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Cited by 66Lipoproteins and Cardiovascular HealthCholesterol and Lipid MetabolismLipid metabolism and disorders

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Future of Cholesteryl Ester Transfer Protein Inhibitors

Rader, Daniel J., deGoma, Emil M.·2014·Annual Review of Medicine
DOI 10.1146/annurev-med-050311-163305
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Abstract

The cholesteryl ester transfer protein (CETP) plays an integral role in the metabolism of plasma lipoproteins. Despite two failures, CETP inhibitors are still in clinical development. We review the genetics of CETP and coronary disease, preclinical data on CETP inhibition and atherosclerosis, and the effects of CETP inhibition on cholesterol efflux and reverse cholesterol transport. We discuss the two failed CETP inhibitors, torcetrapib and dalcetrapib, and attempt to extract lessons learned. Two CETP inhibitors, anacetrapib and evacetrapib, are in phase III development, and we attempt to differentiate them from the failed drugs. Whether pharmacologic CETP inhibition will reduce the risk of cardiovascular disease is one of the most fascinating and important questions in the field of cardiovascular medicine.

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Metadata

Authors
Rader, D. J., & deGoma, E. M.
Affiliations
  • Division of Translational Medicine and Human Genetics, Cardiovascular Institute and Institute for Translational Medicine and Therapeutics, and
  • University of Pennsylvania (US)
ORCID
Venue
Annual Review of Medicine
Publisher
Annual Reviews
Published
2014-01-14
Volume
65
Issue
1
Pages
385-403
ISSN
  • 0066-4219 (ISSN-L)
  • 1545-326X
DOI
10.1146/annurev-med-050311-163305
OpenAlex
W2111699021
Cited by
66
References
65
Citations by year
2025: 1 · 2024: 2 · 2023: 2 · 2022: 2 · 2021: 3 · 2020: 2 · 2019: 4 · 2018: 2 · 2017: 9 · 2016: 13 · 2015: 13 · 2014: 13
FWCI
3.09
Type
journal article
Language
en
Open access
closed
Locations
  • Annual Review of Medicine (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Lipoproteins and Cardiovascular Health
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Cholesterol and Lipid Metabolism
  • Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Lipid metabolism and disorders
Keywords
cholesteryl ester transfer protein, CETP inhibitors, torcetrapib, dalcetrapib, anacetrapib, evacetrapib, coronary disease, atherosclerosis, cholesterol efflux, reverse cholesterol transport, plasma lipoprotein metabolism, cardiovascular risk, drug development failure
MeSH terms
Amides, Anticholesteremic Agents, Benzodiazepines, Cholesterol, Clinical Trials as Topic, Coronary Disease, Esters, Humans, Cholesterol, HDL, Cholesterol, LDL, Quinolines, Sulfhydryl Compounds, Oxazolidinones, Atherosclerosis, Cholesterol Ester Transfer Proteins

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