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.

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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项与氯替泼诺相关的文献（医药）

2026-03-01·CORNEA

Delayed Onset Infectious Crystalline Keratopathy After Corneal Cross-linking

Article

作者: Aldave, Anthony J ; Chen, Angela C ; Deng, Sophie X

Purpose::

To report a case of delayed onset infectious crystalline keratopathy after corneal cross-linking (CXL).

Methods::

Slit-lamp examination, confocal microscopy, anterior segment optical coherence tomography imaging, and corneal culture were performed to characterize the corneal opacification.

Results::

A 49-year-old man presented with progressively worsening vision in the left eye 8 months after uncomplicated epithelium-off CXL for keratoconus. Examination demonstrated focal central corneal stromal thinning with surrounding stromal opacification. Confocal microscopy did not demonstrate evidence of parasitic or fungal infection. Two months later, gray-white crystalline stromal opacities were observed surrounding the area of central stromal thinning, consistent with infectious crystalline keratopathy. Corneal scrapings of the left eye were obtained, which were positive for Enterococcus faecalis. After cessation of topical loteprednol and initiation of topical vancomycin and linezolid, the stromal infiltrate increased in size and a hypopyon developed but had resolved before the discontinuation of 7 weeks of topical antibiotic therapy. A deep anterior lamellar keratoplasty was performed 6 weeks later, with no recurrence of infection 10 months after surgery.

Conclusions::

Infectious crystalline keratopathy can present more than 6 months after CXL. Progressive corneal stromal thinning associated with stromal opacification should raise suspicion of this rare late onset complication of CXL and prompt corneal scraping for stains and cultures to rule out an indolent infectious process.

2026-01-01·NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Which topical ophthalmic drugs work best for Keratoconjunctivitis Sicca? A systematic review and meta-analysis

Review

作者: Chen, Kai-Yang ; Chan, Chi-Ming ; Chan, Hoi-Chun

BACKGROUND:

Dry Eye Disease (DED) is a chronic and multifactorial condition that significantly impacts patient quality of life. Topical ophthalmic drugs (TODs) have emerged as key treatments for DED, offering the potential to address the underlying pathology rather than merely alleviating symptoms. This review aims to assess the efficacy of various TODs in managing the symptoms of DED.

METHODS:

A comprehensive search was conducted across three electronic databases to identify relevant articles for inclusion in this review. Two independent authors screened the articles according to predefined eligibility criteria. A total of 16 randomized controlled trials (RCTs) were included, summarizing data from 2,680 patients. The data were analyzed using Review Manager 5.4, with pooled analysis conducted on key symptoms including corneal fluorescein staining (CFS), Ocular Surface Disease Index (OSDI), tear break-up time (TBUT), and Schirmer test scores.

RESULTS:

From 632 articles identified, 16 RCTs were selected for inclusion. The pooled analysis revealed that cyclosporine therapy resulted in a significant improvement in CFS scores (mean difference (MD) -0.24; 95% confidence interval (CI) (-0.42, -0.07), P = 0.006). However, no significant improvements were observed in OSDI, TBUT, or Schirmer test scores (MD -0.35; 95% CI (-5.66, 4.96), P = 0.9; MD 0.12; 95% CI (-0.65, 0.89), P = 0.76; MD -0.22; 95% CI (-0.46, 0.02), P = 0.07, respectively). Similar results were found for loteprednol etabonate (LE) and diquafosol sodium, with no significant changes in OSDI, CFS, or Schirmer test scores. For diquafosol, no significant improvements were observed in any of the DED symptoms, including OSDI (MD -3.82; 95% CI (-8.31, 0.67), P = 0.10), CFS (MD -0.31; 95% CI (-0.82, 0.20), P = 0.23), TBUT (MD -0.20; 95% CI (-1.37, 0.98), P = 0.74), and Schirmer test (MD -1.00; 95% CI (-2.60, 0.60), P = 0.22).

CONCLUSION:

The study concluded that cyclosporine therapy offers improvements in corneal fluorescein staining but does not significantly affect other common DED symptoms, such as OSDI, TBUT, and Schirmer test scores. Similarly, no significant improvements in DED symptoms were observed with loteprednol etabonate or diquafosol sodium. Further research is needed to explore the efficacy of these treatments in managing DED symptoms more comprehensively.

