Torcetrapib is a cholesteryl ester transfer protein (CETP) inhibitor (IC₅₀ = 37 nM). It raises high-density lipoprotein (HDL) cholesterol and reduces low-density lipoprotein (LDL) cholesterol levels. However, in clinical trials, Torcetrapib displayed unfavorable off-target effects in cardiovascular system. PDGFR, HGFR (c-Met), IL-2 receptor, and ErbB1- tyrosine kinase have subsequently been identified as direct off-targets of this compound.