CP-529414 Torcetrapib

Torcetrapib, also known as CP-529,414 was a drug being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. Its development was halted in 2006 when phase III studies showed excessive all-cause mortality in the treatment group receiving a combination of atorvastatin (Lipitor) and torcetrapib. Torcetrapib acts (as a CETP inhibitor) by inhibiting cholesterylester transfer protein (CETP), which normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL). Inhibition of this process results in higher HDL levels and reduces LDL levels.

Properties: 
Appearance & Physical State: lipid
Density: 1.42g/cm3
Melting Point: 54-58ºC
Boiling Point: 504.8ºC at 760mmHg
Flash Point: 259.1ºC
Refractive Index: 1.511
Vapor Pressure: 2.58E-10mmHg at 25°C

[1]. Clark RW, et al. Raising high-density lipoprotein in humans through inhibition of cholesteryl ester transfer protein: an initial multidose study of torcetrapib. Arterioscler Thromb Vasc Biol. 2004 Mar;24(3):490-7.

[2]. Hu X, et al. Torcetrapib induces aldosterone and cortisol production by an intracellular calcium-mediated mechanism independently of cholesteryl ester transfer protein inhibition. Endocrinology. 2009 May;150(5):2211-9.

[3]. Barter PJ, et al. Effects of torcetrapib in patients at high risk for coronary events. N Engl J Med. 2007 Nov 22;357(21):2109-22.