The class 390 items
CETP inhibition as a strategy: rationale, comparisons and where it stands today.
Studies
- Genetically lower CETP activity reduces dementia risk in a 1,091,775-person Mendelian randomization meta-analysis (Alzheimers Dement 2025)
- Landmark genetic study explains why CETP inhibitors lower LDL cholesterol without reducing cardiovascular events (JAMA 2017)
- Meta-regression of 312 175 patients shows CETP inhibitors deliver less cardiovascular benefit than their LDL-lowering predicts (JAMA 2016)
- Structural study proposes a tunnel-bridging mechanism for how CETP transfers cholesteryl ester between HDL and LDL (Nat Chem Biol 2012)
- First crystal structure of CETP reveals a 60-angstrom tunnel holding four lipid molecules (Nat Struct Mol Biol 2007)
- Cys-13, positioned near CETP's neutral-lipid-binding site, is identified as essential for irreversible inhibitor binding via mutagenesis and mass spectrometry (J Lipid Res 2000)
- A CETP-targeting vaccine cuts plasma CETP activity, raises HDL by 42%, and shrinks aortic lesions 39.6% in rabbits (Arterioscler Thromb Vasc Biol 2000)
- Drug-target Mendelian randomization finds lower CETP concentration cuts Lewy body and Parkinson's dementia risk, especially in APOE-e4 carriers (Alzheimers Res Ther 2024)
- A 425,354-person UK Biobank Mendelian randomization study finds genetically lower CETP cuts coronary artery disease risk with additive benefit alongside PCSK9 (JAMA Cardiol 2022)
- Drug-target Mendelian randomization confirms CETP as an effective target for coronary heart disease with an on-target macular degeneration risk (Nat Commun 2021)
- CETP inhibition is identified as the optimal target for managing dyslipidemia in systemic lupus erythematosus (Int Immunopharmacol 2025)
- Drug-target Mendelian randomization finds genetically proxied CETP inhibition protects against subarachnoid hemorrhage with no safety signal (Eur Stroke J 2025)
- Mendelian randomization finds CETP inhibition uniquely associated with increased breast cancer risk among lipid-lowering drug targets (Cancer Causes Control 2024)
- A genome-wide association study identifies protective CETP gene variants underlying cardiovascular resilience in older adults (J Am Heart Assoc 2023)
- Landmark hypothesis proposes CETP as an immunological gatekeeper that could be repurposed to treat sepsis (Trends Endocrinol Metab 2020)
- Protein-truncating CETP variants lower coronary heart disease risk by 30 percent in a 58 469-participant sequencing study (Circ Res 2017)
- A chimeric anti-CETP vaccine shrinks aortic plaques by over 40 percent in cholesterol-fed rabbits (Life Sci 2005)
- Liver-targeted antisense oligonucleotides against CETP suppress atherosclerosis in cholesterol-fed rabbits (J Biol Chem 1998)
- First demonstration that liver-targeted antisense oligonucleotides against CETP lower LDL and raise HDL in cholesterol-fed rabbits (J Biol Chem 1996)
- A meta-analysis of 62,565 patients confirms CETP inhibitors raise HDL cholesterol by 130 percent yet still fail to reduce cardiovascular events (J Cardiovasc Pharmacol 2026)
- CETP inhibitors reframed: from raising HDL to lowering atherogenic lipoproteins and improving glycaemic control, with obicetrapib the current lead (Circ Res 2026)
- Bayesian network meta-analysis of 84,134 patients ranks evacetrapib and anacetrapib best for cardiovascular outcomes among CETP inhibitors (Medicine 2026)
- Cis-Mendelian randomization finds CETP modification reduces both coronary disease and type 2 diabetes risk (Cardiovasc Diabetol 2026)
- CETP renaissance: a review maps obicetrapib reach beyond LDL-C into dementia, glycaemic control, sepsis and kidney function (Curr Atheroscler Rep 2026)
- From torcetrapib failure to obicetrapib promise: a full review of the mechanism and trial programme through PREVAIL (J Am Heart Assoc 2026)
- Network meta-analysis of 9,248 patients ranks obicetrapib plus ezetimibe plus statin best overall, obicetrapib plus statin safest among CETP-inhibitor combinations (J Cardiovasc Pharmacol 2026)
- Early-phase MACE signals predicted outcomes-trial results in 6 of 7 cholesterol drugs, dalcetrapib the exception (Am Heart J Plus 2026)
- CETP rs3764261 genotype modifies the HDL-C lowering effect of a vegetarian diet in 9,263 adults (Taiwan Biobank) (Front Nutr 2026)
- Mendelian randomization finds genetically proxied CETP inhibition sharply raises the risk of primary Sjögren's syndrome (Curr Pharm Biotechnol 2026)
- Obicetrapib review: an amphipathic CETP inhibitor cutting LDL-C 30-51%, apoB 20-33% and Lp(a) 30-57% across BROOKLYN, BROADWAY and TANDEM (Cardiol Rev 2025)
- Network meta-analysis of 33 RCTs in 120,292 adults: atorvastatin plus obicetrapib ranks best for LDL-C, rosuvastatin plus obicetrapib best for HDL-C (Clin Cardiol 2025)
- CETP inhibitors reduce disease severity in experimental colitis by reprogramming macrophages and boosting gut barrier function (J Lipid Res 2025)
- Mendelian randomization finds genetically proxied CETP inhibition reduces sepsis-related critical care admission and death (World J Emerg Med 2025)
- CETP inhibition as a longevity pathway: apoB lowering, not HDL raising, is the mechanism, with signals in diabetes, dementia and kidney disease (Curr Opin Lipidol 2024)
- First meta-analysis of nine CETP-inhibitor RCTs finds a class-wide reduction in cardiovascular mortality and myocardial infarction (J Cardiovasc Dev Dis 2024)
- CETP-derived peptide Seq-1 directly suppresses pro-fibrotic gene expression in liver cells beyond its role in the anti-CETP vaccine (Arch Med Res 2024)
- Combining CETP and SGLT2 inhibition genetically improves glycaemic control beyond either alone (Front Endocrinol (Lausanne) 2024)
- Drug-target Mendelian randomization links genetically lower CETP to longer human lifespan (Aging 2023)
- Beyond the heart: a review finds no excess macular degeneration risk across over 70,000 CETP-inhibitor trial patients, and surveys links to dementia, diabetes and sepsis (Pharmacol Res 2023)
- Genetic evidence suggests the HDL cholesterol-sepsis association is not causally mediated through CETP (Clin Transl Sci 2023)
- Mendelian randomization finds genetically proxied CETP inhibition, mediated through HDL cholesterol, reduces Crohn's disease risk (Front Immunol 2023)
- From raising HDL-C to lowering LDL-C: a review argues Mendelian randomisation and anacetrapib recast the whole CETP-inhibitor class (Cardiovasc Res 2022)
- CETP inhibition reduces major cardiovascular events through apoB lowering, a review argues, with obicetrapib cutting apoB by up to 30% (Int J Mol Sci 2022)
- Drug-target Mendelian randomization finds CETP and other lipid drug targets have distinct metabolomic signatures despite similar CAD benefit (PLoS Biol 2022)
- JACC review: four CETP inhibitors reached phase 3, one died, two were stopped for futility, and the survivor was shelved over fat accumulation (J Am Coll Cardiol 2019)
- Meta-analysis finds CETP inhibitor therapy cuts diabetes incidence by 12 percent (Diabetes Metab 2018)
