Torcetrapib

Torcetrapib is an inhibitor of cholesteryl ester transfer protein (CETP; IC₅₀s = 47 and 51 nM for cholesteryl and triglyceride transfer, respectively).¹ It is selective for CETP over phospholipid transfer protein (PLTP), lecithin:cholesterol acyltransferase (LCAT), and hepatic and lipoprotein lipases at 10 µM. Torcetrapib (30 mg/kg) inhibits CETP activity and increases HDL cholesterol levels in serum from transgenic mice expressing human CETP and ApoA1.² It increases mean arterial blood pressure in Zucker fa/fa diabetic rats when administered at doses of 60 and 200 mg/kg.

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1. Clark, R.W., Ruggeri, R.B., Cunningham, D., et al. Description of the torcetrapib series of cholesteryl ester transfer protein inhibitors, including mechanism of action. J. Lipid Res. 47(3), 537-552 (2006).

2. Cao, G., Beyer, T.P., Zhang, Y., et al. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure. J. Lipid Res. 52(12), 2169-2176 (2011).