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Cholesteryl Ester Transfer Protein (CETP) Deficiency and CETP Inhibitors
- Source :
- Molecules and Cells
- Publication Year :
- 2014
- Publisher :
- Korean Society for Molecular and Cellular Biology, 2014.
-
Abstract
- Epidemiologic studies have shown that low-density lipoprotein cholesterol (LDL-C) is a strong risk factor, whilst high-density lipoprotein cholesterol (HDL-C) reduces the risk of coronary heart disease (CHD). Therefore, strategies to manage dyslipidemia in an effort to prevent or treat CHD have primarily attempted at decreasing LDL-C and raising HDL-C levels. Cholesteryl ester transfer protein (CETP) mediates the exchange of cholesteryl ester for triglycerides between HDL and VLDL and LDL. We have published the first report indicating that a group of Japanese patients who were lacking CETP had extremely high HDL-C levels, low LDL-C levels and a low incidence of CHD. Animal studies, as well as clinical and epidemiologic evidences, have suggested that inhibition of CETP provides an effective strategy to raise HDL-C and reduce LDL-C levels. Four CETP inhibitors have substantially increased HDL-C levels in dyslipidemic patients. This review will discuss the current status and future prospects of CETP inhibitors in the treatment of CHD. At present anacetrapib by Merck and evacetrapib by Eli Lilly are under development. By 100mg of anacetrapib HDL-C increased by 138%, and LDL-C decreased by 40%. Evacetrapib 500 mg also showed dramatic 132% increase of HDL-C, while LDL-C decreased by 40%. If larger, long-term, randomized, clinical end point trials could corroborate other findings in reducing atherosclerosis, CETP inhibitors could have a significant impact in the management of dyslipidemic CHD patients. Inhibition of CETP synthesis by antisense oligonucleotide or small molecules will produce more similar conditions to human CETP deficiency and may be effective in reducing atherosclerosis and cardiovascular events. We are expecting the final data of prospective clinical trials by CETP inhibitors in 2015.
- Subjects :
- medicine.medical_specialty
Very low-density lipoprotein
Coronary Disease
Lipid Metabolism, Inborn Errors
Benzodiazepines
chemistry.chemical_compound
Anacetrapib
Internal medicine
Cholesterylester transfer protein
Animals
Humans
Medicine
CETP deficiency
Risk factor
Molecular Biology
Oxazolidinones
Clinical Trials as Topic
inhibitors of CETP
biology
business.industry
Cell Biology
General Medicine
Atherosclerosis
medicine.disease
Cholesterol Ester Transfer Proteins
carbohydrates (lipids)
Cholesterol
cholesteryl ester transfer protein (CETP)
Endocrinology
chemistry
biology.protein
Cholesteryl ester
lipids (amino acids, peptides, and proteins)
Minireview
Animal studies
business
hyper-HDL-cholesterolemia
Evacetrapib
Dyslipidemia
HDL & LDL
Subjects
Details
- ISSN :
- 02191032 and 10168478
- Volume :
- 37
- Database :
- OpenAIRE
- Journal :
- Molecules and Cells
- Accession number :
- edsair.doi.dedup.....12c2994539c4c69fcd14a3e054d75d56