- CETP redistributes the vasoprotective lipid sphingosine-1-phosphate from HDL to apoB lipoproteins, changing which signals it triggers (Arterioscler Thromb Vasc Biol 2017)
- Yamashita argues CETP inhibition may backfire by generating small dense LDL and downregulating hepatic SR-BI (Curr Opin Lipidol 2016)
- Mendelian randomization meta-analysis of 40,000 subjects finds lower circulating CETP causally reduces coronary heart disease risk (Circ Cardiovasc Genet 2015)
- BMJ meta-analysis of 117,411 patients finds niacin, fibrates, and CETP inhibitors do not reduce mortality on top of statins (BMJ 2014)
- Provocative 2014 opinion piece argues the evidence had turned against CETP inhibition and calls for an urgent trial review (F1000Res 2014)
- Meta-analysis of 12 trials finds CETP inhibitors raise HDL-c by 20.5 mg/dL and lower LDL-c by 17.1 mg/dL, with a blood-pressure signal from torcetrapib (PLoS One 2013)
- Higher on-statin CETP mass predicts fewer recurrent coronary events in the PROVE IT-TIMI 22 trial (Am J Cardiol 2010)
- Low plasma CETP predicts higher mortality in nondiabetic coronary disease patients in the KAROLA cohort (Eur J Clin Invest 2010)
- LURIC study of 3,256 angiography patients finds low, not high, CETP levels predict mortality (Circulation 2010)
- Higher circulating CETP activity predicts fewer cardiovascular events over 15 years in the Framingham Heart Study (Circulation 2009)
- Genetically low CETP predicts higher 10-year mortality in statin-treated men with coronary artery disease (Eur Heart J 2008)
- Hepatic lipase and CETP gene variants interact to raise HDL-C, but the combined genotype does not lower cardiovascular risk (J Clin Endocrinol Metab 2007)
- CETP haplotype linked to higher HDL-C across three populations shows no association with coronary heart disease risk (Hum Genet 2007)
- CETP inhibition in rabbits blocks one HDL cholesteryl ester removal pathway but does not compromise overall clearance from plasma (Arterioscler Thromb Vasc Biol 2005)
- An apoE-peptide carrier delivers antisense DNA into cell nuclei, cutting CETP mRNA over 50% and CETP activity to 53.8% of control in CHO cells (Arterioscler Thromb Vasc Biol 1999)
- CETP activity enhances plasma cholesteryl ester formation, confirmed in transgenic mice, hamsters, and humans with genetic CETP deficiency (Arterioscler Thromb Vasc Biol 1997)
- CGS 25159, a synthetic isoflavan CETP inhibitor, cuts VLDL+LDL cholesterol 28% and raises HDL cholesterol 29% in hamsters (Atherosclerosis 1997)
- Two novel compounds inhibit CETP by distinct mechanisms: U-95,594 competitively blocks all lipid transfer, U-617 selectively and irreversibly blocks CE transfer (Biochemistry 1995)
- A monoclonal antibody against CETP raises hamster HDL cholesterol 33% and cuts HDL triglyceride 42% in vivo (Atherosclerosis 1994)
- Natural flanking sequences enable dietary cholesterol to boost human CETP gene transcription up to fivefold in transgenic mice (J Clin Invest 1992)
- A neutralizing monoclonal antibody doubles HDL cholesteryl ester in rabbits by blocking CETP in vivo (J Clin Invest 1989)
- Mendelian randomisation suggests genetically proxied CETP inhibition may lower intracranial aneurysm risk (Neurosurg Rev 2026)
- CETP inhibitor trials reframe the HDL hypothesis around apoB lowering rather than HDL-C raising (Drugs 2026)
- A review traces how CETP-inhibitor design evolved from first-generation scaffolds plagued by off-target toxicity to optimized late-generation clinical candidates (Eur J Med Chem 2026)
- CETP inhibitors, state of the science: why torcetrapib, dalcetrapib, anacetrapib and evacetrapib failed and why obicetrapib is different (Curr Cardiol Rep 2026)
- The two faces of CETP inhibitors: a review argues the therapeutic case has shifted from raising HDL-C to lowering apoB, with obicetrapib as proof (Curr Opin Lipidol 2025)
- Review surveys why raising HDL with CETP inhibitors and apoA1 infusion has failed to cut cardiovascular events (Clin Med Res 2025)
- CETP inhibitors cut lipoprotein(a) by 46 percent, the largest reduction among all lipid-lowering drug classes in a 147-trial meta-analysis (Atherosclerosis 2025)
- Mendelian randomization links CETP inhibition to lower lacunar stroke risk via cerebral small vessel disease genetics (Brain 2025)
- Genetic CETP deficiency review: heterozygotes have lower ASCVD risk, homozygotes show no excess risk, and very high HDL-C raises AMD questions (J Atheroscler Thromb 2025)
- Mendelian randomization links CETP inhibition and elevated LDL cholesterol to Lewy body dementia risk (Prog Neuropsychopharmacol Biol Psychiatry 2025)
- Genetic proxies for CETP inhibition are linked to lower preeclampsia risk in a Mendelian randomization study (Int J Womens Health 2025)
- Meta-analysis of seven studies: adding a CETP inhibitor to high-intensity statins significantly raises HDL-C and lowers LDL-C with no added adverse events (Front Endocrinol 2025)
- Is obicetrapib a game changer? A review reframes CETP inhibition around apoB and LDL-C lowering rather than raising HDL-C (Expert Opin Pharmacother 2024)
- Mendelian randomization finds genetically raised HDL via CETP predicted to lower small vessel stroke risk (J Am Heart Assoc 2024)
- Obicetrapib, the rebirth of CETP inhibitors? A review of ROSE and ROSE2 phase 2 data ahead of four ongoing phase 3 trials (Curr Atheroscler Rep 2024)
- Mendelian randomization links the LDL-lowering effect of CETP to reduced obstructive sleep apnea risk (Toxicol Appl Pharmacol 2024)
- Reversing the tide of CETP inhibitor disappointments: a review of obicetrapib and its ROSE2 data ahead of pivotal phase 3 outcomes trials (Curr Atheroscler Rep 2024)
- HDL as a treatment target: a review says the obicetrapib outcomes trial will help decide whether to abandon the HDL hypothesis for good (Curr Atheroscler Rep 2023)
- A multiancestry Mendelian randomization study suggests CETP inhibition may protect against preeclampsia via HDL cholesterol (Hypertension 2023)
- Mendelian randomization identifies CETP inhibition as a potential heart failure prevention strategy, acting mainly through apoB (Eur J Prev Cardiol 2023)
- Review asks whether CETP inhibitors are still worth pursuing after two decades of disappointing trials (Curr Atheroscler Rep 2022)
- A review asks whether genomic analyses and post hoc trial insights can revive CETP inhibitors for cardiovascular prevention after past disappointments (Curr Opin Lipidol 2022)
- Updated meta-analysis confirms CETP inhibitors cut new-onset diabetes risk by 16 percent (Eur Heart J Cardiovasc Pharmacother 2022)
- LDL particle size governs how the natural CETP inhibitor ApoF binds and activates in hyperlipidaemic plasma (J Lipid Res 2022)
- Beyond failed HDL trials: a review argues the dal-GenE genomic-test approach to dalcetrapib and ADCY9 is the key to actionable HDL therapy (J Cardiovasc Pharmacol 2021)
- MK-8262 is invented as a best-in-class CETP inhibitor backup to anacetrapib after its 9% added cardiovascular risk reduction (J Med Chem 2021)