2026-01-01·ARQUIVOS BRASILEIROS DE OFTALMOLOGIA

Different formulations of corticosteroid eye drops at different treatment times in the control of inflammation and prevention of cystoid macular edema after cataract surgery: randomized clinical trial

Article

作者: Albano, Maria Clara de Freitas ; Ribeiro, João Crispim Moraes Lima ; Feitosa, Adriane Macêdo ; Rodriguez, Pedro Javier Yugar ; Miranda, José Eduardo de Oliveira ; Lopes, Sofia Pereira ; Feitosa, Mateus Macêdo ; Oliveira, Thiago Carvalho Barros de ; Machado, André Jucá

PURPOSE:

To evaluate the efficacy of different corticosteroid eye drop formulations (prednisolone acetate 1.0%, dexamethasone 1.0%, and loteprednol etabonate 0.5%) administered for different treatment durations (10 vs. 28 days) in controlling postoperative inflammation following uncomplicated cataract surgery.

METHODS:

This randomized, masked clinical trial was conducted at the Instituto Cearense de Oftalmologia. Eligible participants were aged ≥50 yr and scheduled for routine cataract surgery. Exclusion criteria included preexisting ocular disease (elevated intraocular pressure, retinopathy, maculopathy, or uveitis) or concurrent medication use that could confound results. Patients were randomized to receive prednisolone acetate (1.0%), dexamethasone (1.0%), or loteprednol etabonate (0.5%) four times daily for 28 days (with tapering) or for 10 days. Medication bottles, prescriptions, and examiners were masked. Postoperative assessments included ocular symptoms, visual acuity, intraocular pressure, anterior chamber cell count and flare, pachymetry, endothelial cell density, and macular thickness over a 30-day follow-up.

RESULTS:

A total of 140 eyes from 140 patients were analyzed (29 prednisolone acetate 1.0%, 18 dexamethasone 1.0%, and 21 loteprednol etabonate 0.5% for 28 days; 28 prednisolone acetate 1.0%, 22 dexamethasone 1.0%, and 22 loteprednol etabonate 0.5% for 10 days). No significant differences were found among the six groups during follow-up. However, eyes treated with dexamethasone (1.0%) showed greater intraocular pressure fluctuations, particularly on Days 7 and 30, and a higher incidence of rebound inflammation in the 28-day regimen. Structural cystoid macular edema without visual impact was observed in 5.9% of eyes in the 28-day groups and 14.2% of eyes in the 10-day groups, as detected by optical coherence tomography at 30 days.

CONCLUSION:

Equivalent postoperative inflammation control can be achieved using different corticosteroid eye drop formulations at varying treatment durations following cataract surgery. Brazilian Registry of Clinical Trials (ReBEC): RBR-2frpntv.

项与氯替泼诺相关的新闻（医药）

2026-03-17

·allsci.com

Aldeyra Therapeutics receives CRL for reproxalap citing lack of efficacy in dry eye disease

Aldeyra Therapeutics, Inc. (Nasdaq: ALDX) disclosed that the US FDA issued a Complete Response Letter for the New Drug Application for reproxalap, an investigational reactive aldehyde species trap, for the treatment of signs and symptoms of dry eye disease. The CRL indicates the FDA determined the application does not currently meet the requirements for approval, citing a lack of substantial evidence of efficacy from the submitted clinical program. The FDA stated that the application “failed to demonstrate efficacy in adequate and well controlled studies in the treatment of signs and symptoms of dry eye disease.” The agency noted that inconsistency across study results “raises serious concerns about the reliability and meaningfulness of the positive findings” and that the “totality of evidence from the completed clinical trials does not support the effectiveness of the product.” No safety or manufacturing deficiencies were identified. The FDA recommended that Aldeyra explore reasons for trial failures and identify populations or conditions in which reproxalap may demonstrate efficacy. The agency did not recommend conducting additional clinical trials or request submission of additional confirmatory evidence. Reproxalap is a small molecule that functions by covalently binding and sequestering toxic reactive aldehyde species, such as malondialdehyde and 4-hydroxynonenal, which are elevated in inflammatory conditions. This mechanism differs from existing dry eye treatments, which include calcineurin inhibitors such as cyclosporine, corticosteroids such as loteprednol etabonate, and nicotinic acetylcholine receptor agonists such as varenicline nasal spray. The dry eye disease treatment landscape includes several approved therapies — Miebo (perfluorohexyloctane), Tyrvaya (varenicline), Eysuvis (loteprednol etabonate), and Cequa (cyclosporine) — though the company has described reproxalap as, to its knowledge, the only drug with clinical activity within minutes of administration in this patient population. Reproxalap originated from academic research into aldehyde-mediated inflammation and oxidative stress. Aldeyra Therapeutics was founded to translate this science into therapeutic applications and has retained full ownership and development rights throughout the program’s history. No licensing, partnership, or asset transfer arrangements have been publicly disclosed for reproxalap. The company has funded development through public equity offerings and internal resources. During the NDA review period, the FDA provided label drafts in December 2025 and again in March 2026. Aldeyra stated it does not believe label negotiations were completed prior to issuance of the CRL. The provided source material does not reference prior CRLs for reproxalap, prior advisory committee meetings, or approvals in other regulatory jurisdictions. This appears to be the first CRL issued for this NDA. Aldeyra stated it intends to request a Type A meeting with the FDA to understand the actions needed for NDA approval. Per Prescription Drug User Fee Act goals, the target date for a Type A meeting is within 30 days of receipt of the meeting request. The company stated it does not currently expect to pursue additional clinical trials. Todd C. Brady, M.D., Ph.D., President and Chief Executive Officer, said the company would “work with urgency to support the FDA in enabling market access.” As of December 31, 2025, Aldeyra reported cash, cash equivalents, and marketable securities of $70 million, which the company expects to support operations into 2028. Your email address will not be published. Required fields are marked * Comment * Name * Email * Website

