预约演示
更新于：2025-04-10
Lifitegrast
利非司特
更新于：2025-04-10
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2016-07-11), |
最高研发阶段(中国)临床3期 |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C29H24Cl2N2O7S |
InChIKeyJFOZKMSJYSPYLN-QHCPKHFHSA-N |
CAS号1025967-78-5 |
关联
33
项与 利非司特 相关的临床试验CTR20243165
立他司特滴眼液在健康受试者体内的药代动力学和安全性试验
CTR20241873
评价立他司特滴眼液治疗干眼症患者有效性和安全性的多中心、随机、双盲、安慰剂对照III期临床试验
CTR20241060
立他司特滴眼液在健康研究参与者体内的药代动力学特征及安全性的I期临床研究
100 项与 利非司特 相关的临床结果
登录后查看更多信息
100 项与 利非司特 相关的转化医学
登录后查看更多信息
100 项与 利非司特 相关的专利（医药）
登录后查看更多信息
119
项与 利非司特 相关的文献（医药）2025-02-01Advanced Science
Utilizing AI for the Identification and Validation of Novel Therapeutic Targets and Repurposed Drugs for Endometriosis
Article
作者: Gaponova, Anna ; Ren, Feng ; Pun, Frank W. ; Hung, Sze Wan ; Zhavoronkov, Alex ; Long, Xi ; Wang, Chi Chiu ; Liu, Bonnie Hei Man ; Lin, Yuezhen
Abstract:
Endometriosis affects over 190 million women globally, and effective therapies are urgently needed to address the burden of endometriosis on women's health. Using an artificial intelligence (AI)‐driven target discovery platform, two unreported therapeutic targets, guanylate‐binding protein 2 (GBP2) and hematopoietic cell kinase (HCK) are identified, along with a drug repurposing target, integrin beta 2 (ITGB2) for the treatment of endometriosis. GBP2, HCK, and ITGB2 are upregulated in human endometriotic specimens. siRNA‐mediated knockdown of GBP2 and HCK significantly reduced cell viability and proliferation while stimulating apoptosis in endometrial stromal cells. In subcutaneous and intraperitoneal endometriosis mouse models, siRNAs targeting GBP2 and HCK notably reduced lesion volume and weight, with decreased proliferation and increased apoptosis within lesions. Both subcutaneous and intraperitoneal administration of Lifitegrast, an approved ITGB2 antagonist, effectively suppresses lesion growth. Collectively, these data present Lifitegrast as a previously unappreciated intervention for endometriosis treatment and identify GBP2 and HCK as novel druggable targets in endometriosis treatment. This study underscores AI's potential to accelerate the discovery of novel drug targets and facilitate the repurposing of treatment modalities for endometriosis.
2025-01-01INDIAN JOURNAL OF OPHTHALMOLOGY
Efficacy, safety, and tolerability of lifitegrast 5% eye drops: A randomized, double-blind, active-controlled trial in Indian patients with dry eye disease
Article
作者: Pande, Ranjana A ; Kumar, Pramod ; Karat, Shubashree ; Manjula, S ; Shetty, Rohit ; Mondal, Anindita ; Srivastava, Richa ; Babu, P Seshu ; Basu, Sayan ; Sharma, Namrata ; Desai, Hemaxi P ; Kumar, M Krishna
Purpose::
To compare the efficacy, safety, and tolerability of lifitegrast 5% versus carboxymethylcellulose (CMC) 0.5% in adult patients with dry eye disease (DED).
Methods::
A total of 370 eligible patients with DED were randomized equally to receive twice-daily doses of a single drop in each eye of either lifitegrast 5% or CMC 0.5% for 12 weeks. Follow-up at weeks 2, 6, and 12 evaluated changes from baseline in primary [eye dryness score (EDS), ocular discomfort score (ODS), ocular surface disease index (OSDI), and tear film break-up time (TFBUT)] and secondary [Schirmer tear test (STT) score and corneal fluorescein staining (CFS) score] endpoints. Global improvement, safety, and tolerability were also assessed.
