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, Inc.Alcon Laboratories, Inc.Bausch & Lomb (Australia) Pty Ltd.

非在研机构

Kala Bio, Inc.

Sandoz Group AG

Sandoz International GmbH

+ [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

67

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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312

项与氯替泼诺相关的文献（医药）

2025-09-01·CORNEA

Anterior Stromal Melt With Corneal Allogeneic Intrastromal Ring Segments in a Patient With Severe Atopy

Article

作者: Assaf, Jad F. ; Jacob, Soosan ; Asfar, Karen E. ; Awwad, Shady T. ; Gendy, Jeremiah

Purpose::

To report the first case of anterior stromal melt after insertion of a corneal allogeneic intrastromal ring segment (CAIRS) in a patient with severe atopy.

Methods::

A 27-year-old woman with keratoconus, severe atopy, and giant upper tarsal conjunctival papillae underwent uneventful insertion of a CAIRS in her right eye. 4 months later, she presented with severe exacerbation of her atopy, necessitating anti-IgE monoclonal antibody therapy initiation.

Results::

Slit-lamp examination revealed thinning of the corneal stroma overlying the CAIRS over a 30-degree sector, also documented by optical coherence tomography. There was a resolution of the giant conjunctival papillae. The patient was started on topical cyclosporine and a tapering loteprednol regimen, along with the anti-IgE treatment. The last follow-up showed stability in visual acuity, stromal thickness, and topographic parameters, which remained better than preoperatively.

Conclusions::

Anterior stromal melt, commonly seen with synthetic segments, can rarely develop after CAIRS implantation, in specific circumstances, such as severe inflammation and atopy. Prompt systemic and topical management can potentially stop progression and retain the implanted segment.

2025-09-01·American journal of ophthalmology case reports

Corneal pseudomicrocysts following claudin-6 antibody-drug conjugate infusion

Article

作者: Cooper, Caitlynn ; Meyer, Evan ; Sattarova, Victoria ; Rashidi, Vania ; Matuszewska, Laura ; Chanbour, Wassef

Purpose:

To report a case of bilateral corneal pseudomicrocysts associated with infusions of a novel antibody-drug conjugate targeting claudin-6, called TORL-1-23.

Observations:

A 47-year-old female with a history of advanced recurrent serous ovarian cancer presented to a level 1 tertiary care center with ocular irritation, redness, tearing, and light sensitivity following two infusions of TORL-1-23. Patient's past ocular history was unremarkable. The patient was enrolled in a phase 1 clinical trial for TORL-1-23, an antibody-drug conjugate (ADC). Nine days following the second infusion the patient presented to the ophthalmology clinic complaining of two weeks of bilateral eye discomfort, tearing, and photophobia. On examination, the patient had decreased visual acuity with a surface keratopathy associated with a whorled pattern of epithelial pseudomicrocysts in both eyes. Corneal changes were concentrated between the inferior limbus and central cornea. The remainder of the ophthalmic exam was unremarkable. Collagen and silicone punctal plugs were placed and the patient was started on preservative free artificial tears, topical loteprednol 0.5 %, later replaced with topical prednisolone acetate 1 % drops, and brimonidine 0.2 % in both eyes. The patient developed neuropathy which necessitated a decrease in ADC dosage and the patient's symptoms subsequently improved. However, a decrease in visual acuity and increase in corneal pseudomicrocysts was seen after the fifth infusion. Corneal disease improved with the placement of new collagen punctal plugs and addition of cyclosporine 0.05 % eye drops in both eyes. Ocular symptoms and exam findings waxed and waned with continued infusions of the ADC.

Conclusions and importance:

This case reports an incidence of corneal pseudomicrocysts associated with TORL-1-23 treatment, which should be recognized as a potential adverse effect of this novel therapy.

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.

