The goal of this clinical trial is to compare the efficacy and safety of two different topical corticosteroids in 66 pediatric patients with active anterior chamber granuloma.
The main questions it aims to answer are:
* Does Loteprednol Etabonate 1% provide equivalent inflammation control and granuloma resolution compared to Prednisolone Acetate 1% over a 3-month period?
* Does Loteprednol Etabonate 1% result in a lower frequency of steroid-related intraocular pressure (IOP) elevations than Prednisolone Acetate 1%? Researchers compared a group receiving Loteprednol Etabonate 1% four times daily to a group receiving Prednisolone Acetate 1% six times daily to see if Loteprednol could maintain comparable therapeutic effectiveness while offering a safer intraocular pressure profile.
Participants will Be randomized to receive either Loteprednol Etabonate 1% or Prednisolone Acetate 1% eye drops.
Follow a specific dosing schedule (4 times/day for Loteprednol or 6 times/day for Prednisolone).
Undergo a clinician-guided medication tapering schedule based on clinical response.
Attend follow-up assessments at day 1, 2 weeks, 1 month, and 3 months for eye examinations and pressure monitoring.
Be referred for surgical management if they do not demonstrate adequate clinical improvement after 4 weeks of therapy.

开始日期2025-08-10

申办/合作机构

Fayoum University

EUCTR2022-003825-24-AT

/ Recruiting临床4期IIT

Drug Concentration and degradation profiles of steroid and antibiotic eye drops in human aqueous humor.

开始日期2023-05-16

申办/合作机构

Medical University of Vienna

NCT05542381

/ CompletedN/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

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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专利（医药）

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项与氯替泼诺相关的文献（医药）

2026-08-01·COLLOIDS AND SURFACES B-BIOINTERFACES

Loteprednol etabonate nanostructured lipid carriers for enhanced ocular bioavailability

Article

作者: Burgess, Diane J ; Fanse, Suraj ; Bhorkade, Saurabh ; Maurus, Kellen

Loteprednol etabonate (LTP), a corticosteroid approved for management of post-operative ocular inflammation and dry eye symptoms, suffers from limited ocular bioavailability and high dosing frequency in its current marketed form, Lotemax® suspension. The current study reports the development and optimization of a novel nanostructured lipid carrier (NLC) system for LTP, designed to overcome these limitations through enhanced corneal penetration, sustained release, and improved therapeutic efficacy. Excipient screening assessment identified Gelucire 44/14, Miglyol 829, and Tween 80 as optimal solid lipid, liquid lipid, and surfactant, respectively, for LTP-NLC formulation. LTP-NLCs incorporating Transcutol® P as a permeation enhancer, and LTP-NLCs loaded into gellan gum-based ion-sensitive in situ gels, were systematically investigated. A Box-Behnken design enabled optimization of formulation variables, achieving ∼200 nm particle size with > 98% entrapment at 0.5% w/w drug load through precise control of lipid/surfactant balance and homogenization parameters. The optimized LTP-NLCs demonstrated excellent physicochemical stability (>3 months), amorphous drug dispersion within NLCs, and suitable rheological behavior. In vitro drug release studies (USP App IV) and ex vivo permeation studies across corneal and conjunctival tissues showed sustained release for LTP-NLCs compared to Lotemax®, with superior transcorneal permeation and minimal conjunctival loss. Incorporation of LTP-NLCs into gellan gum loaded in situ gels increased ocular retention but reduced permeability due to high viscosity. On the other hand, Transcutol® P markedly improved the transcorneal flux of LTP-NLCs and enhanced cellular uptake in human corneal epithelial cells. All formulations were non-irritant (HET-CAM), biocompatible, and maintained > 80% cell viability. Overall, the present work introduces a very promising LTP-NLC platform with demonstrated superiority over existing therapies, offering a strategy for enhancing ocular drug delivery, reducing dosing burden, and improving patient outcomes.

2026-06-11·[Zhonghua yan ke za zhi] Chinese journal of ophthalmology

[A case of microsporidial keratoconjunctivitis].

