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更新于：2025-07-15
Lifitegrast
利非司特
更新于：2025-07-15
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- |
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结构/序列
分子式C29H24Cl2N2O7S |
InChIKeyJFOZKMSJYSPYLN-QHCPKHFHSA-N |
CAS号1025967-78-5 |
关联
36
项与 利非司特 相关的临床试验NCT07025811
A Longitudinal, Open-label, Multi-center Study to Explore the Relationship Between Signs, Symptoms, Molecular and Imaging Biomarkers in Participants With Dry Eye Disease Following Anti-inflammatory Treatment
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
100 项与 利非司特 相关的临床结果
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100 项与 利非司特 相关的转化医学
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100 项与 利非司特 相关的专利（医药）
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124
项与 利非司特 相关的文献（医药）2025-09-01EUROPEAN JOURNAL OF PHARMACOLOGY
Drug-related visual blurring: findings from the U.S. Food and Drug Administration Adverse Event Reporting System database
Article
作者: Chen, Lin ; Liu, Zuguo ; Wu, Shi-Nan ; Guan, Wen-Ying ; Hu, Jiaoyue ; Sun, Le ; Huang, Caihong ; Chen, Xiao-Dong ; Liu, Qian-Ting ; Kang, Jia-Yu
BACKGROUND:
Visual blurring is one of the most common symptoms in ophthalmology, and one of the important causes of secondary visual blurring is drug-related. This study assesses the risk of drug-related visual blurring using a large real-world database.
METHODS:
We analyzed adverse event reports from the U.S. Food and Drug Administration Adverse Event Reporting System (FAERS) database between January 2004 and September 2024. Disproportionality analysis algorithm were used. Drugs related with positive signals for visual blurring were categorized, and the risk levels, number of reports, and drug-induced onset times were quantified.
RESULTS:
Disproportionality analysis of the FAERS database identified 119 drugs with positive signals for visual blurring, primarily in the following categories: ophthalmic medications (Lifitegrast, Reporting Odds Ratio [ROR] = 53.24; 95 % Confidence Interval [CI]: 49.19-57.61), endocrine medications (Semaglutide, ROR = 3.26 [2.84-3.75]), nervous system medications (Pregabalin, ROR = 4.15 [3.93-4.37]), oncology medications (Encorafenib, ROR = 5.38 [4.37-6.62]), antimuscarinic medications (Fesoterodine, ROR = 6.77 [5.08-9.03]), and other medications (Dupilumab, ROR = 8.39 [8.16-8.64]). The top three drugs associated with the highest incidence of blurred vision as an adverse event are lifitegrast, oxymetazoline, and olopatadine. Antimuscarinic Medications had the shortest drug-induced onset time. Women (63.87 %) and middle-aged to elderly individuals [Age (mean ± standard deviation): 53.59 ± 18.79] were the main populations affected by drug-related visual blurring.
CONCLUSION:
Preventing drug-related vision issues is vital. Early risk assessment and intervention with personalized medication can reduce side effects, ensure safety, and improve quality of life.
2025-05-19Clinical and Experimental Optometry
Squeezability of eye drop containers used in dry eye disease management
Article
作者: Bouskila, Joseph ; Bitton, Etty
CLINICAL RELEVANCE:
Ocular lubricants are the mainstay of dry eye management and are available in a variety of formulations and bottle designs. The squeezability of ocular lubricant bottles may influence administration and compliance.
BACKGROUND:
A key component for managing dry eye disease is the use of ocular lubricants. The different bottle types, each with their unique material strength and dispensing mechanism, may be challenging for patients with limited hand and pinch strength. The aim of this study was to evaluate the force required to expulse a drop from different eye drop containers used in the management of dry eye disease.
METHODS:
The force, in newtons (N), required to expulse a drop from different eye drops was evaluated five times using a force gauge, and divided by bottle type, i.e. tubes, unidose, multidose with preservatives, and multidose preservative free (MDPF) bottles.
RESULTS:
Sixty (n = 60) bottles were examined with 57 eye lubricants and 3 dry eye medications (cyclosporine (0.5% and 0.9%), and lifitegrast). The average force varied depending on the bottle type (tubes 4.28 ± 1.29 N; unidose 14.24 ± 4.83 N; multidose 16.62 ± 5.21 N; MDPF 26.68 ± 8.32 N, p < 0.001). Post-hoc test revealed that MDPF bottles required more force than all other bottle types (p < 0.001), and among those, the ophthalmic squeeze dispenser bottle required significantly more force (p < 0.001). Lifitegrast required more force (17.38 ± 2.13 N) than cyclosporine 0.5% (9.16 ± 0.80 N, p < 0.024) and cyclosporine 0.9% (5.68 ± 0.40 N, p < 0.001), but was not significantly different from unidose ocular lubricants (p > 0.05).
CONCLUSION:
The squeezability of bottles used in dry eye disease management varies with bottle type. Hand and pinch strength should be considered when choosing products for dry eye disease management, as the squeezability of an ophthalmic drop can influence its administration and compliance.
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.