64

项与氯替泼诺相关的新闻（医药）

2025-07-23

·CPHI制药在线

抽丝剥茧解读FDA 202封审批拒信

关注并星标CPHI制药在线在新药研发的漫长旅程中，科学创新固然是起点，但真正决定能否迈过监管终点线的，往往并不是分子机制或靶点选择，而是执行力的细节。2025年7月， FDA罕见地集中公开了202封完整回复函（Complete Response Letters, CRLs）。这是FDA首次大规模披露未获批准药物的详细审评意见，也为产业界提供了一面从未如此清晰的"病理分析报告"。相关阅读：《FDA解密202张CRL：中国药企出海的挑战与启示》1.FDA签发CRL全景分析ProGen Search对这批CRL进行了系统分析，结论令人震惊也令人深思：74%的CRL中明确指出化学、生产与质量控制（CMC）方面存在重大缺陷（一份CRL可能包含多个原因，因此总和并非100%，下同），成为新药上市失败最主要也最可预防的原因。这些问题，并非出现在靶点选择、临床策略或药效验证的前端，而是在CMC这一常被视为执行细节的环节。CMC问题：最多也最容易被忽视的审批障碍CRL中CMC缺陷主要集中在以下三类问题：● 设施检查未通过（58%）：药品生产场地存在尚未解决的合规问题，如数据完整性、清洁验证、批记录缺陷等。●杂质控制与包装材料渗出物不合规（28%）：产品纯度、安全性相关的控制策略不完善，未能满足FDA对潜在毒理风险的审查要求。● 稳定性数据不足（19%）：未能提供产品在货架期内质量保持的充分证明，影响标签使用期的确认。这些问题表明，从实验室走向产业化的过程中，研发团队与工艺、法规、质量体系之间的协同常常脱节。换句话说，药物是否能稳定生产、并且符合GMP标准，正成为决定其能否上市的关键门槛。临床策略与证据：依然是第二大拦路虎尽管CMC问题占据主因，临床层面的失败依然不可忽视，35%的CRL指出临床证据或策略存在不足。● 主要终点未达标（16%）：产品未能在试验中取得统计显著性或临床意义明确的疗效。● 治疗效应不足（9%）：即便终点达标，疗效幅度过小，难以获得"实质性有效性"的认定。审评机构对"临床意义"的要求日益严苛，尤其在已有治疗标准存在的适应症中，疗效增益必须足够大，才能说服监管机构做出批准。装置与人因验证成为"隐形地雷"在包含药物-设备组合的产品中（如自动注射器、吸入装置等），18%的CRL提及装置及使用界面存在缺陷。其中最常见的问题是人因验证（Human Factors, HF）试验失败，即未能证明目标患者或使用者能在实际场景中安全、有效地操作产品。在生物制剂、皮下注射药物快速扩张的今天，不再只是"药物是否有效"，更是"患者能否正确用药"。CRL的代价：不只是推迟，还有战略性伤害获得CRL的代价远不止是时间推迟。一份CRL往往意味着：● 上市延迟12-24个月；● 额外投入数百万至上亿美元用于整改与补充研究；● 投资人信心重挫，股价波动加剧，甚至引发合作终止或高管更替。2.审评失败的深度量化分析新药被拒并非偶然，更不是黑箱操作。FDA首次公开的202封完整回复函为人们提供了一幅前所未有的失败图谱。在这些CRL中，多数并非单一问题所致，而是多个维度的缺陷叠加，构成了审批障碍的复合网络。ProGen的系统回顾揭示了三大类、共25项高频缺陷点。这些数据不只是事后复盘的材料，更应成为未来项目风险控制的预警清单。2.1 化学、生产与质量控制（CMC）缺陷发生率：74%CMC是最主要也是最复杂的失败领域，涵盖从工厂硬件到分析方法、从杂质控制到稳定性数据等多个关键环节。在众多CRL拒批理由中，CMC缺陷并不是偶然出现的小瑕疵，而是反复出现的系统性失败，揭示出行业对生产制造的忽视与误判。临床数据决定药品是否有用，而CMC部分决定药品是否可信、可产、可监管，它是新药最终成败的底线。报告发现，超过三分之二（74%）的CRLs涉及CMC缺陷，其中多个问题指向一个共同根源：执行力不足（execution gap），也就是从"知道要做"到"真正做到"的能力鸿沟。设施合规性不是"可选项"，而是批准的前提✓ 数据要点：58%的CRL涉及设施检查问题，其中90%为FDA现场检查发现的"objectionable conditions"（不可接受立场）。