Article

作者: Liu, C ; Zhang, Y ; Zhao, L ; Dou, Z X ; Wang, Z Q

A 15-year-old male patient presented with recurrent photophobia, lacrimation, and blurred vision in both eyes for 3 years. He had been repeatedly diagnosed with "bilateral keratitis (unknown etiology)"at other hospitals and failed to respond to multiple topical medications. Initially diagnosed as bilateral Thygeson superficial punctate keratitis, he was treated with 0.5% loteprednol etabonate suspension eye drops and other medications. However, his symptoms worsened after 3 weeks of treatment. Subsequently, corneal epithelial tissue metagenomic testing and scrape cytological examination were performed, confirming the diagnosis of bilateral microsporidial keratoconjunctivitis. The treatment regimen was adjusted to topical application of 1% voriconazole eye drops, 0.3% gatifloxacin ophthalmic gel, and 0.1% tacrolimus eye drops. After 3 weeks of treatment, the patient's visual acuity in both eyes recovered to 1.0, conjunctival hyperemia was alleviated, and corneal epithelial punctate infiltration and fluorescein staining improved. One month after treatment, his symptoms were basically relieved, with the corneal infiltration and palpebral conjunctival papillae resolved. No recurrence was observed during the one-year follow-up.

2026-05-01·Veterinary Medicine and Science

Effects of Topical Steroids and Non‐Steroidal Anti‐Inflammatory Drugs on Gastrointestinal Bleeding in Rats

Article

作者: Ozlem Ozmen ; Aybike Ozbeyli ; Harun Cinar ; Beyza Bektas ; Latif Emrah Yanmaz

ABSTRACT:

Objective:

This study aimed to investigate the potential systemic gastrointestinal (GI) effects of short‐term topical administration of ocular steroids and non‐steroidal anti‐inflammatory drugs (NSAIDs) in rats.

Animals:

A total of 56 adult male Wistar rats were assigned to seven treatment groups ( n = 8 for each group), receiving topical applications of saline, prednisolone acetate, dexamethasone phosphate, loteprednol etabonate, ketorolac tromethamine, nepafenac or diclofenac sodium for 1 week.

Methods:

GI bleeding was assessed using faecal occult blood tests, gastric and duodenal tissues were analysed histopathologically, and endoscopic evaluations were performed.

Results:

Positive faecal occult blood results were observed in the prednisolone acetate group (3/8; 37.5%), dexamethasone phosphate (2/8; 25%), diclofenac sodium (1/8; 12.5%) and loteprednol etabonate (1/8; 12.5%). No positive results were recorded in the ketorolac tromethamine, nepafenac, or saline groups (0%). Differences between groups were not statistically significant ( p > 0.05). No significant within‐group differences between baseline and post‐treatment results were detected ( p > 0.05). Endoscopic scores ranged from 0 to 1 across all groups, and histopathology revealed no abnormalities.

Conclusions and clinical relevance:

Short‐term topical ocular steroid and NSAID treatments were not associated with statistically significant systemic gastrointestinal alterations under the conditions of this study.

