申请人:——
公开号:US20040229318A1
公开(公告)日:2004-11-18
The invention provides biologically active erythropoietin (EPO) conjugate compositions wherein EPO is covalently conjugated to a non-antigenic hydrophilic polymer covalently linked to an organic molecule that increases the circulating serum half-life of the composition. The invention thus relates to EPO derivatives described by the formula EPO—(X—Y)
N
where EPO is erythropoietin or its pharmaceutical acceptable derivatives having biological properties of causing bone marrow cells to increase production of reticulocytes and red blood cells, X is PEG or other water soluble polymers, Y is an organic molecule that increases the circulating half-life of the construct more than the PEG alone and N is an integer from 1 to 15. Other molecules may be included between EPO and X and between X and Y to provide the proper functionality for coupling or valency.
本发明提供了具有生物活性的促红细胞生成素(EPO)共轭组合物,其中 EPO 与共价连接到有机分子上的非抗原性亲水性聚合物共轭,从而延长了组合物的循环血清半衰期。因此,本发明涉及由式 EPO-(X-Y)描述的 EPO 衍生物
N
其中,EPO 是红细胞生成素或其药物可接受的衍生物,具有使骨髓细胞增加网织红细胞和红血球生成的生物学特性;X 是 PEG 或其它水溶性聚合物;Y 是有机分子,比单独的 PEG 更能延长构建物的循环半衰期;N 是 1 到 15 之间的整数。在 EPO 和 X 之间以及 X 和 Y 之间还可加入其他分子,以提供适当的偶联功能或价态。