申请上市

2026-03-15

·药事纵横

干眼症百亿赛道或再添猛将，后来者如何精准落子？

FDA预计将于2026年3月就Reproxalap的批准上市做出决定，这意味着百亿级的干眼症治疗市场或将迎来又一重磅药物。当前，该领域的研发正驶入快车道。面对巨大的市场风口，对于希望入局的药企而言，机遇与挑战并存：关键在于如何根据自身优势，精准选择布局赛道。一、近年来上市的干眼症治疗药物概览按照泪液主要成分或功能异常，一般将干眼症分为水液缺乏型、脂质异常型、黏蛋白缺乏型、泪液动力学异常型和混合型干眼症。长期以来，人工泪液为干眼症基础治疗手段。近年来，新型药物加速研发，并对应于干眼症不同类型，为干眼症尤其是中重度干眼症提供更多选择。以下将对Reproxalap和近年来上市的干眼症治疗药物进行系统梳理，并从立项可行性角度，分析国内企业布局该领域所面临的机遇与挑战。1、Reproxalap滴眼液 Reproxalap是活性醛类物质（RASP）抑制剂，能够结合并捕获游离醛，主要作用机制为抗炎。Reproxalap滴眼液采用了从Ligand公司获得许可的Captisol技术，Captisol是受专利保护的化学修饰的环糊精，可优化药物的溶解度和稳定性。该品种存在专利限制。2、环孢素眼用制剂环孢素眼用制剂作用机制为抗炎，环孢素滴眼液治疗干眼症在国外已实践多年，包括滴眼液、眼用乳剂剂型：然而，上述产品均未进入国内市场，2020年6月，兴齐仿制的环孢素滴眼液按化药3类获批上市，这是中国首款用于治疗干眼症的环孢素眼用制剂，占据显著的先发优势和市场独占性。目前国内企业申报环孢素类制剂用于干眼症较少，主要原因可能是环孢素制备需通过纳米乳剂、微球或水性载体技术实现有效渗透，具有一定技术壁垒。3、立他司特滴眼液（Xiidra®）立他司特是一种淋巴细胞功能关联抗原-1（LFA-1）拮抗剂，作用机制为抗炎，2016年在美国获批上市，是继环孢素后第二个获批的干眼症抗炎药。目前，我国已有2家企业的立他司特滴眼液仿制药获批上市（化药3类）。仿制立他司特滴眼液需开展临床，近两年已有多家企业递交临床申请，属于较为热门品种。4、酒石酸伐尼克兰鼻喷雾剂（Tyrvaya®/星特润®） Oyster Point Pharm的酒石酸伐尼克兰鼻喷雾剂2021年在美国获批上市，2024年在国内获批上市。酒石酸伐尼克兰鼻喷雾剂是干眼症治疗领域目前全球唯一的鼻喷雾剂型，可直接促进眼表天然泪液分泌，此外，该药物还有修复泪腺功能、抗炎的作用，是中重度干眼患者的治疗优选。美国Paragraph IV声明列表中显示最后一个专利（治疗方法专利）到期日为2035年，但本品在国内并无化合物和制剂专利风险。2025年底，国内已有1家企业按化药4类（仿制）提交上市申请，未见开展BE研究。就原料可获得性而言，酒石酸伐尼克兰为成熟化合物，片剂上市多年，目前国内已有11家企业在CDE完成原料药备案。根据说明书，该药品包装为琥珀色I型玻璃瓶，非特殊包材。5、氯替泼诺混悬滴眼液（Eysuvis®）氯替泼诺是一种强效抗炎皮质类固醇，2020年获美国FDA批准上市。其适应症为短期（不超过两周）控制干眼症的体征和症状，同时也是美国首个获批用于干眼症的皮质类固醇药物。Eysuvis®采用了Kalad公司的AMPPLIFY®药物递送技术。该技术通过使用带有专有涂层的活性药物纳米颗粒，使药物能够有效穿透眼部黏液屏障。此品种存在技术壁垒。Eysuvis®目前未在国内上市。6、全氟己基辛烷滴眼液（Miebo®） Miebo®是基于无水药物递送技术平台EyeSol研发的药物，仅由单一组分全氟己基辛烷（F6H8）组成。全氟己基辛烷滴眼液于2014年在欧盟上市，按医疗器械管理，风险等级为IIb；2023年在美国获批上市，按药品管理，商品名为Miebo®；2019年，恒瑞医药从Novaliq公司引进全氟己基辛烷滴眼液，并拥有该产品在中国的独家权利，2025年，全氟己基辛烷滴眼液在国内上市，商品名为恒沁®。全氟己基辛烷滴眼液适用于蒸发型干眼症，尤其是（MGD）相关干眼症。MGD相关干眼症在干眼症中占比较高，一项荟萃分析结果显示，MGD合并干眼症患病率为21.2%[1]。全氟己基辛烷滴眼液是全球唯一获批治疗MGD相关干眼症的药物，独占市场。该品种存在专利限制，组合物专利在2033年届满。