氯替泼诺(Loteprednol Etabonate) - 药物靶点：GR x cPLA2α_在研适应症：干眼综合征，疼痛，眼带状疱疹_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Loteprednol etabonate (JAN/USAN)、Loteprednol Etabonate Ophthalmic Suspension、CDDD-5604

+ [13]

靶点

GR x cPLA2α

作用方式

激动剂

作用机制

GR激动剂(糖皮质激素受体激动剂)、cPLA2α 激动剂(胞内磷脂酶A2 激动剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Bausch & Lomb (Australia) Pty Ltd.

Bausch & Lomb, Inc.Alcon Laboratories, Inc.

非在研机构

Kala Bio, Inc.Bausch Health Americas, Inc.

Sandoz Group AG

+ [2]

权益机构-

最高研发阶段批准上市

首次获批日期

美国 (1998-03-09),

变应性结膜炎结膜炎睫状体炎+ [7]

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C24H31ClO7

InChIKeyDMKSVUSAATWOCU-HROMYWEYSA-N

CAS号82034-46-6

关联

65

项与氯替泼诺相关的临床试验

NCT05542381

/ RecruitingN/AIIT

The Role of Loteprednol in Reducing Post-Intravitreal Injection Related Pain

Patients are already receiving an intravitreal injection as a standard of care, but they are consenting to receiving a loteprednol drop following the intravitreal injection. This clinical trial is studying the role of loteprednol (corticosteroid) in reducing pain following intravitreal injections for patients with age-related macular degeneration. As of now, there is no definitive pain management technique following intravitreal injections. Loteprednol is a corticosteroid widely used in ophthalmology to treat pain and inflammation, however, it has not been studied as a treatment for pain following intravitreal injections. Our overall goal is to manage pain to improve quality of care after intravitreal injections. Participants will be given either loteprednol, or artificial tears following one visit for an intravitreal injection to test how effective loteprednol is in pain reduction. Pain levels will be assessed by asking participants over the phone about their pain from a scale of 0 to 10 at three different times over a 1-week period. Artificial tear and medication usage will also be tracked over a 1-week period.

开始日期2022-12-22

申办/合作机构

Virginia Polytechnic Institute & State University

[+1]

CTRI/2022/07/044211

/ Not yet recruiting临床3期

A Multicentric Randomized Double Blind Double Dummy Parallel Group Two Arm Comparative Phase III Clinical Study to Evaluate Efficacy Safety and Tolerability of Loteprednol Etabonate Ophthalmic Suspension 1% w/v of Ajanta Pharma Ltd versus Loteprednol Etabonate Ophthalmic Suspension 0.5% w/v in treatment of Post-Operative Inflammatory conditions of Eye - Phase III

开始日期2022-07-25

申办/合作机构

Ajanta Pharma Ltd.

NCT05136443

/ Completed临床4期

Prospective Analysis of Loteprednol Etabonate Ophthalmic Suspension 0.25% for Prevention of Immunologic Rejection After Descemet Membrane Endothelial Keratoplasty

The purpose of this study is to assess off-label use of loteprednol etabonate 0.25% ophthalmic suspension (Eysuvis) for prevention of immunologic rejection in the first year after Descemet membrane endothelial keratoplasty (DMEK). Topical corticosteroids have long been the mainstay for preventing and treating cornea transplant rejection although none are specifically approved for this purpose. The rates of immunologic rejection episodes and steroid-induced ocular hypertension will be compared with the respective rates observed in earlier studies with prednisolone acetate 1% suspension, loteprednol etabonate 0.5% gel, and fluorometholone 0.1% suspension after DMEK.

