Compounds > evacetrapib
Page last updated: 2024-11-13

evacetrapib

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Cross-References

ID SourceID
PubMed CID49836058
CHEMBL ID2017179
CHEBI ID188637
SCHEMBL ID141340
SCHEMBL ID108602
SCHEMBL ID108367
MeSH IDM0568701

Synonyms (59)

Synonym
HY-13327
4-[[(5s)-5-[[3,5-bis(triluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid
CHEBI:188637
evacetrapib ,
evacetrapib (usan)
D10121
1186486-62-3
bdbm50381415
evacetrapib (ly2484595)
ly 2484595
trans-4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2-methyl-2h-tetrazol-5- yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzazepin-1-yl)methyl) cyclohexanecarboxylic acid
51xwv9k850 ,
unii-51xwv9k850
ly-2484595
ly2484595
cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2- methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1- yl)methyl)-, trans-
evacetrapib [usan:inn]
CHEMBL2017179
(1r,4r)-4-{[(5s)-5-({[3,5-
PB36744
bis(trifluoromethyl)phenyl]methyl}(2-methyl-2h-
tetrahydro-1h-1-benzazepin-1-yl]methyl}cyclohexane-1-
1,2,3,4-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-
CS-0658
trans-4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzazepin-1-yl)methyl)cyclohexanecarboxylic acid
cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl((2-methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl)methyl)-, trans-
evacetrapib [mi]
cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2-methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl)methyl)-, trans-
evacetrapib [usan]
evacetrapib [who-dd]
(1r,4r)-4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-1-benzazepin-1-yl)methyl)cyclohexane-1-carboxylic acid
evacetrapib [inn]
S2925
SCHEMBL141340
SCHEMBL108602
SCHEMBL108367
trans-4-[[(5s)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2h-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-b enzazepin-1-yl]methyl]-cyclohexanecarboxylic acid
trans-4-[[(5s)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2h-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid
AKOS025290246
(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid
gtpl8401
4-[[(5s)-5-[[3,5-bis(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid
trans-(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid
AC-30238
J-690053
EX-A621
HMS3651J12
mfcd23105886
(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexane-1-carboxylic acid
SW219342-1
DB11655
AKOS032947275
Q553129
4-trans-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid
AS-35108
AMY12209
CCG-270310
ihiugivxarlyhp-syjkbglxsa-n
ihiugivxarlyhp-uxnjhfgpsa-n

Research Excerpts

Overview

Evacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor. It is under development for reducing cardiovascular events in patients with high risk vascular disease.

ExcerptReferenceRelevance
"Evacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor under development for reducing cardiovascular events in patients with high risk vascular disease. "( CYP-mediated drug-drug interactions with evacetrapib, an investigational CETP inhibitor: in vitro prediction and clinical outcome.
Cannady, EA; Friedrich, S; Krueger, KA; Nicholls, SJ; Rehmel, JR; Suico, JG; Wang, MD, 2015)		2.13
"Evacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor that has been recently studied as a cholesterol modifying agent to reduce cardiovascular risk and mortality in high risk cardiovascular disease patients. "( Evacetrapib: Another CETP Inhibitor for Dyslipidemia With No Clinical Benefit.
Eyvazian, VA; Frishman, WH, )		3.02
"Evacetrapib is a novel CETP inhibitor, with favorable effects on plasma lipids and no adverse effects on blood pressure or mineralocorticoid activity in early clinical evaluation."( Evacetrapib.
Nicholls, SJ, 2012)		2.54

Treatment

Eveacetrapib treatment reduced total LDL, but also resulted in polydisperse LDL with LDL particles larger and smaller than the LDL subclasses of the placebo group. Treatment with evacetrapib 130 mg daily for 12 weeks resulted in a statistically significant treatment difference of -25.70% compared with placebo.

ExcerptReferenceRelevance
"Evacetrapib treatment reduced total LDL, but also resulted in polydisperse LDL with LDL particles larger and smaller than the LDL subclasses of the placebo group."( Evacetrapib reduces preβ-1 HDL in patients with atherosclerotic cardiovascular disease or diabetes.
Chen, H; Chen, X; Chen, Y; Dong, J; Ge, J; Jiang, XC; Wang, L; Zhang, X, 2019)		2.68
"Treatment with evacetrapib 130 mg once daily for 12 weeks resulted in statistically significant (P<0.001) change in LDL-C (β quantification) compared with placebo."( Efficacy and Safety of Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib Administered as Monotherapy in Japanese Patients With Primary Hypercholesterolemia.
Iimura, T; Kiyosue, A; Murakami, M; Riesmeyer, JS; Takita, Y; Teramoto, T, 2017)		1.03
"Treatment with evacetrapib 130 mg daily for 12 weeks resulted in a statistically significant treatment difference of -25.70% compared with placebo in percentage decrease in LDL-C (95% CI: -34.73 to -16.68; P<0.001)."( Efficacy and Safety of the Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib in Combination With Atorvastatin in Japanese Patients With Primary Hypercholesterolemia.
Iimura, T; Kiyosue, A; Murakami, M; Riesmeyer, JS; Takita, Y; Teramoto, T, 2017)		1.03

Toxicity

The safety of evacetrapib was assessed by comparing the pooled incidence of adverse events between treatment and placebo groups. Evacetrapib monotherapy or in combination with atorvastatin was not likely to be associated with any significant change in blood pressure.