7、地夸磷索钠滴眼液（Diquas®/丽爱思®）地夸磷索钠滴眼液为眼部促分泌剂，可刺激结膜上皮细胞和杯状细胞分泌水分和黏蛋白，从而改善泪膜的稳定性，并促进角膜上皮修复。参天製薬的Diquas®早在2010年就在日本上市，用法用量为每日6次，每次1滴。Diquas®于2017年在国内上市，商品名为丽爱思®。本品可免临床免BE直接申报上市，但目前国内已有50多家企业仿制，国内仿制赛道已十分拥挤。已有多家地夸磷索钠原料在CDE备案，原料易获得。 2022年，参天製薬升级的地夸磷索钠滴眼液DIQUAS® LX在日本获批上市，DIQUAS® LX新添加PVP（聚乙烯吡咯烷酮，又称聚维酮）作为增稠剂，由此减少用药频次至每日3次，每次1滴。DIQUAS® LX未在国内申报上市。DIQUAS® LX组合物专利2040年到期，仿制跟随该品种存在专利限制。8、瑞巴派特滴眼液（Mucosta®）瑞巴派特是强效的抗氧化剂与自由基清除剂，通过增强泪液分泌并提高覆盖结膜与角膜表面的黏液素的水平而发挥治疗干眼的作用。瑞巴派特滴眼液Mucosta®由大塚製薬研发，2012年在日本获批上市，为单剂量（0.35mL/支）。参天製薬的瑞巴派特滴眼液2023年于日本获批上市，以硝酸银替代防腐剂，以满足多剂量包装（5mL/瓶）的要求。目前国内无瑞巴派特滴眼液上市。瑞巴派特最初是一种口服胃黏膜保护剂，口服制剂在国内外拥有较长应用历史，原料可获得性高。9、Acoltremon（Tryptyr®） Acoltremon是全球首个TRPM8受体激动剂，作为神经调节剂，可刺激角膜感觉神经，启动自然泪液产生。2025年，Tryptyr®在美国获批上市，国内未申报。目前该品种的组合物专利的中国同族在审中，若专利授权，该组合物专利将在2042年届满。10、SkQ1滴眼液（Vizomitin®） Mitotech公司的SkQ1滴眼液是一种线粒体靶向抗氧化剂，早在2012年于俄罗斯上市，商品名为Vizomitin®。SkQ1通过刺激内源性抗氧化活性及增强角膜谷胱甘肽过氧化物酶和谷胱甘肽还原酶的活性，实现对氧化应激的抑制作用。此外，SkQ1增强抗氧化活性和泪膜稳定性，并产生抗炎效果。2018年，亿胜生物与Mitotech公司签订共同开发SkQ1滴眼液的协议，2019年亿胜生物宣布已在Ⅲ期临床第一阶段试验（VISTA-1）中取得顶线结果。目前，SkQ1滴眼液尚未在中国、美国上市。二、干眼症立项启示和策略综合分析来看，虽然值得仿制跟进的品种较为有限，但不同企业仍可结合自身优势，制定差异化的布局策略。1、精细化市场细分中重症市场：轻症市场由玻璃酸钠主导，市场地位稳固，若无颠覆性剂型优势，不建议新入局者强行切入。中重症市场则存在巨大真空，据估计，40岁以上人群中约有10%-20%正受中重度症状困扰[2]。 MGD相关干眼症：MGD相关干眼症是蒸发性干眼病的主要成因，但目前仅有全氟己基辛烷滴眼液上市，存在广阔的蓝海空间。2、瞄准专利空隙部分在国外已上市多年的成熟品种，因原研企业全球战略调整未进入中国市场，其专利已过期或即将过期。这类品种临床价值明确，安全性数据充分，按3类化药开发可大幅降低研发风险。此外，上述大部分受专利限制的品种，其专利主要集中于组合物方面，具备通过技术研究实现规避的可行性。3、凭技术优势攻高端品种环孢素纳米乳剂、阳离子乳剂等高端制剂技术壁垒高，难以仿制。谁能做出更高生物利用度、更低刺激性的剂型，谁就能在这一市场中撕开裂缝。例如，利用创新辅料解决疏水性药物的眼表渗透问题，提升患者长期用药的依从性。4、聚焦复方制剂（1）关注眼部疾病并发症：干眼症常与老花眼等眼部疾病并发。开发具有协同作用的复方制剂，能精准切分这部分顽固患者市场，提升临床处方便捷性。例如一项纵向研究显示，老花眼和干眼症之间存在很强的相关性，老花眼患者罹患干眼症的风险是非老花眼人群的1.8倍。临床就诊5年后，老花眼患者干眼症确诊率为8.8%，非老花眼人群为4.8%；10年后，两组干眼症确诊率分别为15.4%和10.3%[3]。（2）干眼治疗药物复方协同：将两种干眼治疗药物制成复方制剂，可产生协同增效。例如参天製薬公开的专利JP2015160826A中，提出通过将地夸磷索与瑞巴派特制备成复方，从而协同促进泪液分泌。