近日，美国FDA批准滴眼剂溶液Xiidra(lifitegrast ophthalmic solution) 5%上市，每日使用两次，治疗成人干眼症患者。目前，Xiidra是唯一一款可同时改善干眼症症状和体征的处方滴眼剂。
Xiidra是一种新型的小分子整合素抑制剂，可结合白细胞表面的淋巴细胞功能相关抗原-1（LFA-1），阻断LFA-1与其同源配体胞间粘附分子-1 （ICAM-1）的相互作用。
干眼症是现代人极为常见的疾病，在各年龄层发生率从5%到30%不等。干眼症是一种与眼球表面以及眼泪分泌相关的多因素疾病，表现为泪液质、量异常或动力学异常，症状也从干涩、灼热、异物感到红肿、疼痛、畏光甚至于视力减退等。
批准日期：2016年7月11日 公司：Shire US Inc.
XIIDRA（[立他司特[lifitegrast]）眼用溶液5％，用于局部眼科用途
美国最初批准：2016年
最近的重大变化
禁忌症：12/2017
作用机制
Lifitegrast与整合素淋巴细胞功能相关抗原-1（LFA-1）结合，后者是白细胞上发现的细胞表面蛋白，阻断LFA-1与其同源配体细胞间粘附分子-1（ICAM-1）的相互作用。ICAM-1可能在干眼症的角膜和结膜组织中过表达。LFA-1/ ICAM-1相互作用可以促成免疫突触的形成，导致T细胞活化和向靶组织的迁移。 体外研究表明，lifitegrast可抑制人T细胞系中T细胞与ICAM-1的粘附，并可抑制人外周血单核细胞中炎性细胞因子的分泌。 尚不清楚血管疾病在干眼症中的确切作用机制。
适应症和用法
Xiidra（lifitegrast）眼用溶液5％是淋巴细胞功能相关抗原-1（LFA-1）拮抗剂，用于治疗干眼病（DED）的体征和症状。
剂量和给药
每只眼睛每天两次（相隔大约12小时）。
剂量形式和强度
含有lifitegrast的眼用溶液50mg/mL（5％）。
禁忌症
过敏者禁用。
不良反应
使用希德拉后最常见的不良反应（发生率为5-25％）是滴注部位刺激，味觉障碍和视力下降。
包装提供/存储和处理
将Xiidra（lifitegrast眼用溶液）5％（50mg/mL）提供在含有5个低密度聚乙烯0.2mL一次性容器的箔袋中。
NDC 54092-606-01; 纸箱60个一次性容器。
存储：
储存在20至25°C（68至77°F）。将一次性容器存放在原始的铝箔袋中。
产品特点：
Lifitegrast结合至整合素淋巴细胞功能关联抗原-1(LFA-1)，一种在白细胞表面发现细胞表面蛋白和阻断interaction of LFA-1与它的关联配体细胞内黏附分子-1 (ICAM-1)。在干眼病中角膜和结膜组织中ICAM-1表达。LFA-1/ICAM-1相互作用可能促进对一个免疫突触的形成，导致T-细胞活化和迁移至目标组织。在体外研究显示，人T-细胞系lifitegrast可能抑制T-细胞黏附至ICAM-1和可能抑制在人外周血单核细胞中炎性细胞因子的分泌。lifitegrast在干眼病的确切作用机制还未清楚。
XIIDRA(lifitegrast ophthalmic solution) 5%, for topical ophthalmic use
Important Safety Information
Xiidra is contraindicated in patients with known hypersensitivity to lifitegrast or to any of the other ingredients.
In clinical trials, the most common adverse reactions reported in 5-25% of patients were instillation site irritation, dysgeusia and reduced visual acuity. Other adverse reactions reported in 1% to 5% of the patients were blurred vision, conjunctival hyperemia, eye irritation, headache, increased lacrimation, eye discharge, eye discomfort, eye pruritus and sinusitis.
GET READY FOR IMPROVEMENT
Xiidra is the only eye drop approved to treat both the signs and symptoms of Dry Eye Disease.2-4 Xiidra improved patient-reported symptoms of eye dryness and signs of inferior corneal staining in clinical trials.Think about Xiidra for symptomatic Dry Eye patients.
Indication
Xiidra(lifitegrast ophthalmic solution) 5% is indicated for the treatment of signs and symptoms of dry eye disease (DED).
Important Safety Information
Xiidra is contraindicated in patients with known hypersensitivity to lifitegrast or to any of the other ingredients.
In clinical trials, the most common adverse reactions reported in 5-25% of patients were instillation site irritation, dysgeusia and reduced visual acuity. Other adverse reactions reported in 1% to 5% of the patients were blurred vision, conjunctival hyperemia, eye irritation, headache, increased lacrimation, eye discharge, eye discomfort, eye pruritus and sinusitis.
To avoid the potential for eye injury or contamination of the solution, patients should not touch the tip of the single-use container to their eye or to any surface.
Contact lenses should be removed prior to the administration of Xiidra and may be reinserted 15 minutes following administration.
Safety and efficacy in pediatric patients below the age of 17 years have not been established.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ac09d19a-e321-4556-8a5c-66bd27cb6533