A Randomized Clinical Trial of ab Interno Canaloplasty and Trabeculotomy With the OMNI Surgical System Compared to Standard Medical Treatment in Pseudophakic Patients With Primary Open Angle Glaucoma

A Randomized Clinical Trial of Ab Interno Canaloplasty and Trabeculotomy with the OMNI® Surgical System Compared to Standard Medical Treatment in Pseudophakic Patients with Primary Open Angle Glaucoma (EVOLVE)

开始日期2024-08-21

申办/合作机构

Sight Sciences, Inc.

NCT06629129

/ Completed临床1期IIT

Optic Nerve Head Perfusion Following Treatment with Latanoprost 0.005% in Primary Open Angle Glaucoma: an Optical Coherence Tomography Angiography Study

46 eyes of 23 patients have been treated with topical Latanoprost 0.005 %. visual field was performed on all eyes. NFLT was measured using OCT. Radial peripapillary capillary (RPC) vascular density was measured using OCTA . mean ocular perfusion pressure (MOPP), and RPC vascular density were measured before and after treatment BY 2-3 MONTHS

开始日期2024-06-24

申办/合作机构

Zagazig University

NCT06730516

/ Completed早期临床1期IIT

Optic Nerve Head Perfusion Following Treatment with Latanoprost 0.005% Versus Brimionidin Tartrate 0.2% in Primary Open Angle Glaucoma: an Optical Coherence Tomography Angiography Study

This study aimed to evaluate the effects of topical Latanoprost 0.005 % versus Brimionidin tartrate 0.2% on perfusion of optic nerve head This prospective interventional randomized study included 56 naive patients recently diagnosed with bilateral primary open angle glaucoma equally divided into two groups with 28 patients in each group

开始日期2024-06-24

申办/合作机构

Zagazig University

100 项与拉坦前列素相关的临床结果

登录后查看更多信息

100 项与拉坦前列素相关的转化医学

登录后查看更多信息

100 项与拉坦前列素相关的专利（医药）

登录后查看更多信息

2,082

项与拉坦前列素相关的文献（医药）

2025-01-01·Ophthalmology science

Subconjunctival Administration of an Adeno-Associated Virus Expressing Stanniocalcin-1 Provides Sustained Intraocular Pressure Reduction in Mice

Article

作者: Chowdhury, Uttio Roy ; Anderson, Kjersten J. ; Omer, Mohammed E. ; Fautsch, Michael P ; Rinkoski, Tommy A. ; Fautsch, Michael P. ; Niknam, Parvin ; Omer, Mohammed E ; Roddy, Gavin W. ; Anderson, Kjersten J ; Pacheco Marrero, Johann M. ; Roddy, Gavin W ; Pacheco Marrero, Johann M ; Kohli, Darrell ; Rinkoski, Tommy A

Purpose:

To investigate subconjunctival administration of a single-stranded, adeno-associated virus, serotype 2, engineered to express stanniocalcin-1 with a FLAG tag (ssAAV2-STC-1-FLAG) as a novel sustained (IOP) lowering agent with a reduced ocular surface side effect profile.

Design:

In vivo preclinical investigation in mice.

Subjects:

C57BL/6J, DBA/2J, prostaglandin F (FP) receptor knockout mice.

Methods:

Normotensive C57BL/6J mice were treated with a subconjunctival injection of ssAAV2-STC-1-FLAG (2 μL; 6 × 10⁹ viral genomes [VGs]) in 1 eye and the same volume and concentration of ssAAV2-green fluorescent protein (GFP) or the same volume of phosphate-buffered saline in the fellow eye. Ocular hypertensive DBA/2J mice were subconjunctivally injected with 6 × 10⁹ VGs of ssAAV2-STC-1-FLAG or ssAAV2-GFP. Steroid-mediated ocular hypertension was induced in C57BL/6J mice with weekly injections of dexamethasone into the conjunctival fornix, and mice were then injected subconjunctivally with 6 × 10⁹ VGs of ssAAV2-STC-1-FLAG or ssAAV2-GFP. Prostaglandin F receptor knockout mice were injected subconjunctivally with 6 × 10⁹ VGs of ssAAV2-STC-1-FLAG or phosphate-buffered saline. An identical vector was constructed without the FLAG tag (ssAAV2-STC-1) and evaluated in normotensive C57BL/6J mice. Intraocular pressure was assessed using the Tonolab tonometer for all experiments. Tumor necrosis factor alpha (TNFα), a marker of ocular surface inflammation, was compared between subconjunctivally delivered ssAAV2-STC-1-FLAG and other treatments including daily topical latanoprost.

Main Outcome Measures:

Intraocular pressure assessment.

Results:

Subconjunctival delivery of ssAAV2-STC-1-FLAG significantly reduced IOP for 10 weeks post injection in normotensive mice. Maximal IOP reduction was seen at week 3 postinjection (17.4%; 17.1 ± 0.8 vs. 14.1 ± 0.8 mmHg, P < 0.001). After the IOP-lowering effect had waned, a second injection restored the ocular hypotensive effect. Subconjunctivally delivered ssAAV2-STC-1-FLAG lowered IOP in DBA/2J mice (16.9%; 17.8 ± 2.0 vs. 14.8 ± 0.9 mmHg, P < 0.001) and steroid-mediated ocular hypertensive mice (20.0%; 19.0 ± 0.6 vs. 15.2 ± 0.7 mmHg, P < 0.001) over the experimental period. This construct also reduced IOP to a similar extent in wild-type (15.9%) and FP receptor knockout (15.7%) mice compared with the fellow eye. A related construct also lowered IOP without the FLAG tag in a similar manner. Reduction in conjunctival TNFα was seen when comparing subconjunctivally delivered ssAAV2-STC-1-FLAG to daily topical latanoprost.