ExcerptReferenceRelevance
" Evacetrapib monotherapy or in combination with atorvastatin was not likely to be associated with any significant change in blood pressure and did not have any adverse effects on mineralocorticoid or glucocorticoid measures."( Efficacy, safety, tolerability, and pharmacokinetic profile of evacetrapib administered as monotherapy or in combination with atorvastatin in Japanese patients with dyslipidemia.
Krueger, KA; Morisaki, Y; Ruotolo, G; Takeuchi, M; Teramoto, T, 2014)		1.55
" The safety of evacetrapib was assessed by comparing the pooled incidence of adverse events (total adverse events, adverse events leading to study discontinuation, elevations in hepatic and muscular enzymes and blood pressure) between treatment and placebo groups."( Efficacy and Safety of Evacetrapib for Modifying Plasma Lipids: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.
Golledge, J; Guerrero-Romero, F; Sahebkar, A; Simental-Mendía, LE; Watts, GF, 2016)		1.1
" Meta-analysis suggested equivalent rates of adverse events in subjects receiving evacetrapib and placebo."( Efficacy and Safety of Evacetrapib for Modifying Plasma Lipids: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.
Golledge, J; Guerrero-Romero, F; Sahebkar, A; Simental-Mendía, LE; Watts, GF, 2016)		0.97
" Adverse events appeared to be similar in subjects receiving evacetrapib and placebo in short-term follow-ups."( Efficacy and Safety of Evacetrapib for Modifying Plasma Lipids: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.
Golledge, J; Guerrero-Romero, F; Sahebkar, A; Simental-Mendía, LE; Watts, GF, 2016)		0.99
" No deaths, serious adverse events, or discontinuations because of adverse events were reported; 5 patients (18."( Efficacy and Safety of Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib Administered as Monotherapy in Japanese Patients With Primary Hypercholesterolemia.
Iimura, T; Kiyosue, A; Murakami, M; Riesmeyer, JS; Takita, Y; Teramoto, T, 2017)		0.69
" No deaths or serious adverse events were reported."( Efficacy and Safety of the Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib in Combination With Atorvastatin in Japanese Patients With Primary Hypercholesterolemia.
Iimura, T; Kiyosue, A; Murakami, M; Riesmeyer, JS; Takita, Y; Teramoto, T, 2017)		0.69

Pharmacokinetics

In period 2, subjects received a once/day oral dose of omeprazole 40 mg on days 8-20, with a single oral doses of evacetrapib 130 mg administered 2 hours after the omepazole dose on day 14. Plasma evacet Trapib concentrations were mostly undetectable. All pharmacodynamic biomarkers (HDL-C and LDL-C levels and CETP mass and activity) returned to baseline after a 4- to 6-week washout.

ExcerptReferenceRelevance
" Notably, plasma evacetrapib concentrations were mostly undetectable, and all pharmacodynamic biomarkers (HDL-C and LDL-C levels and CETP mass and activity) returned to baseline after a 4- to 6-week washout."( Efficacy, safety, tolerability, and pharmacokinetic profile of evacetrapib administered as monotherapy or in combination with atorvastatin in Japanese patients with dyslipidemia.
Krueger, KA; Morisaki, Y; Ruotolo, G; Takeuchi, M; Teramoto, T, 2014)		0.98
"Anacetrapib, a cholesterol ester transfer protein (CETP) inhibitor, has been reported to have longer elimination half-life after longer treatment."( Assessment of the persistence of anacetrapib and evacetrapib concentrations using two pharmacokinetic modeling approaches.
Friedrich, S; Hall, SD; Ke, AB; Mantlo, N; Rotelli, M; Small, DS, 2015)		0.67
" Non-compartmental pharmacokinetic parameters were estimated from plasma concentration-time data."( Effect of hepatic or renal impairment on the pharmacokinetics of evacetrapib.
Cannady, EA; Downs, D; Ortega, D; Royalty, J; Small, DS; Suico, JG; Zhang, W, 2016)		0.67
" Geometric mean area under the concentration-time curve (AUC) was greater, half-life (t1/2) was longer, and maximum concentration (Cmax) was lower in subjects with moderate and severe hepatic impairment than in controls."( Effect of hepatic or renal impairment on the pharmacokinetics of evacetrapib.
Cannady, EA; Downs, D; Ortega, D; Royalty, J; Small, DS; Suico, JG; Zhang, W, 2016)		0.67
" In period 2, subjects received a once/day oral dose of omeprazole 40 mg on days 8-20, with a single oral dose of evacetrapib 130 mg administered 2 hours after the omeprazole dose on day 14, followed by 7 days of pharmacokinetic sampling."( Impact of Increased Gastric pH on the Pharmacokinetics of Evacetrapib in Healthy Subjects.
Cannady, EA; Downs, D; Hale, C; Royalty, J; Small, DS; Suico, JG; Wang, MD, 2016)		0.89

Compound-Compound Interactions

The cholesteryl ester transfer protein (CETP) inhibitor evacetrapib has been previously shown to increase high-density lipoprotein cholesterol (HDL-C) levels. Evacetrapib daily in combination with atorvastatin was superior to placebo in lowering LDL-C after 12 weeks.

