Pharmacology 226 items
Dose, exposure, interactions, and the tissue accumulation that ended one programme.
Studies
- A 50% rise in CETP activity after probucol tracks plasma drug levels and inversely predicts the fall in HDL cholesterol (Eur J Clin Invest 1991)
- Niacin raises HDL cholesterol by suppressing hepatic CETP expression, not by any CETP-independent route (Arterioscler Thromb Vasc Biol 2008)
- First-in-class phase I trials show anacetrapib raises HDL-C by 129% and lowers LDL-C by 38% without raising blood pressure (Lancet 2007)
- Vitamin E blocks the CETP-lowering effect of pravastatin and raises CETP concentration on its own (Coron Artery Dis 1998)
- Medicinal chemistry paper describes the structure-activity work that led to the discovery of anacetrapib (J Med Chem 2011)
- Ciprofibrate boosts CETP gene expression and speeds cholesterol delivery to the liver in CETP-transgenic mice (Lipids Health Dis 2009)
- Tesaglitazar lowers CETP mass and activity and halts progression of existing atherosclerosis in CETP-transgenic mice (Br J Pharmacol 2009)
- Rising VLDL-triglyceride from bexarotene drives CETP activity up and HDL cholesterol down (Endocrinology 2009)
- Pioglitazone and rosiglitazone move CETP activity in opposite directions despite similar glucose control (Diabetes Metab Res Rev 2007)
- Probucol still lowers HDL cholesterol in humans with complete CETP deficiency, disproving its CETP-dependent mechanism (Atherosclerosis 2003)
- Probucol raises CETP mRNA up to 221% and boosts cholesterol efflux 354% in a dose-dependent manner in CETP-transfected hamster ovary cells (Biochim Biophys Acta 1998)
- CGS 25159, a synthetic isoflavan CETP inhibitor, cuts VLDL+LDL cholesterol 28% and raises HDL cholesterol 29% in hamsters (Atherosclerosis 1997)
- Probucol significantly raises CETP activity while shrinking large LDL and both HDL subfractions (Artery 1993)
- Probucol raises plasma CETP by 64 percent while lowering HDL cholesterol, consistent with enhanced remnant-pathway reverse cholesterol transport (Arterioscler Thromb 1991)
- A neutralizing monoclonal antibody doubles HDL cholesteryl ester in rabbits by blocking CETP in vivo (J Clin Invest 1989)
- 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)
- Drug-drug interaction study finds no clinically meaningful effect of obicetrapib on atorvastatin or rosuvastatin exposure in healthy volunteers (Am J Cardiovasc Drugs 2025)
- Unlike anacetrapib, obicetrapib clears completely from the body and does not accumulate in fat, monkey and human data show (Pharmacol Res Perspect 2024)
- Population PK/PD model predicts obicetrapib ceiling effect: a maximum 51.1% LDL-C fall and 224% HDL-C rise (J Clin Pharmacol 2024)
- Evacetrapib crosses the blood-brain barrier within 30 minutes, positioning CETP inhibitors as candidates for Alzheimer's disease (Front Pharmacol 2023)
- 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 gene variants predict residual atherogenic dyslipidaemia in Thai patients on statin therapy (Pharmgenomics Pers Med 2021)
- Anacetrapib parks itself in the lipid droplets of fat cells without needing active transport, explaining its long half-life and shelving (Drug Metab Dispos 2019)
- A new piperidine-based CETP inhibitor retains potency in hypertriglyceridemic plasma where other CETP inhibitors lose efficacy (J Med Chem 2017)
- Human phase 1 data confirm anacetrapib keeps accumulating in fat for a year while plasma levels plateau, explaining its long residence time (Clin Pharmacol Ther 2017)
- Phase 1 single ascending dose study of the CETP inhibitor CKD-519 shows potent target inhibition (Drug Des Devel Ther 2016)
