{"title":"Treatment of Retinal/Choroidal Vascular Diseases by Sustained Delivery of VEGF Receptor Tyrosine Kinase Inhibitors.","authors":"Dilsher S Dhoot","doi":"10.1016/j.ajo.2025.06.010","DOIUrl":null,"url":null,"abstract":"<p><strong>Purpose: </strong>To review current investigational strategies utilizing sustained delivery of VEGF receptor tyrosine kinase inhibitors (TKIs) for the treatment of retinal and choroidal vascular diseases.</p><p><strong>Design: </strong>Narrative review.</p><p><strong>Methods: </strong>A comprehensive review of preclinical and clinical studies evaluating the safety, efficacy, and durability of VEGF receptor TKIs delivered via sustained-release platforms, including intravitreal hydrogel implants, suprachoroidal injections, subcutaneous delivery systems, and oral formulations.</p><p><strong>Results: </strong>Multiple VEGF receptor TKIs, including axitinib, sunitinib, vorolanib, and dendranib, are under evaluation for sustained treatment of neovascular age-related macular degeneration (nAMD), diabetic macular edema (DME), and diabetic retinopathy (DR). Delivery platforms such as bioerodible implants (OTX-TKI/axitinib, EYP-1901/vorolanib), suprachoroidal injections (CLS-AX/axitinib), microparticle suspensions (GB-102/sunitinib), and oral or subcutaneous therapies (X-82, D-4517.2) have demonstrated variable degrees of treatment durability, reduction in anti-VEGF injection burden, and maintenance of anatomic and functional outcomes in early phase studies. Safety profiles have generally been favorable, though certain formulations showed dose-dependent adverse effects.</p><p><strong>Conclusions: </strong>Sustained delivery of VEGF receptor TKIs represents a promising therapeutic paradigm for retinal and choroidal vascular diseases, potentially reducing treatment burden while maintaining efficacy. Continued evaluation through larger, controlled clinical trials is essential to validate these early findings and define the role of these agents in clinical practice.</p>","PeriodicalId":7568,"journal":{"name":"American Journal of Ophthalmology","volume":" ","pages":""},"PeriodicalIF":4.1000,"publicationDate":"2025-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"American Journal of Ophthalmology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.ajo.2025.06.010","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"OPHTHALMOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
Purpose: To review current investigational strategies utilizing sustained delivery of VEGF receptor tyrosine kinase inhibitors (TKIs) for the treatment of retinal and choroidal vascular diseases.
Design: Narrative review.
Methods: A comprehensive review of preclinical and clinical studies evaluating the safety, efficacy, and durability of VEGF receptor TKIs delivered via sustained-release platforms, including intravitreal hydrogel implants, suprachoroidal injections, subcutaneous delivery systems, and oral formulations.
Results: Multiple VEGF receptor TKIs, including axitinib, sunitinib, vorolanib, and dendranib, are under evaluation for sustained treatment of neovascular age-related macular degeneration (nAMD), diabetic macular edema (DME), and diabetic retinopathy (DR). Delivery platforms such as bioerodible implants (OTX-TKI/axitinib, EYP-1901/vorolanib), suprachoroidal injections (CLS-AX/axitinib), microparticle suspensions (GB-102/sunitinib), and oral or subcutaneous therapies (X-82, D-4517.2) have demonstrated variable degrees of treatment durability, reduction in anti-VEGF injection burden, and maintenance of anatomic and functional outcomes in early phase studies. Safety profiles have generally been favorable, though certain formulations showed dose-dependent adverse effects.
Conclusions: Sustained delivery of VEGF receptor TKIs represents a promising therapeutic paradigm for retinal and choroidal vascular diseases, potentially reducing treatment burden while maintaining efficacy. Continued evaluation through larger, controlled clinical trials is essential to validate these early findings and define the role of these agents in clinical practice.
期刊介绍：
The American Journal of Ophthalmology is a peer-reviewed, scientific publication that welcomes the submission of original, previously unpublished manuscripts directed to ophthalmologists and visual science specialists describing clinical investigations, clinical observations, and clinically relevant laboratory investigations. Published monthly since 1884, the full text of the American Journal of Ophthalmology and supplementary material are also presented online at www.AJO.com and on ScienceDirect.
The American Journal of Ophthalmology publishes Full-Length Articles, Perspectives, Editorials, Correspondences, Books Reports and Announcements. Brief Reports and Case Reports are no longer published. We recommend submitting Brief Reports and Case Reports to our companion publication, the American Journal of Ophthalmology Case Reports.
Manuscripts are accepted with the understanding that they have not been and will not be published elsewhere substantially in any format, and that there are no ethical problems with the content or data collection. Authors may be requested to produce the data upon which the manuscript is based and to answer expeditiously any questions about the manuscript or its authors.
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