ExcerptReferenceRelevance
" Few studies have documented the efficacy and safety of CETP inhibitors in combination with commonly used statins."( Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol: a randomized controlled trial.
Brewer, HB; Hu, B; Kastelein, JJ; Krueger, KA; McErlean, E; Nicholls, SJ; Nissen, SE; Shao, M; Wang, MD, 2011)		0.66
"To examine the biochemical effects, safety, and tolerability of evacetrapib, as monotherapy and in combination with statins, in patients with dyslipidemia."( Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol: a randomized controlled trial.
Brewer, HB; Hu, B; Kastelein, JJ; Krueger, KA; McErlean, E; Nicholls, SJ; Nissen, SE; Shao, M; Wang, MD, 2011)		0.9
" In combination with statin therapy, evacetrapib, 100 mg/d, produced increases in HDL-C of 42."( Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol: a randomized controlled trial.
Brewer, HB; Hu, B; Kastelein, JJ; Krueger, KA; McErlean, E; Nicholls, SJ; Nissen, SE; Shao, M; Wang, MD, 2011)		0.93
"Compared with placebo or statin monotherapy, evacetrapib as monotherapy or in combination with statins increased HDL-C levels and decreased LDL-C levels."( Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol: a randomized controlled trial.
Brewer, HB; Hu, B; Kastelein, JJ; Krueger, KA; McErlean, E; Nicholls, SJ; Nissen, SE; Shao, M; Wang, MD, 2011)		0.92
"The cholesteryl ester transfer protein (CETP) inhibitor evacetrapib has been previously shown to increase high-density lipoprotein cholesterol (HDL-C) and decrease low-density lipoprotein cholesterol (LDL-C) levels, as monotherapy or in combination with statins."( Efficacy, safety, tolerability, and pharmacokinetic profile of evacetrapib administered as monotherapy or in combination with atorvastatin in Japanese patients with dyslipidemia.
Krueger, KA; Morisaki, Y; Ruotolo, G; Takeuchi, M; Teramoto, T, 2014)		0.89
" CETP inhibitors are likely to be utilized as 'add-on' therapy to statins in patients receiving concomitant medications, so the potential for evacetrapib to cause clinically important drug-drug interactions (DDIs) with cytochromes P450 (CYP) was evaluated."( CYP-mediated drug-drug interactions with evacetrapib, an investigational CETP inhibitor: in vitro prediction and clinical outcome.
Cannady, EA; Friedrich, S; Krueger, KA; Nicholls, SJ; Rehmel, JR; Suico, JG; Wang, MD, 2015)		0.88
"VLDL and LDL particle concentrations and sizes (using nuclear magnetic resonance spectroscopy) and lipoprotein(a) concentration (using nephelometry) were measured at baseline and week 12 in a placebo-controlled trial of 393 patients treated with evacetrapib as monotherapy (30 mg/d, 100 mg/d, or 500 mg/d) or in combination with statins (100 mg plus simvastatin 40 mg/d, atorvastatin 20 mg/d, or rosuvastatin 10 mg/d; Clinicaltrials."( Evacetrapib alone or in combination with statins lowers lipoprotein(a) and total and small LDL particle concentrations in mildly hypercholesterolemic patients.
Brewer, HB; Deeg, MA; Krueger, KA; Liu, L; Nicholls, SJ; Nissen, SE; Ruotolo, G; Wang, MD; Willey, MB, )		1.76
"Evacetrapib daily in combination with atorvastatin was superior to placebo in lowering LDL-C after 12 weeks, and resulted in a statistically significant increase of HDL-C compared with placebo."( Efficacy and Safety of the Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib in Combination With Atorvastatin in Japanese Patients With Primary Hypercholesterolemia.
Iimura, T; Kiyosue, A; Murakami, M; Riesmeyer, JS; Takita, Y; Teramoto, T, 2017)		2.13

Bioavailability

ExcerptReferenceRelevance
"This open-label, single-period study in healthy subjects estimated evacetrapib absolute bioavailability following simultaneous administration of a 130-mg evacetrapib oral dose and 4-h intravenous (IV) infusion of 175 µg [(13) C8 ]-evacetrapib as a tracer."( Absolute bioavailability of evacetrapib in healthy subjects determined by simultaneous administration of oral evacetrapib and intravenous [(13) C8 ]-evacetrapib as a tracer.
Aburub, A; Annes, WF; Begum, SL; Cannady, EA; Czeskis, B; Hinds, C; Lin, Q; Ortega, D; Pack, BW; Royalty, J; Ruterbories, K; Small, DS; Suico, JG; Ward, C, 2016)		0.96

Dosage Studied

A 1200-mg supratherapeutic dose of evacetrapib was considered to be well tolerated after 10 days of daily dosing in healthy participants. No blood pressure elevation was observed in rats dosed with evacetraptib at high exposure multiples compared with the positive control, torcetrapIB.