- White adipose tissue accumulates anacetrapib up to 40-fold, explaining its long elimination half-life in mice (Drug Metab Dispos 2016)
- Modeling predicts a 550-day half-life for the tissue depot of anacetrapib, but no comparable accumulation for evacetrapib (J Clin Pharmacol 2015)
- First-in-human data: TA-8995 (obicetrapib) blocks 92-99% of CETP activity and is well tolerated across 1 to 150mg doses (Br J Clin Pharmacol 2014)
- At the highest dose, evacetrapib inhibits CETP by 91% and raises HDL-C by 87% without moving 24-hour blood pressure (J Pharm Pharmacol 2014)
- CETP inhibitors reduce hepatic LDL receptor and PCSK9 via an off-target SREBP2 mechanism (Atherosclerosis 2014)
- Even at 8 times the therapeutic dose, anacetrapib does not clinically prolong the QTcF interval (J Clin Pharmacol 2014)
- Anacetrapib lipid effects and detectable plasma drug persist for years after stopping treatment (Am J Cardiol 2014)
- Perspective argues HDL functionality, not HDL-C concentration, should guide the future evaluation of CETP inhibitors (Clin Pharmacokinet 2013)
- Review distills lessons from the torcetrapib failure for the CETP inhibitors that followed it into clinical development (Curr Clin Pharmacol 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)
- Eight weeks after stopping anacetrapib, HDL-C remains up to 43.4% higher, tracking residual drug levels and CETP inhibition (Am Heart J 2011)
- Population PK/PD modeling picks the 100 mg tablet dose for anacetrapib phase III without a dedicated phase IIb trial to test it (AAPS J 2011)
- A high-fat meal can raise anacetrapib exposure up to eight-fold, but age, sex, and obesity barely move it (Br J Clin Pharmacol 2009)
- Multiple-dose study of the CETP inhibitor CP-800,569 shows dose-dependent HDL rise and LDL fall (Clin Pharmacol Ther 2009)
- Anacetrapib leaves simvastatin pharmacokinetics unchanged while adding incremental LDL-C lowering when combined (Br J Clin Pharmacol 2009)
- Cyclosporine and Rapamycin, but not Tacrolimus or Mycophenolate, raise in vitro CETP activity while all four immunosuppressants suppress lipoprotein lipase (Int J Pharm 2008)
- Fenofibrate lowers CETP activity while raising PLTP activity, reshaping apoB-100 kinetics in metabolic syndrome (Clin Sci (Lond) 2006)
- Review highlights two small-molecule CETP inhibitors substantially raising HDL cholesterol in clinical trials (Curr Opin Cardiol 2005)
- Review surveys CETP as both an unresolved genetic risk marker and a newly validated drug target (Curr Opin Lipidol 2003)
- Review focuses on CETP inhibitors and ABC1-inducing nuclear receptor agonists as new HDL-raising drug approaches (Mini Rev Med Chem 2002)
- Pravastatin lowers serum CETP 21% while probucol raises it 23%, with baseline CETP predicting Achilles tendon xanthoma regression (Atherosclerosis 1999)
- Probucol and bezafibrate change HDL-cholesterol in cholesterol-fed rabbits via CETP activity, not liver CETP mRNA (Jpn Circ J 1999)
- Cholestyramine lowers plasma CETP alongside LDL cholesterol, likely explaining its HDL-raising effect (Clin Pharmacol Ther 1997)
- Gemfibrozil raises HDL3 cholesterol 34.5% and plasma CETP activity 15.8% in hypertriglyceridaemic patients (J Intern Med 1995)
- Etophylline clofibrate lowers CETP mass while improving lipoprotein profile in mixed hyperlipidemia (Atherosclerosis 1995)
- Probucol raises plasma CETP 31% while paradoxically lowering adipose CETP mRNA, suggesting effects beyond local synthesis (J Lipid Res 1993)
- Beyond small-molecule inhibitors: a review surveys CETP-targeted immunotherapy and vaccines as an emerging route to raising HDL (Hum Vaccin Immunother 2025)