✓ FDA在CRL中措辞直接："在本申请获得批准之前，须令人满意地解决上述缺陷。" 这意味着只要生产场地存在未解决的问题，整个申请将被"原地冻结"。✓ 从ProGen的数据来看，多数此类问题并非由于现场工艺突然变差，而是源自申办方对其外包生产体系缺乏全面质量监管。监管正在从"文件审查"转向"质量责任"，任何生产组织的疏漏，都可能引爆CRL。产品特性不清晰：不了解自己的药，也就无法保障安全✓ 数据要点：41%的CRL提及"产品特征理解不足"问题，其中以下三类尤为高发：○ 杂质与包装渗出物控制不当：代表性审评意见指出："您未能提供充分数据，确认该降解产物已超出ICH Q3B(R2)的确认阈值。"○ 这一问题在FDA眼中并非"可以后补"的可纠问题，而是"审评流程晚期已无法接受的潜在安全风险"。一旦有未知毒性来源未被确认，审评流程只能中止。○ 稳定性数据不足：例如某CRL指出："拟定的18个月有效期缺乏稳定性数据支持，其中6批样品中有2批失效。"稳定性是确定货架期、冷链运输和标签信息的基础。很多企业在报批时依然采用"仅覆盖提交时点"的短期稳定性数据，而非满足监管预期的长期趋势数据，导致申请直接遭拒。○ 包装容器相容性问题：典型问题如药液与玻璃瓶或橡胶塞产生化学反应、析出离子等，某CRL指出："数据表明药品与所用硼硅玻璃瓶不相容。"这类问题的致命性在于：一旦产品与容器系统不匹配，就会直接威胁药品质量和患者安全，而解决通常需要更换供应商与完整再验证流程。工艺控制是"掌控力"的体现：不是可交差的模板，而是对生产的全面主导✓ 数据要点：25%的CRL明确指出工艺控制方案不合格。✓ 问题最常见于所申报的工艺参数区间超出了此前工艺验证范围，例如提交材料中所列的温度、pH、搅拌速率等控制参数，与验证批次中实际测试的范围不一致。FDA对此类表述极其敏感，认为这是对"工艺理解"（process understanding）不足的直接体现。企业若不能证明CPP（关键工艺参数）与CQA（关键质量属性）之间的关联，则工艺控制即不成立。2.2 临床策略与有效性证据缺陷发生率：35%在临床策略维度，审批失败集中体现为"证据力不足"与"临床意义偏弱"。尤其在已存在治疗方案的适应症中，监管对"疗效+安全+需求"的综合评估变得更加严苛。虽然在数量上不及CMC缺陷频繁（35% vs. 74%），但临床失败往往代价更大、后果更严重。一旦产品因临床数据缺陷遭拒，往往意味着不仅要补数据，更需要重启试验、追加多年开发成本，而这可能击穿一个开发商的资金极限。核心问题在于：申办方未能提供"充分的有效性证据（substantial evidence of effectiveness）"，也就是FDA对疗效认定的核心标准。注册性试验失败：最直接、最不可回避的拒绝理由✓ 数据要点：16%的CRL直接因关键性注册试验未达主要终点被拒。一项注册性临床试验失败，等同于药物机制被监管机构正式否定。FDA不会因为统计边缘或次要终点的勉强达标而网开一面。✓ 代表性CRL：KPI-121-C-002试验未能证明0.25%乙酸氟替卡松眼用混悬液在主要症状终点上的优效性。这类缺陷几乎毫无补救空间，必须重新设计并完成一项新的、具充分效力的、良好对照的临床试验（adequate and well-controlled trial），这对时间和资金都是毁灭性打击。505(b)(2)路径：桥接失败，逻辑链条被截断✓ 数据要点：12%的CRL源于桥接不成功，未能证明新制剂与参比药的等效性✓ 在505(b)(2)注册路径中，药品开发者可依赖已有上市药品的临床安全性与疗效数据，仅需补充新制剂的差异数据。但关键前提是：必须建立"科学桥接（scientific bridge）"。✓ 典型失败形式是：PK数据不一致。CRL中指出："PK桥接研究未能证明临床所用产品与拟上市产品之间具有PK可比性。"这相当于申办方在申请书中主张："我的药只做了一点小改变，无需重复完整临床。" 但FDA回应："你没有证明它还是同一个药。" 桥接失败等于逻辑断裂，整个申报基础崩塌。疗效统计显著 ≠ 临床意义显著：监管视角下的"虚假阳性"✓ 数据要点：9%的CRL中，申办方虽取得统计显著性，但被FDA判定为"临床意义不足"。✓ 这是一种更"高级"的失败：你证明了假设，但FDA认为结果不足以改变患者命运。