葡萄糖反應性胰島素結合物农业专利-农业学术服务平台

发明人:: LIN, SONGNIAN,林　松楠,YAN, LIN,阳　琳,陽　琳,KEKEC, AHMET,科克　亚曼特,科克　亞曼特,ZHU, YUPING,卓　尤平,HUNTER, DAVID N.,杭特　大卫Ｎ,杭特　大衛Ｎ,HUO, PEI,胡　佩,FENG, DANQING,封　丹青,NARGUND, RAVI P.,纳格恩　瑞维Ｐ,納格恩　瑞維Ｐ,MOYES,林松楠,阳琳,陽琳,科克亚曼特,科克亞曼特,卓尤平,杭特大卫N,杭特大衛N,胡佩,封丹青,纳格恩瑞维P,納格恩瑞維P

摘要：: Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein the saccharide for at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.本發明揭示胰島素結合物，其包含共價連接至至少一個具有兩臂之雙齒連接子的胰島素分子，每個臂獨立地連接至包含醣之配位體且其中該連接子之至少一個配位體的醣為岩藻糖。該等胰島素結合物即使在沒有諸如Con A之外源多價醣結合分子之存在下投與有需要之個體時，仍可展現對諸如葡萄糖或α-甲基甘露糖之醣類全身濃度之反應性之藥物動力學(PK)及/或藥效學(PD)型態。