(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one
Title | Journal |
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Anacetrapib lowers LDL by increasing ApoB clearance in mildly hypercholesterolemic subjects. | The Journal of clinical investigation 20150601 |
Anacetrapib as lipid-modifying therapy in patients with heterozygous familial hypercholesterolaemia (REALIZE): a randomised, double-blind, placebo-controlled, phase 3 study. | Lancet (London, England) 20150530 |
Cholesteryl ester-transfer protein inhibitors stimulate aldosterone biosynthesis in adipocytes through Nox-dependent processes. | The Journal of pharmacology and experimental therapeutics 20150401 |
Future of cholesteryl ester transfer protein inhibitors. | Annual review of medicine 20140101 |
Tangier disease: epidemiology, pathophysiology, and management. | American journal of cardiovascular drugs : drugs, devices, and other interventions 20121001 |
Cholesteryl ester transfer protein inhibition as a strategy to reduce cardiovascular risk. | Journal of lipid research 20120901 |
Rationale for cholesteryl ester transfer protein inhibition. | Current opinion in lipidology 20120801 |
HDL and CETP Inhibition: Will This DEFINE the Future? | Current treatment options in cardiovascular medicine 20120801 |
Safety of inhibition of cholesteryl ester transfer protein with anacetrapib: the DEFINE study. | Expert review of cardiovascular therapy 20120801 |
Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects. | British journal of clinical pharmacology 20120701 |
Increasing high-density lipoprotein cholesterol by cholesteryl ester transfer protein-inhibition: a rocky road and lessons learned? The early demise of the dal-HEART programme. | European heart journal 20120701 |
An update on the clinical development of dalcetrapib (RO4607381), a cholesteryl ester transfer protein modulator that increases HDL cholesterol levels. | Future cardiology 20120701 |
Current status of CETP inhibitors in the treatment of hyperlipidemia: an update. | Current clinical pharmacology 20120501 |
Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors. | Bioorganic & medicinal chemistry letters 20120501 |
On- and off-target pharmacology of torcetrapib: current understanding and implications for the structure activity relationships (SAR), discovery and development of cholesteryl ester-transfer protein (CETP) inhibitors. | Drugs 20120305 |
Changes in lipoprotein subfraction concentration and composition in healthy individuals treated with the CETP inhibitor anacetrapib. | Journal of lipid research 20120301 |
New horizons for cholesterol ester transfer protein inhibitors. | Current atherosclerosis reports 20120201 |
Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction. | Clinical pharmacology and therapeutics 20120101 |
SAR studies on the central phenyl ring of substituted biphenyl oxazolidinone-potent CETP inhibitors. | Bioorganic & medicinal chemistry letters 20120101 |
Anacetrapib, a cholesteryl ester transfer protein inhibitor. | Expert opinion on investigational drugs 20120101 |
Lipid exchange mechanism of the cholesteryl ester transfer protein clarified by atomistic and coarse-grained simulations. | PLoS computational biology 20120101 |
Regulation of reverse cholesterol transport - a comprehensive appraisal of available animal studies. | Nutrition & metabolism 20120101 |
Cholesteryl ester transfer-protein modulator and inhibitors and their potential for the treatment of cardiovascular diseases. | Vascular health and risk management 20120101 |
Mipomersen: evidence-based review of its potential in the treatment of homozygous and severe heterozygous familial hypercholesterolemia. | Core evidence 20120101 |
Patient considerations and clinical impact of cholesteryl ester transfer protein inhibitors in the management of dyslipidemia: focus on anacetrapib. | Vascular health and risk management 20120101 |
Cholesteryl ester transfer protein inhibitors for dyslipidemia: focus on dalcetrapib. | Drug design, development and therapy 20120101 |
[Secondary coronary heart disease prevention. Will CEPT inhibitors be the next breakthrough?]. | MMW Fortschritte der Medizin 20111208 |
Cholesteryl ester transfer protein inhibition in cardiovascular risk management: ongoing trials will end the confusion. | Cardiovascular therapeutics 20111201 |
Familial hypercholesterolemia: present and future management. | Current cardiology reports 20111201 |
Multidimensional profiling of plasma lipoproteins by size exclusion chromatography followed by reverse-phase protein arrays. | Journal of lipid research 20111201 |
Lack of an effect of anacetrapib on the pharmacokinetics of digoxin in healthy subjects. | Biopharmaceutics & drug disposition 20111201 |
Cholesteryl ester transfer protein inhibition to reduce cardiovascular risk: Where are we now? | Trends in pharmacological sciences 20111201 |
Update on therapies targeting HDL: the mystery continues. | Current opinion in lipidology 20111201 |
Leoligin, the major lignan from Edelweiss, activates cholesteryl ester transfer protein. | Atherosclerosis 20111101 |
