Pegaptanib, a targeted anti-VEGF aptamer for ocular vascular disease

被引：1151

作者：

Ng, EWM ^{[1
]}

Shima, DT ^{[1
]}

Calias, P ^{[1
]}

Cunningham, ET ^{[1
]}

Guyer, DR ^{[1
]}

Adamis, AP ^{[1
]}

机构：

[1] Eyetech Pharmaceut Inc, New York, NY 10036 USA

来源：

NATURE REVIEWS DRUG DISCOVERY | 2006年 / 5卷 / 02期

关键词：

D O I：

10.1038/nrd1955

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Aptamers are oligonucleotide ligands that are selected for high-affinity binding to molecular targets. Pegaptanib sodium (Macugen; Eyetech Pharmaceuticals/Pfizer) is an RNA aptamer directed against vascular endothelial growth factor (VEGF)-165, the VEGF isoform primarily responsible for pathological ocular neovascularization and vascular permeability. After nearly a decade of preclinical development to optimize and characterize its biological effects, pegaptanib was shown in clinical trials to be effective in treating choroidal neovascularization associated with age-related macular degeneration. Pegaptanib therefore has the notable distinction of being the first aptamer therapeutic approved for use in humans, paving the way for future aptamer applications.

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页码：123 / 132

页数：10

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