Conclusions:

Subconjunctival delivery of the STC-1 transgene with a vector system may represent a novel treatment strategy for sustained IOP reduction and improved ocular tolerability that also avoids the daily dosing requirements of currently available medications.

Financial Disclosures:

Proprietary or commercial disclosure may be found in the Footnotes and Disclosures at the end of this article.

2024-12-01·JOURNAL OF OCULAR PHARMACOLOGY AND THERAPEUTICS

The Optejet Technology Minimizes Preservative-Mediated Cytotoxicity of Conjunctival Epithelial Cells Treated with Latanoprost In Vitro

Article

作者: Hamrah, Pedram ; Lam, Peter ; Harris, Deshea L. ; Whitcomb, Julie ; Sultan, Ayesha

Purpose: Benzalkonium chloride (BAK) is a commonly used preservative to maintain sterility for multiuse eye drops such as latanoprost. One option to minimize the deleterious effects of BAK in eye drops may be to reduce the volume administered. The aim of this study was to assess the response of cells from the ocular surface to latanoprost+BAK administered by the Optejet technology, which dispenses a microdose (∼8 µL) ophthalmical spray. Methods: Cultured human conjunctival epithelial cells were exposed to the following treatments: (1) no treatment, (2) drop form of latanoprost without BAK (∼35 µL), (3) drop form of latanoprost with 0.01% BAK (∼35 µL), (4) ophthalmical spray form of latanoprost with 0.01% BAK delivered by the Optejet technology (∼8 µL). After 5 h, cells were assessed for changes in cytotoxicity, morphology, and inflammatory marker expression. Results: Latanoprost+BAK delivered by a drop induced cytotoxicity, cytoplasmic shrinkage, and loss of cell-cell contact, and expression of chemokine (C-C motif) ligand 2 and interleukin-6. In contrast, latanoprost+BAK delivered by the Optejet technology was both well tolerated and similar to no treatment controls and BAK-free latanoprost treatment. Conclusions: A microdose of latanoprost+BAK ophthalmical spray administered with the Optejet technology prevented the cytotoxicity associated with larger volumes found in eye drops. Precision dosing by the Optejet technology has the potential to decrease ocular surface disorder typically associated with eye drops containing preservatives.

2024-12-01·JOURNAL OF PHARMACEUTICAL SCIENCES

Study of polymer component migrated in medicinal product from transportation packaging component: A systematic assessment beyond regulatory expectations

Article

作者: Inamdar, Kavita ; Kale, Amit ; Gosar, Amit ; Zokande, Sandeep

Light Density Polyethylene (LDPE) bottles with a specific resin were chosen as container closure system (CCS) to fill "Latanoprost ophthalmic solution" (a generic drug product). As an alternative packaging component, additional manufacturer of LDPE bottles with the same characteristics as the previously selected LDPE bottles was chosen. The appropriateness of both packaging components was evaluated using an extractables and leachable (E&L) study and a formal stability programme that monitored quality of latanoprost ophthalmic solution. The results of relevant quality attributes in stability samples of latanoprost ophthalmic solution packed in both LDPE bottles were compared. It noticed that an unknown impurity in latanoprost ophthalmic solution packaged in LDPE bottles manufactured by an additional manufacturer. Further study revealed that this unknown impurity is Epsilon-caprolactam, a leachable of plastic used in the transportation of LDPE bottles. The leachability was validated through an extraction analysis of a plastic bag used for transportation. Thus, in certain cases, when the source of leachable is not identifiable by an E&L examination of primary, secondary, and tertiary packaging components, the assessment could be extended to include packaging components utilized throughout the supply chain.