ExcerptRelevanceReference
" Importantly, no blood pressure elevation was observed in rats dosed with evacetrapib at high exposure multiples compared with the positive control, torcetrapib."( Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure.
Beyer, TP; Cannady, EA; Cao, G; Chen, YQ; Cockerham, SL; Fields, T; Karathanasis, SK; Mantlo, NB; Schmidt, RJ; Zhang, Y; Zimmerman, KM, 2011)		2.04
" The primary end point was the comparison of evacetrapib effect on the population-corrected QT interval (QTcP) to that of placebo at 7 time points following dosing on day 10."( Evacetrapib at a supratherapeutic steady state concentration does not prolong QT in a thorough QT/QTc study in healthy participants.
Friedrich, S; Krueger, KA; Suico, JG; Zhang, W, 2014)		2.1
" A 1200-mg supratherapeutic dose of evacetrapib was considered to be well tolerated after 10 days of daily dosing in healthy participants."( Evacetrapib at a supratherapeutic steady state concentration does not prolong QT in a thorough QT/QTc study in healthy participants.
Friedrich, S; Krueger, KA; Suico, JG; Zhang, W, 2014)		2.12
" Plasma samples collected through 24 hours were analyzed for evacetrapib concentrations and pharmacokinetic parameter estimates including area under the concentration-time curve during a dosing interval (AUCτ), maximum observed concentration (Cmax), and time of Cmax (tmax) were calculated."( A Multidose Study to Examine the Effect of Food on Evacetrapib Exposure at Steady State.
Cannady, EA; Downs, D; Friedrich, S; Royalty, J; Small, DS; Suico, JG; Zhang, W, 2015)		0.91
" For rabbit EFD studies, animals were dosed from GDs 7 to 19 or from 1 week before mating through GD 19."( Fertility and Embryo-Fetal Development Assessment in Rats and Rabbits with Evacetrapib: A Cholesteryl Ester Transfer Protein Inhibitor.
Breslin, WJ; Cannady, EA; Edwards, TL; Hilbish, KG, 2017)		0.69
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzazepineA group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cholesteryl ester transfer proteinHomo sapiens (human)IC50 (µMol)0.11000.00300.21694.1000AID1476688
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
triglyceride metabolic processCholesteryl ester transfer proteinHomo sapiens (human)
lipid transportCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol metabolic processCholesteryl ester transfer proteinHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationCholesteryl ester transfer proteinHomo sapiens (human)
regulation of cholesterol effluxCholesteryl ester transfer proteinHomo sapiens (human)
phospholipid transportCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol transportCholesteryl ester transfer proteinHomo sapiens (human)
positive regulation of cholesterol transportCholesteryl ester transfer proteinHomo sapiens (human)
triglyceride transportCholesteryl ester transfer proteinHomo sapiens (human)
very-low-density lipoprotein particle remodelingCholesteryl ester transfer proteinHomo sapiens (human)
low-density lipoprotein particle remodelingCholesteryl ester transfer proteinHomo sapiens (human)
high-density lipoprotein particle remodelingCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol homeostasisCholesteryl ester transfer proteinHomo sapiens (human)
reverse cholesterol transportCholesteryl ester transfer proteinHomo sapiens (human)
phosphatidylcholine metabolic processCholesteryl ester transfer proteinHomo sapiens (human)
lipid homeostasisCholesteryl ester transfer proteinHomo sapiens (human)
phospholipid homeostasisCholesteryl ester transfer proteinHomo sapiens (human)
triglyceride homeostasisCholesteryl ester transfer proteinHomo sapiens (human)
positive regulation of phospholipid transportCholesteryl ester transfer proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
phospholipid transporter activityCholesteryl ester transfer proteinHomo sapiens (human)
lipid bindingCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol bindingCholesteryl ester transfer proteinHomo sapiens (human)
triglyceride bindingCholesteryl ester transfer proteinHomo sapiens (human)
phosphatidylcholine bindingCholesteryl ester transfer proteinHomo sapiens (human)
cholesterol transfer activityCholesteryl ester transfer proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
extracellular regionCholesteryl ester transfer proteinHomo sapiens (human)
extracellular spaceCholesteryl ester transfer proteinHomo sapiens (human)
vesicleCholesteryl ester transfer proteinHomo sapiens (human)
extracellular exosomeCholesteryl ester transfer proteinHomo sapiens (human)
high-density lipoprotein particleCholesteryl ester transfer proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1783825Inhibition of recombinant CETP (unknown origin) assessed as maximal inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein between exogenous [3H]LDL in 95% human serum at 10 uM by liquid scintillation analysis2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID1166825Terminal elimination half life in healthy human administered as single oral dose2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Potent cholesteryl ester transfer protein inhibitors of reduced lipophilicity: 1,1'-spiro-substituted hexahydrofuroquinoline derivatives.
AID1783924Terminal half life in DIO NFR-transgenic mouse liver at 30 mg/kg, po once daily for 14 days2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID1783925Terminal half life in DIO NFR-transgenic mouse adipose tissue at 30 mg/kg, po once daily for 14 days2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID657499Inhibition of CETP in human plasma assessed as reduction in fluorescent intensity by fluorescence analysis2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.
AID1500886Octanol-water partition coefficient, log P of the compound at pH 7.4 by HPLC based shake flask method2017European journal of medicinal chemistry, Oct-20, Volume: 139Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.
AID1783993Increase in HDL-cholesterol in transgenic mouse at 100 mg/kg, po treated for 2 weeks relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID1783923Terminal half life in DIO NFR-transgenic mouse plasma at 30 mg/kg, po once daily for 14 days2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID14766901-Octanol-phosphate buffered saline partition coefficient, log D of compound at pH 7.6 by tandem mass spectrometry method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
AID1187829Ex vivo inhibition of human CETP overexpressed in po dosed double transgenic mouse harboring human apoA1 assessed as elevation of HDL-cholesterol level measured at 8 hrs post dose2014European journal of medicinal chemistry, Oct-06, Volume: 85Some molecular targets for antihyperlipidemic drug research.
AID1476688Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (72)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's63 (87.50)24.3611
2020's9 (12.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.32

