| Different effects of compounds decreasing cholesteryl ester transfer protein activity on lipoprotein metabolism. | |
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MedLine Citation:
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PMID: 21587074 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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PURPOSE OF REVIEW: Review literature on the effect of decreasing cholesteryl ester transfer protein (CETP) activity through pharmacological inhibition or modulation in preclinical and clinical settings compared to human CETP deficiency on lipoprotein characteristics, HDL remodelling and function. RECENT FINDINGS: Torcetrapib, anacetrapib and dalcetrapib inhibited the heterotypic transfer of cholesteryl ester from HDL to LDL and/or VLDL with similar potency, although the potency of dalcetrapib was time dependent. Homotypic transfer of cholesteryl ester from HDL3 to HDL2 via recombinant human CETP was inhibited by torcetrapib and anacetrapib (CETP inhibitors, CETPi) but not by dalcetrapib (CETP modulator, CETPm). In a hamster model of reverse cholesterol transport, only dalcetrapib increased efflux of fecal sterols from macrophages to feces. In clinical studies, dose-responses of CETPi and CETPm demonstrate qualitative and quantitative changes in HDL and LDL particle composition and distribution. SUMMARY: Recent studies of the CETPi torcetrapib and anacetrapib and the CETPm dalcetrapib have shown differences in the resulting increase in HDL-cholesterol and in the level of HDL remodelling and potential for effective reverse cholesterol transport. Results from ongoing clinical outcomes studies with anacetrapib and dalcetrapib will clarify the relevance of CETP inhibition versus modulation towards HDL remodelling in the treatment of cardiovascular diseases. |
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Authors:
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Eric J Niesor |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-5-16 |
Journal Detail:
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Title: Current opinion in lipidology Volume: - ISSN: 1473-6535 ISO Abbreviation: - Publication Date: 2011 May |
Date Detail:
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Created Date: 2011-5-18 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9010000 Medline TA: Curr Opin Lipidol Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Pharmaceuticals Division, F. Hoffmann-La Roche Ltd, Basel, Switzerland. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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