Retina Associates Ltd , Elmhurst, IL, USA.
Department of Ophthalmology, Cullen Eye Institute, Baylor College of Medicine , Houston, TX, USA.
Expert Opin Biol Ther. 2020 Sep;20(9):999-1008. doi: 10.1080/14712598.2020.1782379. Epub 2020 Jul 3.
The development of intravitreal anti-vascular endothelial growth factor (VEGF) therapy has revolutionized management of neovascular age-related macular degeneration (nAMD) and serves as the standard of care for treating this chronic, progressive disease. One shortcoming is the need for frequent intravitreal injections to maintain visual gains, which has led to pursuit of long-acting agents to reduce treatment burden.
A literature search was conducted using the keywords 'abicipar pegol' and 'DARPin' on PubMed.
DARPin (Designed Ankyrin Repeat Proteins) molecules such as abicipar pegol offer potential therapeutic advantages over antibodies or antibody fragments, including high affinity, stability, and high molar concentration. The phase III SEQUOIA and CEDAR clinical trials suggest that abicipar allows >90% of patients to maintain stable vision with 12-week dosing intervals, comparable to results achieved with monthly ranibizumab injections. Relative to other anti-VEGF agents, intraocular inflammation has been noted in a concerning percentage of patients, which is hypothesized to be related to the manufacturing process rather than the drug itself. Modifications to reduce pro-inflammatory components resulted in reduced inflammation (8.9%) in the MAPLE study. If this high inflammation rate can be further reduced, abicipar has the potential to decrease treatment burden for nAMD patients.
玻璃体内抗血管内皮生长因子（VEGF）治疗的发展彻底改变了新生血管性年龄相关性黄斑变性（nAMD）的治疗方法，并成为治疗这种慢性进行性疾病的标准治疗方法。其缺点之一是需要频繁进行玻璃体内注射以维持视力的提高，这促使人们寻求长效药物来减轻治疗负担。
使用“abicipar pegol”和“DARPin”等关键词在 PubMed 上进行了文献检索。
DARPin（设计的锚蛋白重复蛋白）分子，如 abicipar pegol，与抗体或抗体片段相比具有潜在的治疗优势，包括高亲和力、稳定性和高摩尔浓度。III 期 SEQUOIA 和 CEDAR 临床试验表明，abicipar 允许>90%的患者在 12 周的给药间隔内保持稳定的视力，与每月雷珠单抗注射的结果相当。与其他抗 VEGF 药物相比，在相当大比例的患者中观察到眼内炎症，这被假设与制造过程而非药物本身有关。为了减少炎症成分，在 MAPLE 研究中对其进行了改良，从而使炎症减少（8.9%）。如果这种高炎症率能够进一步降低，那么 abicipar 有可能减轻 nAMD 患者的治疗负担。