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.32 (24.57)
Research Supply Index4.56 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials20 (26.67%)5.53%
Reviews21 (28.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other34 (45.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (26)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase 2 Efficacy and Safety Study of LY2484595 Alone and in Combination With Atorvastatin, Simvastatin, and Rosuvastatin in Patients With Hypercholesterolemia or Low HDL-C [NCT01105975]Phase 2398 participants (Actual)Interventional2010-04-30Completed
A Bioequivalence Study in Healthy Subjects Administered Evacetrapib Tablets of Varying Tablet Solid Fractions [NCT01903434]Phase 160 participants (Actual)Interventional2013-07-31Completed
Effect of Evacetrapib on the Pharmacokinetics of Pravastatin in Healthy Japanese and Non-Japanese Subjects [NCT01958489]Phase 124 participants (Actual)Interventional2013-10-31Completed
A Double-Blind Efficacy and Safety Study of Evacetrapib in Combination With Atorvastatin in Japanese Patients With Primary Hypercholesterolemia [NCT02260648]Phase 3149 participants (Actual)Interventional2015-01-31Terminated(stopped due to Study termination due to insufficient efficacy.)
Pharmacokinetics of Evacetrapib (LY2484595) Following Administration to Subjects With Impaired Renal Function [NCT01825889]Phase 120 participants (Actual)Interventional2013-04-30Completed
Pharmacokinetics of Evacetrapib (LY2484595) in Subjects With Hepatic Impairment [NCT01836185]Phase 132 participants (Actual)Interventional2013-04-30Completed
An Absolute Bioavailability Study of Evacetrapib in Healthy Subjects Using the Intravenous Tracer Method [NCT02271425]Phase 18 participants (Actual)Interventional2014-10-31Completed
Effects of Evacetrapib (LY2484595) on the Pharmacokinetics of an Oral Contraceptive in Healthy Female Subjects [NCT01746732]Phase 123 participants (Actual)Interventional2012-12-31Completed
Assessment of Clinical Effects of Cholesteryl Ester Transfer Protein Inhibition With Evacetrapib in Patients at a High-Risk for Vascular Outcomes [NCT01687998]Phase 312,092 participants (Actual)Interventional2012-10-31Terminated(stopped due to Study termination due to insufficient efficacy.)
A Double-Blind Efficacy and Safety Study of Evacetrapib Followed by an Open-Label Extension in Japanese Patients With Primary Hypercholesterolemia [NCT02260635]Phase 354 participants (Actual)Interventional2014-11-30Terminated(stopped due to Study termination due to insufficient efficacy.)
Effect of Evacetrapib on the Pharmacokinetics and Pharmacodynamics of Warfarin in Healthy Subjects [NCT02161731]Phase 124 participants (Actual)Interventional2014-06-30Completed
A Bioequivalence Study in Healthy Subjects Administered Evacetrapib Tablets of Varying Particle Sizes [NCT02497391]Phase 195 participants (Actual)Interventional2015-07-31Completed
Effect of Evacetrapib on the Pharmacokinetics and Pharmacodynamics of Warfarin in Healthy Subjects [NCT01825876]Phase 117 participants (Actual)Interventional2013-04-30Completed
Effect of Food on the Pharmacokinetics of Evacetrapib (LY2484595) in Healthy Subjects [NCT01810432]Phase 140 participants (Actual)Interventional2013-03-31Completed
Effect of Gemfibrozil on the Pharmacokinetics of Evacetrapib (LY2484595) in Healthy Subjects [NCT01736254]Phase 124 participants (Actual)Interventional2012-12-31Completed
A Phase 2 Dose Response Study of LY2484595 in Japanese Subjects [NCT01375075]Phase 2165 participants (Actual)Interventional2011-06-30Completed
A Placebo- and Positive-Controlled Study of the Effect of LY2484595 on QT Interval in Healthy Subjects [NCT01537887]Phase 172 participants (Actual)Interventional2012-02-29Completed
Effect of Evacetrapib on the Pharmacokinetics of Digoxin in Healthy Subjects [NCT01897493]Phase 116 participants (Actual)Interventional2013-07-31Completed
Effect of Rifampin on the Pharmacokinetics of Evacetrapib in Healthy Subjects [NCT01908582]Phase 126 participants (Actual)Interventional2013-07-31Completed
Single Dose LY2484595 Tablet Formulations to Determine the Impact of Dose Level, Food, and Ethnicity on the Pharmacokinetics in Healthy Subjects [NCT01450098]Phase 139 participants (Actual)Interventional2011-10-31Completed
Evaluation of the Impact of Increased Gastric pH Following Omeprazole Administration on the Pharmacokinetics of Evacetrapib in Healthy Subjects [NCT02365558]Phase 134 participants (Actual)Interventional2015-01-31Completed
A Bioequivalence and Food Effect Study of Evacetrapib Evaluating a Single Tablet Compared to Two Tablets in Healthy Japanese Subjects [NCT02226653]Phase 148 participants (Actual)Interventional2014-09-30Completed
A Phase 1 Study to Evaluate the Safety and Tolerability of LY2484595 SDSD-PG Tablets and the Effect of CYP3A Inhibition by Ketoconazole on the Pharmacokinetics of LY2484595 in Healthy Subjects [NCT01448824]Phase 182 participants (Actual)Interventional2011-10-31Completed
A Phase 1b Study to Characterize the Pharmacokinetics of Evacetrapib and Potential for Accumulation After Dosing for 12, 24, and 52 Weeks [NCT02168803]Phase 1101 participants (Actual)Interventional2014-05-31Completed
The Addition of Evacetrapib to Atorvastatin Compared to Placebo, High Intensity Atorvastatin, and Atorvastatin With Ezetimibe to Evaluate LDL-C Lowering in Patients With Primary Hyperlipidemia - The ACCENTUATE Study [NCT02227784]Phase 3366 participants (Actual)Interventional2014-10-31Terminated(stopped due to Study termination due to program termination.)