- CETP inhibitors in precision medicine: a review ties three phase 3 failures, the shelving of anacetrapib over fat accumulation, and the ADCY9 pharmacogenomic clue together (Clin Chim Acta 2020)
- A review argues the failure of CETP inhibitors and niacin to reduce cardiovascular events undermines the HDL cardioprotection hypothesis (Drugs 2020)
- Meta-analysis of 62,431 patients across 11 RCTs finds CETP inhibitors do not reduce major adverse cardiovascular events (RR 0.97) (Cardiology 2020)
- Liposomal CETP vaccine protects rabbits against atherosclerosis where the failed clinical peptide vaccine did not (Pharm Dev Technol 2019)
- An anacetrapib analog cuts CETP activity by 89% and reduces neointimal hyperplasia in bypassed rabbit veins by 38% (Sci Rep 2019)
- Meta-analysis of 332,912 patients: lowering apoB only cuts cardiovascular risk when it works through the LDL receptor, not via CETP inhibitors or fibrates (Eur J Prev Cardiol 2020)
- Do CETP inhibitors have a role in treating cardiovascular disease? A review weighs harm, futility and modest benefit against emerging genomic clues (Am J Cardiovasc Drugs 2019)
- Review contrasts disappointing CETP antagonists with the anti-inflammatory promise of the CETP agonist probucol (Atherosclerosis 2018)
- Unlike statins, anacetrapib lowers rather than raises new-onset diabetes risk on top of a coronary benefit, a review argues for a statin-plus-CETP-inhibitor combination (Atherosclerosis 2018)
- What the cetrapib trials taught us: torcetrapib, evacetrapib and anacetrapib all raised atherogenic apoproteins, muddying the HDL-raising story (Curr Opin Lipidol 2018)
- CETP and its inhibitors, a foundational review: structure, mechanism, non-lipid functions and the full outcomes-trial record for four small-molecule inhibitors (J Lipid Res 2018)
- Modeling shows adding a CETP inhibitor would push LDL-target attainment above 95 percent in familial hypercholesterolemia, versus just 54 percent with ezetimibe alone (J Clin Lipidol 2018)
- The present therapeutic role of CETP inhibitors: REVEAL numbers, HDL-C +104%, LDL-C -18%, major coronary events RR 0.91, against three prior failures (Pharmacol Res 2018)
- A new piperidine-based CETP inhibitor retains potency in hypertriglyceridemic plasma where other CETP inhibitors lose efficacy (J Med Chem 2017)
- Inhibiting CETP with des-fluoro-anacetrapib cuts in-stent intimal area by 43% via a scavenger receptor-B1-dependent pathway (ATVB 2017)
- Trials and tribulations of CETP inhibitors: the REVEAL benefit traces to lower non-HDL-C, not higher HDL-C, plus a small diabetes reduction (Circ Res 2018)
- Pharmacogenetics of HDL-targeting and statin therapies: dal-OUTCOMES and dal-PLAQUE-2 gave concordant results for dalcetrapib in the favourable genotype (Curr Atheroscler Rep 2017)
- Electron microscopy shows torcetrapib and anacetrapib block CETP by favoring binary complexes over ternary lipoprotein bridging (Biochim Biophys Acta 2017)
- Molecular dynamics simulations show torcetrapib, anacetrapib, and evacetrapib all destabilize the hydrophobic tunnel of CETP (J Biomol Struct Dyn 2018)
- Only 42% of 96,944 CETP-inhibitor trial subjects ever appeared in a published report, a case study in biomarker-driven drug development finds (Circ Cardiovasc Qual Outcomes 2017)
- Mendelian randomization finds HDL-raising CETP variants also raise the risk of age-related macular degeneration (Ophthalmology 2017)
- A Mediterranean diet enriched with olive oil lowers CETP activity and improves multiple HDL functions in the year-long PREDIMED trial (Circulation 2017)
- CETP rs708272 B2 allele is linked to a more antiatherogenic LDL subfraction profile in statin-treated coronary heart disease patients (Biochem Genet 2016)
- Plasma CETP causes pancreatic beta cell dysfunction via islet cholesterol accumulation in mice (Nutr Metab 2016)
- Phase 1 single ascending dose study of the CETP inhibitor CKD-519 shows potent target inhibition (Drug Des Devel Ther 2016)
- A review argues the failure of niacin to reduce cardiovascular events, alongside CETP inhibitor trial results, exposes the flaws of the HDL cholesterol hypothesis (Curr Atheroscler Rep 2015)
- Inhibiting CETP with des-fluoro-anacetrapib doubles capillary density in ischemic rabbit hindlimbs via SR-B1 and PI3K/Akt signaling (Int J Cardiol 2015)
- Inhibiting CETP with des-fluoro-anacetrapib nearly doubles re-endothelialization after balloon injury in rabbit aortas (ATVB 2015)
- A review argues cholesterol efflux capacity, not HDL cholesterol, is the more meaningful marker after CETP inhibitor and niacin trials failed to reduce cardiovascular outcomes (Prog Cardiovasc Dis 2015)
- Review from the discoverer of CETP deficiency in Japan surveys anacetrapib and evacetrapib as candidate cures for atherogenic dyslipidemia (Mol Cells 2014)
- Atomistic simulations show anacetrapib lodges in the N-terminal tunnel of CETP to block cholesteryl ester diffusion (PLoS Comput Biol 2014)
- Less lipophilic hexahydrofuroquinoline CETP inhibitor clears fat tissue quickly and avoids off-target hypertension signals (J Med Chem 2014)
- Meta-analysis of 69,515 patients finds niacin and CETP inhibitors do not reduce cardiovascular mortality (Nutr Metab Cardiovasc Dis 2015)
- Review asks whether anacetrapib and evacetrapib can succeed where torcetrapib and dalcetrapib failed to reduce cardiovascular risk (Annu Rev Med 2014)
- 10-Dehydrogingerdione raises HDL cholesterol by suppressing CETP and curbs oxidative and inflammatory markers in rabbits (Atherosclerosis 2013)
- Perspective argues HDL functionality, not HDL-C concentration, should guide the future evaluation of CETP inhibitors (Clin Pharmacokinet 2013)
- Antisense CETP inhibition, unlike anacetrapib, boosts macrophage reverse cholesterol transport in CETP-transgenic mice (J Lipid Res 2013)
- Schaefer argues CETP inhibitors fail to cut coronary risk because they disrupt normal HDL metabolism (Curr Opin Lipidol 2013)
- CETP inhibition boosts postprandial insulin secretion via enhanced cholesterol efflux from beta cells (Circ Res 2013)
- Endogenous CETP activity above 34% marks high cardiovascular risk in a cohort of 1,403 patients (Atherosclerosis 2013)
- Review tallies the HDL-C and LDL-C effects of each CETP inhibitor ahead of anacetrapib and evacetrapib outcomes in 2017 (Curr Pharm Des 2013)
- Unlike torcetrapib, dalcetrapib, evacetrapib, and anacetrapib do not raise blood pressure or aldosterone (Curr Opin Lipidol 2012)
- Review tallies CETP inhibitor trial results from the 2006 failure of torcetrapib to the early promise of evacetrapib (Curr Opin Lipidol 2012)
- Review weighs whether CETP inhibition can rescue the HDL-raising hypothesis after AIM-HIGH, HERS, ILLUMINATE, and dal-OUTCOMES (Curr Treat Options Cardiovasc Med 2012)
- Barter and Rye review the CETP inhibition hypothesis after the harm caused by torcetrapib and the futility of dalcetrapib (J Lipid Res 2012)