101

项与拉坦前列素相关的新闻（医药）

2024-12-05

·医药速览

评估眼科药物代谢稳定性：体外模型的建立和应用

前言随着人口老龄化的加剧及人们生活方式的改变，眼部疾病的发病率愈发增高，且呈现低龄化患病趋势。屈光不正、干眼症、白内障、青光眼、黄斑病变等眼部疾病极大地影响人们的视力和生活质量。为改变这一现象，诸多科学家致力于进行眼科药物的研发，而在该类药物研发过程中，目前主要面临以下挑战，一是眼部各组织的复杂结构造成了许多生理屏障，二是眼部各组织中的代谢酶，使药物经过眼部各个组织到达病变部位发挥药效受到影响。本文将分别从眼球的基本结构、眼部组织代谢酶的表达与分布、眼科药物的给药方式等方面进行阐述，并介绍眼科药物的体外代谢稳定性研究体系的建立。眼球的基本结构及眼部组织代谢酶眼组织是身体最复杂的器官之一。其中眼球以晶状体为界被分为两部分，即眼前段和眼后段，晶状体及晶状体之前的眼结构被称为眼前段，约占眼球的1/3，主要由角膜、房水、虹膜、睫状体、结膜和晶状体组成，眼前段疾病主要有干眼症、白内障、青光眼等；晶状体之后的眼结构为眼后段，约占眼球的2/3，主要由玻璃体腔、视网膜、脉络膜、巩膜和视神经组成，眼后段疾病主要有年龄相关性黄斑变性、视网膜疾病如色素性视网膜炎、糖尿病性视网膜病变等[1]。图1. 眼球的基本结构[2] 眼球的复杂结构造成许多眼部屏障，如泪液流出、不同眼层的亲脂性差异、角膜前排泄、房水逆流、结膜吸收、玻璃体内的扩散、消除性分泌物以及通过角膜上皮、视网膜色素上皮和其他膜的通透性等，使得可能发生的病变部位多且复杂。同时，药物经过眼部各组织时，也会被其中的代谢酶所代谢[1,3,4]。这些屏障在正常情况下可以保护眼组织免受外部刺激，但当眼部病变时，则有可能阻碍药物到达病变部位发挥药效。与肝脏相比，虽然眼组织的代谢能力较弱，很少会被认为是药物的代谢器官，但在眼部各种结构中含有多种I相和II相代谢酶。表1. 不同眼部组织I相和II相代谢酶的表达与分布[5-6] 通过检测药物在眼组织的代谢情况，可以帮助化学家优化药物设计，以改善药物疗效和减少药物的副作用，此外还可以通过代谢激活改善眼科药物递送的潜力。眼部代谢酶目前已得到较好的表征，这使得它们成为眼科药物设计和开发中不可或缺的考虑因素，因此在进行眼科药物的设计时，可考虑通过眼部代谢酶作用来优化设计，如前药和联合药物等方法[7]。眼科药物的给药方式目前眼科药物有2种给药途径，即系统给药和眼组织局部给药。系统给药患者依从性高，但由于血脑屏障，常难以发挥药效。因此，对于眼科药物，临床上主要采用眼组织局部给药方式。眼组织局部给药又分为眼表给药、眼内给药和眼周给药。眼表给药是最常用的眼部给药方式，大约90%的药物以滴眼液的形式给药，主要用于治疗眼前段疾病，患者能够自行给药，但需要突破角膜屏障；眼内给药方式的生物利用度高，但由于是侵入性给药，患者依从性不高。其中玻璃体注射，主要用于治疗眼后段疾病，也可扩散到眼前段组织；前房注射主要用于治疗眼前段疾病，无法治疗眼后段疾病；眼周给药作用持久，可扩散到眼前段和眼后段，但有出血风险，且对眼后段的疾病治疗效果不如玻璃体注射[3,8]。图2. 眼部不同给药方式[2] 所以，用于治疗眼前段疾病的药物常采用眼表给药方式，其中以滴眼液形式给药最多。治疗眼后段疾病的药物常采用眼内给药和眼周给药方式，其中玻璃体注射是常用的方法。表2. 不同眼部给药方式的优势与局限性眼科药物的体外代谢稳定性研究体系的建立 1 实验体系和测试化合物选择眼表给药和眼内给药中的玻璃体注射分别是常用于治疗眼前段和眼后段疾病的给药方式。眼表给药需要突破角膜屏障，角膜由上皮、Bowman层、基质、后弹力层和内皮五个不同的层组成，角膜上皮是角膜屏障最重要的部分，约占角膜的10%，它具有多层角膜上皮细胞，会严重限制药物的眼部渗透，尤其是许多类型的亲水分子，基质约占角膜的90%，限制疏水分子的通过，角膜中表达多种代谢酶，分布在角膜各个组织层，其中角膜上皮和内皮细胞内代谢酶的种类和含量较多，眼表给药会受到角膜生理屏障和清除机制的双重影响[9,10]。图3. 角膜组织各层示意图[11] 玻璃体是半固体结构，在眼组织的前段和后段之间提供屏障，它是凝胶状结构，所以玻璃体中的药物分布模式是异质的，药物分布在很大程度上取决于药物的分子量和玻璃体病理生理状况，小分子可以在玻璃体中迅速扩散，而分子量超过40 kDa的线性分子或大于70 kDa的球状分子在玻璃体中的保留时间较长，且药物的消除和分布与药物通过玻璃体的扩散速率及其半衰期成正比。玻璃体内注射可以使玻璃体和眼内组织，包括脉络膜和视网膜中的局部药物浓度较高，有助于药物扩散至病变部位发挥药效[10]。对于在眼组织局部起效的药物，需要在眼组织进行代谢研究，针对眼表给药和玻璃体注射给药的眼科药物，药明康德DMPK对眼科药物在角膜组织和玻璃体液中的体外稳定性进行了研究。角膜组织和玻璃体液中均含有酯酶，Rhopressa（奈他地尔）会在角膜组织和玻璃体液中产生代谢，此外，我们选取了3个眼部用药的酯类前药Latanoprost（拉坦前列素）、Dipivefrin（地匹福林）、Mycophenolate mofetil（霉酚酸酯）进行验证。Rhopressa 是Rho激酶抑制剂，可用于治疗青光眼和角膜内皮损伤；Latanoprost为异丙酯化的前药，可被角膜中的酯酶水解转化为具有生物活性的拉坦前列素酸，可用于治疗青光眼；Dipivefrin是肾上腺素的双特戊酸二酯盐，角膜是地匹福林眼内水解的主要部位，其进入眼组织后在酶的作用下迅速水解成肾上腺素，可用于治疗青光眼[12]；Mycophenolate mofetil是霉酚酸的酯类前体药物，可用于治疗对甲状腺相关性眼病。这些测试化合物分别在不同种属的角膜组织和玻璃体液中进行稳定性验证实验。 2 测试化合物在不同种属角膜组织匀浆中的代谢将测试化合物Dipivefrin、Latanoprost、Mycophenolate mofetil、Rhopressa分别在兔子、猴、大鼠的角膜组织匀浆中，经37℃水浴孵育6小时后，所得实验结果如图4所示。所有测试化合物均有明显代谢趋势；其中Dipivefrin、Latanoprost、Mycophenolate mofetil在兔子和大鼠的角膜组织匀浆中的代谢速度明显快于猴的角膜组织匀浆；Rhopressa在兔子的角膜组织匀浆中的代谢速度稍快于猴和大鼠的角膜组织匀浆。图4. 测试化合物在不同种属角膜组织匀浆中的代谢稳定性 3 测试化合物在不同种属玻璃体液中的代谢将测试化合物Dipivefrin、Latanoprost、Mycophenolate mofetil、Rhopressa分别在兔子、猴、大鼠的玻璃体液中，经37℃水浴孵育6小时后，所得实验结果如图5所示，所有测试化合物在兔子、猴、大鼠的玻璃体液中均有明显代谢趋势，其中Dipivefrin、Mycophenolate mofeti、Rhopressa在兔子玻璃体液的代谢速度明显快于大鼠和猴的玻璃体液；Latanoprost在大鼠玻璃体液的代谢速度明显快于兔子和猴的玻璃体液。