ArticleJournal of lipid research2011
Anacetrapib promotes reverse cholesterol transport and bulk cholesterol excretion in Syrian golden hamsters.
Article in Journal of lipid research, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 79 citations in OpenAlex.
- Cholesteryl Ester Transfer Protein Inhibition With Anacetrapib Decreases Fractional Clearance Rates of High-Density Lipoprotein Apolipoprotein A-I and Plasma Cholesteryl Ester Transfer Protein.Arteriosclerosis, thrombosis, and vascular biology · 2016Trial
- Anacetrapib lowers LDL by increasing ApoB clearance in mildly hypercholesterolemic subjects.The Journal of clinical investigation · 2015 · on this mapTrial
- Cholesteryl Ester Transfer Protein Deficiency and Hyperalphalipoproteinemia.Journal of atherosclerosis and thrombosis · 2025Review
- Idol Depletion Protects against Spontaneous Atherosclerosis in a Hamster Model of Familial Hypercholesterolemia.Oxidative medicine and cellular longevity · 2022Article
- Genetically Engineered Hamster Models of Dyslipidemia and Atherosclerosis.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Genetically-engineered hamster models: applications and perspective in dyslipidemia and atherosclerosis-related cardiovascular disease.Medical review (2021) · 2021Article
- Dietary-Induced Elevations of Triglyceride-Rich Lipoproteins Promote Atherosclerosis in the Low-Density Lipoprotein Receptor Knockout Syrian Golden Hamster.Frontiers in cardiovascular medicine · 2021Article
- Simultaneous Determination of Biliary and Intestinal Cholesterol Secretion Reveals That CETP (Cholesteryl Ester Transfer Protein) Alters Elimination Route in Mice.Arteriosclerosis, thrombosis, and vascular biology · 2019Article
- Cholesteryl ester transfer protein and its inhibitors.Journal of lipid research · 2018Review
- Anacetrapib as a potential cardioprotective strategy.Drug design, development and therapy · 2017Review
- Dysfunctional HDL and atherosclerotic cardiovascular disease.Nature reviews. Cardiology · 2016Review
- Glucagon receptor antagonism induces increased cholesterol absorption.Journal of lipid research · 2015Article
- A new model of reverse cholesterol transport: enTICEing strategies to stimulate intestinal cholesterol excretion.Trends in pharmacological sciences · 2015Review
- PPARδ activation induces hepatic long-chain acyl-CoA synthetase 4 expression in vivo and in vitro.Biochimica et biophysica acta · 2015Article
- Cardiovascular and cancer events in hyper-high-density lipoprotein cholesterolemic patients: a post hoc analysis of the MEGA study.Lipids in health and disease · 2014Article
- CETP inhibitors downregulate hepatic LDL receptor and PCSK9 expression in vitro and in vivo through a SREBP2 dependent mechanism.Atherosclerosis · 2014Article
- Sequencing, annotation and analysis of the Syrian hamster (Mesocricetus auratus) transcriptome.PloS one · 2014Article
- Pharmacotherapies for lipid modification: beyond the statins.Nature reviews. Cardiology · 2013Review
- In vivo effects of anacetrapib on preβ HDL: improvement in HDL remodeling without effects on cholesterol absorption.Journal of lipid research · 2013Article
- Antisense oligonucleotide inhibition of cholesteryl ester transfer protein enhances RCT in hyperlipidemic, CETP transgenic, LDLr-/- mice.Journal of lipid research · 2013Article
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cholesteryl ester transfer protein (CETP) transfers cholesteryl ester (CE) and triglyceride between HDL and apoB-containing lipoproteins. Anacetrapib (ANA), a reversible inhibitor of CETP, raises HDL cholesterol (HDL-C) and lowers LDL cholesterol in dyslipidemic patients; however, the effects of ANA on cholesterol/lipoprotein metabolism in a dyslipidemic hamster model have not been demonstrated. To test whether ANA (60 mg/kg/day, 2 weeks) promoted reverse cholesterol transport (RCT), ³H-cholesterol-loaded macrophages were injected and (3)H-tracer levels were measured in HDL, liver, and feces. Compared to controls, ANA inhibited CETP (94%) and increased HDL-C (47%). ³H-tracer in HDL increased by 69% in hamsters treated with ANA, suggesting increased cholesterol efflux from macrophages to HDL. ³H-tracer in fecal cholesterol and bile acids increased by 90% and 57%, respectively, indicating increased macrophage-to-feces RCT. Mass spectrometry analysis of HDL from ANA-treated hamsters revealed an increase in free unlabeled cholesterol and CE. Furthermore, bulk cholesterol and cholic acid were increased in feces from ANA-treated hamsters. Using two independent approaches to assess cholesterol metabolism, the current study demonstrates that CETP inhibition with ANA promotes macrophage-to-feces RCT and results in increased fecal cholesterol/bile acid excretion, further supporting its development as a novel lipid therapy for the treatment of dyslipidemia and atherosclerotic vascular disease.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.