根据该专利，使用白兔开展的药效学实验结果表明，地夸磷索钠与瑞巴派特联合使用，在促进泪液分泌方面产生了显著的协同效应，其效果远超两者单用效果之和。 5、多靶点分子破解干眼困局干眼发病机制复杂，单一靶点往往效果有限，可优先考虑具有多靶点、多重作用的分子。欧康维视自主研发的OT202是一款双靶点创新药物，作为脾酪氨酸激酶（Syk）/血管内皮生长因子受体2（VEGFR-2）双重抑制剂，它通过协同阻断Syk介导的上游炎症信号与VEGFR-2相关的下游血管生成及炎症放大，从源头打断干眼炎症循环。其II期临床研究证实，该双靶点药物治疗中重度干眼症疗效显著[4]。立他司特是一种淋巴细胞功能关联抗原-1（LFA-1）拮抗剂，在干眼症患者中，角膜和结膜组织中的细胞间粘附分子1（ICAM-1）可能存在过表达，立他司特的作用机制在于抑制LFA-1与ICAM-1结合，进而降低T淋巴细胞介导的炎症水平，从而有效缓解干眼症状并减轻眼部损伤。Reproxalap是一种新型小分子活性醛类（RASP）抑制剂，可共价结合游离醛并降低过量的RASP水平，从而起到抗炎作用。翊石医药公开的专利WO2025223511A1通过将立他司特与ADX-102（即Reproxalap）拼合，拼合后的化合物具有优异的活性醛类清除能力和抑制LFA-1与ICAM-1结合的能力。 6、剂型创新打开新局酒石酸伐尼克兰鼻喷雾剂的成功商业化揭示了行业破局新路径：面对眼药水市场同质化竞争，创新给药方式往往能开辟全新蓝海。传统滴眼液存在诸多痛点，如药液常随泪液流失，老人儿童操作不便，长期使用的防腐剂更会损伤眼表。而鼻喷雾剂则巧妙绕开眼表障碍，通过鼻腔给药直达病灶，为睑板腺功能障碍、眼表严重损伤等无法耐受传统滴眼液的患者带来全新治疗体验。这一突破证明，眼用凝胶、缓释植入剂、接触镜载药等新型给药方式的探索，正是破解眼科用药困境的重要方向。参考文献： [1] McCann P,Abraham AG, Mukhopadhyay A, et al. Prevalence and Incidence of Dry Eye and Meibomian Gland Dysfunction in the United States: A Systematic Review and Meta-analysis.JAMA Ophthalmol.2022;140(12):1181–1192. doi:10.1001/jamaophthalmol.2022.4394 [2] Britten-Jones AC, Wang MTM, Samuels I, Jennings C, Stapleton F, Craig JP. Epidemiology and Risk Factors of Dry Eye Disease: Considerations for Clinical Management.Medicina (Kaunas). 2024;60(9):1458. Published 2024 Sep 5. doi:10.3390/medicina60091458 [3] Mai ELC, Lin CC, Lian I, Liao R, Chen M, Chang C. Population-based study on the epidemiology of dry eye disease and its association with presbyopia and other risk factors.Int Ophthalmol. 2019;39(12):2731-2739. doi:10.1007/s10792-019-01117-5 [4] Wang H, Jin X, Zheng H, et al. Efficacy and Safety of Spleen Tyrosine Kinase and VEGFR-2 Dual-Target Kinase Inhibitor (OT202) in Dry Eye: A Randomized, Vehicle-Controlled Phase 2 Trial.Ophthalmology. Published online November 3, 2025. doi:10.1016/j.ophtha.2025.10.023 立即扫码加入药事纵横交流群

