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Discovery of novel thiophene-3-carboxamide derivatives as potential VEGFR-2 inhibitors with anti-angiogenic properties.发现新型噻吩-3-甲酰胺衍生物作为具有抗血管生成特性的潜在 VEGFR-2 抑制剂。
Bioorg Chem. 2024 Jun;147:107358. doi: 10.1016/j.bioorg.2024.107358. Epub 2024 Apr 9.
2
Drug-like properties of tyrosine kinase inhibitors in ophthalmology: Formulation and topical availability.眼科中酪氨酸激酶抑制剂的类药性:制剂和局部可用性。
Int J Pharm. 2024 Apr 25;655:124018. doi: 10.1016/j.ijpharm.2024.124018. Epub 2024 Mar 19.
3
Corticosteroid implants for chronic non-infectious uveitis.皮质类固醇植入物治疗慢性非感染性葡萄膜炎。
Cochrane Database Syst Rev. 2023 Aug 29;8(8):CD010469. doi: 10.1002/14651858.CD010469.pub4.
4
Biology and therapeutic targeting of vascular endothelial growth factor A.血管内皮生长因子 A 的生物学和治疗靶向。
Nat Rev Mol Cell Biol. 2023 Nov;24(11):816-834. doi: 10.1038/s41580-023-00631-w. Epub 2023 Jul 25.
5
Tyrosine Kinase Inhibitors and their role in treating neovascular age-related macular degeneration and diabetic macular oedema.酪氨酸激酶抑制剂及其在治疗新生血管性年龄相关性黄斑变性和糖尿病性黄斑水肿中的作用。
Eye (Lond). 2023 Dec;37(18):3725-3733. doi: 10.1038/s41433-023-02610-z. Epub 2023 Jun 7.
6
A Randomized Controlled Trial of OPT-302, a VEGF-C/D Inhibitor for Neovascular Age-Related Macular Degeneration.随机对照试验:OPG302,一种用于新生血管性年龄相关性黄斑变性的 VEGF-C/D 抑制剂。
Ophthalmology. 2023 Jun;130(6):588-597. doi: 10.1016/j.ophtha.2023.02.001. Epub 2023 Feb 6.
7
Diabetic retinopathy: Looking forward to 2030.糖尿病视网膜病变:展望 2030 年。
Front Endocrinol (Lausanne). 2023 Jan 9;13:1077669. doi: 10.3389/fendo.2022.1077669. eCollection 2022.
8
Current and Novel Therapeutic Approaches for Treatment of Neovascular Age-Related Macular Degeneration.当前和新型治疗方法治疗新生血管性年龄相关性黄斑变性。
Biomolecules. 2022 Nov 3;12(11):1629. doi: 10.3390/biom12111629.
9
Recent Advances in Age-Related Macular Degeneration Therapies.年龄相关性黄斑变性治疗的最新进展。
Molecules. 2022 Aug 10;27(16):5089. doi: 10.3390/molecules27165089.
10
Aflibercept versus Faricimab in the Treatment of Neovascular Age-Related Macular Degeneration and Diabetic Macular Edema: A Review.阿柏西普与 faricimab 在新生血管性年龄相关性黄斑变性和糖尿病性黄斑水肿治疗中的比较:综述。
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EYP-1901 在新生血管性年龄相关性黄斑变性和糖尿病眼病中的作用:I/II 期临床试验综述。

Role of EYP-1901 in neovascular age-related macular degeneration and diabetic eye diseases: review of Phase I/II trials.

机构信息

University of Illinois Chicago, Chicago, IL 60607, USA.

Department of Surgery, University of Illinois College of Medicine, Peoria, IL 61605, USA.

出版信息

Ther Deliv. 2024;15(11):829-843. doi: 10.1080/20415990.2024.2406226. Epub 2024 Oct 3.

DOI:10.1080/20415990.2024.2406226
PMID:39360955
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11497975/
Abstract

EYP-1901 (Duravyu) has demonstrated promising outcomes in Phases I and II clinical trials for the treatment of neovascular age-related macular degeneration (nAMD) and diabetic macular edema (DME)/diabetic retinopathy. This innovative treatment capitalizes on the potent anti-angiogenic properties of vorolanib, an inhibitor that targets all isoforms of VEGF, effectively mitigating the pathological neovascularization and vascular permeability that underpin these retinal conditions. EYP-1901 is integrated with the Durasert drug delivery system to administer a sustained release of vorolanib directly to the posterior segment of the eye. This delivery system ensures a consistent therapeutic effect over an extended period and significantly reduces the frequency of clinical interventions required, offering a more convenient treatment regimen while maintaining patient safety.

摘要

EYP-1901(杜拉鲁宾)在治疗新生血管性年龄相关性黄斑变性(nAMD)和糖尿病性黄斑水肿(DME)/糖尿病性视网膜病变的 I 期和 II 期临床试验中显示出了有前景的结果。这种创新的治疗方法利用了 vorolanib 的强大抗血管生成特性,vorolanib 是一种针对所有 VEGF 同工型的抑制剂,能够有效减轻这些视网膜疾病中潜在的病理性新生血管形成和血管通透性。EYP-1901 与 Durasert 药物输送系统相结合,可将 vorolanib 持续释放到眼睛的后段。这种输送系统可确保在较长时间内保持一致的治疗效果,并显著减少所需的临床干预次数,提供更方便的治疗方案,同时保持患者安全。