- Review distills lessons from the torcetrapib failure for the CETP inhibitors that followed it into clinical development (Curr Clin Pharmacol 2012)
- Review argues the off-target harm of torcetrapib is not a class effect shared by dalcetrapib, anacetrapib, and evacetrapib (Drugs 2012)
- First-in-human single dose study of the CETP inhibitor BAY 60-5521 shows dose-dependent CETP inhibition and HDL rise (Br J Clin Pharmacol 2012)
- Schwartz reviews conflicting CETP genetic and animal evidence ahead of the anacetrapib and dalcetrapib outcomes trials (Curr Atheroscler Rep 2012)
- A Nature Reviews Endocrinology paper argues HDL actively regulates glucose metabolism, positioning CETP inhibitors for rapid clinical translation to diabetes (Nat Rev Endocrinol 2012)
- Hop-derived xanthohumol prevents atherosclerosis in CETP-transgenic mice by inhibiting CETP and enriching HDL with apoE (PLoS One 2012)
- Review compiles dal-VESSEL, dal-PLAQUE, and DEFINE lipid results ahead of dal-OUTCOMES and REVEAL in 2013 and 2017 (Vasc Health Risk Manag 2012)
- Review recounts the termination of dalcetrapib and the broader questions it raises for CETP inhibition and the HDL hypothesis (Drug Des Devel Ther 2012)
- Barter and Rye ask where CETP inhibition stands after the off-target failure of torcetrapib (Trends Pharmacol Sci 2011)
- Sirtori weighs the cancer and sepsis signals of torcetrapib against the dramatic 139% HDL rise seen with anacetrapib (Expert Opin Investig Drugs 2011)
- Oxazolidinone-substituted benzoxazole CETP inhibitors raise HDL cholesterol up to 33 mg/dl in mice while avoiding hERG channel binding (Bioorg Med Chem Lett 2011)
- The original benzoxazole scaffold-redesign paper discovers CETP inhibitor 11v, raising HDL cholesterol by 24 mg/dl in mice (Bioorg Med Chem Lett 2011)
- Review argues CETP may be atheroprotective and aid host defense, complicating the case for inhibiting it (Cardiovasc Ther 2011)
- A review argues CETP inhibitor trial failures show HDL-C elevation alone is insufficient, motivating apoA-I-targeted therapies instead (Drugs 2010)
- Davidson explains how triglycerides turn CETP into a generator of small, dense, atherogenic LDL and HDL particles (J Clin Lipidol 2010)
- Chapman and colleagues place CETP at the center of how statins, fibrates, niacin, and CETP inhibitors modulate HDL (Eur Heart J 2010)
- Multiple-dose study of the CETP inhibitor CP-800,569 shows dose-dependent HDL rise and LDL fall (Clin Pharmacol Ther 2009)
- Hegele argues the pressor effect of torcetrapib, not CETP inhibition itself, doomed the drug and asks if the class deserves another chance (Curr Opin Cardiol 2009)
- Apolipoprotein CI regulates CETP activity in human plasma but not in rabbit plasma, a species-specific mechanism (J Lipid Res 2009)
- Serum cholesterol efflux capacity is preserved or enhanced in genetically CETP-deficient patients (Clin Chim Acta 2008)
- Review questions whether CETP inhibitors remain a viable therapeutic approach after a major trial failure (Cardiovasc Ther 2008)
- Review traces CETP inhibition from a Japanese deficiency discovery to the ILLUMINATE termination of torcetrapib and early anacetrapib data (Cardiol Rev 2008)
- CETP overexpression in transgenic mice does not impair macrophage reverse cholesterol transport or HDL's LDL-antioxidant activity (Atherosclerosis 2007)
- Rare CETP variants, not the common TaqIB marker, best explain the link of the gene to coronary artery disease in 4,811 patients (J Am Coll Cardiol 2007)
- Low serum albumin is the main driver of elevated CETP in children with active nephrotic syndrome (Clin Biochem 2007)
- Chimeric fusions of CETP with the bacterial-binding protein BPI retain function from both parent proteins up to a threshold (Biochemistry 2006)
- A review describes proof-of-principle preclinical and clinical results for a semi-annual CETP vaccine to raise HDL and address unmet cardiovascular need (Vascul Pharmacol 2006)
- Partial, not complete, CETP inhibition preferentially blocks lipid transfer to LDL while sparing HDL flux (Atherosclerosis 2006)
- Plasma cholesteryl ester transfer, driven by CETP and triglycerides, predicts carotid intima-media thickness in type 2 diabetes (Diabetes 2005)
- Human apoA-I overexpression strips apoC-I from HDL and removes most of HDL's natural CETP-inhibitory capacity in transgenic rats (J Lipid Res 2005)
- Review highlights two small-molecule CETP inhibitors substantially raising HDL cholesterol in clinical trials (Curr Opin Cardiol 2005)
- Type 2 diabetes eliminates the CETP elevation normally seen in obesity by suppressing hepatic CETP expression (J Clin Endocrinol Metab 2005)
- Elevated CETP mass helps explain smaller, denser LDL particles in familial hypercholesterolemia (J Lipid Res 2004)
- Insulin down-regulates CETP gene expression, reversing the elevation seen with insulin deficiency in transgenic mice (J Lipid Res 2003)
- Phase 1 trial finds a CETP vaccine induces anti-CETP antibodies and is well tolerated in healthy adults (Atherosclerosis 2003)
- Chiral optimization yields the most potent acyclic CETP inhibitor reported, with an IC50 of 0.77 nanomolar in buffer (J Med Chem 2003)
- Antisense knockdown of CETP in HepG2 cells raises cholesterol efflux to apoA-I but impairs SR-BI-mediated HDL cholesteryl ester uptake by the liver (Am J Physiol Endocrinol Metab 2003)
- Chiral resolution of a trifluoro-3-amino-2-propanol lead reveals a 40-fold potency boost, reaching IC50 0.02 micromolar against CETP (J Med Chem 2002)
- Clamp-induced suppression of CETP activity is unrelated to whole-body insulin sensitivity, exercise-training study finds (Metabolism 2001)
- A fructose-enriched diet raises plasma and adipose CETP in hamsters despite lowering, not raising, insulin levels (Life Sci 2001)
- Serum CETP is higher in women and higher still in Chinese myocardial infarction and stroke patients than in healthy controls (Clin Chim Acta 2001)
- One week of a high-cholesterol diet paradoxically shrinks myocardial infarct size in CETP-transgenic mice (Coron Artery Dis 2001)
- Insulin fails to activate the CETP gene promoter in transfected rat fibroblasts, despite a role for C/EBPalpha (Mol Cell Biochem 2000)
- Blocking CETP-mediated cholesteryl ester transfer with an antibody makes LDL more resistant to oxidative modification (J Lipid Res 2000)
- CETP is expressed early in human preadipocyte-to-adipocyte differentiation, ahead of known adipogenic transcription factors (Atherosclerosis 1999)
- Ovariectomy reduces CETP activity in liver and adipose tissue of transgenic mice, and hormone replacement fails to restore it (Metabolism 1998)
- A 28-residue peptide from hog plasma, related to apoC-III, inhibits CETP and clears 75 percent of plasma activity within an hour in vivo (Biochim Biophys Acta 1998)
- Simvastatin and cholestyramine both lower serum CETP activity in rabbits while leaving LCAT activity essentially unchanged (Cardiovasc Drugs Ther 1998)
- CETP contains an essential free cysteine in a hydrophobic pocket, inactivated by thiol-modifying reagents at nanomolar concentrations (Biochem Biophys Res Commun 1996)