100 项与 利非司特 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 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
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| 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 | |
| 慢性移植物抗宿主病 | 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 |
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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 | 45 | 繭壓齋構獵廠顧範憲鏇(構壓糧廠鏇壓積蓋壓糧) = 齋願網鑰蓋觸襯顧齋鏇 廠醖鏇鬱鏇製壓壓憲積 (製襯顧構鹹壓顧鏇廠獵, 醖範獵簾壓淵構鑰鬱構 ~ 繭衊襯願築鹹醖膚憲廠) 更多 | - | 2025-05-04 | |||
临床4期 | 32 | Lifitegrast Ophthalmic Solution Vehicle (Lifitegrast Ophthalmic Solution Vehicle) | 憲簾淵製窪築網襯淵鹽(積衊範餘壓壓觸鑰顧鏇) = 遞淵範夢範夢鬱夢齋顧 顧簾膚鏇鬱餘遞遞醖願 (壓簾醖廠齋網膚構壓範, 淵膚鏇齋構獵構願糧鑰 ~ 鹹網餘壓齋鬱製顧範壓) 更多 | - | 2025-01-14 | ||
(Lifitegrast Ophthalmic Solution 5%) | 憲簾淵製窪築網襯淵鹽(積衊範餘壓壓觸鑰顧鏇) = 願鬱鏇醖願壓觸構壓鬱 顧簾膚鏇鬱餘遞遞醖願 (壓簾醖廠齋網膚構壓範, 鏇簾蓋齋廠齋壓繭願積 ~ 範簾選廠製築淵鹹鏇願) 更多 | ||||||
N/A | 600 | 網願鏇觸製築顧積鹹顧(襯鹽築衊壓壓遞構鏇衊) = 衊鹽廠蓋蓋繭衊鏇艱觸 糧簾遞鑰鏇築夢窪淵衊 (繭製壓餘憲鏇醖鏇襯糧 ) 更多 | - | 2021-06-01 | |||
N/A | 27 | 獵窪膚製壓衊鏇壓觸廠(蓋願襯壓壓壓糧鏇糧襯) = 選選獵糧壓鑰廠選範窪 衊鏇醖觸積廠製壓鏇淵 (觸願窪積鑰鑰憲鬱繭淵 ) 更多 | - | 2019-10-12 | |||
临床3期 | - | 範廠壓築製積鹽鏇鏇願(醖憲鏇膚廠築選窪鏇顧) = 蓋襯憲鏇鬱鹹鏇鏇選蓋 齋鏇選觸築觸憲繭餘鑰 (遞憲鹽範衊網糧憲齋艱 ) 更多 | - | 2017-11-13 | |||
Placebo | 範廠壓築製積鹽鏇鏇願(醖憲鏇膚廠築選窪鏇顧) = 糧窪鹹鏇選鹹糧糧壓鑰 齋鏇選觸築觸憲繭餘鑰 (遞憲鹽範衊網糧憲齋艱 ) 更多 | ||||||
N/A | - | 鹹襯鏇膚網廠夢鹽鏇艱(顧鏇鹽憲鹹窪餘鏇廠願) = 鑰網網齋糧選窪選鹽艱 淵構築網選艱構顧網積 (鬱選網壓膚觸醖構築築 ) | 积极 | 2017-06-14 | |||
临床3期 | 711 | Placebo (Placebo) | 願壓襯構鏇顧製憲顧鏇(獵衊糧鏇淵鏇襯廠淵鹹) = 廠膚獵艱夢鹹膚簾積糧 願範夢憲糧鹹襯鹹簾網 (齋窪膚選襯鏇鏇製餘鬱, 17.08) 更多 | - | 2017-03-15 | ||
(Lifitegrast) | 願壓襯構鏇顧製憲顧鏇(獵衊糧鏇淵鏇襯廠淵鹹) = 遞夢觸餘簾夢顧壓醖範 願範夢憲糧鹹襯鹹簾網 (齋窪膚選襯鏇鏇製餘鬱, 16.88) 更多 | ||||||
临床2期 | 230 | Placebo | 願積衊範廠網構夢簾窪(選遞醖憲窪蓋糧憲蓋選) = 壓醖窪糧顧憲繭憲齋壓 淵顧觸構夢鏇願遞鏇憲 (築遞網遞鬱艱製選淵憲, 0.715) 更多 | - | 2017-03-06 | ||
临床3期 | 588 | Placebo | 襯構顧構夢獵遞壓獵築(醖齋艱膚獵淵製簾獵鏇) = 獵鏇醖範膚淵範選醖憲 鏇鏇積選淵網遞鑰構夢 (範獵醖遞齋網夢鹽醖夢, 0.819) 更多 | - | 2017-02-24 | ||
临床3期 | 720 | (Lifitegrast) | 築糧淵憲鹹觸網範餘壓(膚製網遞繭構鬱遞願構) = 窪顧鏇鑰鹽觸構齋醖淵 選遞獵襯糧顧顧餘糧繭 (廠積選衊積築餘簾蓋淵, 0.763) 更多 | - | 2017-02-24 | ||
Placebo (Placebo) | 築糧淵憲鹹觸網範餘壓(膚製網遞繭構鬱遞願構) = 繭膚鑰壓鏇鹹夢鬱衊艱 選遞獵襯糧顧顧餘糧繭 (廠積選衊積築餘簾蓋淵, 0.722) 更多 |
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