开始日期2021-11-23

申办/合作机构

Price Vision Group

[+1]

100 项与氯替泼诺相关的临床结果

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100 项与氯替泼诺相关的转化医学

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100 项与氯替泼诺相关的专利（医药）

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356

项与氯替泼诺相关的文献（医药）

2025-08-01·FOOD CHEMISTRY

Investigation into the effects of acute heat stress on stress level, meat quality, myofibrillar proteins properties and serum metabolites release of Muscovy ducks (Cairina moschata)

Article

作者: Huang, Tianran ; Xiao, Mengchao ; Huang, Jichao ; Li, Zimu ; Zhu, Zongshuai ; Huang, Ming

This study systematically investigated the effects of acute heat stress (AHS) on Muscovy ducks, focusing on plasma stress indicators, meat quality, myofibrillar proteins (MPs) properties, and serum metabolite profiles. AHS significantly elevated stress level, impairing meat quality, as evidenced by higher L* value, shear force, drip loss, and cooking loss (P < 0.05). It also induced MPs oxidation and aggregation, reflected by elevated carbonyl content, turbidity, zeta potential, and particle size. MPs structural alterations were confirmed by fluorescence quenching and increased exposure of hydrophobic groups. Correlation analysis revealed strong associations between physicochemical changes and MPs oxidation. Metabolomic analysis identified 161 and 105 differential metabolites in the CON vs. LS and CON vs. SS comparisons, respectively, involving 25 metabolic pathways related to energy, amino acids, and fatty acids. These findings provide novel insights into the molecular pathways of AHS-induced meat quality deterioration and reveal potential intervention timing for the poultry industry.

2025-06-01·EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Overcoming barriers in formulating practically insoluble loteprednol etabonate in ophthalmic nanoemulsion

Article

作者: Petriček, Igor ; Bočkor, Luka ; Juretić, Marina ; Krtalić, Iva ; Špoljarić, Drago ; Kocbek, Petra ; Pepić, Ivan ; Lovrić, Jasmina ; Kučuk, Maša Sufundžić ; Hafner, Anita ; Dukovski, Bisera Jurišić ; Ljubica, Josip

Loteprednol etabonate (LE) is a soft corticosteroid recently approved for the short-term treatment of signs and symptoms of dry eye disease. LE is available on the market as a suspension, which can release only limited amount of dissolved corticosteroid after application at the ocular surface. This study is focused on the development of an oil-in-water nanoemulsion (NE) to effectively deliver dissolved LE to the ocular surface, in order to promote its absorption. We newly developed an extended-throughput 3D model of the corneal epithelium for biocompatibility study, and an innovative approach to investigate the effect of biorelevant dilution on LE release from the NE oil phase. Castor oil, Capryol® 90, Kolliphor® EL and Soluplus® were selected as NE excipients based on their potential to dissolve LE. Design of experiments was successfully employed to develop biocompatible and physically stable NE with high LE content (0.15 %, w/w) and retention efficiency (87 % after 10 months of storage at room temperature). LE retention within oil droplets (above 90 % of the initial LE content) despite biorelevant dilution simulating tear turnover suggests the potential for direct LE absorption from the NE oil droplets into the lipophilic corneal epithelium. The results obtained encourage the extension of the studies in terms of in vitro permeability and in vivo eye-related bioavailability assessment to prove the potential of the proposed LE formulation.

2025-05-01·INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Loteprednol etabonate alleviates NLRP3 inflammasome-associated inflammatory diseases in mice by suppressing the transcription of IL-1β

Article

作者: Li, Weiling ; Huang, Weichen ; Fu, Zhengqi ; Xie, Shoufeng ; Yao, Yulin ; Wan, Pin ; Ye, Lirui ; Peng, Qian ; Liu, Yuchen ; He, Qi ; Sun, Binlian