- PK/PD trial in 48 healthy Chinese volunteers shows obicetrapib behaves like it does in White participants, supporting the global phase 3 programme (J Clin Pharmacol 2024)
- Multi-stage virtual screening identifies five novel CETP inhibitor lead compounds, confirmed active by biochemical assay (BMC Chem 2024)
- Ginseng compound Ginsenoside Re protects rat hearts from hypertrophy partly by suppressing CETP, matching the classical inhibitor anacetrapib (Cureus 2024)
- Newly synthesised fluorinated diaryl sulfonamides reach 100% CETP inhibition in vitro, guided by molecular modelling (Curr Comput Aided Drug Des 2024)
- Simulating CETP as it really is, not the crystallography mutant, finds a new lead compound that jams its tunnel shut (Int J Mol Sci 2023)
- Review proposes probucol as an alternative stroke-prevention therapy for patients at high haemorrhage risk (Brain Circ 2023)
- Trifluoromethylated sulfonamides reach 100% CETP inhibition in vitro, guided by induced fit docking and pharmacophore mapping (Med Chem 2023)
- Bacterial iron-chelating pigments called ferroverdins turn out to be potent CETP inhibitors, with 43 new structural variants identified (Biomolecules 2022)
- Walnut supplementation as a statin adjuvant lowers CETP activity and raises HDL cholesterol in hypertensive patients (Clin Exp Hypertens 2022)
- EPA, but not DHA, significantly lowers CETP activity in a crossover trial of omega-3 fatty acid supplementation (J Clin Lipidol 2022)
- Viewpoint charts efforts to optimize anacetrapib into a best-in-class CETP inhibitor (J Med Chem 2021)
- Anacetrapib pharmacokinetics in healthy Chinese subjects closely match those seen in black and white populations (Adv Ther 2021)
- Repeated dosing shows dalcetrapib does not accumulate in rats despite forming covalent disulfide bonds with tissue thiols (Xenobiotica 2021)
- A PBPK model correctly predicts higher exposure to the active thiol form of dalcetrapib in chronic kidney disease (Xenobiotica 2021)
- Population pharmacokinetic-pharmacodynamic model recommends a 200 to 400 mg dose of the CETP inhibitor CKD-519 (Pharmaceutics 2020)
- CETP genetic variants predict how much LDL cholesterol falls with statin therapy (Pharmacogenomics J 2020)
- Anacetrapib accumulates to 0.6 mmol/L in mouse adipose tissue without impairing adipose function, even after weight loss (Pharmacol Res Perspect 2019)
- Hydrocarbon-stapled peptides jam the self-binding switch of CETP more than fivefold better, a new route to blocking the protein (J Mol Graph Model 2020)
- Steered molecular dynamics show torcetrapib and anacetrapib block CETP by physically plugging its lipid-transfer tunnel (Biochemistry 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)
- Cynanchum wilfordii extract lowers CETP alongside cholesterol and apoB in adults with high LDL cholesterol (Nutrients 2019)
- A review of dalcetrapib pharmacokinetics finds no clinically significant drug interactions across over 13,000 patients and volunteers (Clin Pharmacokinet 2018)
- The lipid-lowering effect of anacetrapib is smaller in Black subjects than White subjects despite identical pharmacokinetics (J Clin Pharmacol 2018)
- Existing CETP inhibitors were designed against an unglycosylated crystal structure, but simulations show four sugar chains reshape the tunnel dynamics of the protein (Proteins 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)
- Metabolite profiling identifies more than 80 breakdown products of dalcetrapib in human plasma, none of them major (J Pharm Biomed Anal 2018)
- Curcumin does not significantly change serum CETP levels in metabolic syndrome, trial finds (Avicenna J Phytomed 2018)
- New benzyl benzamide compound inhibits CETP by 82.2% in vitro, with docking confirming it fits the drug pocket (Arch Pharm 2017)
