Mayo College of Medicine, Jacksonville, FL, USA.
Expert Rev Clin Pharmacol. 2013 Mar;6(2):103-13. doi: 10.1586/ecp.12.81.
Aflibercept, a soluble receptor molecule that binds VEGF, has been recently approved for the treatment of exudative age-related macular degeneration. This fusion protein with binding sequences from VEGF receptors 1 and 2 possesses high binding affinity for isomers of VEGF-A, VEGF-B and PlGF, and prevents VEGF from initiating proliferation and migration of vascular endothelial cells. Phase III trials showed that intravitreal aflibercept given monthly or every 2 months produces visual improvement and decrease in macular thickness comparable with monthly ranibizumab. The second year of the trials demonstrated that as-needed aflibercept maintained vision with few required injections. Aflibercept promises to decrease the treatment burden faced by patients with exudative age-related macular degeneration.
阿柏西普是一种可溶性受体分子,可与 VEGF 结合,最近已被批准用于治疗渗出性年龄相关性黄斑变性。这种融合蛋白具有与 VEGF 受体 1 和 2 的结合序列,对 VEGF-A、VEGF-B 和 PlGF 的异构体具有高结合亲和力,并可阻止 VEGF 引发血管内皮细胞的增殖和迁移。III 期临床试验表明,每月或每 2 个月玻璃体内注射阿柏西普可产生与每月雷珠单抗相当的视力改善和黄斑厚度减少。试验的第二年表明,按需注射阿柏西普可保持视力,所需注射次数较少。阿柏西普有望减轻渗出性年龄相关性黄斑变性患者的治疗负担。