Evacetrapib 56 items
ACCELERATE and the end of the simple HDL hypothesis.
Trials, agents, guidance
- Agent Evacetrapib
- Trial ACCELERATE
Studies
- Evacetrapib failed to reduce cardiovascular events despite large lipid changes in ACCELERATE (N Engl J Med 2017)
- Why raising HDL with CETP inhibitors did not help: evacetrapib and torcetrapib both boosted the harmful apoC3-containing HDL subspecies most (Arterioscler Thromb Vasc Biol 2022)
- Discovery paper introduces evacetrapib, a potent CETP inhibitor that raises HDL cholesterol without inducing aldosterone or raising blood pressure (J Lipid Res 2011)
- Reducing CETP activity with evacetrapib preserves memory in an Alzheimer's mouse model, independent of amyloid or tau markers (EMBO Mol Med 2026)
- Bayesian network meta-analysis of 84,134 patients ranks evacetrapib and anacetrapib best for cardiovascular outcomes among CETP inhibitors (Medicine 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)
- Meta-analysis of nearly 13,000 patients confirms evacetrapib lowers LDL-C by 34 mg/dL and raises HDL-C substantially (Prostaglandins Leukot Essent Fatty Acids 2021)
- Evacetrapib raises large and medium HDL but cuts the functionally important preβ-1 HDL by 36%, a clue to why raising HDL-C didn't help (Atherosclerosis 2019)
- ACCELERATE nested case-control study finds no significant ADCY9 genotype interaction with evacetrapib, unlike the dalcetrapib signal (JAMA Cardiol 2018)
- ACCENTUATE: evacetrapib beat ezetimibe and higher-dose statin on LDL-C and Lp(a), but also raised hsCRP, a clue to why ACCELERATE later failed (Atherosclerosis 2017)
- Anacetrapib impairs endothelial function in CETP-transgenic mice despite raising HDL-C fivefold, while evacetrapib does not (Atherosclerosis 2017)
- Evacetrapib cuts small LDL particles by up to 95% and lipoprotein(a) by up to 40%, alone or added to statins (J Clin Lipidol 2016)
- Evacetrapib raises ABCA1-specific cholesterol efflux capacity and pre-beta-1 HDL, effects that statins alone do not share (JACC 2015)
- Evacetrapib raised HDL-C up to 129% and lowered LDL-C up to 36% alone or with statins in a 398-patient dose-ranging trial (JAMA 2011)
- Evacetrapib more than doubled circulating ApoA5 in the ACCELERATE and ACCENTUATE trials, explaining how CETP inhibitors lower triglycerides (J Clin Lipidol 2025)
- Evacetrapib crosses the blood-brain barrier within 30 minutes, positioning CETP inhibitors as candidates for Alzheimer's disease (Front Pharmacol 2023)
- In ACCELERATE, a rising hsCRP trajectory over follow-up predicts MACE better than a single baseline reading, even when levels stay under 2 mg/L (Am J Cardiol 2022)
- In ACCELERATE, elevated Lp(a) only predicted death, MI and stroke when hsCRP was also 2 mg/L or higher (JAMA Cardiol 2020)
- In 8,236 diabetes patients from ACCELERATE, evacetrapib raised HDL by 131% and lowered LDL by 32%, yet produced no clinical benefit (BMJ Open Diabetes Res Care 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)
- Unlike torcetrapib, evacetrapib left plasma aldosterone unchanged in ACCELERATE, and aldosterone did not predict cardiovascular events (J Am Heart Assoc 2019)
- What the cetrapib trials taught us: torcetrapib, evacetrapib and anacetrapib all raised atherogenic apoproteins, muddying the HDL-raising story (Curr Opin Lipidol 2018)
- No benefit with evacetrapib despite raising HDL 130% and cutting LDL 37%: is this the end of the road for the cetrapibs? (Expert Opin Pharmacother 2017)
- In Japanese patients, evacetrapib added to atorvastatin cuts LDL-C by 25.70% versus placebo and more than doubles HDL-C (Circ J 2017)