图5. 测试化合物在不同种属玻璃体液中的代谢稳定性以上结果表明，Rhopressa在兔子的角膜组织匀浆和玻璃体液中有明显代谢趋势，说明其可以被角膜组织和玻璃体液中的代谢酶所代谢；酯类前药Latanoprost、Dipivefrin、Mycophenolate mofetil在角膜组织匀浆和玻璃体液中均有明显代谢趋势，说明Latanoprost、Dipivefrin、Mycophenolate mofetil可以通过角膜组织和玻璃体液中的酯酶代谢，其中在角膜组织中的代谢速度明显快于玻璃体液，说明角膜组织中酯酶的表达可能高于玻璃体液，且这4个化合物在角膜组织和玻璃体液中代谢均具有种属差异，可能因为不同种属酶的表达与含量有所区别[6]。综上所述，我们分别建立了角膜组织匀浆代谢稳定性模型和玻璃体液代谢稳定性模型，用于评估眼科药物的体外代谢。对于眼表给药的药物和玻璃体注射给药的眼科药物，可在体外角膜组织和玻璃体液进行代谢研究，可选动物种属包括小鼠、大鼠、兔子、犬和猴。结语对于在眼组织局部起效的药物，需要在房水、玻璃体液、角膜等部位进行分布、代谢和消除过程的评估，体内代谢研究动物实验操作复杂，样品生物分析难度大，因此体外模型评估眼科药物的代谢稳定性有着更为直接和高效的优势。针对眼表给药和玻璃体注射给药的眼科药物，药明康德DMPK建立了评估眼科药物体外代谢稳定性的研究体系，可在体外角膜组织和玻璃体液中进行研究。该研究体系可针对眼科药物的研发进行早期化合物筛选、指导结构修饰、开发药物构效关系，还可以提供通过代谢激活以改善眼科药物递送的潜力。参考文献： [1] Fang G, Yang X, Wang Q, et al. Hydrogels-based ophthalmic drug delivery systems for treatment of ocular diseases. Mater Sci Eng C Mater Biol Appl. 2021,127:112212. [2] https://dmpkservice.wuxiapptec.com/cn/brochures/16-id/ [3] Amrutkar CS, Patil SB. Nanocarriers for ocular drug delivery: Recent advances and future opportunities. Indian J Ophthalmol. 2023,71(6):2355-2366. [4] Zhao L, Song J, Du Y, et al. Therapeutic applications of contact lens-based drug delivery systems in ophthalmic diseases. Drug Deliv. 2023,30(1):2219419. [5] Duvvuri S, Majumdar S, Mitra AK. Role of metabolism in ocular drug delivery. Curr Drug Metab. 2004,5(6):507-15. [6] Argikar UA, Dumouchel JL, Dunne CE, et al. Ocular non-P450 oxidative, reductive, hydrolytic, and conjugative drug metabolizing enzymes. Drug Metab Rev. 2017,49(3):372-394. [7] Al-Ghananeem AM, Crooks PA. Phase I and phase II ocular metabolic activities and the role of metabolism in ophthalmic prodrug and codrug design and delivery. Molecules. 2007,12(3):373-88. [8] Wei D, Pu N, Li SY, et al. Application of iontophoresis in ophthalmic practice: an innovative strategy to deliver drugs into the eye. Drug Deliv. 2023,30(1):2165736. [9] Melnyk S, Bollag WB. Aquaporins in the Cornea. Int J Mol Sci. 2024,25(7):3748. [10] Weng Y, Liu J, Jin S, et al. Nanotechnology-based strategies for treatment of ocular disease. Acta Pharm Sin B. 2017,7(3):281-291. [11] Price MO, Mehta JS, Jurkunas UV, et al. Corneal endothelial dysfunction: Evolving understanding and treatment options. Prog Retin Eye Res. 2021,82:100904. [12] Guo SS, Li C, Zhao ZG. Research progress of ocular prodrug and its pharmacokinetics. Chin Pharm J. 2022,57(9):684-690. （下滑查看更多）作者：何慧，唐登辉，秦雷磊，刘海娟，王翔凌，陈根富编辑：富罗娜·克里木，钱卉娟设计：倪德伟，张莹莹推荐阅读往期链接 “小小疫苗”养成记 | 医药公司管线盘点人人学懂免疫学 | 人人学懂免疫学（语音版）综述文章解读 | 文献略读 | 医学科普 | 医药前沿笔记 PROTAC技术 | 抗体药物 | 抗体药物偶联-ADC 核酸疫苗 | CAR技术 | 化学生物学温馨提示医药速览公众号目前已经有近12个交流群（好学，有趣且奔波于医药圈人才聚集于此）。进群加作者微信（yiyaoxueshu666）或者扫描公众号二维码添加作者，备注“姓名/昵称-企业/高校-具体研究领域/专业”，此群仅为科研交流群，非诚勿扰。简单操作即可星标⭐️医药速览，第一时间收到我们的推送 ①点击标题下方“医药速览” ②至右上角“...” ③点击“设为星标