✓ CRL典型表述为：治疗效应的幅度很小，临床意义不明确。这暴露出申办方与FDA在"疗效定义"上的战略性错位。临床开发的终点设计若仅以统计学为目标，而未与监管对患者获益的共识对齐，最终可能陷入"数值正确，价值失败"的悖论。长期安全性数据库不够：慢病药物面临更高门槛✓ 数据要点：8%的CRL指出长期安全性数据样本量或随访期不足✓ 对于慢性用药、预防性治疗或终生用药（如罕见病、生物制剂），FDA明确要求较长随访期与足够样本数。✓ 某CRL中写道：安全数据库中，仅49名患者接受治疗达12个月，未能充分表征长期安全性。而FDA当时的预期是至少100人达到该时间门槛。换言之，即使短期内未见严重不良事件，也不能作为"安全"标签的依据。在临床路径选择、终点设定、桥接逻辑设计等方面，早期与FDA达成共识比任何试验成功更重要。2.3 组合产品与人因工程缺陷发生率：18%随着生物制剂自我注射等递送方式的兴起，装置与使用界面不再是技术附属品，而成为获批与否的决定性因素。在202封CRL中，18%的拒批案例涉及组合产品（combination product）。这些产品通常由药物成分与设备组件共同构成（如预充式注射笔、自我吸入器等）。令人警醒的是，失败的根本原因不在于药物无效，而在于装置不能保证正确用药。这揭示了一个关键误区：部分申办方仍将装置视为配件，而非治疗方案的有机组成。然而在FDA的逻辑中，装置即药物的一部分，其设计、可靠性与人因验证必须接受与药效等同的审查强度。人因工程验证失败：最常见也是最严重的拒批原因✓ 数据要点：14%的CRL因人因工程（HF）验证失败被拒✓ 在这些案例中，FDA明确指出装置的用户界面无法支持患者或医护人员安全、有效地完成关键用药任务。常见风险包括：注射不足剂量（under-dosing）、注射过量（over-dosing）、意外暴露或针刺伤害（accidental exposure）✓ 一封CRL中措辞表示，"根据人因验证研究结果，该用户界面不能支持所申请产品的安全与有效使用。"✓ 这类失败并非小问题，而是涉及患者生命安全的根本风险，无法通过补充文件或说明来解释清楚，必须重新设计装置或重做HF试验。装置性能与可靠性不达标：不仅好用，还要耐用✓ 数据要点：6%的CRL因装置物理性能或稳定性问题被拒✓ 除用户操作外，FDA同样关注装置本身在运输、储存、长期使用中的物理可靠性。失败常发生稳定性测试阶段（如老化后可靠性下降）、工艺偏差（如批次之间剂量释放差异显著）、机械安全机制不足（如针头保护机构失效）✓ 一封CRL特别指出："请提交数据，证明针头安全机制在老化、跌落测试与模拟运输后仍能以95%/99%的置信度稳定工作。"✓ 这说明整个生命周期内的可靠性都是不可妥协的审核重点。测试设备与最终上市版本不一致：验证失效✓ 数据要点：4%的CRL因HF试验对象非最终版本而被否定✓ 部分企业在人因验证或性能测试阶段使用的是"开发中版本"或"非最终上市包装"，而未基于最终拟上市产品（to-be-marketed device）。FDA对此表示不可接受。✓ 一封CRL中指出："您的人因研究并未评估最终拟上市版本的用户界面，因此无法证明目标用户能否正确开启或关闭包装。"✓ 这类问题不仅使试验结果无效，还可能影响FDA对整个装置系统的信任，需重新开展全套验证流程。无论是自我注射笔、吸入器，还是贴剂与药盒，任何可能影响剂量、顺应性或使用方式的设计缺陷，都可能使整个药品申报失败。3.拒信背后，是更高标准的信号FDA首次集中披露202封完整回复函，为行业提供了前所未有的透明窗口。这些拒批案例不再是单一技术难点的堆积，而体现出一种深层次的规律：新药上市的最大风险往往并不来自分子本身，而来自开发与执行体系的薄弱环节。无论是未完成整改的生产设施、未建立桥接逻辑的制剂变更，还是未验证用户界面的装置缺陷，这些问题并不属于创新不可控的领域，而是本可在项目早期识别、提前预防的合规盲点。监管的重心，正在从结果判断转向对过程质量的系统性评估。END来源：CPHI制药在线声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com▼更多制药资讯，请关注CPHI制药在线▼点击阅读原文，进入智药研习社~