A Pharmacokinetic, Pharmacodynamic, and Drug-Drug Interaction Study of Evacetrapib With Selected Statins in Healthy Chinese Subjects [NCT02156492]Phase 162 participants (Actual)Interventional2014-06-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01105975 (17) [back to overview]Change From Baseline to 12 Weeks Endpoint in Plasma Renin Activity
NCT01105975 (17) [back to overview]Change From Baseline to 12 Weeks Endpoint in Serum Aldosterone
NCT01105975 (17) [back to overview]Change From Baseline to 12 Weeks Endpoint in Serum Bicarbonate
NCT01105975 (17) [back to overview]Change From Baseline to 12 Weeks Endpoint in Serum Potassium
NCT01105975 (17) [back to overview]Change From Baseline to 12 Weeks Endpoint in Serum Sodium
NCT01105975 (17) [back to overview]Change From Baseline to 18 Weeks Endpoint in EuroQoL Questionnaire - 5 Dimensions (EQ-5D) Score
NCT01105975 (17) [back to overview]Percent Change From Baseline to 12 Weeks Endpoint in High Density Lipoprotein Cholesterol (HDL-C) With LY2484595 and Placebo
NCT01105975 (17) [back to overview]Percent Change From Baseline to 12 Weeks Endpoint in High Density Lipoprotein Cholesterol (HDL-C) With LY2484595 in Combination With Atorvastatin and Atorvastatin Monotherapy
NCT01105975 (17) [back to overview]Percent Change From Baseline to 12 Weeks Endpoint in High Density Lipoprotein Cholesterol (HDL-C) With LY2484595 in Combination With Simvastatin or Rosuvastatin and Simvastatin/Rosuvastatin Monotherapy
NCT01105975 (17) [back to overview]Percent Change From Baseline to 12 Weeks Endpoint in Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 and Placebo
NCT01105975 (17) [back to overview]Percent Change From Baseline to 12 Weeks Endpoint in Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 in Combination With Atorvastatin and Atorvastatin Monotherapy
NCT01105975 (17) [back to overview]Percent Change From Baseline to 12 Weeks Endpoint in Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 in Combination With Simvastatin or Rosuvastatin and Simvastatin/Rosuvastatin Monotherapy
NCT01105975 (17) [back to overview]Percent Change From Baseline to 12 Weeks Endpoint in Plasma Cholesteryl Ester Transfer Protein (CETP) Activity
NCT01105975 (17) [back to overview]Percent Change From Baseline to 12 Weeks Endpoint in Plasma Cholesteryl Ester Transfer Protein (CETP) Mass
NCT01105975 (17) [back to overview]Pharmacokinetics - LY2484595 Area Under the Concentration-Time Curve (AUC) at Steady-State
NCT01105975 (17) [back to overview]Change From Baseline to 12 Weeks Endpoint in Blood Pressure (BP)
NCT01105975 (17) [back to overview]The Number of Episodes of Rashes at Any Time From Baseline Through Week 12
NCT01375075 (13) [back to overview]Number of Myopathy and Liver Injury Events
NCT01375075 (13) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) and Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 in Combination With Atorvastatin
NCT01375075 (13) [back to overview]Percent Change From Baseline in Plasma Cholesteryl Ester Transfer Protein (CETP) Activity
NCT01375075 (13) [back to overview]Percent Change From Baseline to 12 Weeks in High Density Lipoprotein Cholesterol (HDL-C) and Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 and Placebo
NCT01375075 (13) [back to overview]The Number and Severity of Episodes of Rashes at Any Time From Baseline Through Week 12
NCT01375075 (13) [back to overview]Change From Baseline to 12 Weeks in Blood Pressure
NCT01375075 (13) [back to overview]Change From Baseline in Plasma CETP Mass
NCT01375075 (13) [back to overview]Pharmacokinetics - Area Under the Curve (AUC) of LY2484595 and Atorvastatin
NCT01375075 (13) [back to overview]Change From Baseline to 12 Weeks in Serum Sodium
NCT01375075 (13) [back to overview]Change From Baseline to 12 Weeks in Serum Bicarbonate
NCT01375075 (13) [back to overview]Change From Baseline to 12 Weeks in Plasma Renin Activity
NCT01375075 (13) [back to overview]Change From Baseline to 12 Weeks in Aldosterone
NCT01375075 (13) [back to overview]Change From Baseline to 12 Week Endpoint in Highly-Sensitive C-Reactive Protein (hsCRP)
NCT01448824 (9) [back to overview]Pharmacokinetics: Area Under the Concentration-time Curve (AUC) of LY2484595
NCT01448824 (9) [back to overview]Pharmacodynamics: Change From Baseline to Day 21 in Cholesteryl Ester Transfer Protein (CETP) Activity
NCT01448824 (9) [back to overview]Pharmacokinetics: Time of Maximum Observed Plasma Concentration (Tmax) of LY2484595
NCT01448824 (9) [back to overview]Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY2484595
NCT01448824 (9) [back to overview]Pharmacokinetics: Area Under the Concentration-time Curve (AUC) of LY2484595
NCT01448824 (9) [back to overview]Pharmacodynamics: Change From Baseline to Day 21 in High-density Lipoprotein Cholesterol (HDL-C), Low-density Lipoprotein Cholesterol (LDL-C), and Triglycerides (TG)
NCT01448824 (9) [back to overview]Part 1: Number of Participants With 1 or More Adverse Events (AEs) or Any Serious AEs
NCT01448824 (9) [back to overview]Pharmacokinetics: Time of Maximum Observed Plasma Concentration (Tmax) of LY2484595
NCT01448824 (9) [back to overview]Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY2484595
NCT01450098 (3) [back to overview]Pharmacokinetics: Area Under the Plasma Concentration Versus Time Curve (AUC) of LY2484595
NCT01450098 (3) [back to overview]Number of Participants With One or More Drug-related Adverse Events (AEs) or Any Serious AEs
