Refocusing On Use of Cholesteryl Ester Transfer Protein Inhibitors
Abstract
Cholesteryl ester transfer protein (CETP) plays an important role in cholesterol metabolism because it is responsible for the transfer of cholesteryl esters from high-density lipoprotein (HDL) to very-low-density lipoproteins and low-density lipoproteins (LDLs). The development of CETP inhibitors represented a novel approach for raising HDL cholesterol and reducing LDL cholesterol levels to alter atherogenesis. However, results from recent clinical trials question the therapeutic use of at least 1 CETP inhibitor, torcetrapib (Pfizer Inc, New York, NY), which was demonstrated to increase blood pressure and have no effect on decreasing the progression of coronary atherosclerosis. This article discusses the use of CETP inhibitors and their effects on lipoprotein metabolism and whether they can ultimately lead to reductions in cardiovascular events.
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Drug-based inhibition of CETP in humans leads to a significant increase in HDL-C and a drop in LDL-C.
“Drug-based inhibition of CETP in humans leads to a significant increase in HDL-C and a drop in LDL-C [104, 105].”
From HDL cholesterol: reappraisal of its clinical relevance (2017) · cites this paper as [105]
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References 16 · Cited by 20
- Authors
- Kastelein, J. J. P.
- Affiliations
- Amsterdam UMC Location University of Amsterdam (NL)
- Corresponding author
- Kastelein, John J.P.
- ORCID
- Kastelein, John J.P.
- Venue
- The American Journal of Cardiology
- Publisher
- Elsevier BV
- Published
- 2007-12
- Volume
- 100
- Issue
- 11
- Pages
- S47-S52
- ISSN
- 0002-9149 (ISSN-L)
- OpenAlex
- W2020241535
- Cited by
- 20
- References
- 16
- Citations by year
- 2026: 1 · 2025: 1 · 2020: 1 · 2019: 1 · 2017: 2 · 2016: 1 · 2013: 1 · 2012: 2
- FWCI
- 2.32
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The American Journal of Cardiology (publishedVersion)
- PubMed (publishedVersion)
- Data Archiving and Networked Services (DANS) (submittedVersion)
- Pure Amsterdam UMC (submittedVersion)
- Topics
- Health Sciences › Medicine › Surgery › Lipoproteins and Cardiovascular Health
- Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Clinical Biochemistry › Paraoxonase enzyme and polymorphisms
- Keywords
- cholesteryl ester transfer protein, CETP inhibitors, torcetrapib, HDL cholesterol, LDL cholesterol, lipoprotein metabolism, atherosclerosis, cardiovascular events, blood pressure, cholesterol ester transfer
- MeSH terms
- Anticholesteremic Agents, Coronary Artery Disease, Humans, Cholesterol, HDL, Quinolines, Cholesterol Ester Transfer Proteins
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