公开(公告)号：EP1737497A2

公开(公告)日：2007-01-03

申请号：EP05778139.5

申请日：2005-04-13

申请人： (OSI) EYETECH, INC.

发明人： CALIAS, Pericles ,  COOK, Gary P. ,  SHIMA, David T. ,  ADAMIS, Anthony P. ,  NG, Yin-Shan ,  ROBINSON, Gregory S. ,  TURNER, David I. ,  GANLEY, Mary A.

IPC分类号： A61K47/48

CPC分类号： A61K49/0002 ,  A61K47/60 ,  A61K47/61

摘要： The invention provides compositions and methods for making and using sterically enhanced antagonist aptamer conjugates that include a nucleic acid sequence having a specific affinity for a target molecule and a soluble, high molecular weight steric group that augments or facilitates the inhibition of binding to, or interaction with, the target molecule binding partner by the target molecule when bound to the aptamer conjugate. The present invention also provides methods and formulations for ocular delivery of a biologically active molecule by attaching a charged moiety to the biologically active molecule and delivering the biologically active molecule by iontophoresis. Iontophoresis of a biologically active molecule that is conjugated to a high molecular weight neutral moiety, in enhanced by substituting the high molecular weight neutral moiety with a charged molecule of comparable size.