- CETP mRNA abundance in human adipose tissue tracks membrane cholesterol content, not stored lipid droplet cholesterol (J Lipid Res 1995)
- Acute hyperinsulinemia lowers plasma CETP activity in diabetic patients but not in healthy subjects (Metabolism 1994)
- Antibody-mediated CETP inhibition raises HDL 30 to 40 percent and produces large apoE-rich HDL particles in hamsters, peaking at day 4 (J Lipid Res 1994)
- A natural CETP inhibitor in selectively bred high-HDL baboons is identified as an N-terminal apoC-I fragment that binds apoA-I (J Lipid Res 1993)
- CETP activity tracks its own mRNA closely in cholesterol-fed rabbits, while hepatic lipase regulation appears mostly post-transcriptional (Biochim Biophys Acta 1991)
- A neutralizing antibody's epitope maps to CETP's C-terminal lipid-binding region, revealing its inhibition mechanism (J Biol Chem 1989)
- Inhibiting CETP amplifies apoA-IV and apoE redistribution among lipoproteins during ex vivo plasma incubation (J Lipid Res 1989)
- Review highlights CETP inhibition improving survival in a mouse model of sepsis (Curr Opin Lipidol 2026)
- Molecular dynamics show mixed cholesteryl-ester and triglyceride cargo twists CETP into strained, asymmetric conformations (Phys Chem Chem Phys 2026)
- Review surveys how current and emerging lipid therapies, including CETP inhibitors, affect lipoprotein(a) levels (Eur Cardiol 2026)
- Beyond small-molecule inhibitors: a review surveys CETP-targeted immunotherapy and vaccines as an emerging route to raising HDL (Hum Vaccin Immunother 2025)
- Chlorinated diaryl sulfonamides identified as potent new CETP inhibitors reaching 100 percent inhibition (Curr Comput Aided Drug Des 2025)
- Unlike statins and ezetimibe, CETP inhibitors show only a slight, non-significant rise in CRP across a 53-trial meta-analysis (Cardiovasc Res 2024)
- Review questions whether elevated HDL cholesterol truly protects against cardiovascular disease (J Clin Endocrinol Metab 2024)
- Novel trifluoromethyl benzamides identified as potent CETP inhibitors with sub-micromolar activity (Curr Comput Aided Drug Des 2024)
- Review names CETP among four validated targets for novel lipid-lowering therapies to prevent cardiovascular disease (Nat Rev Cardiol 2023)
- How CETP moves cholesterol between lipoproteins: a structural review of the mechanism behind torcetrapib, anacetrapib and obicetrapib (Curr Atheroscler Rep 2023)
- Mendelian randomization finds HDL cholesterol protective against diabetic retinopathy, but genetically proxied CETP inhibition shows no effect (Atherosclerosis 2023)
- A review of HDL biology in atherosclerotic cardiovascular disease highlights the shift from HDL quantity to HDL quality, with attention to CETP inhibitor trial outcomes (Clin Investig Arterioscler 2023)
- Bis(trifluoromethyl) benzylamino benzamides identified as potent new CETP inhibitor lead compounds (Med Chem 2022)
- Viewpoint charts efforts to optimize anacetrapib into a best-in-class CETP inhibitor (J Med Chem 2021)
- Molecular dynamics simulations reveal how sugar chains on CETP shape its lipid-transfer tunnel (J Chem Inf Model 2021)
- CETP pathophysiology and inhibition, an update: the drug class biology, trial status and adverse effects surveyed before obicetrapib phase 3 (Drug Discov Today 2021)
- Trivalent implant vaccine targets PCSK9, ApoB, and CETP as "cholesterol checkpoint" proteins (Adv Ther (Weinh) 2021)
- Cyclic and bicyclic urea and sulfamide cores yield new CETP inhibitors effective in vivo (Bioorg Med Chem Lett 2020)
- Apolipoprotein F emerges as a natural, LDL-selective inhibitor of CETP (Curr Opin Lipidol 2020)
- Population pharmacokinetic-pharmacodynamic model recommends a 200 to 400 mg dose of the CETP inhibitor CKD-519 (Pharmaceutics 2020)
- Book chapter reviews CETP research from its discovery to the disappointing clinical-trial era (Adv Exp Med Biol 2020)
- LXR and PPAR-alpha agonists suppress ApoF, the natural CETP regulator, via a shared hormone response element (Biochim Biophys Acta Mol Cell Biol Lipids 2019)
- A reformulated version of the CETP inhibitor DRL-17822 reduces its food-driven exposure spike (Clin Pharmacol Drug Dev 2019)
- Lead triphenylethanamine CETP inhibitor shows clean blood pressure profile and robust efficacy (ACS Med Chem Lett 2019)
- Review asks whether anacetrapib, the fourth CETP inhibitor tested, finally outperforms its predecessor drugs (Cardiol Rev 2019)
- Meta-analysis of 154,601 patients: HDL-raising drugs including CETP inhibitors do not cut cardiovascular or all-cause mortality, and any MI benefit traces to fibrates (Eur J Prev Cardiol 2019)
- Anacetrapib reproduced the CETP-deficiency phenotype and showed a highly significant, if moderate, coronary benefit in REVEAL, a review on HDL and atherogenic inflammation notes (Atherosclerosis 2018)
- CV risk, CV benefit, or both? A review takes stock of CETP inhibitors after preclinical promise met mostly disappointing outcome trials (Clin Pharmacol Ther 2018)
- Combining policosanol with 10-dehydrogingerdione strengthens CETP inhibition and lowers platelet activation in dyslipidaemic rabbits (Appl Biochem Biotechnol 2018)
- CETP inhibitors as agents to reduce coronary heart disease risk: after earlier trial failures, REVEAL showed anacetrapib actually works (Cardiol Clin 2018)
- Patent review tracks CETP inhibitor development from 2009 to 2017 despite four phase 3 drugs falling short on cardiovascular outcomes (Expert Opin Ther Pat 2018)
- Nat Rev Cardiol commentary: the REVEAL coronary benefit from CETP inhibition is probably down to lowering non-HDL-C, not raising HDL-C (Nat Rev Cardiol 2017)
- N,N-substituted amine derivatives yield a sub-micromolar CETP inhibitor lead compound (Molecules 2017)
- A review traces the evolution of HDL-raising therapeutics from niacin and fibrates to CETP inhibitors, reconstituted HDL, and apoA-I mimetics (Curr Pharm Des 2017)
- Fluorinated benzamide CETP inhibitors reach sub-micromolar potency, with fluorine position dictating activity (Med Chem 2017)
- Review weighs whether anacetrapib can succeed as a cardioprotective CETP inhibitor where earlier drugs failed (Drug Des Devel Ther 2017)
- MF59-adjuvanted CETP vaccine protects rabbits from atherosclerosis without a strong antibody or CETP-activity effect (Iran J Basic Med Sci 2016)
- Review surveys CETP inhibitor outcome trials from the harm of torcetrapib to the futility of later agents (Curr Opin Lipidol 2016)
- Review compares torcetrapib, evacetrapib, dalcetrapib and anacetrapib trial outcomes and the future of CETP inhibition (J Cardiovasc Pharmacol Ther 2017)
- CETP inhibitors, challenges and perspectives: off-target failure for torcetrapib, futility for dalcetrapib and evacetrapib, early promise for anacetrapib and TA-8995 (Expert Rev Cardiovasc Ther 2016)
- Review distinguishes humanized-mouse from rabbit models to find where CETP inhibition truly protects against atherosclerosis (Eur J Clin Invest 2016)
