量临床研究证实了其降眼压疗效,不良反应发生较少且程度较轻。除降眼压外,还具有一定的改善眼血流量、视神经保护以及对其他眼组织的保护作用。近年来许多临床试验聚焦于无防腐剂他氟前列素滴眼液关于眼表安全性的评估。2022年无防腐剂他氟前列素滴眼液进入我国临床。本文对他氟前列素的发现、药理学机制和药代动力学进行介绍,并总结无防腐剂他氟前列素滴眼液的临床疗效、安全性和耐受性,以期为其临床使用提供指导。

Tafluprost is a prostaglandin analogue(PGA)with strong FP receptor affinity,which was first reported in 2003.Whereafter,Tafluprost eye drops,as the first originally developed preservative-free PGA agent,came on the market,and has been used as the first-line drug in the treatment of open-angle glaucoma and ocular hypertension.The unique difluoride atomic structure gives tafluprost stronger metabolic stability,making it perform similar efficacy with a lower concentration compared to other PGA.A large number of clinical studies on tafluprost eye drops have confirmed its effect of reducing intraocular pressure,and the adverse reactions occur less and to a lesser degree.In addition to reducing intraocular pressure,tafluprost is considered to have other pharmacological effects,including ocular blood flow improvement and optic nerve protection,as well as a protective effect on other ocular tissues.Recent clinical trials have begun to focus more on the evaluation of the safety of preservative-free tafluprost eye drops,especially for the ocular surface condition.In 2022,the preservative-free tafluprost eye drops(Tapros)were marketed in China.This article will review the pharmacological mechanism and pharmacokinetics of tafluprost,and discuss its clinical efficacy,safety,and tolerability of preservative-free tafluprost eye drops to provide clinical guidance.