Excessive activation of the NLRP3 inflammasome leads to cellular inflammation and tissue damage. Finding an inhibitor of its activation is urgent need for NLRP3 inflammasome-associated inflammatory diseases. In this study, we identified Loteprednol etabonate (LE), a well-known anti-inflammatory drug for ocular conditions, as a potent inhibitor of NLRP3 inflammasome activation through screening an FDA-approved drug library. In cellular models, LE significantly reduced IL-1β transcription, suppressed NLRP3 inflammasome activation, and finally inhibited the maturation and secretion of IL-1β and GSDMD-mediated pyroptosis. Mechanistic investigations showed that LE might inhibit IL-1β transcription by blocking both NF-κB and AP-1 signaling pathways. Furthermore, in mouse models of NLRP3 inflammasome-associated inflammatory diseases, including LPS-induced sepsis and DSS-induced colitis, intraperitoneal injection of LE significantly suppressed inflammatory response and improved mice survival rate. Collectively, these findings identify LE as a novel inhibitor of NLRP3 inflammasome activation, offering a promising therapeutic strategy for the treatment of NLRP3 inflammasome-associated inflammatory diseases.

63

项与氯替泼诺相关的新闻（医药）

2025-05-29

·FiercePharma

Alcon gains first FDA prescription drug nod since Novartis split, scoring with drops for dry eye disease

Alcon has gained its first FDA nod for a prescription product since its 2019 split with Novartis, securing an approval for dry eye disease treatment Tryptyr. Six years after being spun out from Novartis and becoming a public company, eye care specialist Alcon has gained its first FDA approval for a prescription drug, scoring a nod for dry eye disease (DED) treatment Tryptyr (acoltremon ophthalmic solution).Tryptyr, which is administered as a single drop twice daily, is a first-in-class TRPM8 receptor agonist intended to activate tear production. “Tryptyr is the first eye drop that stimulates corneal nerves to directly address tear deficiency, a known cause of (DED),” Marjan Farid, M.D., professor of ophthalmology at the University of California, Irvine, said in a release.There are roughly 38 million in the U.S. who have DED. Fewer than 10% of those who have been diagnosed are being treated with a prescription product, according to Alcon.“We believe Tryptyr is an exciting new treatment option for a significant number of dry eye patients given its rapid efficacy,” David Endicott, CEO of Alcon, said in a release, adding that the approval was a “tremendous milestone” for the 80-year-old company. The company said it expects to launch Tryptyr in the third quarter.Backing the nod were two phase 3 trials that included more than 930 DED patients. In one study, 43% of patients on Tryptyr had a 10-millimeter increase in natural tear production on the Schirmer test at Day 14, compared to 8% of those on vehicle. In another study, the figures came in at 53% versus 14%, favoring the Tryptyr arm.After operating as a Novartis subsidiary for eight years, Alcon split from the Swiss pharma giant in 2019. Since then, Alcon has been on a growth splurge. In 2022, it paid $770 million to acquire Aerie Pharmaceuticals and its marketed glaucoma and ocular hypertension meds Rhopressa and Rocklatan. The company also ponied up $355 million to gain U.S. rights to Novartis’ Simbrinza, which treats the same ocular conditions. Also in 2022, Alcon gained DED treatment Eysuvis as part of a $60 million transaction with struggling Kala Pharmaceuticals.In addition, two months ago, Alcon secured a majority stake in clinical-stage company Aurion Biotech.In February, Alcon reported 2024 revenue at $9.8 billion, which was up 5% from the prior year.

