Future of Cholesteryl Ester Transfer Protein (CETP) Inhibitors: A Pharmacological Perspective

Safety, Tolerability and Pharmacokinetics of Dalcetrapib Following Single and Multiple Ascending Doses in Healthy Subjects

(2013) Michael Derks et al.   CLINICAL DRUG INVESTIGATION

In vivo evaluation of drug-drug interactions linked to UGT inhibition: the effect of probenecid on dalcetrapib pharmacokinetics

(2013) Pau Aceves Baldó et al.   INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS

Carboxylesterase-2 is a highly sensitive target of the antiobesity agent orlistat with profound implications in the activation of anticancer prodrugs

(2012) Da Xiao et al.   BIOCHEMICAL PHARMACOLOGY

Design, synthesis and structure–activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors

(2012) Maria-Carmen Fernandez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects

(2012) Rajesh Krishna et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Rationale for cholesteryl ester transfer protein inhibition

(2012) Bernd Hewing et al.   CURRENT OPINION IN LIPIDOLOGY

Vascular effects and safety of dalcetrapib in patients with or at risk of coronary heart disease: the dal-VESSEL randomized clinical trial

(2012) Thomas F. Lüscher et al.   EUROPEAN HEART JOURNAL

A Phase 0 study of the inhibition of cholesteryl ester transfer protein activity by JNJ-28545595 in plasma from normolipidemic and dyslipidemic humans

(2012) Troy C. Sarich et al.   INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS

No clinically relevant drug–drug interactions when dalcetrapib is co-administered with a monophasic oral contraceptive (Microgynon® 30)

(2012) Annie Young et al.   INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS

Evidence of a Drug–Drug Interaction Linked to Inhibition of Ester Hydrolysis by Orlistat

(2012) Darren Bentley et al.   JOURNAL OF CARDIOVASCULAR PHARMACOLOGY

Cholesteryl ester transfer protein inhibition as a strategy to reduce cardiovascular risk

(2012) Philip J. Barter et al.   JOURNAL OF LIPID RESEARCH

Plasma HDL cholesterol and risk of myocardial infarction: a mendelian randomisation study

(2012) Benjamin F Voight et al.   LANCET

Effects of Dalcetrapib in Patients with a Recent Acute Coronary Syndrome

(2012) Gregory G. Schwartz et al.   NEW ENGLAND JOURNAL OF MEDICINE

Lack of an effect of anacetrapib on the pharmacokinetics of digoxin in healthy subjects

(2011) Rajesh Krishna et al.   BIOPHARMACEUTICS & DRUG DISPOSITION

Prediction of a potentially effective dose in humans for BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein (CETP) by allometric species scaling and combined pharmacodynamic and physiologically-based pharmacokinetic modelling

(2011) Olaf Weber et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Characterization of antioxidant/anti-inflammatory properties and apoA-I-containing subpopulations of HDL from family subjects with monogenic low HDL disorders

(2011) Georgios Daniil et al.   CLINICA CHIMICA ACTA

Effects of Food Intake on the Pharmacokinetic Properties of Dalcetrapib: Findings From Three Phase I, Single-Dose Crossover Studies in Healthy Volunteers

(2011) Michael Derks et al.   CLINICAL THERAPEUTICS

Effects of the CETP Inhibitor Evacetrapib Administered as Monotherapy or in Combination With Statins on HDL and LDL Cholesterol

(2011) Stephen J. Nicholls et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure

(2011) Guoqing Cao et al.   JOURNAL OF LIPID RESEARCH

Changes in lipoprotein subfraction concentration and composition in healthy individuals treated with the CETP inhibitor anacetrapib

(2011) Ronald M. Krauss et al.   JOURNAL OF LIPID RESEARCH

Safety and efficacy of dalcetrapib on atherosclerotic disease using novel non-invasive multimodality imaging (dal-PLAQUE): a randomised clinical trial

(2011) Zahi A Fayad et al.   LANCET

Cholesterol Efflux Capacity, High-Density Lipoprotein Function, and Atherosclerosis

(2011) Amit V. Khera et al.   NEW ENGLAND JOURNAL OF MEDICINE

Dalcetrapib pharmacokinetics and metabolism in the cynomolgus monkey

(2011) Olaf Kuhlmann et al.   XENOBIOTICA

Cholesterol Efflux Potential and Antiinflammatory Properties of High-Density Lipoprotein After Treatment With Niacin or Anacetrapib