NCT01450098 (3) [back to overview]Pharmacokinetics: Peak Plasma Concentration (Cmax) of LY2484595
NCT01537887 (4) [back to overview]Pharmacokinetics: Maximum Drug Concentration (Cmax) of LY2484595 During One Dosing Interval at Steady State
NCT01537887 (4) [back to overview]Pharmacokinetics: Area Under the Concentration Curve (AUC) of LY2484595 During One Dosing Interval at Steady State
NCT01537887 (4) [back to overview]Percentage Change From Baseline to Day 11 in Fasting Lipids and Apolipoproteins
NCT01537887 (4) [back to overview]Change From Baseline to Day 10 in QT Interval Corrected for Heart Rate (QTc) for LY2484595 Versus Placebo
NCT01687998 (6) [back to overview]Number of Participants With Composite Endpoint of All-Cause Mortality, MI, Stroke, Coronary Revascularization, or Hospitalization for UA
NCT01687998 (6) [back to overview]Number of Participants With Composite Endpoint of CV Death, MI, or Coronary Revascularization
NCT01687998 (6) [back to overview]Number of Participants With Composite Endpoint of CV Death, MI, Stroke, or Hospitalization for UA
NCT01687998 (6) [back to overview]Number of Participants With Composite Primary Endpoint of Cardiovascular (CV) Death, Myocardial Infarction (MI), Stroke, Coronary Revascularization, or Hospitalization for Unstable Angina (UA)
NCT01687998 (6) [back to overview]Number of Participants With Triple Composite Endpoint of CV Death, MI, or Stroke
NCT01687998 (6) [back to overview]Mean Percent Change From Baseline to 3 Months in Low-Density (LDL-C) and High-Density Lipoprotein Cholesterol (HDL-C) Levels
NCT01736254 (6) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Curve Over a 12 Hour Dosing Interval (AUCτ) of Gemfibrozil
NCT01736254 (6) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Evacetrapib
NCT01736254 (6) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib
NCT01736254 (6) [back to overview]Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Gemfibrozil
NCT01736254 (6) [back to overview]Pharmacokinetics (PK): Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib
NCT01736254 (6) [back to overview]Pharmacokinetics (PK): Time of Maximum Observed Drug Concentration (Tmax) of Gemfibrozil
NCT01746732 (8) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Ethinyl Estradiol
NCT01746732 (8) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Norelgestromin
NCT01746732 (8) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Ethinyl Estradiol
NCT01746732 (8) [back to overview]PK: Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Ethinyl Estradiol
NCT01746732 (8) [back to overview]PK: Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Norelgestromin
NCT01746732 (8) [back to overview]PK: Maximum Concentration (Cmax) of Norelgestromin
NCT01746732 (8) [back to overview]PK: Minimum Observed Drug Concentration (Cmin) of Ethinyl Estradiol
NCT01746732 (8) [back to overview]PK: Minimum Observed Drug Concentration (Cmin) of Norelgestromin
NCT01810432 (3) [back to overview]PK: Area Under Concentration Versus Time Curve Over the 24-hour Dosing Interval (AUCτ) of Evacetrapib
NCT01810432 (3) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib
NCT01810432 (3) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib
NCT01825876 (6) [back to overview]Pharmacodynamics (PD): Area Under the International Normalized Ratio Curve (AUCINR) of Warfarin
NCT01825876 (6) [back to overview]PK: Maximum Observed Concentration (Cmax) of S-Warfarin
NCT01825876 (6) [back to overview]PK: Cmax of R-Warfarin
NCT01825876 (6) [back to overview]PK: AUC0-∞ of R-Warfarin
NCT01825876 (6) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-∞) of S-Warfarin
NCT01825876 (6) [back to overview]PD: Maximum Observed INR Response (INRmax) of Warfarin
NCT01825889 (3) [back to overview]Pharmacokinetics (PK): Observed Maximum Concentration (Cmax) of Evacetrapib
NCT01825889 (3) [back to overview]Pharmacokinetics (PK): Area Under The Concentration Versus Time Curve From Time Zero To Time Tlast, Where Tlast is the Last Time Point With a Measurable Concentration (AUC[0-Tlast]) of Evacetrapib
NCT01825889 (3) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time Zero to Infinity (AUC[0-∞]) of Evacetrapib
NCT01836185 (3) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib
NCT01836185 (3) [back to overview]PK: Maximum Observed Concentration (Cmax) of Evacetrapib
NCT01836185 (3) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Time Tlast (AUC0-tlast) of Evacetrapib
NCT01897493 (4) [back to overview]Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Digoxin
NCT01897493 (4) [back to overview]PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-∞) of Digoxin
NCT01897493 (4) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Digoxin
NCT01897493 (4) [back to overview]Renal Clearance (CLr) of Digoxin
NCT01903434 (2) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib (LY2484595)
NCT01903434 (2) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib (LY2484595)
NCT01908582 (3) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib
NCT01908582 (3) [back to overview]Pharmacokinetics (PK): Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib
NCT01908582 (3) [back to overview]Pharmacokinetics, Area Under the Plasma Concentration-Time Curve From Time 0 Hour (h) to Infinity (AUC0-∞) of Evacetrapib
NCT01958489 (3) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Pravastatin
NCT01958489 (3) [back to overview]PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity [AUC(0-∞)] of Pravastatin
NCT01958489 (3) [back to overview]PK: Time of Maximum Observed Concentration (Tmax) of Pravastatin