- A single dose of anacetrapib inhibits CETP equally well in young Japanese and white men, with a Japanese breakfast boosting exposure similarly (J Clin Pharmacol 2018)
- Review compares torcetrapib, evacetrapib, dalcetrapib and anacetrapib trial outcomes and the future of CETP inhibition (J Cardiovasc Pharmacol Ther 2017)
- Raising gastric pH with omeprazole modestly increases evacetrapib exposure, but not enough to matter clinically (Pharmacotherapy 2016)
- Severe hepatic impairment, but not severe renal impairment, raises evacetrapib exposure and prolongs its half-life (Eur J Clin Pharmacol 2016)
- Evacetrapib inhibits every major CYP enzyme in vitro, but clinical drug-drug interactions turn out weak (Br J Clin Pharmacol 2015)
- CYP3A handles about 90% of the metabolic clearance of evacetrapib, but even strong CYP3A inhibitors barely raise its exposure (Pharmacol Res Perspect 2015)
- Novel CETP inhibitor K-312 lowers PCSK9 through a CETP-independent SREBP mechanism (Am J Physiol Endocrinol Metab 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)
- A high-fat breakfast raises steady-state evacetrapib exposure by 44%, with correspondingly larger lipid and CETP-activity changes (J Cardiovasc Pharmacol Ther 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)
- Lipid-based drug delivery greatly improves oral exposure to two CETP inhibitors, torcetrapib and CP-532,623, in beagle dogs (Eur J Pharm Biopharm 2014)
- Dalcetrapib is rapidly hydrolyzed to its active thiol and excreted largely unchanged in rats and monkeys (Xenobiotica 2014)
- Neither moderate hepatic nor severe renal impairment meaningfully alters anacetrapib pharmacokinetics (J Clin Pharmacol 2014)
- Population PK/PD model finds evacetrapib exposure predicts up to a 177% HDL-C increase and 44.1% LDL-C decrease (CPT Pharmacometrics Syst Pharmacol 2014)
- Anti-CETP vaccine reduces atherosclerosis and fatty liver disease in cholesterol-fed rabbits (PLoS One 2014)
- Novel non-THQ torcetrapib analog PF-04445597 avoids the aldosterone-inducing effect linked to torcetrapib toxicity (Xenobiotica 2014)
- Chronic rifampin dosing slashes anacetrapib exposure by 65% through CYP3A induction, while a single dose barely moves it (J Clin Pharmacol 2013)
- Hepatic and renal impairment increase dalcetrapib active-thiol exposure by up to 81% (Clin Pharmacokinet 2013)
- The weight-loss drug orlistat cuts exposure to active dalcetrapib by more than half by blocking its ester hydrolysis (J Cardiovasc Pharmacol 2012)
- Anacetrapib has no clinically meaningful interaction with warfarin, sparing patients a dosage adjustment (Br J Clin Pharmacol 2012)
- Review details the mode of action and clinical profile of dalcetrapib as dal-OUTCOMES interim results end its development (Expert Opin Investig Drugs 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)
- Anacetrapib does not meaningfully inhibit P-glycoprotein, leaving digoxin exposure essentially unchanged (Biopharm Drug Dispos 2011)
- Leoligin, a lignan from Edelweiss, is identified as a novel CETP activator (Atherosclerosis 2011)
- A high-fat meal raises exposure to dalcetrapib by up to 44 percent across three phase I crossover studies (Clin Ther 2011)
- Intestinal and hepatic first-pass metabolism strips more than 90 percent of active dalcetrapib-thiol in monkeys (Xenobiotica 2011)
- Ezetimibe does not blunt the HDL-raising effect of dalcetrapib, and each drug leaves the other pharmacokinetics largely unchanged (Br J Clin Pharmacol 2010)
- Atorvastatin reduces exposure to dalcetrapib without diminishing its cardiovascular benefit, two crossover studies find (Expert Opin Investig Drugs 2010)