项与氯替泼诺相关的新闻（医药）

2026-03-30

·EYE.AI视界

2025-2026眼科药物盘点：4款新药获批，AI与纳米技术将如何重塑眼病治疗？

🦐 全球至少22亿人受视力问题困扰，2025年眼科新药迎来了哪些突破？一组令人警醒的数据世界卫生组织（WHO）估算，全球至少22亿人存在某种形式的视力障碍。其中至少10亿人的视力损害本可预防或尚待干预——这不仅是公共卫生危机，更是对医疗系统和经济的巨大压力。慢性致盲性眼病如青光眼、老年黄斑变性（AMD）、糖尿病视网膜病变（DR），以及困扰大量患者的眼表疾病（包括干眼症、睑板腺功能障碍、神经性角膜炎等），每一类都在深刻影响着数以亿计人群的生活质量。眼科药物研发的核心挑战，在于眼睛那极其复杂且精密的解剖结构——血-视网膜屏障、泪液引流系统等多重生理屏障，让药物难以抵达目标组织并维持足够浓度。 2025年，FDA批准了多款眼科新药/新适应证，同时纳米载体和AI技术也在重塑眼科药物研发的格局。Optometry Times的最新年度盘点[1]为我们梳理了这些进展，以下是深度解读。2025年FDA批准的眼科新药1. 洛替泼诺依他泊酸酯眼用凝胶 0.38%（Lupin）分类：糖皮质激素\ 适应证：眼科手术后炎症和疼痛这是Bausch & Lomb的Lotemax SM生物等效制剂，以更低的浓度（0.38% vs 传统0.5%）实现同等抗炎效果。凝胶剂型可延长药物在眼表的停留时间，减少用药频次，对刚做完手术的患者而言是更温和的选择。2. 醋酸阿克林眼用溶液 0.003%（Tryptyr / Alcon）分类： TRPM8受体激动剂\ 适应证：干眼症（DED）\ 批准时间： 2025年7月这是2025年最具创新机制的新药之一。作用机制非常有意思：眼睛表面分布着一种叫“TRPM8”的冷受体，通常被低温激活。醋酸阿克林能模拟这一过程——不需要真正的降温，只需"欺骗"TRPM8受体，就能触发自然的泪液分泌。这与之前获批的鼻喷型酒石酸伐尼克兰（Tyrvaya）原理类似——都是通过刺激泪腺功能单位来促进泪液生成，但醋酸阿克林是直接眼药水形式，使用更便捷。更关键的是，由于它通过生理通路而非抗炎机制起效，起效速度比传统抗炎药物更快，有望成为需要术前快速改善眼表状态患者的理想选择。3. 醋酸阿塞利丁眼用溶液 1.44%（Vizz / LENZ Therapeutics）分类：瞳孔选择性缩瞳剂\ 适应证：老花眼（presbyopia）\ 批准时间： 2025年7月31日这是2025年最受业界关注的新药之一，也是老花眼治疗领域的重磅新选手。核心亮点：• 机制创新：通过与虹膜相互作用，以最小的睫状肌刺激实现瞳孔收缩（瞳孔缩小），从而改善近视力，且不会导致明显的近视漂移（即看远视力不受影响）• 每日一次，不含防腐剂• 在欧洲，醋酸阿塞利丁一直用于治疗青光眼，但用于老花眼是美国历史上的首次批准• III期CLARITY临床试验数据亮眼：93%的受试者在30分钟内达到≥20/40的近视力改善，效果持续长达10小时[2-8] 💡 老花眼影响着全球数亿40岁以上人群。 Vizz提供了一种无需手术的药物解决方案，打开了"老花眼滴眼液"这一全新品类的市场想象空间。4. 雷珠单抗注射液 100 mg/mL（Susvimo / Genentech）分类：抗VEGF（血管内皮生长因子）\ 新获批适应证：糖尿病视网膜病变（DR）\ 批准时间： 2025年 Susvimo的核心创新不是新分子，而是持续给药系统。关键信息：• 这是目前唯一获得FDA批准的连续给药抗VEGF治疗方式• 通过可重复填充的眼内植入物，在一次门诊手术植入后，每9个月仅需补充一次药物，即可持续维持VEGF抑制状态• 雷珠单抗本身就是成熟的抗VEGF药物（结合并抑制VEGF-A蛋白，减少新生血管形成和血管渗漏）• 此前（2021年）已获批用于湿性AMD，2025年初获批用于糖尿病黄斑水肿，此次扩展至整个糖尿病视网膜病变适应证临床意义：抗VEGF治疗需要反复眼内注射（通常每1-2个月一次），患者依从性差是临床痛点。Susvimo将给药间隔延长至每9个月一次，极大减轻了患者负担，有望从根本上改变DR management的格局。纳米技术：眼科药物递送的下一场革命？传统眼药水的问题在于：药物浓度波动大、生物利用度低、频繁给药患者依从性差。纳米技术正在从根源上解决这些问题——纳米载体（如纳米粒、脂质体、胶束、纳米乳等）可以：• 提高药物的眼部穿透能力和滞留时间• 实现缓释，减少给药频次• 同时负载亲水性和疏水性药物• 跨越血-视网膜屏障，触达眼后段 2025年发表的多项研究[10,11]系统综述了纳米载体在眼前段和眼后段疾病中的最新进展，显示这一领域正在从基础研究向临床转化迈进。但挑战依然存在：规模化生产工艺、长期安全性、监管路径——这些都需要进一步研究来填补。AI如何加速眼科药物研发？药物研发是出了名的"十年十亿"——周期长、成本高、失败率高。AI正在从多个维度改变这一现状[12]： AI应用方向具体作用药代/药效动力学预测利用机器学习算法和多组学数据集，预测药物在眼内的分布和效应新靶点发现从海量数据中识别与眼病相关的分子靶点毒性预测早期识别候选药物的潜在毒性，降低临床失败风险生物标志物发现AI辅助的多模态眼内生物标志物分析，支持精准医学临床试验优化提升效率、缩短周期、降低成本不过，AI在眼科的应用仍处于早期探索阶段，且面临着算法标准化、监管框架不完善、数据公平性等挑战。深度解读：这些进展意味着什么？1. 从"单次治愈"到"持续控制"——给药系统的范式转移 2025年最具标志性的进展，不是某个新分子，而是Susvimo的连续给药模式。眼科作为慢性病主导的专科（青光眼、AMD、DR都需要长期抗VEGF治疗），谁能解决依从性问题，谁就掌握未来。