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Pegaptanib for wet macular degeneration.

机译：哌加他尼用于湿性黄斑变性。

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Pegaptanib sodium injection (Macugen, Eyetech Pharmaceuticals, Pfizer, New York, NY, USA) is a relatively new medication intended to treat the so-called wet (neovascular ) form of age-related macular degeneration (AMD). This form of AMD is characterized by the growth of unwanted new blood vessels into the macula (angiogenesis). The aqueous solution containing pegaptanib is injected into the vitreous of the eye, where it binds to the 165 amino acid isoform of vascular endothelial growth factor (VEGF), a secreted protein that is thought to play a major role in the pathologic angiogenesis that occurs in wet AMD. Neovascular AMD is the leading cause of severe vision loss in people over age 60 in the United States and other industrialized countries (1). Pegaptanib acts as a selective VEGF antagonist through its molecular structure as an aptamer, a pegylated modified oligonucleotide that adopts a three-dimensional configuration, enabling it to bind to extracellular VEGF (Fig. 1). Aptamers are macromolecules composed of chemically synthesized single-stranded nucleic acids (either RNA or DNA) that bind with a high degree of selectivity and affinity when exposed to target proteins. Pegaptanib binds VEGF165, and bound VEGF165 is not able to bind to the VEGF receptor, thereby negating its ability to cause angiogenesis and vascular permeability. Other aptamers exist, as do other forms of treatment for AMD. To date, however, no treatment for AMD has allowed for better vision after treatment, with most surgical treatments leading to almost immediate loss of some vision in the expectation of preventing more severe loss. Research in the field of macular degeneration is advancing rapidly, and treatment with an aptamer such as pegaptanib is a viable option despite the possibility of adverse events.
机译：哌加他尼钠注射液（Macugen，Eyetech Pharmaceuticals，Pfizer，纽约，纽约，美国）是一种相对较新的药物，旨在治疗所谓的湿性（新生血管）形式的老年性黄斑变性（AMD）。这种形式的AMD的特征是不需要的新血管向黄斑部生长（血管生成）。含有培加他尼的水溶液被注入眼玻璃体内，并与血管内皮生长因子（VEGF）的165个氨基酸同工型结合，后者是一种分泌蛋白，被认为在病理性血管生成中起主要作用。湿AMD。在美国和其他工业化国家，新血管性AMD是导致60岁以上人群严重视力丧失的主要原因（1）。 Pegaptanib通过其分子结构作为适体（一种采用三维构型的聚乙二醇化修饰寡核苷酸）充当选择性VEGF拮抗剂，使其能够与细胞外VEGF结合（图1）。适体是由化学合成的单链核酸（RNA或DNA）组成的大分子，当暴露于靶蛋白时，它们具有高度的选择性和亲和力。哌加他尼与VEGF165结合，而结合的VEGF165无法与VEGF受体结合，从而否定其引起血管生成和血管通透性的能力。存在其他适体，以及AMD的其他治疗形式。然而，迄今为止，还没有针对AMD的治疗方法能够在治疗后获得更好的视力，大多数外科手术疗法几乎都会导致某些视力的立即丧失，以期预防更严重的丧失。黄斑变性领域的研究正在迅速发展，尽管有可能发生不良事件，但用适体如培加他尼治疗是一种可行的选择。

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