- Even at more than 6 times the therapeutic dose, dalcetrapib does not prolong the QT interval in healthy subjects (Eur J Clin Pharmacol 2010)
- Rosuvastatin raises its own peak concentration by 26 percent when combined with dalcetrapib, but the LDL benefit of the combination still exceeds statin alone (J Clin Pharmacol 2010)
- Anacetrapib shows moderate oral bioavailability in rats and monkeys, with most of the dose excreted unchanged in feces (Drug Metab Dispos 2010)
- Nearly 87% of an oral anacetrapib dose is eliminated unchanged in feces, with only trace CYP3A4-generated metabolites (Drug Metab Dispos 2010)
- Patent landscape review tracks CETP inhibitor development from 2000 through the termination of torcetrapib (Expert Opin Ther Pat 2009)
- Dalcetrapib inhibits CYP enzymes in vitro but has no clinically relevant drug interaction with a five-probe drug cocktail (Curr Med Res Opin 2009)
- Tetrahydroquinoline platform yields a 39nM CETP inhibitor for raising HDL-C (Bioorg Med Chem Lett 2009)
- Ketoconazole unexpectedly lowers exposure to dalcetrapib rather than raising it, contrary to typical CYP3A4-inhibitor interactions (Clin Ther 2009)
- Anacetrapib neither inhibits nor induces CYP3A, but ketoconazole raises its own exposure more than fourfold (J Clin Pharmacol 2009)
- ALPS study finds CETP mass changes track LDL cholesterol, not HDL, with the probucol derivative AGI-1067 (J Clin Lipidol 2007)
- A review of torcetrapib/atorvastatin combination therapy covers the chemistry, mechanism, and pharmacokinetics behind their complementary lipid effects (Expert Rev Cardiovasc Ther 2005)
- Review names CETP inhibition as an emerging strategy for HDL-targeted cardiovascular drug development (Nat Rev Drug Discov 2005)
- Review reports CETP autoimmunization vaccine has reached human trials alongside apolipoprotein mimetics (Curr Atheroscler Rep 2004)
- Review proposes CETP has a novel biological function transporting water-insoluble drugs between lipoproteins (Biochem Pharmacol 2002)
- CETP inhibitory peptide P28 cuts CETP activity 50% and raises HDL/total-cholesterol ratio 150% in CETP-transgenic mice (J Biochem Mol Biol 2002)
- 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)
- Pravastatin lowers CETP activity in both fasting and postprandial states in hypercholesterolaemia (Atherosclerosis 1998)
- Phage-display screening yields a pentapeptide, WRMWY, that competitively inhibits CETP (J Pept Res 1998)
- Species already low in CETP and high in lipoprotein lipase respond most to NO-1886, a compound that raises HDL cholesterol without touching CETP activity (Metabolism 1997)
- Fenofibrate cuts CETP-driven cholesteryl ester transfer from HDL to VLDL by 38% and normalizes dense LDL (ATVB 1996)
- Gemfibrozil enlarges LDL particles and trends toward lowering CETP activity without changing LDL receptor binding (Atherosclerosis 1995)
- Adding bezafibrate to long-term probucol therapy can trigger severe HDL and apolipoprotein A-I deficiency (Eur J Clin Pharmacol 1995)
- Bezafibrate suppresses CETP activity by 17% and LCAT by 21% while shrinking small, heavy LDL (Atherosclerosis 1994)
- A review identifies probucol as the sole drug shown to stimulate CETP activity and boost reverse cholesterol transport (Pharmacol Ther 1994)
- Simvastatin lowers cholesteryl ester transfer by reducing CETP concentration itself, not by altering HDL (Atherosclerosis 1993)
- Heavy alcohol drinkers with sky-high HDL show sharply reduced CETP activity and mass, mimicking genetic deficiency (Metabolism 1992)
- A review credits probucol as the only drug shown to directly raise CETP activity and mass, potentially aiding cholesterol removal from tissues (Atherosclerosis 1991)