这与整个慢病管理的大趋势一致——从"记住每天用药"到"半年一次手术搞定"，给患者带来的生活质量改善是革命性的。2. 老花眼：一个被长期忽视的蓝海市场 Vizz的获批标志着老花眼正式进入药物治疗时代。全球40岁以上老花眼患者数量庞大，长期依赖老花镜或手术。Vizz提供了一种无创、每天一次、效果持续10小时的药物方案。这一品类的竞争才刚刚开始——未来更多老花眼候选药物已经在路上。3. TRPM8通路：干眼治疗的第三条路传统干眼治疗要么是抗炎（环孢素、Lifitegrast），要么是人工泪液补充。TRPM8激动剂绕开这两条路，通过激活眼表的"冷受体"触发神经介导的泪液分泌，为那些需要快速起效、或对现有抗炎药物不耐受的患者提供了新选择。4. AI+眼科：不是噱头，而是基础设施 AI在眼科的应用已经走出了"读片"阶段，开始向药物发现、临床决策、个性化治疗延伸。考虑到眼睛的影像数据丰富、疾病表型清晰，眼科是AI医疗落地条件最成熟的领域之一。总结与展望 2025年的眼科新药进展，可以用"老药新用、新机制突破、给药系统革命、AI蓄势待发"来概括：• 4款FDA新批药物覆盖了术后抗炎、干眼、老花眼和糖尿病视网膜病变• 纳米载体正在攻克传统眼药水的生物利用度难题• AI和数字技术开始渗透药物发现的早期阶段• 连续给药系统（Susvimo）代表了慢病管理的未来方向当然，挑战依然严峻：药物可及性、医保覆盖、基层医疗机构的设备配套，以及AI的监管框架——这些都是眼科创新真正落地需要跨越的最后一公里。但方向已经清晰：更智能的给药、更精准的靶点、更个性化和更便捷的治疗，正在从愿景走向现实。引用文献 [1] Optometry Times. What's new in 2025-2026: Ophthalmic drugs and drug delivery systems. January 26, 2026. Accessed March 30, 2026. [2] Lee A. Acoltremon: first approval. Drugs. 2025;85(10):1307-1310. doi:10.1007/s40265-025-02218-5 [3] DeFino A. Alcon launches Tryptyr for dry eye in US. Healio. July 31, 2025. [4] Aslam HG, Fatima M, Sajid H, et al. FDA approval of aceclidine (Vizz): a new chapter in nonsurgical presbyopia management. Ann Med Surg (Lond). 2025;87(11):6923-6925. doi:10.1097/MS9.0000000000004008 [5] McCabe CM, Schmidt EE. The emerging era of presbyopia-correcting eye drops: what's next? Ophthalmology Times. August 20, 2025. [6] LENZ launches Vizz for presbyopia in adults. News release. The Ophthalmologist. October 9, 2025. [7] Harp MD. Lupin launches loteprednol etabonate ophthalmic suspension, 0.5%, in the United States. Ophthalmology Times. July 19, 2025. [8] Harp MD, Maharjan EK. Genentech's Susvimo receives new FDA indication for diabetic retinopathy. Ophthalmology Times. May 22, 2025. [9] World Health Organization. Blindness and vision impairment. Fact sheet. August 10, 2023. [10] Khan S, Do CW, Ho EA. Recent updates on drug delivery approaches for improved ocular delivery with an insight into nanostructured drug delivery carriers for anterior and posterior segment disorders. Drug Deliv Transl Res. 2025;15(6):1828-1876. [11] Bairagi RD, Reon RR, Hasan M, et al. Ocular drug delivery systems based on nanotechnology: a comprehensive review for the treatment of eye diseases. Discov Nano. 2025;20(1):75. [12] Cheng H, Wong JLY, Quek CWN, et al. Ophthalmic drug discovery and development using artificial intelligence and digital health technologies. NPJ Digit Med. 2025;8(1):573.