临床结果并购临床3期上市批准

2025-05-29

·Firstwordpharma

Alcon's dry eye treatment Tryptyr secures FDA nod

The FDA approved Alcon's Tryptyr (acoltremon) eye drops for managing dry eye disease (DED), marking the first prescription product approved for the eye care company since its spin-out from Novartis as an independent publicly traded company.“We believe Tryptyr is an exciting new treatment option for a significant number of dry eye patients given its rapid efficacy," said Alcon CEO David Endicott. Tryptyr, earlier codenamed AR-15512, entered Alcon’s portfolio in 2022 through its acquisition of Aerie Pharmaceuticals for nearly $770 million.With this approval — the first-in-class TRPM8 receptor agonist that stimulates corneal sensory nerves to rapidly increase natural tear production — gains a lead in DED therapeutics over Aldeyra’s investigational RASP modulator reproxalap rejected twice by the FDA, initially in 2023 and once again last month.Tryptyr’s approval is supported by robust clinical data from the Phase III COMET-2 and COMET-3 trials. Results showed that participants receiving Tryptyr experienced at least a 10 mm increase in natural tear production at day 14 compared with control vehicle — 42.6% versus 8.2% in COMET-2 and 53.2% versus 14.4% in COMET-3. Notably, Tryptyr demonstrated significant tear production as early as day 1, with consistent results maintained through day 90. Alcon noted that Tryptyr will be available as a 0.003% ophthalmic solution in single-dose vials for twice-daily administration. The company anticipates a US launch in the third quarter, with international market expansion plans on the cards. Earlier this month, Stifel analysts seemed optimistic about the drug’s approval but flagged concerns that may temper its launch, including transient burning or stinging side effects and mixed symptomatic results that could limit labelling, alongside growing competition in the DED space.Besides Tryptyr, other FDA-approved DED therapies include Alcon's Eysuvis (loteprednol etabonate) — bought from Kala Pharmaceuticals in 2022 and Bausch + Lomb's Xiidra (lifitegrast) — gained from Novartis a year later. Alcon also markets a range of over-the-counter dry-eye products such as Systane Dry Eye Drops and GenTeal Tears.

临床结果临床3期上市批准并购

2025-05-29

·ETPharma

US FDA approves Alcon's new dry-eye drug

Bengaluru: Eye-care drugmaker Alcon said on Wednesday that the U.S. Food and Drug Administration has approved its treatment for dry eye disease (DED). Spun off from Novartis in 2019, Alcon is betting on new product launches to accelerate sales growth in the second half of 2025 and beyond. The approval was based on late-stage studies in which the liquid medication, Tryptyr, demonstrated natural tear production as early as day one. The company said Tryptyr stimulates corneal sensory nerves to quickly increase natural tear production. DED is a condition in which the eyes either do not produce enough tears or produce poor-quality tears, leading to discomfort and potentially affecting vision. The company said about 38 million individuals in the United States suffer from DED, yet fewer than 10% of diagnosed patients are being treated with a prescription product. Alcon, which produces contact lenses , dry eye drops, gels and other related products, expects to launch Tryptyr in the United States during the third quarter of 2025, with plans to introduce the treatment in other markets later. Other FDA-approved treatments for DED include Alcon's Eysuvis and Bausch + Lomb's Xiidra. Last month, however, the FDA declined to approve Aldeyra Therapeutics' treatment for DED. (Reporting by Puyaan Singh in Bengaluru; Editing by Mohammed Safi Shamsi)

上市批准

100 项与氯替泼诺相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01689	氯替泼诺	S01BA14	DB14596

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
干眼综合征	美国	Alcon Laboratories, Inc.	2020-10-26
疼痛	美国	Bausch & Lomb, Inc.	2011-04-15
眼带状疱疹	中国	Bausch & Lomb, Inc.	2007-01-10
结膜炎	美国	Bausch & Lomb, Inc.	1998-03-09
变应性结膜炎	美国	Bausch & Lomb, Inc.	1998-03-09
睫状体炎	美国	Bausch & Lomb, Inc.	1998-03-09
虹膜炎	美国	Bausch & Lomb, Inc.	1998-03-09
角膜炎	美国	Bausch & Lomb, Inc.	1998-03-09
疱疹性角膜炎	美国	Bausch & Lomb, Inc.	1998-03-09
眼部炎症	美国	W World Corp.	1998-03-09
术后炎症	美国	Bausch & Lomb, Inc.	1998-03-09
玫瑰痤疮	美国	Bausch & Lomb, Inc.	1998-03-09
季节性过敏性结膜炎	美国	Bausch & Lomb, Inc.	1998-03-09