核酸药物

2024-12-02

·GlobeNewswire-Health Care

Nicox’s Denali Phase 3 Trial of NCX 470 Fully Enrolled in China Earlier than Expected

Press ReleaseNicox’s Denali Phase 3 Trial of NCX 470 Fully Enrolled in China Earlier than Expected Confirms topline results expected to be reported Q3 2025 NCX 470 demonstrated robust efficacy and safety in topline results from first Phase 3 trial, Mont BlancNCX 470 partnering efforts will focus on routes for bringing the product to market in the U.S.Results from the NCX 470 Phase 3b Whistler Mechanism of Action trial expected in Q1 2025 December 2, 2024 – release at 7:30 am CETSophia Antipolis, FranceNicox SA (Euronext Growth Paris: FR0013018124, ALCOX), an international ophthalmology company, today announced that its Denali Phase 3 trial, evaluating the efficacy and safety of NCX 470 in patients with open-angle glaucoma or ocular hypertension, is now fully enrolled in China and screening has been closed. Completion of recruitment of patients in the U.S. for the trial was announced in July 2024 and therefore the target number of patients to be enrolled in the Denali trial has been met. Topline results are expected in Q3 2025.“Following completion of the recruitment of the Denali trial in the United States, we have seen an acceleration in the number of Chinese patients randomized in this multi-center international trial, allowing us to close Chinese patient recruitment earlier than expected.” said Doug Hubatsch, Chief Scientific Officer of Nicox. “I would like to thank the teams at both Nicox and Ocumension and the clinical staff and patients at our sites, as well as our partner organisations for their dedication through the final stages of the recruitment. We look forward to announcing the topline results in Q3 next year. Whilst we continue the final stages of this trial, we are also completing the additional development steps necessary to support the preparation of New Drug Applications in both the United States and China to ensure that these could be submitted as soon as possible after the receipt of the Denali topline data.” “NCX 470 continues to generate interest from potential commercialisation partners. With strong collaborations in Japan, China, Korea and Southeast Asia already in place, we are focussing on the route to commercialisation for NCX 470 in the United States, with potential for regional partnerships elsewhere.” added Emmet Purtill, VP Business Development. The Denali trial is evaluating the intraocular pressure (IOP) lowering efficacy of once-daily dosed NCX 470 ophthalmic solution 0.1% compared to latanoprost ophthalmic solution 0.005% in patients with open-angle glaucoma or ocular hypertension. It is a multi-country (U.S. and China) clinical trial financed equally by Nicox and Ocumension, Nicox’s exclusive licensee for China, Korea and Southeast Asia. The Denali trial, together with the Mont Blanc trial, was designed to fulfill the clinical regulatory requirements to support New Drug Application (NDA) submissions of NCX 470 in the U.S. and China. The company estimates that a U.S. NDA for NCX 470 could potentially be submitted in H1 2026, subject to the company entering into a partnership for the commercialization of NCX 470 in the U.S. or obtaining appropriate financing.Topline results from the first Phase 3 trial, Mont Blanc, showed the IOP-lowering effect from baseline was 8.0 to 9.7 mmHg for NCX 470 vs. 7.1 to 9.4 mmHg for latanoprost. Statistical non-inferiority was met vs. latanoprost in the primary efficacy analysis and 4 out of 6 timepoints additionally demonstrated superiority; the trial therefore met the efficacy requirements for approval in the U.S. NCX 470 was well tolerated and discontinuation rates were low. The results of the Mont Blanc trial have been published in the prestigious American Journal of Ophthalmology, and numerous post hoc analyses have been presented. Full details of all presentations and publications can be found at nicox.com/pipeline-markets-and-science/#publications.About NCX 470NCX 470 is a novel nitric oxide (NO)-donating bimatoprost eye drop that leverages the potent IOP lowering effects of NO and prostaglandin analogs (PGAs). NCX 470 incorporates Nicox’s proprietary NO-donating research platform and bimatoprost in a single molecule. NCX 470 is designed to release bimatoprost and NO into the eye to lower IOP by two different pathways in patients with open-angle glaucoma or ocular hypertension. NO is a well-known small, naturally occurring signaling molecule that plays a key role in the regulation of IOP through activation of soluble guanylate cyclase. NO brings additional IOP-lowering efficacy by enhancing aqueous humor drainage from the eye via a different mechanism of action to that of PGAs. Bimatoprost, marketed under the brand name LUMIGAN® by AbbVie, Inc., is the leading branded PGA. PGAs are the most widely used class of drugs for IOP-lowering in patients with open-angle glaucoma or ocular hypertension.About NicoxNicox SA is an international ophthalmology company developing innovative solutions to help maintain vision and improve ocular health. Nicox’s lead program in clinical development is NCX 470 (bimatoprost grenod), a novel nitric oxide-donating bimatoprost eye drop, for lowering intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Nicox also has a preclinical research program on NCX 1728, a nitric oxide-donating phosphodiesterase-5 inhibitor, with Glaukos. Nicox’s first product, VYZULTA® in glaucoma, licensed exclusively worldwide to Bausch + Lomb, is available commercially in the U.S. and over 15 other territories. Nicox generates revenue from ZERVIATE® in allergic conjunctivitis, licensed in multiple geographies, including to Harrow, Inc. in the U.S., and Ocumension Therapeutics in the Chinese and in the majority of Southeast Asian markets. Nicox, headquartered in Sophia Antipolis, France, is listed on Euronext Growth Paris (Ticker symbol: ALCOX) and is part of the CAC Healthcare index. For more information www.nicox.comAnalyst coverageH.C. Wainwright & Co Yi Chen New York, U.S. The views expressed by analysts in their coverage of Nicox are those of the author and do not reflect the views of Nicox. Additionally, the information contained in their reports may not be correct or current. Nicox disavows any obligation to correct or to update the information contained in analyst reports.Contacts NicoxGavin SpencerChief Executive OfficerT +33 (0)4 97 24 53 00communications@nicox.com DisclaimerThe information contained in this document may be modified without prior notice. This information includes forward-looking statements. Such forward-looking statements are not guarantees of future performance. These statements are based on current expectations or beliefs of the management of Nicox S.A. and are subject to a number of factors and uncertainties that could cause actual results to differ materially from those described in the forward-looking statements. Nicox S.A. and its affiliates, directors, officers, employees, advisers or agents, do not undertake, nor do they have any obligation, to provide updates or to revise any forward-looking statements.Risks factors which are likely to have a material effect on Nicox’s business are presented in section 3 of the “Rapport Annuel 2023” and in section 4 of the “Rapport semestriel financier et d’activité 2024” which are available on Nicox’s website (www.nicox.com).Finally, this press release may be drafted in the French and English languages. If both versions are interpreted differently, the French language version shall prevail.Nicox S.A.Sundesk Sophia Antipolis, Bâtiment C, Emerald Square, Rue Evariste Galois, 06410 Biot, FranceT +33 (0)4 97 24 53 00 Attachment EN_DenaliLastPatient_PR_20241202_FINAL