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

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

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 (CALM, 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	獵築範齋夢壓鬱夢選築 = 壓獵製夢憲蓋鏇壓築襯壓顧鹽艱築鑰餘壓觸壓 (選夢選構簾顧繭窪簾齋, 鏇顧淵製艱顧艱壓願鏇 ~ 範廠廠範遞窪範窪窪繭) 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	餘繭糧膚網構餘蓋淵構(觸衊築選糧衊觸壓醖獵) = 醖鏇鑰觸夢餘製鑰鏇夢構窪構醖繭淵窪淵鏇積 (觸衊獵夢齋淵範膚鹹齋 ) 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)	廠膚遞顧鑰窪網構衊鏇(構襯膚鑰積鬱衊範築鏇) = 選遞糧憲憲鏇憲糧壓鹹膚鹽繭憲積糧願遞糧鬱 (夢憲遞鑰繭顧觸繭繭鹹, 1.5) 更多	-	2023-10-11
				Cyclosporine+Dexamethasone Ophthalmic 0.4 Mg Ophthalmic Insert (Restasis and Dextenza)	廠膚遞顧鑰窪網構衊鏇(構襯膚鑰積鬱衊範築鏇) = 醖壓構壓廠願築齋網壓膚鹽繭憲積糧願遞糧鬱 (夢憲遞鑰繭顧觸繭繭鹹, 1.0) 更多
NCT02120079 (CTgov)	临床4期	干眼综合征	37	In Vivo Confocal Microscopy (IVCM)+Lotemax (Lotemax)	網構鹹鏇壓鹹獵窪鏇壓(獵鹹鏇積齋糧簾選鏇鹽) = 衊憲鹽構願衊選鬱蓋夢糧糧範鑰窪獵夢窪網積 (夢築廠鹹繭醖壓糧夢鹽, 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))	網構鹹鏇壓鹹獵窪鏇壓(獵鹹鏇積齋糧簾選鏇鹽) = 獵憲淵獵淵衊簾鹹簾簾糧糧範鑰窪獵夢窪網積 (夢築廠鹹繭醖壓糧夢鹽, 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)	築鬱艱選鑰鹽構顧簾繭(醖遞範構顧鹽簾壓夢製) = 簾鑰網廠顧獵網齋獵簾醖憲鬱廠範繭壓構願夢 (遞願鹹繭壓艱醖觸淵憲, 19.379) 更多	-	2021-04-02
				Vehicle (Vehicle of KPI-121 0.25% Ophthalmic Suspension)	築鬱艱選鑰鹽構顧簾繭(醖遞範構顧鹽簾壓夢製) = 願網鑰網觸艱遞鹹鏇築醖憲鬱廠範繭壓構願夢 (遞願鹹繭壓艱醖觸淵憲, 17.579) 更多