专利到期上市批准

2026-01-21

·世易眼科汇

2025-2026年眼科药物及给药系统的新进展

眼科药物及给药系统亟需持续创新。世界卫生组织估计，全球至少有22亿人存在不同程度的视力损害，其中至少10亿例视力损害本可预防或尚未得到有效干预，给社会带来沉重的经济负担。青光眼、年龄相关性黄斑变性（AMD）和糖尿病视网膜病变等慢性眼病可导致严重视力损害。其他眼部疾病，如眼表疾病（包括干眼症、睑缘炎、睑板腺功能障碍、神经营养性角膜病变等），同样会对患者视力及生活质量产生不利影响。眼球解剖结构极其复杂，存在多重生理屏障（如血-视网膜屏障、泪液引流系统），限制药物吸收并降低其在靶组织中的生物利用度。因此，新型眼科给药系统的目标在于在靶部位实现最佳且可持续的药物浓度。眼前节与眼后节在给药方面面临不同挑战。通过缓释给药方式减少给药频率，有望改善患者依从性并最终改善临床结局。传统滴眼液往往导致药物浓度波动，难以达到理想效果。眼前节给药的挑战包括角膜通透性不足、鼻泪管引流以及泪液冲洗；眼后节给药的挑战则包括玻璃体体积大及血-视网膜屏障。眼部独特而复杂的解剖结构形成了显著的生理屏障，从而限制了药物生物利用度（如泪液更新、血-视网膜屏障）。下文将列出2025年获批的新型眼科药物，并重点阐述其对患者的潜在获益。过去一年中，美国食品药品监督管理局（FDA）批准了以下眼科用药：抗炎及干眼治疗药物 Lupin公司的氯替泼诺眼用凝胶0.38%为一种糖皮质激素，用于眼科手术后炎症和疼痛的治疗。据报道，该制剂与博士伦公司的Lotemax SM眼用凝胶具有生物等效性。 Acoltremon眼用溶液0.003%是一种TRPM8受体激动剂，可显著增加早期自然泪液分泌，已获批用于干眼症治疗。该药物通过激活眼表TRPM8冷觉受体发挥作用，机制新颖，类似于伐尼克兰溶液鼻喷剂对泪腺功能单元的刺激，可促使患者泪液分泌持续数小时。Acoltremon眼用溶液0.003%有望用于术前患者，在需要较传统抗炎药物更快起效的情境中具有潜在优势。老视治疗药物醋克利定眼用溶液于2025年7月31日获得FDA批准，用于成人老视治疗。该制剂采用新型选择性缩瞳机制以改善近视力。醋克利定眼用溶液1.44%此前未在美国获批，但在欧洲用于青光眼治疗。该药物为每日一次给药，不含防腐剂，其主要成分醋克利定通过对睫状肌的最小刺激作用于虹膜，从而改善近视力而不引起近视性屈光改变。CLARITY Ⅲ期临床试验数据显示，93%的受试者在30分钟内近视力达到20/40或更好，且疗效可持续长达10小时。抗VEGF药物雷珠单抗注射液100 mg/mL已获批其持续给药系统用于糖尿病视网膜病变（DR）治疗，是目前唯一获得FDA批准、可持续抑制VEGF的给药方式。研究表明，该系统仅需每9个月补充一次药物即可维持DR患者的视力。雷珠单抗最初于2021年获批用于湿性AMD治疗，并于2025年初获批用于糖尿病黄斑水肿。该药物通过一次性门诊手术植入可补充式眼内植入物，持续释放定制配方的雷珠单抗。雷珠单抗为VEGF抑制剂，可结合并抑制VEGF-A，这是一种在新生血管形成及血管通透性增加中起关键作用的蛋白。眼科药物、给药系统及研发项目的创新过程复杂、周期长且成本高昂。基于纳米技术的平台正在不断发展并被深入研究，尽管其在眼科给药中具有提高生物利用度和治疗效果的潜力，但仍存在优势、局限性与挑战。这类纳米给药系统正受到越来越多的关注，仍需进一步研究以推动相关创新。最后，人工智能（AI）及其他数字技术有望加速眼科药物创新与研发。借助机器学习算法及临床与多组学数据，AI可用于预测药代动力学和药效学、识别新的药物靶点，并发现潜在的药物毒性问题。AI辅助的多模态眼部生物标志物及其动态监测，将为未来个体化医疗提供支持。将AI整合入眼科药物创新流程，有望通过提高效率、降低成本来缩短漫长的研发周期。目前，我们仍处于理解AI在眼科药物研发中潜力的初期阶段。在眼科医疗领域，有必要建立更加完善和标准化的AI监管体系，以确保其在患者和社区中的安全、公平应用。 Reference: 1. https://www.optometrytimes.com/view/what-s-new-in-2025-26-ophthalmic-drugs-and-drug-delivery-systems