- In liver cells, miR-30b-3p cuts CETP reporter activity by 86% at the mRNA level, but CETP protein itself does not budge (Mol Biol Rep 2026)
- CETP TaqIB genotype shows no association with the effect of dulaglutide on HbA1c or hepatic steatosis, unlike PNPLA3 (Endocrine 2024)
- A validated mass spectrometry assay quantifies anacetrapib in fat tissue across three animal species and humans (Bioanalysis 2024)
- A purple perilla extract lowers plasma CETP and reduces atheroma formation in apoE-deficient mice (Nutr Res Pract 2023)
- A probiotic strain lowers CETP expression alongside cholesterol-lowering effects in cell and animal models (J Med Food 2023)
- A probiotic normalises diet-induced CETP gene upregulation in a rabbit model of fatty liver disease (Sci Rep 2023)
- CETP variant rs1532624 is among the five most prevalent clinically relevant pharmacogenomic markers found in Pakistani ethnic groups (Evol Bioinform Online 2022)
- Atorvastatin exposure is about twice as high in healthy Korean volunteers as in Caucasians, partly explained by eight variants including one in CETP (Front Genet 2022)
- An acoustic-fusion formulation of torcetrapib boosts drug exposure roughly 8-fold over a crystalline suspension in rats (Int J Pharm 2021)
- Calcitriol raises CETP levels alongside HDL-C in a rabbit model of atherosclerosis (Int J Vitam Nutr Res 2019)
- Preclinical pharmacokinetic modeling predicts a human dose of the CETP inhibitor CKD519 before phase 1 data revealed a gap (Pharmaceutics 2019)
- QSAR modelling and molecular docking chart a path to new CETP inhibitor compounds for coronary heart disease (J Biomol Struct Dyn 2020)
- Review of new oral dyslipidaemia drugs names anacetrapib the only CETP antagonist that reduces cardiovascular events (Eur J Prev Cardiol 2020)
- Shrinking anacetrapib nanoparticles below 100 nm boosts bioavailability in dogs beyond what dissolution rate alone explains (J Pharm Sci 2019)
- A simple diffusion-like mathematical model estimates how much triglyceride CETP shuttles between lipoproteins from routine lipid measurements (BMC Syst Biol 2019)
- Multi-model computational study of 140 benzoxazole compounds maps the structural requirements for potent CETP inhibition (J Biomol Struct Dyn 2019)
- Early formulation work solves the poor solubility of the CETP inhibitor CKD-519 ahead of phase 1 testing (Int J Pharm 2018)
- Lipid-based formulations boost oral exposure of a poorly soluble CETP inhibitor up to 10-fold in preclinical species (J Pharm Sci 2018)
- Formulation science: a lipid-based delivery system boosts oral absorption of the CETP inhibitor CP-532,623, and supersaturation, not just solubility, predicts how well (Mol Pharm 2017)
- Saffron-derived crocin raises CETP levels within treated patients, but not significantly versus placebo (ARYA Atheroscler 2017)
- A new dissolution test detects as little as 10% crystalline drug contamination in evacetrapib spray-dried dispersion tablets (J Pharm Biomed Anal 2017)
- CETP TaqIB genotype shapes how herbal tea affects HDL cholesterol and triglycerides in hypercholesterolemic patients (Asia Pac J Clin Nutr 2017)
- Pharmacokinetic review details the long elimination half-life and faeces-dominant clearance of anacetrapib (Expert Opin Drug Metab Toxicol 2017)
- A new cycloalkene-scaffold CETP inhibitor raises HDL cholesterol in hamsters (Eur J Med Chem 2016)
- Molecular dynamics simulations support a tunnel mechanism for lipid transfer by CETP (J Biol Chem 2016)
- Molecular dynamics studies show small-molecule CETP inhibitors act by physically blocking the lipid transfer tunnel (J Phys Chem B 2016)
