torcetrapib

Torcetrapib (CP-529414) is a cholesteryl ester transfer protein (CETP) inhibitor designed to reduce the heterotypic transfer of cholesteryl ester from HDL to LDL and or VLDL. It failed in phase III trials due to an excess of deaths.

CP-532623, a close structural analog of Torcetrapib, is a CETP inhibitor with highly lipophilic properties. It elevates high-density lipoprotein cholesterol.

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.