- CETP inhibition is not yet dead, argues a pro perspective ahead of the REVEAL trial (Arterioscler Thromb Vasc Biol 2016)
- Review weighs past CETP inhibitor trial failures against hopes for newer, more favourable agents (Clin Med Insights Cardiol 2016)
- Review asks whether anacetrapib is the last surviving CETP inhibitor as REVEAL results loom (Expert Opin Pharmacother 2016)
- Optimised benzylaminopropanamide derivative HL16 emerges as a sub-micromolar CETP inhibitor active in hamsters (Bioorg Med Chem 2015)
- Review previews two pending phase 3 trials that will decide the future of CETP inhibition (Curr Opin Lipidol 2015)
- Policosanol-loaded reconstituted HDL inhibits CETP activity by up to 47 percent and promotes tissue regeneration (Rejuvenation Res 2015)
- Review argues CETP inhibitors remain the most potent HDL-raising agents but their cardiovascular benefit is still unproven (Clin Ther 2015)
- Review argues patient stratification, and caution in sepsis, are needed before CETP can succeed as a drug target (Expert Opin Ther Targets 2015)
- Meta-analysis finds adding a CETP inhibitor to statin therapy does not reduce cardiovascular events (Int J Cardiol 2015)
- Modeling shows the short half-life of the CETP inhibitor RG7232 drives oscillating on/off effects on lipoprotein metabolism (CPT Pharmacometrics Syst Pharmacol 2015)
- Meta-regression of 167 311 patients finds raising HDL cholesterol with CETP inhibitors does not predict clinical benefit (Heart 2015)
- Systematic review tracks CETP inhibitors from the toxicity of torcetrapib to the greater potency and safety of anacetrapib and evacetrapib (Am J Ther 2015)
- Review argues HDL-raising therapy remains an unmet cardiovascular need after torcetrapib and dalcetrapib failures (Transl Med UniSa 2015)
- A review names failed CETP-inhibitor and niacin trials as key evidence complicating the HDL-cholesterol paradigm for cardiovascular prevention (Clin Pharmacol Ther 2014)
- Amino-acid-modified fungal pigment derivatives yield micromolar, non-competitive CETP inhibitors (Nat Prod Res 2014)
- Unlike torcetrapib, anacetrapib raises HDL-C by 138% without elevating blood pressure or disturbing electrolytes (Cardiol Rev 2014)
- Review names CETP inhibition among the most promising pharmacological approaches to raising HDL despite recent trial failures (Curr Opin Lipidol 2013)
- A review names CETP inhibition among three specific pharmacological strategies to boost reverse cholesterol transport (Indian J Exp Biol 2013)
- Perspective reviews the discovery and development of CETP inhibitors for reducing residual cardiovascular risk (J Med Chem 2014)
- Review narrates the CETP inhibitor class from the mortality excess of torcetrapib to the still-pending REVEAL and ACCELERATE trials (Curr Opin Cardiol 2013)
- Review surveys torcetrapib, dalcetrapib, anacetrapib, and evacetrapib as HDL-raising targets after the mortality signal in ILLUMINATE (Curr Vasc Pharmacol 2012)
- Baseline plasma CETP activity is elevated in dyslipidaemic patients and correlates with triglycerides (Int J Clin Pharmacol Ther 2012)
- Optimised DPPE-derivative CETP inhibitor shows robust efficacy without raising blood pressure in telemetered rats (J Med Chem 2012)
- Tetrahydronaphthyridine CETP inhibitors reach nanomolar potency and raise HDL-C in transgenic mice (Bioorg Med Chem Lett 2012)
- Modeling predicts an effective human dose for the CETP inhibitor BAY 60-5521, later confirmed in a first-in-man study (Br J Clin Pharmacol 2012)
- Review positions anacetrapib as free of the off-target toxicity of torcetrapib, with phase III trial results still awaited (Expert Opin Investig Drugs 2012)
- Review by the developers of anacetrapib frames CETP inhibition as a new approach to cutting cardiovascular risk (Clin Pharmacol Ther 2012)
- Review calls anacetrapib a new weapon against dyslipidemia, pending long-term mortality data (Curr Clin Pharmacol 2011)
- Review surveys the controversial CETP-atherosclerosis relationship and emerging roles in Alzheimer's disease, inflammation and obesity (IUBMB Life 2011)
- A review classifies novel HDL-raising drugs into four strategies, including CETP inhibition, to address residual cardiovascular risk (Nat Rev Cardiol 2011)
- Review argues lipid therapy must look beyond LDL, citing CETP inhibition as promising but still unproven in outcome trials (Curr Pharm Des 2011)
- Review finds anacetrapib and dalcetrapib safely raise HDL-C without the off-target effects that doomed torcetrapib (Ann Pharmacother 2011)
- Two CETP inhibitors reach systemic circulation mainly via lymphatic transport, 22 to 28% of dose (Pharm Res 2010)
- Review asks whether anacetrapib offers the greatest HDL-raising, LDL-lowering promise among CETP inhibitors (Cardiovasc Ther 2011)
- Drug profile tracks the path of anacetrapib from Merck development into a 76-week international phase III trial (Am J Cardiovasc Drugs 2010)
- Review finds the lipoprotein effects of anacetrapib surpass both torcetrapib and dalcetrapib, though long-term safety remains unproven (Curr Opin Investig Drugs 2009)
- Patent landscape review tracks CETP inhibitor development from 2000 through the termination of torcetrapib (Expert Opin Ther Pat 2009)
- Review highlights a paradox, CETP protects against bacterial infection but promotes atherosclerosis (Atherosclerosis 2009)
- Review asks whether JTT-705 (dalcetrapib) or anacetrapib can still succeed after the collapse of torcetrapib (Expert Opin Investig Drugs 2008)
- Neither high CETP activity nor low HDL cholesterol predicts cardiovascular events in stage V chronic kidney disease (Nephrol Dial Transplant 2008)
- Review reconsiders the protective reputation of HDL after the abrupt ILLUMINATE failure of torcetrapib (Biochem Pharmacol 2008)
- A review classifies CETP among the HDL-elevating drug targets, distinct from ApoA1-mimetic fast-acting approaches, for treating atherosclerosis (Cardiovasc Hematol Agents Med Chem 2007)
- Review of thirteen clinical CETP-inhibition studies finds pharmacological inhibitors raise HDL-C more consistently than vaccines (Curr Med Res Opin 2006)
- Review dissects biochemical pathways beyond HDL-C by which CETP inhibition might protect against atherosclerosis (Arterioscler Thromb Vasc Biol 2006)
- Displaying CETP B cell epitopes on asparaginase induces high-titer anti-CETP antibodies lasting over eighteen weeks in mice (Protein Pept Lett 2006)
- ABCG1's discovery as a large-HDL cholesterol exporter suggests CETP inhibition may enhance, not reduce, cholesterol efflux (Curr Opin Lipidol 2005)
- Clinician update reviews how CETP inhibition raises HDL by 50 to 100 percent in humans but flags mixed results across metabolic contexts (Circulation 2005)
- Review names CETP inhibition as one of the two most important new targets for raising HDL cholesterol (Neth Heart J 2004)
- Review surveys CETP as a pivotal HDL-raising drug target as human CETP inhibitor data become available (J Lipid Res 2004)