- All-atom simulations show a complete cholesteryl ester can pass through the CETP tunnel at a physiologically realistic rate (J Biol Chem 2016)
- Novel benzylaminopropionanilide CETP inhibitors raise HDL and lower LDL in hamsters (Bioorg Med Chem 2016)
- Policosanol combined with reconstituted HDL outperforms anacetrapib at inhibiting CETP in a hyperlipidemic zebrafish model (Rejuvenation Res 2016)
- A structure-guided approach discovers a novel indoline series of CETP inhibitors (ACS Med Chem Lett 2016)
- High-pressure crystallization confirms a predicted, more stable polymorph of dalcetrapib before late-stage development (Nat Commun 2015)
- Handbook chapter surveys emerging HDL-targeted drugs, from CETP inhibitors to PPAR and LXR agonists (Handb Exp Pharmacol 2015)
- Plant-produced chimeric protein targeting ApoB100 and CETP epitopes elicits antibody responses in mice (Mol Biotechnol 2014)
- Review updates the pipeline of emerging hyperlipidaemia drugs, focused mainly on anacetrapib and evacetrapib (Expert Opin Emerg Drugs 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)
- Probenecid raises exposure to the active thiol form of dalcetrapib by up to 21 percent (Int J Clin Pharmacol Ther 2013)
- Dalcetrapib is hydrolyzed within 20 seconds in human intestinal fluid, but is stable in gastric fluid at low pH (Int J Pharm 2012)
- Dalcetrapib does not affect the pharmacokinetics of a combined oral contraceptive in a crossover trial (Int J Clin Pharmacol Ther 2012)
- Chinese medicine preparation SUB885C cuts CETP activity 74% and raises HDL-C in ApoE*3Leiden.CETP mice (PLoS One 2012)
- 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)
- A workaround measures two acyl-glucuronide metabolites of torcetrapib in monkey urine without ever having reference standards for them (Biomed Chromatogr 2010)
- Novel tetrahydrochinoline derivatives yield a potent CETP inhibitor with favourable pharmacokinetics for clinical development (Bioorg Med Chem Lett 2010)
- A new benzoxazine class of CETP inhibitors raises HDL cholesterol in transgenic mice and hamsters (Bioorg Med Chem Lett 2010)
- Adding a bile correction factor sharpens allometric prediction of human pharmacokinetic parameters for orally dosed torcetrapib (Eur J Drug Metab Pharmacokinet 2009)
- Thyromimetic T-0681 cuts atherosclerosis 80% in rabbits by raising hepatic LDL receptors, not by changing CETP (J Lipid Res 2008)
- Long-term danazol use lowers CETP mass without significantly affecting HDL cholesterol or atherosclerosis markers (Clin Ther 2008)
- Torcetrapib is extensively metabolized in humans with terminal half-lives of 211 to 373 hours (Drug Metab Dispos 2008)
- A new LC-MS/MS assay quantifies torcetrapib in hamster and dog plasma down to 1 nanogram per mL (Biomed Chromatogr 2008)
- Review surveys a CETP-inhibiting vaccine among emerging anti-atherosclerotic vaccine strategies (Cardiol Rev 2008)
- A chiral HPLC method separates the two torcetrapib enantiomers in hamster plasma down to 0.1 microgram per mL (J Chromatogr B 2007)
- Torcetrapib shifts almost entirely into triglyceride-rich lipoproteins in hyperlipidemic human plasma (Pharm Res 2006)
- LXR agonists raise LDL cholesterol in CETP-expressing hamsters and monkeys, an effect invisible in CETP-lacking mice (J Lipid Res 2005)
- Review names CETP inhibitors among emerging HDL-targeted therapies for insulin resistance syndrome (Semin Vasc Med 2004)
- Plant stanol ester spread lowers CETP mass alongside LDL cholesterol and oxidized LDL in a Japanese trial (Nutrition 2003)
- Review names CETP inhibitors among five emerging drug targets for lipid disorders beyond statins (Curr Atheroscler Rep 2002)