Anacetrapib promotes reverse cholesterol transport and bulk cholesterol excretion in Syrian golden hamsters. | Journal of lipid research 20111101 |
Investigational CETP antagonists for hyperlipidemia and atherosclerosis prevention. | Expert opinion on investigational drugs 20111101 |
Anacetrapib: a new weapon against dyslipidemia. | Current clinical pharmacology 20111101 |
Anacetrapib: hope for CETP inhibitors? | Cardiovascular therapeutics 20111001 |
Efficacy and safety after cessation of treatment with the cholesteryl ester transfer protein inhibitor anacetrapib (MK-0859) in patients with primary hypercholesterolemia or mixed hyperlipidemia. | American heart journal 20111001 |
Different effects of compounds decreasing cholesteryl ester transfer protein activity on lipoprotein metabolism. | Current opinion in lipidology 20110801 |
Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib. | Journal of medicinal chemistry 20110714 |
Model-based development of anacetrapib, a novel cholesteryl ester transfer protein inhibitor. | The AAPS journal 20110601 |
Triglyceride-rich lipoproteins and high-density lipoprotein cholesterol in patients at high risk of cardiovascular disease: evidence and guidance for management. | European heart journal 20110601 |
The cholesterol ester transfer protein inhibitor, anacetrapib. | Current opinion in lipidology 20110601 |
[Cholesteryl ester transfer protein inhibition in the management of atherosclerotic cardiovascular disease: second act 'A rebirth of hope']. | Revista medica de Chile 20110601 |
A bivariate genome-wide approach to metabolic syndrome: STAMPEED consortium. | Diabetes 20110401 |
Preparative scale synthesis of the biaryl core of anacetrapib via a ruthenium-catalyzed direct arylation reaction: unexpected effect of solvent impurity on the arylation reaction. | The Journal of organic chemistry 20110304 |
Effect of diltiazem, a moderate CYP3A inhibitor, on the pharmacokinetics of anacetrapib, a potent cholesteryl ester transfer protein inhibitor, in healthy subjects. | Journal of clinical pharmacology 20110301 |
The DEFINE study: a bright future for CETP inhibitors? | Expert opinion on investigational drugs 20110301 |
Clinical Trials Update AHA Congress 2010. | Cardiovascular drugs and therapy 20110201 |
CETP inhibition shows promise as way to reduce cardiovascular disease risk. | JAMA 20110112 |
Trial watch: hope renewed for strategy to raise HDL cholesterol. | Nature reviews. Drug discovery 20110101 |
Anacetrapib and dalcetrapib: two novel cholesteryl ester transfer protein inhibitors. | The Annals of pharmacotherapy 20110101 |
[Novel therapy for atherosclerosis and inflammatory vascular disease]. | Nihon rinsho. Japanese journal of clinical medicine 20110101 |
Cardiovascular disease and dyslipidemia: beyond LDL. | Current pharmaceutical design 20110101 |
Analysis of in vitro bioactivity data extracted from drug discovery literature and patents: Ranking 1654 human protein targets by assayed compounds and molecular scaffolds. | Journal of cheminformatics 20110101 |
Dyslipidaemia of obesity, metabolic syndrome and type 2 diabetes mellitus: the case for residual risk reduction after statin treatment. | The open cardiovascular medicine journal 20110101 |
Primary prevention of coronary heart disease: integration of new data, evolving views, revised goals, and role of rosuvastatin in management. A comprehensive survey. | Drug design, development and therapy 20110101 |
Association between the interleukin-6 promoter polymorphism -174G/C and serum lipoprotein(a) concentrations in humans. | PloS one 20110101 |
Emerging therapeutic strategies to enhance HDL function. | Lipids in health and disease 20110101 |
New insights into the mechanism of low high-density lipoprotein cholesterol in obesity. | Lipids in health and disease 20110101 |
Medical angioplasty - hope and expectations: an optimistic overview. | Journal of family & community medicine 20110101 |
Safety of anacetrapib in patients with or at high risk for coronary heart disease. | The New England journal of medicine 20101216 |
Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. | Journal of lipid research 20101201 |
Good news for 'good' cholesterol. | Nature 20101118 |
Emerging drugs for hyperlipidemia. | Expert opinion on emerging drugs 20100901 |
Biochemical characterization of cholesteryl ester transfer protein inhibitors. | Journal of lipid research 20100901 |
Drug off-target effects predicted using structural analysis in the context of a metabolic network model. | PLoS computational biology 20100901 |
Dissociating HDL cholesterol from cardiovascular risk. | Lancet (London, England) 20100731 |
Cholesterol efflux potential and antiinflammatory properties of high-density lipoprotein after treatment with niacin or anacetrapib. | Arteriosclerosis, thrombosis, and vascular biology 20100701 |
Dalcetrapib: a review of Phase II data. | Expert opinion on investigational drugs 20100601 |
[Recent advances in the research on HDL subfraction]. | Rinsho byori. The Japanese journal of clinical pathology 20100601 |