临床3期临床结果引进/卖出

2024-11-22

·米内网

10亿眼科明星药集采止跌！TOP20洗牌，康弘、兴齐……国产品牌突围，恒瑞、信达新药来袭

精彩内容近期，眼科用药市场波澜再起。成都康弘药业集团的玻璃酸钠滴眼液、苏州乐珠制药的盐酸氮䓬斯汀滴眼液等4个产品同日获批。今年以来，眼科用药已有20个品种（133个受理号）获批上市。米内网数据显示，眼科用药在近年中国公立医疗机构终端销售规模均超过100亿元，2024年上半年同比下滑6.21%。5个国采品种中仅玻璃酸钠滴眼液正增长，从TOP20来看，康柏西普眼用注射液领跑，康弘、兴齐等国产品牌突围。眼科用药有52个品种（270个受理号）报产在审，辰欣佛都药业、扬州中宝药业等企业冲击首仿，5个新药亮眼。 4个眼科用药同日获批，兴齐、齐鲁、万汉制药领跑过评榜 11月以来眼科用药获批情况来源：米内网中国申报进度（MED）数据库 11月21日，国家药监局官网显示，华熙生物科技的玻璃酸钠滴眼液、成都康弘药业集团的玻璃酸钠滴眼液、苏州乐珠制药的盐酸氮䓬斯汀滴眼液和地夸磷索钠滴眼液同日获批，视同过评。在此之前，妥布霉素滴眼液第2家过评企业诞生，苏州乐珠制药和浙江莎普爱思药业均以仿制4类报产同日获批，视同过评。今年以来，眼科用药已有20个品种（133个受理号）获批上市，数量超过2023年全年。过评企业数10家及以上的眼科用药来源：米内网中国申报进度（MED）数据库截至目前，眼科用药有24个品种（256个品规）过评，7个品种有10家及以上企业过评，其中，玻璃酸钠滴眼液（41家）最为火热，其次是盐酸莫西沙星滴眼液（40家）、地夸磷索钠滴眼液（30家）。 8个品种独家过评，分别为成都普什制药的氯化钠滴眼液、沈阳兴齐眼药的环孢素滴眼液(Ⅱ)、四川禾亿制药的盐酸利多卡因眼用凝胶、兆科(广州)眼科药物的贝美素噻吗洛尔滴眼液、Maxmind的拉坦前列素滴眼液、汇禹远和(海南)药业的复方托吡卡胺滴眼液、山东绅联药业的盐酸环喷托酯滴眼液、苏州欧康维视生物的盐酸西替利嗪滴眼液，其中，山东绅联药业的盐酸环喷托酯滴眼液和苏州欧康维视生物的盐酸西替利嗪滴眼液均在今年获批。过评5个及以上眼科用药的集团来源：米内网中国申报进度（MED）数据库从集团过评品种数来看，沈阳兴齐眼药、齐鲁制药、中山万汉制药领跑，各有8个；远大健康、成都普什制药、欧康维视生物各有6个；扬子江药业、众生药业、莎普爱思药业、苏州乐珠制药等6家各有5个。 10亿明星药集采止跌！TOP20洗牌，康弘、兴齐……国产品牌突围米内网数据显示，近年中国公立医疗机构终端眼科用药（化学药+生物药）销售规模均超过100亿元，2024年上半年同比下滑6.21%，眼部血管病变治疗药、抗感染药、抗炎药是3大畅销小类。2024年上半年中国公立医疗机构终端眼科用药TOP5集团来源：米内网中国公立医疗机构药品终端竞争格局从集团格局来看，诺华集团、康弘药业、参天制药、沈阳兴齐眼药、拜耳位居前五，其中，康弘药业和沈阳兴齐眼药两家国内药企逆势上扬，销售额增速分别为25.74%和4.82%。 2024年上半年中国公立医疗机构终端眼科用药产品TOP20来源：米内网中国公立医疗机构药品终端竞争格局产品TOP20中，13个产品销售额超过1亿元，康柏西普眼用注射液是超10亿元的重磅品种，右旋糖酐羟丙甲纤维素滴眼液为新上榜产品。从在销企业数来看，妥布霉素滴眼液最多，有21家；其次是玻璃酸钠滴眼液和左氧氟沙星滴眼液均超过10家。目前，眼科用药已有5个产品纳入国采，左氧氟沙星滴眼液（第三批）、玻璃酸钠滴眼液（第四批）、地夸磷索钠滴眼液（第九批）均在产品TOP20之列。5个集采产品中仅有玻璃酸钠滴眼液正增长，4个产品均有下滑，地夸磷索钠滴眼液跌幅最大。近年中国公立医疗机构终端玻璃酸钠滴眼液销售情况（单位：万元）来源：米内网中国公立医疗机构药品终端竞争格局玻璃酸钠滴眼液在中国公立医疗机构终端销售额峰值超过10亿元，受集采影响连续下滑后，2023年止跌回升，2024年上半年同比增长近5%，是眼科用药TOP3产品。该产品目前有54家企业拥有生产批文，参天制药、URSAPHARM、成都普什制药的市场份额位居前三。 2024年上半年中国公立医疗机构终端眼科用药品牌TOP20来源：米内网中国公立医疗机构药品终端竞争格局品牌TOP20中，成都康弘生物的康柏西普眼用注射液、诺华的雷珠单抗注射液、拜耳的阿柏西普眼内注射溶液位居前三，爱尔康的右旋糖酐羟丙甲纤维素滴眼液和沈阳兴齐眼药的加替沙星眼用凝胶则是新上榜品牌。 4个品牌增速超过20%，其中，成都康弘生物的康柏西普眼用注射液、沈阳兴齐眼药的环孢素滴眼液(Ⅱ)、珠海亿胜生物制药的牛碱性成纤维细胞生长因子滴眼液3个均是独家产品。从品牌数量来看，诺华最多，有4个上榜；参天制药和沈阳兴齐眼药各有2个上榜。辰欣、兆科……冲击首仿，恒瑞、信达新药来袭 11月22日，CDE官网显示，江苏福邦药业的玻璃酸钠滴眼液以仿制4类报产在审。在此之前，辰欣佛都药业的盐酸奥布卡因滴眼液、深圳市宇健生物医药|中山万汉制药的地夸磷索钠滴眼液同日报产在审。截至目前，眼科用药有52个品种（270个受理号）报产在审，地夸磷索钠滴眼液最火，有27家企业，其次是玻璃酸钠滴眼液，有20家。从企业数量来看，14家企业有5个及以上产品报产在审，其中，莎普爱思药业和宁波视方医药科技各有7个，沈阳兴齐眼药、兆科药业、石家庄格瑞药业等8家各有6个。国内无仿制药获批且报产在审的眼科用药来源：米内网中国申报进度（MED）数据库曲伏噻吗滴眼液、氟比洛芬钠滴眼液、盐酸依匹斯汀滴眼液等眼科用药国内暂无仿制药获批，辰欣佛都药业、扬州中宝药业、兆科(广州)眼科药物等企业有望拿下首仿。眼科用药新药报产在审情况来源：米内网中国申报进度（MED）数据库此外，信达生物制药(苏州)的替妥尤单抗注射液、山东博安生物技术的阿柏西普眼内注射溶液等5个眼科用药新药报产在审，其中，成都盛迪医药的SHR8058滴眼液为化药1类新药。资料来源：国家药监局官网、米内网数据库等注：米内网《中国公立医疗机构药品终端竞争格局》，统计范围是：中国城市公立医院、县级公立医院、城市社区中心以及乡镇卫生院，不含民营医院、私人诊所、村卫生室；上述销售额以产品在终端的平均零售价计算。如有疏漏，欢迎指正！本文为原创稿件，转载请注明来源和作者，否则将追究侵权责任。投稿及报料请发邮件到872470254@qq.com稿件要求详询米内微信首页菜单栏商务及内容合作可联系QQ：412539092 【分享、点赞、在看】点一点不失联哦

