公开(公告)号：EP2963055A1

公开(公告)日：2016-01-06

申请号：EP14757574.0

申请日：2014-02-26

申请人： Hanmi Pharm. Co., Ltd.

发明人： JANG, Myung Hyun ,  KIM, Dae Jin ,  HWANG, Sang Youn ,  KIM, Hyun Uk ,  JUNG, Sung Youb ,  KWON, Se Chang

IPC分类号： C07K14/62 ,  C07K17/08 ,  A61K38/28 ,  A61P3/10

CPC分类号： A61K47/6849 ,  A61K38/28 ,  A61K47/68 ,  A61K47/6811 ,  A61K47/6889 ,  C07K14/62 ,  C07K17/08 ,  C07K2319/30

摘要： 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.

摘要翻译： 提供了具有改善的胰岛素受体结合亲和力和增加的活性的胰岛素缀合物，其中非肽基聚合物和免疫球蛋白Fc区经由胰岛素位点与胰岛素β链的除N末端之外的氨基酸残基位点特异性地连接 共价键，包含其的长效制剂及其制备方法。 本发明的胰岛素缀合物用于提供显示出肽的体内活性显着增加的胰岛素制剂。