- Adjuvant-free Hsp65-CETP fusion vaccine induces antibodies lasting over 12 weeks and partially normalizes CETP activity in mice (Vaccine 2004)
- Review confirms CETP promoter variant -629 C to A, not TaqIB, drives CETP activity, and finds no TaqIB-pravastatin pharmacogenetic interaction (Curr Opin Lipidol 2004)
- Review positions CETP as a new therapeutic target, noting statins and fibrates already attenuate its activity indirectly (Pharmacol Ther 2004)
- Review proposes CETP-driven cholesteryl ester transfer as the metabolic link between high triglycerides and low HDL cholesterol in insulin resistance (Eur J Clin Invest 2003)
- Early phase I and II data show CETP inhibitors raise HDL-C by up to 70 percent, though effects on triglycerides remain unclear (Curr Opin Investig Drugs 2003)
- Review argues the time is right to test CETP inhibition in randomized human atherosclerosis trials (Arterioscler Thromb Vasc Biol 2003)
- Early review surveys progress toward antisense and small-molecule CETP inhibitors as HDL-raising therapies (Curr Opin Drug Discov Devel 2001)
- Replacing a tetrafluoroethoxy group with 2-furyl heteroaryl moieties yields submicromolar CETP inhibitors in a new trifluoro-propanol series (Bioorg Med Chem Lett 2001)
- Different dietary fatty acids produce distinct postprandial CETP activity responses in healthy young men (Am J Clin Nutr 2001)
- A chiral CETP inhibitor binds the protein 5,000-fold more efficiently than its natural lipid substrate (Biochemistry 2000)
- Ferroverdin B, isolated from a soil Streptomyces, is among the most potent microbial CETP inhibitors known, with an IC50 of 0.62 micromolar (J Antibiot (Tokyo) 1999)
- Fungal azaphilones inhibit CETP by forming a covalent bond with a lysine amine, with potency tracking ketone placement on the isochromane ring (J Antibiot (Tokyo) 1999)
- An (i, i+4) residue array between His466 and Asp470 stabilizes an amphipathic alpha-helix in CETP's C-terminus (Biochim Biophys Acta 1998)
- Phage-display screening yields a pentapeptide, WRMWY, that competitively inhibits CETP (J Pept Res 1998)
- Negatively charged surface lipids slow CETP-mediated cholesteryl ester transfer between microemulsion particles, positively charged lipids speed it up (Biochem J 1997)
- Hepatic CETP secretion rises with dietary cholesterol in a dose-dependent, strain-independent manner in rabbits (Comp Biochem Physiol B Biochem Mol Biol 1996)
- Antibody-mediated CETP inhibition in hamsters produces apoE-rich, apoA-I-poor HDL particles that revert toward baseline within two weeks (Lipids 1995)
- Palmitic and lauric acid diets do not differ in CETP activity from each other, but lauric acid raises CETP activity above baseline (J Nutr 1995)
- PD 140195, a triazole-thiol CETP inhibitor that mimics cholesteryl ester structurally, works noncompetitively and selectively blocks cholesteryl ester over triglyceride transfer (Lipids 1994)
- Sodium butyrate induces a 3- to 4-fold rise in CETP mRNA in HepG2 liver cells, a model for CETP hepatic regulation (Eur J Biochem 1993)
- Review forecasts CETP activity as a promising future pharmaceutical target beyond conventional lipid-lowering (Circulation 1993)
- CETP variants rs2033254 and rs12708980 associate with lower intestinal cholesterol absorption markers in a European GWAS (Nutrients 2026)
- Preclinical safety battery clears the anti-CETP intranasal vaccine HB-ATV-8 for cardiac, mutagenic and metabolic risk (Arch Med Res 2026)
- Review surveys the evolving landscape of lipid-lowering drug targets, from statins to CETP and Lp(a) inhibition (Eur Heart J 2025)
- A review positions CETP alongside PCSK9 and CYP7A1 as the three central druggable regulators of cholesterol homeostasis (Life Sci 2024)
- Review links HDL dysfunction in type 2 diabetes to impaired glycaemic control and highlights CETP inhibitors as a candidate therapy (Curr Med Chem 2024)
- Review proposes CETP inhibition among potential HDL-directed treatments for sepsis (Int J Mol Sci 2022)
- QSAR models predict CETP inhibitory potency of 108 oxazolidinone derivatives (SAR QSAR Environ Res 2020)
- Ursolic acid ester derivatives designed as novel plant-based CETP inhibitors (Bioorg Med Chem Lett 2019)
- Preclinical pharmacokinetic modeling predicts a human dose of the CETP inhibitor CKD519 before phase 1 data revealed a gap (Pharmaceutics 2019)
- Review of new oral dyslipidaemia drugs names anacetrapib the only CETP antagonist that reduces cardiovascular events (Eur J Prev Cardiol 2020)
- Review questions whether HDL cholesterol is a modifiable treatment target after disappointing CETP inhibitor trials (JRSM Cardiovasc Dis 2019)
- Early formulation work solves the poor solubility of the CETP inhibitor CKD-519 ahead of phase 1 testing (Int J Pharm 2018)
- Review ranks CETP and ANGPTL3 inhibition among the most promising novel LDL-lowering strategies (Curr Opin Lipidol 2018)
- CETP inhibitors do not appear to raise new-onset diabetes risk unlike LDL-receptor-acting drugs (J Cardiovasc Pharmacol Ther 2018)
- Lipid-based formulations boost oral exposure of a poorly soluble CETP inhibitor up to 10-fold in preclinical species (J Pharm Sci 2018)
- A hospital pharmacy bulletin sums up CETP inhibitors for practising pharmacists: three failures, then a REVEAL success for anacetrapib (Hosp Pharm 2017)
- Review maps CETP-mediated transfer as the indirect route of reverse cholesterol transport to the liver (Anatol J Cardiol 2017)
- CETP inhibitors lower lipoprotein(a) by around 50 percent, review notes, in comparison with apheresis and other new drugs (Atheroscler Suppl 2017)
- A new cycloalkene-scaffold CETP inhibitor raises HDL cholesterol in hamsters (Eur J Med Chem 2016)
- Novel benzylaminopropionanilide CETP inhibitors raise HDL and lower LDL in hamsters (Bioorg Med Chem 2016)
- A structure-guided approach discovers a novel indoline series of CETP inhibitors (ACS Med Chem Lett 2016)
- Handbook chapter surveys emerging HDL-targeted drugs, from CETP inhibitors to PPAR and LXR agonists (Handb Exp Pharmacol 2015)
- Review updates the pipeline of emerging hyperlipidaemia drugs, focused mainly on anacetrapib and evacetrapib (Expert Opin Emerg Drugs 2014)
- New synthesis route scales a polycyclic CETP inhibitor to multikilogram quantities (Org Lett 2014)
- Review of hypertriglyceridemia drugs places CETP and ANGPTL3/4 inhibitors among agents enhancing triglyceride-rich lipoprotein clearance (Prog Lipid Res 2014)
- Review previews upcoming dyslipidaemia drugs, from CETP inhibitors to PCSK9 inhibitors and MTP inhibitors (J Cardiovasc Pharmacol Ther 2015)
- Review questions where CETP inhibitors will fit clinically outside patients with very low HDL cholesterol (Expert Opin Investig Drugs 2014)
- Diphenylpyridylethanamine-based aminoheterocycles optimised as CETP inhibitors with better metabolic stability (Bioorg Med Chem Lett 2014)
- Review surveys HDL-targeted therapies as CETP inhibitor trials split between discontinuation and ongoing phase III testing (Circ Res 2014)