上市批准一致性评价医药出海

100 项与拉坦前列素相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D00356	拉坦前列素	S01EE01	DB00654

研发状态

批准上市

10 条最早获批的记录,

后查看更多信息

适应症	国家/地区	公司	日期
青光眼	日本	Viatris, Inc.	1999-03-12
开角型青光眼	美国	Upjohn US 2 LLC	1996-06-05
高眼压症	美国	Upjohn US 2 LLC	1996-06-05

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
干眼综合征	临床前	德国	Novaliq GmbH	2024-05-15

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04133311 (CTgov)	临床3期	开角型青光眼	386	DE-130A (DE-130A)	憲積夢蓋築網繭製網鬱(製膚鏇鬱醖蓋廠壓糧餘) = 醖廠選廠繭構築壓鏇艱糧餘廠憲淵鹽鹹積膚衊 (鏇獵構繭積憲窪鑰醖餘, 獵餘夢鬱齋醖製遞艱餘 ~ 繭願衊鏇網築範廠願窪) 更多	-	2024-05-28
				Xalatan® (Xalatan®)	憲積夢蓋築網繭製網鬱(製膚鏇鬱醖蓋廠壓糧餘) = 觸顧構繭獵遞膚淵鬱窪糧餘廠憲淵鹽鹹積膚衊 (鏇獵構繭積憲窪鑰醖餘, 夢簾繭鏇襯衊觸壓膚構 ~ 窪鑰積窪網夢鏇糧艱襯) 更多
EURETINA2023	N/A	葡萄膜渗漏综合征	-	Topical Latanoprost	襯憲願夢淵選膚窪鹽遞(餘鑰遞鑰築膚壓醖蓋簾) = exacerbation of uveal effusion in nanophthalmic eyes 鑰壓顧壓築糧製範醖壓 (選窪範觸獵簾淵繭鹽襯 )	-	2023-10-05
				Topical Corticosteroids
NCT04405245 (CTgov)	临床2期	开角型青光眼	194	AKB-9778 4%+Latanoprost ophthalmic solution (AKB-9778 4% QD + Latanoprost)	窪壓廠遞糧壓鬱醖築鑰(廠鬱膚獵淵願膚窪鏇積) = 網構築鑰願鬱襯餘壓鬱壓夢糧選襯鬱鹽繭膚衊 (製蓋鬱積襯網艱襯糧鹽, 膚選鏇選衊簾餘鬱範顧 ~ 鬱鏇鏇觸鹽餘壓構廠膚) 更多	-	2023-05-25
				AKB-9778 4%+Latanoprost ophthalmic solution (AKB-9778 4% BID + Latanoprost)	窪壓廠遞糧壓鬱醖築鑰(廠鬱膚獵淵願膚窪鏇積) = 範糧艱齋顧鏇製獵鹹齋壓夢糧選襯鬱鹽繭膚衊 (製蓋鬱積襯網艱襯糧鹽, 構鏇製夢鏇構獵簾廠願 ~ 齋簾觸鬱衊夢獵膚膚餘) 更多
ARVO2023	N/A	青光眼	107	Preservative-free surfactant-free latanoprost eyedrop	鹽願選網鏇鏇鑰積糧艱(鹽鹹廠窪廠壓淵鹹願齋) = 鏇鹽獵壓觸糧鹹範衊憲壓繭繭範餘觸製廠廠鹽 (鹽鬱願齋築蓋鹹窪窪觸 )	-	2023-04-23
NCT03949244 (CTgov)	临床4期	开角型青光眼	47	Nailfold capillaroscopy+Latanoprost 0.005% (Latanoprost 0.005%)	餘淵遞顧艱積構膚顧憲(淵顧積積鏇選糧鑰遞築) = 膚淵觸鹽鬱餘蓋鹽鹹鹽蓋襯鏇網積築繭襯糧鹹 (遞淵夢築蓋鏇獵衊憲衊, 膚膚繭鹽齋鏇遞範鑰鏇 ~ 齋築積齋選廠艱艱鏇範) 更多	-	2021-08-23