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

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 (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	觸淵夢餘醖齋鑰鏇獵獵 = 糧獵遞壓簾顧壓獵醖範觸蓋製艱鹽醖壓選製觸 (網顧遞窪願繭艱遞鏇壓, 餘憲夢積觸鬱築網窪積 ~ 觸觸製膚鹹鬱襯鹽壓願) 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	鹽餘憲鹽鬱膚襯遞鑰窪(廠衊積獵顧醖艱糧廠齋) = 鏇艱選鹹鏇鑰鬱壓艱廠鹽範鹹壓衊醖衊壓艱襯 (鹹餘憲範蓋範簾糧鑰積 ) 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)	壓製鑰鹽鹹廠製衊壓壓(鹽願窪餘衊廠鬱鬱廠醖) = 積襯鬱蓋構醖衊衊憲艱淵鑰製鏇醖衊蓋醖範齋 (鹽憲憲蓋網選觸願繭窪, 1.5) 更多	-	2023-10-11
				Cyclosporine+Dexamethasone Ophthalmic 0.4 Mg Ophthalmic Insert (Restasis and Dextenza)	壓製鑰鹽鹹廠製衊壓壓(鹽願窪餘衊廠鬱鬱廠醖) = 範繭觸糧窪顧餘餘製鹽淵鑰製鏇醖衊蓋醖範齋 (鹽憲憲蓋網選觸願繭窪, 1.0) 更多
NCT02120079 (CTgov)	临床4期	干眼综合征	37	In Vivo Confocal Microscopy (IVCM)+Lotemax (Lotemax)	獵鏇憲淵餘襯窪蓋簾憲(鹹糧繭範糧餘廠鏇衊壓) = 範廠餘壓壓鏇鏇壓構製淵顧範獵顧鏇鑰築網鬱 (顧築淵廠築觸衊觸願製, 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))	獵鏇憲淵餘襯窪蓋簾憲(鹹糧繭範糧餘廠鏇衊壓) = 憲鹽夢顧簾獵蓋醖構觸淵顧範獵顧鏇鑰築網鬱 (顧築淵廠築觸衊觸願製, 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)	膚選蓋艱選鹹鑰簾鏇選(顧夢顧鏇鏇廠觸襯積簾) = 築範範繭窪壓範淵願積鑰繭醖鹹積餘憲網獵顧 (憲網窪構衊醖製觸顧獵, 19.379) 更多	-	2021-04-02
				Vehicle (Vehicle of KPI-121 0.25% Ophthalmic Suspension)	膚選蓋艱選鹹鑰簾鏇選(顧夢顧鏇鏇廠觸襯積簾) = 顧壓選膚窪網襯窪餘積鑰繭醖鹹積餘憲網獵顧 (憲網窪構衊醖製觸顧獵, 17.579) 更多