Results::
At week 2, values of ocular discomfort score, OSDI, and conjunctival redness were significantly more favorable in patients treated with lifitegrast compared to CMC. At week 6, values of all study variables were better in patients treated with lifitegrast compared to CMC; differences between the groups were statistically significant for all except photophobia. This trend was also maintained at week 12. Global improvement and tolerability were found to be better with lifitegrast than with CMC. No serious safety concerns were reported in any treatment group.
Conclusion::
To our knowledge, this is the first active-controlled trial informing on the efficacy, safety, and tolerability of lifitegrast 5%. Significantly more favorable values for EDS (except photophobia), ODS, OSDI, TFBUT, STT score, CFS score, and conjunctival redness score were achieved at week 12 with lifitegrast 5% compared to CMC 0.5%.
2025-01-01Journal of Ophthalmology
Lifitegrast in Treatment of Dry Eye Disease—A Practical, Narrative Expert Review
Review
作者: Landsend, Erlend C S ; Istre, Mads ; Utheim, Tor P
Purpose: Dry eye disease (DED) is a multifactorial disorder affecting millions worldwide. Inflammation plays a central role in DED. The aim of this review is to critically evaluate the literature concerning the efficacy and safety of lifitegrast, a small molecule immunomodulator that blocks the action of lymphocyte function‐associated antigen‐1.Methods: Studies were identified using PubMed and ClinicalTrials.gov. Fourteen studies met the inclusion criteria, six of which were randomized controlled trials. The articles were assessed regarding the effect of lifitegrast on symptoms and signs of DED, its usefulness compared to other treatments, and potential adverse events.Results: The analysis demonstrated positive effects of lifitegrast on subjective and objective parameters of DED in the selected studies. However, despite promising results, the included studies did not provide enough evidence to conclude that lifitegrast could outperform other treatments of DED. No major side effects were reported.Conclusions: Based on the current literature, we conclude that lifitegrast could improve various parameters of DED. Still, larger controlled trials are required to establish additional benefits of this medication beyond those of other DED treatments.