				Nailfold capillaroscopy+Latanoprost bunod 0.024% (Latanoprost Bunod 0.024%)	餘淵遞顧艱積構膚顧憲(淵顧積積鏇選糧鑰遞築) = 簾築糧鬱淵襯鹹蓋願窪蓋襯鏇網積築繭襯糧鹹 (遞淵夢築蓋鏇獵衊憲衊, 鏇齋繭鏇淵選鏇遞糧膚 ~ 鑰製憲齋鏇範遞醖構鹽) 更多
NCT00934089 (CTgov)	临床2期	开角型青光眼	31	Taprenepag+Latanoprost (Taprenepag+Latanoprost)	糧襯鹹鏇網遞積製鹹簾(構簾窪鬱簾觸餘襯選鏇) = 願壓鬱醖築鬱積廠壓簾範夢簾製憲廠鑰選憲簾 (廠網糧鹽艱壓壓襯築獵, 鑰顧遞襯鹽膚鹽製鏇廠 ~ 齋鏇壓願鹹願遞鑰鹽淵) 更多	-	2021-05-03
				Taprenepag+Latanoprost (Taprenepag+Latanoprost Vehicle)	糧襯鹹鏇網遞積製鹹簾(構簾窪鬱簾觸餘襯選鏇) = 醖衊製壓積壓遞遞鏇範範夢簾製憲廠鑰選憲簾 (廠網糧鹽艱壓壓襯築獵, 齋鏇鹽範壓糧觸築鹽膚 ~ 獵觸鬱遞鬱夢壓遞窪鏇) 更多
NCT02466399 (CTgov)	临床2期	开角型青光眼	80	POLAT-001 (POLAT-001)	蓋範窪遞齋構憲鹹鑰鏇(範糧淵獵淵顧鬱鏇顧糧) = 鏇鬱淵膚餘襯鏇繭醖廠鏇繭鏇願糧壓齋顧網製 (鑰醖築醖顧網膚艱襯範, 憲獵遞繭製齋醖選衊夢 ~ 鏇蓋鬱窪醖憲鹽艱夢夢) 更多	-	2020-11-16
				Latanoprost ophthalmic solution (Latanoprost Ophthalmic Solution)	蓋範窪遞齋構憲鹹鑰鏇(範糧淵獵淵顧鬱鏇顧糧) = 淵遞醖築憲壓鹽夢襯齋鏇繭鏇願糧壓齋顧網製 (鑰醖築醖顧網膚艱襯範, 遞淵鹹膚蓋夢廠鏇齋蓋 ~ 鹽襯範窪願憲廠繭鏇壓) 更多
NCT02017327 (CTgov)	临床4期	开角型青光眼	379	Monoprost (Monoprost)	糧網鏇艱餘鹽衊願夢鹹(艱醖齋糧簾獵餘鏇範願): P-Value = 0.0045	-	2020-04-02
				Lumigan 0.01% (Lumigan 0.01%)
NCT04178863 (Pubmed \| Clin Ophthalmol)	临床4期	青光眼	72	Latanoprost 0.005%	廠範鑰獵齋膚鹽遞獵網(鑰範膚膚窪膚齋構壓醖) = 鑰鏇壓遞淵築鑰夢觸襯遞壓廠範範鏇範遞獵憲 (選繭遞蓋網築憲窪糧衊 ) 更多	-	2020-01-01
				Timolol maleate 0.5%	廠範鑰獵齋膚鹽遞獵網(鑰範膚膚窪膚齋構壓醖) = 觸齋鬱製繭憲鬱簾壓餘遞壓廠範範鏇範遞獵憲 (選繭遞蓋網築憲窪糧衊 ) 更多
NCT02801617 (COMPLIANCE, CTgov)	临床3期	开角型青光眼	116	GAAP Ofteno®+PRO-067 (Sequence 1 (PRO-067))	範窪膚網餘醖襯觸範願(製構醖醖淵憲膚淵積簾) = 糧鬱願築醖憲淵選艱鹽窪夢遞獵鹽簾夢艱膚衊 (願範鹽窪築膚製蓋簾夢, 選觸鑰簾製顧簾網壓壓 ~ 襯簾憲壓鬱壓獵顧積壓) 更多	-	2019-10-28
				GAAP Ofteno®+PRO-067 (Sequence 2 (GAAP Ofteno®))	範窪膚網餘醖襯觸範願(製構醖醖淵憲膚淵積簾) = 憲蓋鑰窪醖鹽鑰醖鹹餘窪夢遞獵鹽簾夢艱膚衊 (願範鹽窪築膚製蓋簾夢, 觸構艱衊繭鹹選窪簾遞 ~ 製獵選鑰鏇鹽簾築鹹構) 更多