- CETP inhibitory peptide P28 selectively blocks HDL-to-LDL but not HDL-to-HDL cholesteryl ester transfer (Lipids 2002)
- Review names CETP inhibitors among four novel drug classes targeting low HDL cholesterol (Expert Opin Investig Drugs 2001)
- Atorvastatin cuts CETP activity by up to 26.4% while reshaping apolipoprotein distribution in hypertriglyceridemia (Metabolism 2000)
- Bezafibrate, but not gemfibrozil, significantly lowers cholesteryl ester transfer activity in type IIb hyperlipoproteinaemia (Atherosclerosis 1998)
- Ethanol oxidation, not reduced CETP synthesis, explains alcohol's redistribution of CETP among lipoproteins (ATVB 1996)
- A wild valerian relative and beta-sitosterol inhibit CETP and lower lipids in triton-induced hyperlipidemic rats (Food Sci Nutr 2024)
- A new palladium-catalysed C-H fluorination reaction offers a concise late-stage route to anacetrapib (Chem Commun 2021)
- Simvastatin lowers HMGR but not CETP expression in bovine adipocytes (Anim Biotechnol 2020)
- Fragment-based design yields a novel pentacyclic triterpenoid CETP inhibitor with sub-micromolar potency (Eur J Med Chem 2017)
- Structural study designs a self-binding CETP peptide stabilized by pi-pi stacking and halogen bonding (Bioorg Chem 2016)
- LC-MS/MS method measures anacetrapib pharmacokinetics and low protein binding in rats (Biomed Chromatogr 2017)
- LC-MS/MS method quantifies anacetrapib, a stable-isotope tracer, and four metabolites in human plasma (J Chromatogr B 2016)
- Stable-isotope tracer study measures evacetrapib absolute oral bioavailability at 44.8% (J Labelled Comp Radiopharm 2016)
- QSAR models guide design of twelve new diphenylpyridylethanamine CETP inhibitors (Bioorg Med Chem Lett 2015)
- New diterpenes isolated from Engleromyces goetzii fungus show CETP inhibitory activity (Nat Prod Bioprospect 2015)
- Isotope-labeled anacetrapib and its metabolites are synthesized to support bioavailability and drug-metabolism studies (J Labelled Comp Radiopharm 2013)
- New tetrazolyl tetrahydroquinoline CETP inhibitors raise HDL cholesterol in a transgenic mouse model (Bioorg Med Chem Lett 2012)
- LC-MS/MS method quantifies dalcetrapib-thiol and its S-methyl and S-glucuronide metabolites down to 5 ng/mL (J Pharm Biomed Anal 2012)
- Xanthohumol from hops shows the strongest CETP-inhibitory activity among screened plant chalcones (Food Chem 2012)
- SAR study on the central phenyl ring of biphenyl oxazolidinone CETP inhibitors finds analogs matching anacetrapib in potency (Bioorg Med Chem Lett 2012)
- A hidden solvent impurity turns out to enable a scalable, chromatography-free synthesis of the anacetrapib biaryl core (J Org Chem 2011)
- Molecular docking maps the hydrophobic P1/P2 binding pockets used by trifluoro-aminopropanol CETP inhibitors (J Mol Model 2011)
- Modifying the alpha-alkoxyamide moiety of arylbenzoxazole CETP inhibitors yields an orally bioavailable lead (Bioorg Med Chem Lett 2010)
- A review catalogs the chiral and achiral bioanalytical methods developed to measure torcetrapib across six species (Bioanalysis 2009)
- Torcetrapib forms more than 28 species-dependent metabolites in rats, monkeys, and mice (Drug Metab Dispos 2008)
- Chiral LC-MS/MS assay separates torcetrapib enantiomers in hamster plasma down to 5 ng/mL (J Chromatogr B 2007)
- Self-emulsifying formulation cuts the food effect of torcetrapib from 5-fold to 3-fold in dogs (Int J Pharm 2008)
- Low-dose testosterone in women lowers HDL cholesterol without changing CETP activity (Clin Endocrinol 1998)
- Bile acid sequestrant cholebine shrinks large light LDL without touching CETP or LCAT activity (Atherosclerosis 1997)