2007-01-01

Will torcetrapib be the next big thing in coronary heart disease risk reduction?

James M McKenney, John A Hoekstra

Index: Curr. Atheroscler. Rep. 9(1) , 48-56, (2007)

Full Text: HTML

Abstract

Scientists are seeking ways to increase high-density lipoprotein (HDL) cholesterol to lower coronary heart disease (CHD). Emerging from this search is torcetrapib, a partial inhibitor of cholesteryl ester transfer protein. Via this mechanism, cholesteryl ester is prevented from being transferred to apolipoprotein B-containing lipoproteins and is retained in HDL particles, where ostensibly it may be delivered directly to the liver for elimination. Proof that this may reduce atherosclerotic vascular disease is provided by population studies of cholesteryl ester transfer protein (CETP) deficiencies and single nucleotide polymorphisms of CETP, and experiments in animal models treated with torcetrapib. Torcetrapib effectively raises HDL cholesterol when used alone and when added to background therapy with atorvastatin. The drug appears to be well tolerated. Large surrogate and survival outcome trials are underway to document its impact on CHD.


Related Compounds

  • Torcetrapib

Related Articles:

Cholesteryl ester-transfer protein inhibitors stimulate aldosterone biosynthesis in adipocytes through Nox-dependent processes.

2015-04-01

[J. Pharmacol. Exp. Ther. 353(1) , 27-34, (2015)]

Effect on cardiovascular risk of high density lipoprotein targeted drug treatments niacin, fibrates, and CETP inhibitors: meta-analysis of randomised controlled trials including 117,411 patients.

2014-01-01

[BMJ 349 , g4379, (2014)]

Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility.

2014-07-01

[Xenobiotica 44(7) , 591-605, (2014)]

Upregulating reverse cholesterol transport with cholesteryl ester transfer protein inhibition requires combination with the LDL-lowering drug berberine in dyslipidemic hamsters.

2013-01-01

[Arterioscler. Thromb. Vasc. Biol. 33(1) , 13-23, (2013)]

Effect of dalcetrapib, a CETP modulator, on non-cholesterol sterol markers of cholesterol homeostasis in healthy subjects

2011-12-01

[Atherosclerosis 219(2) , 761-7, (2011)]

More Articles...