High-density lipoprotein-mediated anti-atherosclerotic and endothelial-protective effects: a potential novel therapeutic target in cardiovascular disease. | Current pharmaceutical design 20100501 |
Pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys. | Drug metabolism and disposition: the biological fate of chemicals 20100301 |
Metabolism and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in humans. | Drug metabolism and disposition: the biological fate of chemicals 20100301 |
[HDL and CETP in atherogenesis]. | Deutsche medizinische Wochenschrift (1946) 20100201 |
Cholesteryl ester transfer protein: at the heart of the action of lipid-modulating therapy with statins, fibrates, niacin, and cholesteryl ester transfer protein inhibitors. | European heart journal 20100101 |
Current status and future directions in lipid management: emphasizing low-density lipoproteins, high-density lipoproteins, and triglycerides as targets for therapy. | Vascular health and risk management 20100101 |
Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20100101 |
Anacetrapib. | American journal of cardiovascular drugs : drugs, devices, and other interventions 20100101 |
Effects of fenofibrate on lipid profiles, cholesterol ester transfer activity, and in-stent intimal hyperplasia in patients after elective coronary stenting. | Lipids in health and disease 20100101 |
Update on CETP inhibition. | Journal of clinical lipidology 20100101 |
Treatment of dyslipidemia in patients with type 2 diabetes. | Lipids in health and disease 20100101 |
High density lipoproteins-based therapies for cardiovascular disease. | Journal of cardiovascular disease research 20100101 |
The pharmacology and off-target effects of some cholesterol ester transfer protein inhibitors. | The American journal of cardiology 20091116 |
Triglycerides and HDL cholesterol: stars or second leads in diabetes? | Diabetes care 20091101 |
Design of the DEFINE trial: determining the EFficacy and tolerability of CETP INhibition with AnacEtrapib. | American heart journal 20091001 |
Single-dose pharmacokinetics and pharmacodynamics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects. | British journal of clinical pharmacology 20091001 |
Cholesteryl ester transfer protein inhibitors as high-density lipoprotein raising agents. | Expert opinion on therapeutic patents 20090901 |
Anacetrapib, a cholesterol ester transfer protein (CETP) inhibitor for the treatment of atherosclerosis. | Current opinion in investigational drugs (London, England : 2000) 20090901 |
The end of the road for CETP inhibitors after torcetrapib? | Current opinion in cardiology 20090701 |
Effect of cholesteryl ester transfer protein inhibitor on vitamin E transport should be studied. | American heart journal 20090701 |
Drug discovery using chemical systems biology: identification of the protein-ligand binding network to explain the side effects of CETP inhibitors. | PLoS computational biology 20090501 |
Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects. | British journal of clinical pharmacology 20090501 |
Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20090401 |
Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib as monotherapy and coadministered with atorvastatin in dyslipidemic patients. | American heart journal 20090201 |
Assessment of the CYP3A-mediated drug interaction potential of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy volunteers. | Journal of clinical pharmacology 20090101 |
High-density lipoprotein cholesterol: current perspective for clinicians. | Angiology 20090101 |
Raising HDL cholesterol in women. | International journal of women's health 20090101 |
Multiple-dose pharmacodynamics and pharmacokinetics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects. | Clinical pharmacology and therapeutics 20081201 |
JTT-705: is there still future for a CETP inhibitor after torcetrapib? | Expert opinion on investigational drugs 20081001 |
The failure of torcetrapib: what have we learned? | British journal of pharmacology 20080801 |
Torcetrapib-induced blood pressure elevation is independent of CETP inhibition and is accompanied by increased circulating levels of aldosterone. | British journal of pharmacology 20080801 |
Anacetrapib: new hope for cholesteryl ester transfer protein inhibitors in the treatment of dyslipidemia. | Nature clinical practice. Cardiovascular medicine 20080601 |
Treating high-density lipoprotein cholesterol: a return to inhibition of cholesteryl ester transfer protein? | Current atherosclerosis reports 20080601 |
Cholesteryl ester transfer protein inhibition and HDL increase: has the dream ended? | Expert opinion on investigational drugs 20080401 |
Gateways to clinical trials. | Methods and findings in experimental and clinical pharmacology 20080301 |
HDL metabolism and CETP inhibition. | Cardiology in review 20080101 |
Effect of the cholesteryl ester transfer protein inhibitor, anacetrapib, on lipoproteins in patients with dyslipidaemia and on 24-h ambulatory blood pressure in healthy individuals: two double-blind, randomised placebo-controlled phase I studies. | Lancet (London, England) 20071208 |