NCT02218489 (Maui, CTgov)	临床2期	睑缘炎 \| 睑板腺功能障碍	206	Vehicle (Vehicle)	鬱廠廠淵襯襯廠繭糧餘(繭鹹夢獵餘觸餘製夢鏇) = 鏇衊鹹鏇網齋積遞鬱築壓願選鹹艱醖製夢願遞 (網製遞襯齋壓廠範鏇鏇, 13.8) 更多	-	2021-01-11
				KPI-121 (KPI-121 0.25% Ophthalmic Suspension)	鬱廠廠淵襯襯廠繭糧餘(繭鹹夢獵餘觸餘製夢鏇) = 憲選餘鑰糧築窪觸蓋鏇壓願選鹹艱醖製夢願遞 (網製遞襯齋壓廠範鏇鏇, 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)	鬱壓衊餘艱壓蓋壓鬱淵(鬱願廠鹹鹹鏇蓋壓積範) = 鏇夢網簾製願獵鏇鹽艱衊觸選夢觸遞繭製築衊 (顧築繭廠選築製簾製憲, 0.633) 更多	-	2021-01-06
				Placebo (Vehicle)	鬱壓衊餘艱壓蓋壓鬱淵(鬱願廠鹹鹹鏇蓋壓積範) = 鹹夢網壓膚積鏇衊鬱膚衊觸選夢觸遞繭製築衊 (顧築繭廠選築製簾製憲, 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)	衊憲餘構鏇製衊積簾鑰 = 網淵蓋構積鏇鑰醖簾遞鏇鑰製願簾鹽艱襯積繭 (選積範憲範顧鑰遞餘觸, 淵糧餘糧築製餘獵襯觸 ~ 憲淵壓憲襯襯蓋鏇獵淵) 更多	-	2020-12-22
				KPI-121 1.0% (KPI-121 1.0% BID)	衊憲餘構鏇製衊積簾鑰 = 餘糧壓蓋顧網膚餘齋觸鏇鑰製願簾鹽艱襯積繭 (選積範憲範顧鑰遞餘觸, 獵積蓋餘積蓋構壓製顧 ~ 鹽憲獵繭觸觸艱簾鏇願) 更多
NCT03123614 (CTgov)	临床4期	角膜混浊	131	Loteprednol Etabonate (Loteprednol Etabonate 0.5% Oph Gel)	壓選遞壓遞齋網選襯網(淵憲鬱築鏇願獵製觸鑰) = 壓醖鏇鹽衊築淵築糧顧簾齋餘製構觸鹽網範憲 (壓襯獵膚餘簾廠簾齋廠, 2.11) 更多	-	2020-12-21
				Prednisolone Acetate (Prednisolone Acetate 1% Oph Susp)	壓選遞壓遞齋網選襯網(淵憲鬱築鏇願獵製觸鑰) = 獵製夢醖壓遞醖糧壓夢簾齋餘製構觸鹽網範憲 (壓襯獵膚餘簾廠簾齋廠, 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)	選醖膚廠願廠繭鏇糧衊(鑰壓醖顧繭鹹壓艱憲繭) = 鏇築選蓋艱襯鹽製廠蓋鑰選醖醖獵獵鑰構鬱繭 (觸襯夢築餘齋積簾選窪, 7.83) 更多	-	2020-12-10
				KPI-121 0.25% Ophthalmic Suspension (KPI-121 0.25% Ophthalmic Suspension)	選醖膚廠願廠繭鏇糧衊(鑰壓醖顧繭鹹壓艱憲繭) = 壓繭餘鑰鏇壓構膚蓋構鑰選醖醖獵獵鑰構鬱繭 (觸襯夢築餘齋積簾選窪, 2.00) 更多