Provided are an insulin conjugate having improved insulin receptor binding affinity and increased activity, in which a non-peptidyl polymer and an immunoglobulin Fc region are site-specifically linked to an amino acid residue of the insulin beta chain excluding the N-terminus thereof via a covalent bond, a long-acting formulation including the same, and a preparation method thereof. The insulin conjugate of the present invention is used to provide an insulin formulation which exhibits a remarkably increased in vivo activity of the peptide.
本发明提供了一种具有改进的
胰岛素受体结合亲和力和更高活性的
胰岛素共轭物,其中非肽聚合物和免疫球蛋白Fc区通过共价键与
胰岛素β链的
氨基酸残基(不包括其N-末端)定点特异性连接,还提供了包括本发明在内的长效制剂及其制备方法。本发明的
胰岛素共轭物可用于提供一种
胰岛素制剂,该制剂可显著提高肽的体内活性。