Discovery of Zetia: the long and winding road for the extraordinary journey from ACAT to Zetia to NPC1L1

ORGN 33

Brian McKittrick, brian.mckittrick@spcorp.com, Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033
In an effort to develop novel treatments for the reduction of serum cholesterol, a series of biologically active azetidinones was discovered. The optimization of these leads, and further discovery of Zetia, a first in class drug for the treatment of elevated LDL in man, will be discussed. Recent results from the in vitro SAR and the elucidation of the mechanism of action studies will be included.