(2010) Laurent Yvan-Charvet et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Lack of clinically relevant drug-drug interactions when dalcetrapib is co-administered with ezetimibe

(2010) Michael Derks et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

No clinically relevant drug–drug interactions when dalcetrapib is co-administered with atorvastatin

(2010) Michael Derks et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Coadministration of Dalcetrapib With Pravastatin, Rosuvastatin, or Simvastatin: No Clinically Relevant Drug-Drug Interactions

(2010) Michael Derks et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport

(2010) Eric J. Niesor et al.   JOURNAL OF LIPID RESEARCH

Safety of Anacetrapib in Patients with or at High Risk for Coronary Heart Disease

(2010) Christopher P. Cannon et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Pharmacology and Off-Target Effects of Some Cholesterol Ester Transfer Protein Inhibitors

(2009) Menno Vergeer et al.   AMERICAN JOURNAL OF CARDIOLOGY

Meta-analysis of the effect of nicotinic acid alone or in combination on cardiovascular events and atherosclerosis

(2009) Eric Bruckert et al.   ATHEROSCLEROSIS

Single-dose pharmacokinetics and pharmacodynamics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects

(2009) Rajesh Krishna et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects

(2009) Rajesh Krishna et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Functional Lecithin: Cholesterol Acyltransferase Is Not Required for Efficient Atheroprotection in Humans

(2009) Laura Calabresi et al.   CIRCULATION

Polymorphism in the CETP Gene Region, HDL Cholesterol, and Risk of Future Myocardial Infarction

(2009) Paul M. Ridker et al.   Circulation-Cardiovascular Genetics

Pharmacokinetic, Pharmacodynamic, and Safety Profile of a New Cholesteryl Ester Transfer Protein Inhibitor in Healthy Human Subjects

(2009) R Wolk et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Pharmacokinetics, Metabolism, and Excretion of Anacetrapib, a Novel Inhibitor of the Cholesteryl Ester Transfer Protein, in Rats and Rhesus Monkeys

(2009) E. Y. Tan et al.   DRUG METABOLISM AND DISPOSITION

Metabolism and Excretion of Anacetrapib, a Novel Inhibitor of the Cholesteryl Ester Transfer Protein, in Humans

(2009) S. Kumar et al.   DRUG METABOLISM AND DISPOSITION

Macrophage cholesterol efflux correlates with lipoprotein subclass distribution and risk of obstructive coronary artery disease in patients undergoing coronary angiography

(2009) Patrick Linsel-Nitschke et al.   Lipids in Health and Disease

Multiple-Dose Pharmacodynamics and Pharmacokinetics of Anacetrapib, a Potent Cholesteryl Ester Transfer Protein (CETP) Inhibitor, in Healthy Subjects

(2008) R Krishna et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Metabolism, Pharmacokinetics, and Excretion of a Cholesteryl Ester Transfer Protein Inhibitor, Torcetrapib, in Rats, Monkeys, and Mice: Characterization of Unusual and Novel Metabolites by High-Resolution Liquid Chromatography-Tandem Mass Spectrometry and 1H Nuclear Magnetic Resonance

(2008) C. Prakash et al.   DRUG METABOLISM AND DISPOSITION

Pharmacokinetics, Metabolism, and Excretion of Torcetrapib, a Cholesteryl Ester Transfer Protein Inhibitor, in Humans

(2008) D. Dalvie et al.   DRUG METABOLISM AND DISPOSITION

Association of Loss-of-Function Mutations in the ABCA1 Gene With High-Density Lipoprotein Cholesterol Levels and Risk of Ischemic Heart Disease

(2008) Ruth Frikke-Schmidt   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Relationship of Paraoxonase 1 (PON1) Gene Polymorphisms and Functional Activity With Systemic Oxidative Stress and Cardiovascular Risk

(2008) Tamali Bhattacharyya   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Association of Cholesteryl Ester Transfer Protein Genotypes With CETP Mass and Activity, Lipid Levels, and Coronary Risk

(2008) Alexander Thompson   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Assessment of the CYP3A-Mediated Drug Interaction Potential of Anacetrapib, a Potent Cholesteryl Ester Transfer Protein (CETP) Inhibitor, in Healthy Volunteers

(2008) Rajesh Krishna et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Cholesterol efflux pathways and other potential mechanisms involved in the athero-protective effect of high density lipoproteins

(2008) A. R. Tall   JOURNAL OF INTERNAL MEDICINE