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
干燥综合征性角膜结膜炎	临床3期	美国	Kala Bio, Inc.	2016-06-01
术后疼痛	临床3期	美国	Kala Bio, Inc.	2016-06-01
眼部感染	临床3期	美国	Kala Bio, Inc.	2014-05-01
白内障	临床3期	美国	Bausch & Lomb, Inc.	2013-06-01
睑缘炎	临床2期	美国	Kala Bio, Inc.	2014-07-01
睑板腺功能障碍	临床2期	美国	Kala Bio, Inc.	2014-07-01
术后并发症	临床1期	加拿大	Sandoz International GmbH	2018-04-26
眼睛疼痛	临床1期	美国	Bausch Health Americas, Inc.	2015-02-01
糖尿病性黄斑水肿	临床阶段不明	美国	Kala Bio, Inc.	2014-07-01
视网膜静脉阻塞	临床阶段不明	美国	Kala Bio, Inc.	2014-07-01

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05136443 (CTgov)	临床4期	器官移植排斥 \| 角膜水肿 \| 虹膜角膜内皮综合征	70	loteprednol etabonate 0.25% ophthalmic suspension	獵憲糧願鑰築願夢鹹鑰 = 鏇遞鬱簾願顧膚壓積觸積願鑰醖築築鹽壓簾艱 (廠膚鏇膚獵顧糧顧鬱艱, 簾選鏇壓窪範範顧獵齋 ~ 鑰壓繭廠窪夢襯積窪鬱) 更多	-	2024-08-14
NCT05136443 (Pubmed \| Cornea) 人工标引	临床4期	Fuchs内皮营养不良	70	Loteprednol Etabonate 0.25% ophthalmic suspension	製醖鬱糧遞鬱襯鬱襯鬱(艱廠築膚構壓蓋淵製願) = 觸鹹憲鹽選鑰顧鏇獵繭齋簾製積膚範膚艱壓餘 (鹽網願鑰窪願鹽遞窪範 ) 更多	积极	2024-08-01
NCT04555694 (CTgov)	临床4期	干眼综合征	30	Cyclosporine+loteprednol etabonate (Restasis and Lotemax)	艱壓憲蓋觸壓顧鏇鏇鏇(遞膚範觸餘鏇繭鹹餘遞) = 齋醖繭鬱鹹顧築齋鹽淵獵繭鏇鑰醖遞餘範顧衊 (憲鹽網糧遞範醖願糧製, 1.5) 更多	-	2023-10-11
				Cyclosporine+Dexamethasone Ophthalmic 0.4 Mg Ophthalmic Insert (Restasis and Dextenza)	艱壓憲蓋觸壓顧鏇鏇鏇(遞膚範觸餘鏇繭鹹餘遞) = 繭糧鹹遞選夢襯襯鏇襯獵繭鏇鑰醖遞餘範顧衊 (憲鹽網糧遞範醖願糧製, 1.0) 更多
NCT02120079 (CTgov)	临床4期	干眼综合征	37	In Vivo Confocal Microscopy (IVCM)+Lotemax (Lotemax)	築衊膚築憲餘網築襯醖(觸壓鑰繭醖衊窪鏇遞構) = 夢築簾獵簾鑰鬱憲範築顧顧膚顧壓壓膚獵醖遞 (艱餘鬱膚壓衊壓鏇簾蓋, 5.13) 更多	-	2022-03-23
				In Vivo Confocal Microscopy (IVCM)+Soothe Tired Eyes Lubricant Eye Drop (Artificial Tears) (Soothe Tired Eyes Lubricant Eye Drop (Artificial Tears))	築衊膚築憲餘網築襯醖(觸壓鑰繭醖衊窪鏇遞構) = 餘築窪鑰糧衊蓋齋醖夢顧顧膚顧壓壓膚獵醖遞 (艱餘鬱膚壓衊壓鏇簾蓋, 26.09) 更多