- Review argues CETP inhibitor failures show over-reliance on HDL cholesterol as an efficacy marker (Clin Lipidol 2013)
- Review asks why targeting HDL for cardiovascular protection has not delivered clinical benefit (J Cardiovasc Pharmacol 2013)
- Validated comparative QSAR modelling of 104 CETP inhibitors identifies key structural drivers of potency (Comput Biol Med 2013)
- A stroke-prevention review flags CETP inhibitor trial success as a potential turning point for dyslipidemia treatment (Maturitas 2013)
- Review notes CETP inhibitors raise HDL-C by 31-138 percent, but whether this lowers coronary risk remains unresolved (Circ J 2013)
- Broad review on residual cardiovascular risk after statins notes anacetrapib and evacetrapib survive where two other CETP compounds failed (Vasc Health Risk Manag 2013)
- Fluorinated diphenylpyridylethanamine derivatives balance metabolic stability and CETP potency (Bioorg Med Chem Lett 2012)
- Quinoline-3-carboxamide derivatives reach 80.1 percent CETP inhibitory activity in newly designed series (Molecules 2012)
- Review synthesises structural and biophysical evidence for how CETP moves lipids between HDL and LDL (Biochem Soc Trans 2011)
- Natural compound isolated from ginger rhizome inhibits CETP with an IC50 of 35 micromolar (Arch Pharm Res 2011)
- New biphenyl oxazolidinone CETP inhibitor scaffold reaches sub-100 nanomolar potency (ACS Med Chem Lett 2011)
- Chromanol derivatives emerge as a novel class of orally active CETP inhibitors suitable for clinical development (Bioorg Med Chem Lett 2011)
- 2-Arylbenzoxazole CETP inhibitors raise HDL cholesterol in cynoCETP transgenic mice (Bioorg Med Chem Lett 2011)
- Lead biphenyl CETP inhibitor 12d significantly raises HDL in a transgenic mouse model (Bioorg Med Chem Lett 2010)
- Lead benzylamino-methanone compound achieves 30 percent CETP inhibition at 10 micromolar (Molecules 2010)
- Novel tetrahydrochinoline derivatives yield a potent CETP inhibitor with favourable pharmacokinetics for clinical development (Bioorg Med Chem Lett 2010)
- Pharmacophore and QSAR modelling identifies new CETP inhibitor leads including NSC 40331 at 6.5 micromolar (Eur J Med Chem 2010)
- A new benzoxazine class of CETP inhibitors raises HDL cholesterol in transgenic mice and hamsters (Bioorg Med Chem Lett 2010)
- Lead 2-arylbenzoxazole compound inhibits CETP with an IC50 of 28 nanomolar (Bioorg Med Chem Lett 2009)
- Improved asymmetric synthesis route delivers a potent tetrahydroquinoline CETP inhibitor without a hazardous aryltin reagent (Org Lett 2009)
- Review surveys CETP's role in lipid metabolism and the state of small-molecule inhibitor development for raising HDL-C (Curr Top Med Chem 2009)
- Clinician's overview names CETP inhibitors the most potent HDL-raising drugs, but torcetrapib fell to excess cardiovascular harm (Angiology 2009)
- 3D-QSAR modelling of 61 dibenzodioxepinone and dibenzodioxocinone compounds maps the structural features driving CETP inhibitory potency (Molecules 2008)
- Review weighs conflicting evidence for CETP as a pro- versus antiatherogenic therapeutic target (Expert Opin Ther Targets 2008)
- Serum CETP is lowest at birth and rises sharply to peak levels in infancy, reference data from healthy Chinese children (Clin Biochem 2008)
- Array synthesis optimizes a high-throughput screening hit into a novel 2-arylbenzoxazole CETP inhibitor series (Bioorg Med Chem Lett 2008)
- Review recounts how ILLUMINATE, RADIANCE, and ERASE ended the promise of torcetrapib for isolated low HDL syndrome (Am J Ther 2008)
- 2D and hologram QSAR models of 85 trifluoro-aminopropanol CETP inhibitors identify key structural drivers of potency (Bioorg Med Chem 2007)
- Tetrazole and ester substituted tetrahydroquinoxalines emerge as a potent new class of CETP inhibitors (Bioorg Med Chem Lett 2007)
- Review surveys recent findings on plasma lipid transfer proteins including CETP's role in HDL delivery and coronary risk (Curr Opin Lipidol 2006)
- Review traces how statins raise HDL cholesterol partly via a secondary reduction in CETP activity (Curr Atheroscler Rep 2006)
- Optimized dibenzodioxocinone derivatives yield low-nanomolar CETP inhibitors stable in rat plasma (Bioorg Med Chem Lett 2005)
- Review makes the case for pharmacological CETP inhibition as a therapeutic strategy pending clinical trial confirmation (Curr Top Med Chem 2005)
- Review weighs CETP inhibition's physiology and animal-to-human evidence as a candidate route to raising HDL cholesterol (Curr Atheroscler Rep 2004)
- CETP localizes to germinal centre B cells and their neoplastic lymphoma counterparts (Histopathology 2004)
- Electron-withdrawing substituents boost potency in a new propanethioate class of CETP inhibitors, reaching 50 percent inhibition at 2 micromolar (Bioorg Med Chem Lett 2004)
- Chemically induced P-407 mouse model of hyperlipidemia indirectly raises CETP activity while directly inhibiting lipoprotein and hepatic lipase (J Cardiovasc Pharmacol 2004)
- Review argues the role of CETP and reverse cholesterol transport defects in diabetic atherosclerosis remains unproven, despite altered HDL composition (Diabetes Metab Res Rev 2000)
- A domino Mukaiyama-Michael/Michael/Aldol cyclization efficiently builds pentasubstituted arene cores for potent CETP inhibitors (Angew Chem Int Ed Engl 1999)
- Erabulenols A and B, new fungal metabolites from a soil Penicillium isolate, inhibit human CETP with IC50 values of 47.7 and 58.2 micromolar (J Antibiot (Tokyo) 1998)
- A fungal depsipeptide, SCH 58149, shows weak CETP inhibitory activity with an IC50 of 50 micromolar (Bioorg Med Chem Lett 1998)
- Polyacetylene compounds isolated from Korean ginseng roots inhibit human CETP (Chem Pharm Bull (Tokyo) 1996)
- A multi-step synthesis from diosgenin yields two novel cholest-15-one steroids tested for CETP-inhibiting activity (Bioorg Med Chem 1995)
- Review weighs the shuttle versus ternary-complex models for how CETP transfers lipids and flags evidence for a pro-atherogenic role (Clin Exp Pharmacol Physiol 1994)
- Fragment-based design yields a novel pentacyclic triterpenoid CETP inhibitor with sub-micromolar potency (Eur J Med Chem 2017)
- Brief review previews CETP inhibitor trial results as REVEAL data for anacetrapib approaches (Eur Cardiol 2015)
- New tetrazolyl tetrahydroquinoline CETP inhibitors raise HDL cholesterol in a transgenic mouse model (Bioorg Med Chem Lett 2012)
- Modifying the alpha-alkoxyamide moiety of arylbenzoxazole CETP inhibitors yields an orally bioavailable lead (Bioorg Med Chem Lett 2010)
- CETi-1, AVANT Immunotherapeutics CETP-targeting vaccine, entered Phase II trials for hypercholesterolemia and atherosclerosis by 2001 (Curr Opin Investig Drugs 2004)
- Ferroverdins B and C, natural CETP inhibitors from Streptomyces, are elucidated as iron complexes of nitroso-hydroxybenzoate ligands (J Antibiot (Tokyo) 1999)
- Erabulenols A and B, fungal CETP inhibitors, share a phenalenone-tetrahydrofuran core, with a hydroxy-methylketonyl benzyl group distinguishing erabulenol B (J Antibiot (Tokyo) 1998)