- Evacetrapib monotherapy lowers LDL-C by 34.3% and raises HDL-C by 124% in Japanese patients with hypercholesterolemia (Circ J 2017)
- Rabbit developmental study finds the offspring-survival NOAEL for evacetrapib is a third of the maternal NOAEL (Birth Defects Res 2017)
- High-dose evacetrapib causes toxicity in parent rats but leaves fertility and fetal development unharmed in rats and rabbits (Birth Defects Res 2017)
- Review details how evacetrapib raised HDL-C by 128% and cut LDL-C by 35% yet produced no clinical benefit in ACCELERATE (Cardiol Rev 2017)
- Meta-analysis finds evacetrapib raises HDL-C by 86% and cuts LDL-C by 21%, with no effect on triglycerides (Curr Pharm Des 2016)
- ACCELERATE trial design targets 12,092 high-risk patients to test the effect of evacetrapib on cardiovascular outcomes (Am Heart J 2015)
- Modeling predicts a 550-day half-life for the tissue depot of anacetrapib, but no comparable accumulation for evacetrapib (J Clin Pharmacol 2015)
- 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)
- Dose-ranging phase 2 trial in Japanese patients shows evacetrapib 500 mg raises HDL-C by 136% and cuts CETP activity by 95% (Am J Cardiol 2014)
- A thorough QT study finds evacetrapib safe on cardiac rhythm even at 5-fold the exposure planned for phase 3 (J Cardiovasc Pharmacol Ther 2014)
- Evacetrapib suppresses colorectal cancer cell growth by blocking Wnt/beta-catenin signaling and activating JNK (Biol Pharm Bull 2022)
- In the ACCELERATE diabetes cohort, higher baseline HbA1c independently predicted cardiovascular events despite statin therapy (J Am Heart Assoc 2020)
- Raising gastric pH with omeprazole modestly increases evacetrapib exposure, but not enough to matter clinically (Pharmacotherapy 2016)
- 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)
- Severe hepatic impairment, but not severe renal impairment, raises evacetrapib exposure and prolongs its half-life (Eur J Clin Pharmacol 2016)
- Commentary marks evacetrapib as another CETP inhibitor lost to the gap between lipid improvement and clinical benefit (Bratisl Lek Listy 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)
- A high-fat breakfast raises steady-state evacetrapib exposure by 44%, with correspondingly larger lipid and CETP-activity changes (J Cardiovasc Pharmacol Ther 2015)
- 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)
- Review profiles the early safety advantage of evacetrapib over torcetrapib as cardiovascular outcomes remain unknown (Curr Cardiol Rep 2012)
- N-alkylated benzazepine derivatives inhibit CETP with an IC50 of 75.54 ± 8.70 nM in a fluorescence assay (Bioorg Chem 2026)
- Chikungunya virus is sensitive to evacetrapib in cell culture, but through an off-target effect independent of CETP itself (Viruses 2025)
- Repurposed as a cancer drug: evacetrapib blocks a CEA-KRT1 interaction that drives oxaliplatin resistance in gastric cancer (Drug Resist Updat 2025)
- In ACCELERATE, higher baseline fasting insulin independently predicted MACE and future revascularisation in diabetes patients (Diab Vasc Dis Res 2019)
- A new dissolution test detects as little as 10% crystalline drug contamination in evacetrapib spray-dried dispersion tablets (J Pharm Biomed Anal 2017)
- Stable-isotope tracer study measures evacetrapib absolute oral bioavailability at 44.8% (J Labelled Comp Radiopharm 2016)
- A chiral HPLC method resolves the methyl ester of evacetrapib from its stereoisomers and five impurities (J Chromatogr A 2015)
- A brush-type Whelk-O 1 chiral column resolves evacetrapib from its enantiomer, two diastereomers, and six impurities (J Chromatogr A 2014)