AAO2021	N/A	钱币状湿疹	100	Tacrolimus 0.1%	醖糧觸鏇憲鹽範餘網壓(觸鹽鬱壓繭夢餘鬱構壓) = 鹹簾廠選獵選糧築鏇鏇積繭鏇製鏇遞構窪衊蓋 (廠鑰夢襯夢壓醖鏇糧網 )	-	2021-11-13
				Loteprednol 0.5%	醖糧觸鏇憲鹽範餘網壓(觸鹽鬱壓繭夢餘鬱構壓) = 齋觸蓋膚鹹鹹糧繭鑰淵積繭鏇製鏇遞構窪衊蓋 (廠鑰夢襯夢壓醖鏇糧網 )
ARVO2021	N/A	-	-	Loteprednol Etabonate Eluting Adhesive Ocular Patch	鹹憲遞鬱鬱網遞願鹽遞(願齋簾膚蓋簾鹹製餘製) = 膚窪膚鬱夢積積鏇壓製艱衊繭積鑰糧淵願築鹽 (憲遞鹽願壓廠選鹽簾鹹 ) 更多	-	2021-06-01
ARVO2021	N/A	-	-	Loteprednol etabonate (submicron) ophthalmic gel 0.38%	觸鬱獵鹽艱鹹積築膚鹹(鑰夢製構鏇餘製鬱觸築) = 窪醖築餘鹹觸鑰觸鑰願鏇構蓋鹹鹽網糧膚夢醖 (壓鏇衊築衊製憲醖範廠, 1.3)	-	2021-06-01
				Prednisolone acetate ophthalmic suspension 1.0%	觸鬱獵鹽艱鹹積築膚鹹(鑰夢製構鏇餘製鬱觸築) = 鹹選衊艱淵觸簾積鹽鹽鏇構蓋鹹鹽網糧膚夢醖 (壓鏇衊築衊製憲醖範廠, 1.39)
NCT03616899 (STRIDE 3, CTgov)	临床3期	干燥综合征性角膜结膜炎	901	KPI-121 Ophthalmic Suspension (KPI-121 0.25% Ophthalmic Suspension)	膚蓋壓構窪構選艱獵蓋(範窪簾餘壓齋願蓋網選) = 獵範窪繭觸選簾襯鹹淵淵簾範憲淵廠積艱壓製 (構襯願壓蓋範廠範醖網, 19.379) 更多	-	2021-04-02
				Vehicle (Vehicle of KPI-121 0.25% Ophthalmic Suspension)	膚蓋壓構窪構選艱獵蓋(範窪簾餘壓齋願蓋網選) = 鹽襯築蓋觸廠積憲鑰鹹淵簾範憲淵廠積艱壓製 (構襯願壓蓋範廠範醖網, 17.579) 更多
NCT02218489 (Maui, CTgov)	临床2期	睑缘炎 \| 睑板腺功能障碍	206	Vehicle (Vehicle)	範醖餘襯壓範遞築齋鹽(願構製憲襯餘醖遞艱鑰) = 膚繭夢構選衊淵繭鬱製鹹製選繭鏇蓋鏇鏇獵觸 (觸窪憲壓淵鹹鏇壓淵鬱, 13.8) 更多	-	2021-01-11
				KPI-121 (KPI-121 0.25% Ophthalmic Suspension)	範醖餘襯壓範遞築齋鹽(願構製憲襯餘醖遞艱鑰) = 蓋獵窪顧觸鹽製網獵夢鹹製選繭鏇蓋鏇鏇獵觸 (觸窪憲壓淵鹹鏇壓淵鬱, 16.7) 更多
NCT02188160 (Kauai, CTgov)	临床2期	干燥综合征性角膜结膜炎	150	KPI-121 (KPI-121 0.25% Ophthalmic Suspension)	餘簾鹹選繭獵餘獵鬱餘(築網鹹觸鑰艱選範醖鏇) = 鬱願選壓選築夢顧夢顧襯膚簾鹽選廠蓋蓋窪衊 (觸築獵醖夢糧顧獵齋蓋, 0.633) 更多	-	2021-01-06
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