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
炎症	临床3期	英国	Bausch & Lomb, Inc.	2010-06-07
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

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临床结果

适应症

分期

评价

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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	遞觸顧淵繭蓋壓廠壓築 = 餘襯蓋遞網遞鏇遞構築遞淵糧鏇衊糧鑰築獵艱 (蓋鏇餘襯築鏇鹹膚遞襯, 糧願鹹願糧憲壓鹽窪夢 ~ 築鹹製網繭築獵憲膚鹹) 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	襯積壓鹽窪廠衊壓醖獵(鑰蓋淵獵網築顧膚獵選) = 餘蓋憲簾窪憲鬱選鹹醖鏇醖餘窪鑰憲鹹顧築觸 (網積構廠繭廠襯襯醖範 ) 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)	鹽壓構製選蓋憲衊壓製(鬱鹹鏇觸築膚範選衊鑰) = 簾鹹齋憲壓膚築構築觸淵淵餘壓壓壓廠獵憲餘 (願鏇醖壓憲襯觸鏇製壓, 1.5) 更多	-	2023-10-11
				Cyclosporine+Dexamethasone Ophthalmic 0.4 Mg Ophthalmic Insert (Restasis and Dextenza)	鹽壓構製選蓋憲衊壓製(鬱鹹鏇觸築膚範選衊鑰) = 鑰築糧夢構蓋願選選鹽淵淵餘壓壓壓廠獵憲餘 (願鏇醖壓憲襯觸鏇製壓, 1.0) 更多
NCT02120079 (CTgov)	临床4期	干眼综合征	37	In Vivo Confocal Microscopy (IVCM)+Lotemax (Lotemax)	糧觸艱壓廠遞窪鬱鏇築(網齋獵顧繭齋廠遞淵淵) = 顧願繭齋顧艱製襯膚簾醖壓鏇選願積觸願積範 (繭蓋襯範積膚範鬱繭網, 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))	糧觸艱壓廠遞窪鬱鏇築(網齋獵顧繭齋廠遞淵淵) = 構簾憲製糧憲繭獵膚網醖壓鏇選願積觸願積範 (繭蓋襯範積膚範鬱繭網, 26.09) 更多
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)	觸築積襯網淵顧簾淵築(簾範遞獵膚蓋憲廠鑰繭) = 鹹鬱獵網襯艱餘構鑰願夢網齋窪醖鑰憲觸積窪 (顧鑰壓夢壓願壓艱壓淵, 19.379) 更多	-	2021-04-02
				Vehicle (Vehicle of KPI-121 0.25% Ophthalmic Suspension)	觸築積襯網淵顧簾淵築(簾範遞獵膚蓋憲廠鑰繭) = 蓋鏇繭遞夢衊憲觸築觸夢網齋窪醖鑰憲觸積窪 (顧鑰壓夢壓願壓艱壓淵, 17.579) 更多
