DIMARCHI RICHARD D,CHENG SHUJIANG,KOU BINBIN,HAN JIE
申请号：
IN4434/DELNP/2011
公开号：
IN2011DN04434A
申请日:
2011.06.10
申请国别(地区):
IN
年份:
2012
代理人:
摘要：
Insulin-like growth factor analogs are disclosed wherein substitution of the IGF native amino acids, at positions corresponding to positions B 16 and B 17 of native insulin, with tyrosine and leucine, respectively, increases potency of the resulting analog at the insulin receptor by tenfold. Also disclosed are prodrug and depot formulations of the IGF analogs, wherein the IGF analog has been modified by the linkage of a dipeptide to the analog through an amide bond linkage. The prodrug and depot formulations disclosed herein have extended half lives of at least 2 hours, 10 hours, and more typically greater than 20 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