NCT02218489 (Maui, CTgov)	临床2期	睑缘炎 \| 睑板腺功能障碍	206	Vehicle (Vehicle)	壓鏇廠製繭蓋觸餘鹽夢(夢齋範築夢願繭網蓋蓋) = 獵遞廠憲網顧鏇鏇廠範襯鑰膚選襯鑰蓋淵鏇壓 (繭齋構夢願選襯襯鹹積, 13.8) 更多	-	2021-01-11
				KPI-121 (KPI-121 0.25% Ophthalmic Suspension)	壓鏇廠製繭蓋觸餘鹽夢(夢齋範築夢願繭網蓋蓋) = 鏇壓鹹廠夢壓糧齋製獵襯鑰膚選襯鑰蓋淵鏇壓 (繭齋構夢願選襯襯鹹積, 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)	鬱選遞鑰築顧鹹鑰夢鹹(醖簾構壓夢餘膚簾築醖) = 餘鏇衊觸窪廠餘積簾選膚鹹顧製簾鹹築願選鬱 (鹽構鏇鑰窪選繭製繭顧, 0.633) 更多	-	2021-01-06
				Placebo (Vehicle)	鬱選遞鑰築顧鹹鑰夢鹹(醖簾構壓夢餘膚簾築醖) = 範遞蓋衊範衊簾衊壓衊膚鹹顧製簾鹹築願選鬱 (鹽構鏇鑰窪選繭製繭顧, 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)	範鑰鏇選壓醖積齋壓淵 = 構膚構鏇蓋淵積醖憲鹹艱鹽構窪壓襯積鏇範衊 (範範範餘憲夢衊選鏇鏇, 繭鹽顧製選糧窪築構窪 ~ 鹹願觸範醖壓積網淵範) 更多	-	2020-12-22
				KPI-121 1.0% (KPI-121 1.0% BID)	範鑰鏇選壓醖積齋壓淵 = 製築顧構簾醖鬱築壓構艱鹽構窪壓襯積鏇範衊 (範範範餘憲夢衊選鏇鏇, 蓋築蓋膚鹽觸膚積遞淵 ~ 願艱範繭範餘壓觸顧遞) 更多
NCT03123614 (CTgov)	临床4期	角膜混浊	131	Loteprednol Etabonate (Loteprednol Etabonate 0.5% Oph Gel)	選製膚築醖醖築願醖憲(齋選齋壓憲鑰鹹膚繭鏇) = 壓構顧醖獵廠顧積遞範淵膚壓繭簾餘鑰壓積壓 (淵齋築製鏇鹽觸艱築鑰, 2.11) 更多	-	2020-12-21
				Prednisolone Acetate (Prednisolone Acetate 1% Oph Susp)	選製膚築醖醖築願醖憲(齋選齋壓憲鑰鹹膚繭鏇) = 窪願醖積齋觸蓋蓋淵醖淵膚壓繭簾餘鑰壓積壓 (淵齋築製鏇鹽觸艱築鑰, 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)	鏇製鏇齋製衊廠膚觸鹽(餘醖壓製襯網艱鏇範製) = 簾獵遞觸壓構廠築淵簾憲願齋獵廠構壓糧繭窪 (蓋襯醖顧衊製鑰鹽襯夢, 7.83) 更多	-	2020-12-10
				KPI-121 0.25% Ophthalmic Suspension (KPI-121 0.25% Ophthalmic Suspension)	鏇製鏇齋製衊廠膚觸鹽(餘醖壓製襯網艱鏇範製) = 獵鏇襯夢醖襯餘範壓夢憲願齋獵廠構壓糧繭窪 (蓋襯醖顧衊製鑰鹽襯夢, 2.00) 更多