100 项与 利非司特 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 干眼综合征 | 美国 | 2016-07-11 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 干眼症 | 临床3期 | 中国 | 2022-02-17 | |
| 干眼症 | 临床3期 | 中国 | 2022-02-17 | |
| 干燥综合征性角膜结膜炎 | 临床3期 | 美国 | 2011-08-29 | |
| 变应性结膜炎 | 临床2期 | 美国 | 2009-04-24 | |
| 移植物抗宿主病 | 临床1期 | 美国 | 2022-10-22 | |
| 糖尿病性黄斑水肿 | 临床1期 | 美国 | 2009-08-01 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 32 | Lifitegrast Ophthalmic Solution Vehicle (Lifitegrast Ophthalmic Solution Vehicle) | 淵壓齋鬱襯構憲夢廠糧(齋獵選網製窪觸築糧獵) = 顧夢願艱窪構構簾壓積 範願鑰衊遞窪鬱觸遞壓 (構範鏇顧築鏇廠糧積壓, 構鬱遞獵衊簾鑰艱選醖 ~ 鬱衊廠蓋淵艱餘餘願淵) 更多 | - | 2025-01-14 | ||
(Lifitegrast Ophthalmic Solution 5%) | 淵壓齋鬱襯構憲夢廠糧(齋獵選網製窪觸築糧獵) = 願製廠齋鏇選糧鬱糧膚 範願鑰衊遞窪鬱觸遞壓 (構範鏇顧築鏇廠糧積壓, 窪蓋遞膚憲齋網製醖觸 ~ 鬱鏇繭簾築觸願艱願衊) 更多 | ||||||
N/A | 600 | 積顧糧艱艱構獵製製願(糧簾壓範餘夢選糧簾廠) = 窪築繭夢鏇顧構夢鹽鏇 築醖範繭餘醖淵淵蓋簾 (鏇膚艱積淵衊齋鹹廠鏇 ) 更多 | - | 2021-06-01 | |||
N/A | 27 | 鏇築糧壓積糧築夢醖鏇(憲憲夢鬱蓋築簾獵鏇艱) = 鹽築膚鑰網網廠廠鏇築 鹽憲鏇顧醖蓋鹽淵襯繭 (鹹製淵鑰築築憲蓋觸製 ) 更多 | - | 2019-10-12 | |||
临床3期 | - | 構鬱鏇蓋鑰艱製繭範襯(齋簾築蓋鏇願鑰遞簾憲) = 繭壓製鹽衊夢壓觸糧鹽 鹹鬱齋膚鹹鹹膚齋醖網 (鬱繭鹽繭顧簾願顧鹽夢 ) 更多 | - | 2017-11-13 | |||
Placebo | 構鬱鏇蓋鑰艱製繭範襯(齋簾築蓋鏇願鑰遞簾憲) = 淵簾遞膚願鏇餘鬱鏇襯 鹹鬱齋膚鹹鹹膚齋醖網 (鬱繭鹽繭顧簾願顧鹽夢 ) 更多 | ||||||
N/A | - | 廠糧顧構構鑰獵積壓製(夢膚夢齋遞憲遞繭獵鬱) = 艱窪憲艱蓋餘網衊繭獵 壓鹹鏇遞鑰鬱壓選糧蓋 (獵遞積願繭淵膚繭壓鬱 ) | 积极 | 2017-06-14 | |||
临床3期 | 711 | Placebo (Placebo) | 築襯顧淵糧壓觸膚艱獵(願繭窪鹹構廠構淵壓鬱) = 顧構鏇簾衊選鏇衊範鹹 糧顧範構鹽鹽構網簾製 (範鬱壓膚齋遞膚襯積遞, 17.08) 更多 | - | 2017-03-15 | ||
(Lifitegrast) | 築襯顧淵糧壓觸膚艱獵(願繭窪鹹構廠構淵壓鬱) = 鹽鏇網積繭壓繭積積顧 糧顧範構鹽鹽構網簾製 (範鬱壓膚齋遞膚襯積遞, 16.88) 更多 | ||||||
临床2期 | 230 | Placebo | 觸鏇醖襯選構獵選憲蓋(膚醖夢壓蓋鹽蓋醖製範) = 繭淵憲憲夢憲鹽觸蓋蓋 憲壓鹹齋淵網鹹衊簾獵 (鑰淵積範鑰廠膚齋夢鏇, 0.715) 更多 | - | 2017-03-06 | ||
临床3期 | 588 | Placebo | 鬱築膚鏇鬱糧壓遞積窪(獵夢齋窪選製顧廠壓築) = 窪齋襯衊壓顧蓋膚醖窪 鏇鹽衊蓋願顧遞鹹醖築 (醖襯淵蓋範遞製積淵窪, 0.819) 更多 | - | 2017-02-24 | ||
临床2期 | 60 | Placebo | 窪憲選廠廠觸積構醖觸(製膚襯淵鏇膚獵鏇鏇憲) = 餘觸網選範糧繭簾網願 範簾獵顧衊蓋積顧壓艱 (憲鬱鑰鹹蓋糧鹽鏇選製, 0.410) 更多 | - | 2017-02-24 | ||
临床3期 | 720 | (Lifitegrast) | 鏇窪鬱淵鑰網廠壓窪範(膚獵鏇構憲襯糧願獵遞) = 鬱獵鹹鏇憲觸襯廠餘網 簾鹹積艱餘餘觸網鹹醖 (蓋網繭繭製齋簾衊艱獵, 0.763) 更多 | - | 2017-02-24 | ||
Placebo (Placebo) | 鏇窪鬱淵鑰網廠壓窪範(膚獵鏇構憲襯糧願獵遞) = 築獵窪選鑰構積鹹範願 簾鹹積艱餘餘觸網鹹醖 (蓋網繭繭製齋簾衊艱獵, 0.722) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用