NCT02218489 (Maui, CTgov)	临床2期	睑缘炎 \| 睑板腺功能障碍	206	Vehicle (Vehicle)	顧簾選製鏇壓獵鏇願選(顧鬱製積範廠繭襯遞衊) = 廠窪鹽選醖範醖壓製觸夢衊製觸獵蓋網網鏇餘 (蓋齋淵製遞簾範簾遞廠, 13.8) 更多	-	2021-01-11
				KPI-121 (KPI-121 0.25% Ophthalmic Suspension)	顧簾選製鏇壓獵鏇願選(顧鬱製積範廠繭襯遞衊) = 廠齋築繭選餘膚觸選觸夢衊製觸獵蓋網網鏇餘 (蓋齋淵製遞簾範簾遞廠, 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)	獵廠網選蓋夢夢選選蓋(鹹廠願鹽觸鏇齋餘窪積) = 齋簾艱選網觸製憲糧範鏇範艱範窪鹽襯範淵廠 (構願鹽膚壓窪窪膚構繭, 0.633) 更多	-	2021-01-06
				Placebo (Vehicle)	獵廠網選蓋夢夢選選蓋(鹹廠願鹽觸鏇齋餘窪積) = 糧構製製鬱齋襯選遞鹽鏇範艱範窪鹽襯範淵廠 (構願鹽膚壓窪窪膚構繭, 0.626) 更多
NCT02163824 (Hawaii-1, CTgov)	临床3期	眼部感染 \| 炎症	380	KPI-121 0.25% (KPI-121 0.25% QID)	膚糧廠築構選願簾廠選 = 簾鏇製範窪窪網餘遞淵繭鹹選觸窪簾選衊衊選 (蓋選艱鹽鏇範觸顧選餘, 鏇選獵製願糧餘顧壓齋 ~ 壓遞鬱蓋獵範選製衊艱) 更多	-	2020-12-22
				KPI-121 1.0% (KPI-121 1.0% BID)	膚糧廠築構選願簾廠選 = 鏇構鹹艱鑰鹹鹹繭願鏇繭鹹選觸窪簾選衊衊選 (蓋選艱鹽鏇範觸顧選餘, 餘淵鬱廠網艱網艱憲願 ~ 廠鬱艱夢顧製鏇繭鑰夢) 更多
NCT03123614 (CTgov)	临床4期	角膜混浊	131	Loteprednol Etabonate (Loteprednol Etabonate 0.5% Oph Gel)	廠鬱鬱衊積觸製膚鬱窪(築觸蓋網簾鹽繭範鏇鏇) = 鑰壓襯襯築窪襯鏇醖繭簾範窪築簾鏇製蓋構網 (夢構蓋窪鏇齋製壓鏇顧, 2.11) 更多	-	2020-12-21
				Prednisolone Acetate (Prednisolone Acetate 1% Oph Susp)	廠鬱鬱衊積觸製膚鬱窪(築觸蓋網簾鹽繭範鏇鏇) = 憲鹽壓範鏇窪衊築壓鑰簾範窪築簾鏇製蓋構網 (夢構蓋窪鏇齋製壓鏇顧, 2.13) 更多
NCT02245516 (Molokini, CTgov)	N/A	糖尿病性黄斑水肿 \| 视网膜静脉阻塞	16	KPI-121 1.0% Ophthalmic Suspension (KPI-121 1.0% Ophthalmic Suspension)	簾選網鬱壓遞製襯齋淵(廠憲艱醖鏇廠窪淵壓網) = 顧鹹繭鑰廠夢艱襯製夢醖鏇醖襯艱遞餘遞網膚 (糧觸廠範艱構願壓積網, 7.83) 更多	-	2020-12-10
				KPI-121 0.25% Ophthalmic Suspension (KPI-121 0.25% Ophthalmic Suspension)	簾選網鬱壓遞製襯齋淵(廠憲艱醖鏇廠窪淵壓網) = 淵簾範鹽築願夢顧範艱醖鏇醖襯艱遞餘遞網膚 (糧觸廠範艱構願壓積網, 2.00) 更多