NCT02156492 (7) [back to overview]PK: Cmax of Evacetrapib Alone and With Simvastatin or Atorvastatin
NCT02156492 (7) [back to overview]PK: AUC of Evacetrapib Alone and With Simvastatin or Atorvastatin
NCT02156492 (7) [back to overview]Pharmacokinetics (PK): Area Under Curve (AUC 0-inf) of Evacetrapib
NCT02156492 (7) [back to overview]Effect of Evacetrapib Single and Multiple Doses on High Density Lipoprotein Cholesterol (HDL-C), Low Density Lipoprotein Cholesterol (LDL-C), and Triglycerides (TG)
NCT02156492 (7) [back to overview]PK: Tmax of Evacetrapib Alone and With Simvastatin or Atorvastatin
NCT02156492 (7) [back to overview]PK: Maximum Concentration (Cmax) of Evacetrapib
NCT02156492 (7) [back to overview]PK: Time to Maximum Concentration (Tmax) of Evacetrapib
NCT02161731 (6) [back to overview]PK: Maximum Observed Concentration (Cmax) of S-warfarin
NCT02161731 (6) [back to overview]PK: Cmax of R-warfarin
NCT02161731 (6) [back to overview]PK: AUC[0-∞] of R-warfarin
NCT02161731 (6) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of S-Warfarin
NCT02161731 (6) [back to overview]Pharmacodynamics (PD): Area Under the International Normalized Ratio Curve (AUC[INR]) of Warfarin
NCT02161731 (6) [back to overview]PD: Maximum Observed International Normalized Ratio Response (INRmax) of Warfarin
NCT02168803 (7) [back to overview]PD Parameters of Evacetrapib: Triglyceride Level
NCT02168803 (7) [back to overview]PD Parameters of Evacetrapib: Total Cholesterol Level
NCT02168803 (7) [back to overview]PD Parameters of Evacetrapib: Low-Density Lipoprotein Cholesterol (LDL-C) Level
NCT02168803 (7) [back to overview]PD Parameters of Evacetrapib: High Density Lipoprotein Cholesterol (HDL-C) Level
NCT02168803 (7) [back to overview]PK Parameters of Evacetrapib: Terminal Half-life
NCT02168803 (7) [back to overview]PK Parameters of Evacetrapib: Maximum Concentration (Cmax)
NCT02168803 (7) [back to overview]Pharmacokinetics (PK) Parameters of Evacetrapib: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast])
NCT02226653 (5) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib (Fasted)
NCT02226653 (5) [back to overview]PK: AUC(0-∞)of Evacetrapib (Fasted and Fed)
NCT02226653 (5) [back to overview]PK: Cmax of Evacetrapib (Fasted and Fed)
NCT02226653 (5) [back to overview]PK: Maximum Concentration (Cmax) of Evacetrapib (Fasted)
NCT02226653 (5) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib (Fasted and Fed)
NCT02227784 (7) [back to overview]Percent Change From Baseline to 3 Months in Apolipoprotein B (apoB)
NCT02227784 (7) [back to overview]Percent Change From Baseline to 3 Months in Cholesterol Efflux Capacity
NCT02227784 (7) [back to overview]Percent Change From Baseline to 3 Months in High-Density Lipoprotein Cholesterol (HDL-C)
NCT02227784 (7) [back to overview]Percent Change From Baseline to 3 Months in Lipoprotein(a) (Lp[a])
NCT02227784 (7) [back to overview]Percent Change From Baseline to 3 Months in Low-Density Lipoprotein Cholesterol (LDL-C)
NCT02227784 (7) [back to overview]Percent Change From Baseline to 3 Months in Non-HDL-C
NCT02227784 (7) [back to overview]Percent Change From Baseline to 3 Months in Apolipoprotein AI (apoAI)
NCT02260635 (7) [back to overview]Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C)
NCT02260635 (7) [back to overview]Percent Change From Baseline in LDL-C (Direct)
NCT02260635 (7) [back to overview]Percent Change From Baseline in Non HDL-C
NCT02260635 (7) [back to overview]Percent Change From Baseline to Week 12 in Low-Density Lipoprotein Cholesterol (LDL-C) Measured by Beta Quantification
NCT02260635 (7) [back to overview]Percent Change From Baseline in Apolipoprotein A-I
NCT02260635 (7) [back to overview]Percent Change From Baseline in Apolipoprotein B
NCT02260635 (7) [back to overview]Percent Change From Baseline in Lipoprotein-a
NCT02260648 (7) [back to overview]Percent Change From Baseline to Week 12 in Apolipoprotein B
NCT02260648 (7) [back to overview]Percent Change From Baseline to Week 12 in Non HDL-C
NCT02260648 (7) [back to overview]Percent Change From Baseline to Week 12 in Low-Density Lipoprotein Cholesterol (LDL-C) Measured by Beta Quantification
NCT02260648 (7) [back to overview]Percent Change From Baseline to Week 12 in Lipoprotein-a
NCT02260648 (7) [back to overview]Percent Change From Baseline to Week 12 in LDL-C (Direct)
NCT02260648 (7) [back to overview]Percent Change From Baseline to Week 12 in High-Density Lipoprotein Cholesterol (HDL-C)
NCT02260648 (7) [back to overview]Percent Change From Baseline to Week 12 in Apolipoprotein A-I
NCT02271425 (1) [back to overview]Pharmacokinetics (PK): Dose Normalized Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib
NCT02365558 (3) [back to overview]Pharmacokinetics (PK): Time of Maximum Observed Concentration (Tmax) of Evacetrapib
NCT02365558 (3) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞])
NCT02365558 (3) [back to overview]Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Evacetrapib
NCT02497391 (2) [back to overview]Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Evacetrapib
NCT02497391 (2) [back to overview]PK: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib

Change From Baseline to 12 Weeks Endpoint in Plasma Renin Activity

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionnanograms/milliliter/hour (ng/mL/h) (Least Squares Mean)
30 mg LY2484595 Monotherapy-0.06
100 mg LY2484595 Monotherapy-0.11
500 mg LY2484595 Monotherapy-0.58
Placebo-0.30
20 mg Atorvastatin Monotherapy-0.58
100 mg LY2484595 + 20 mg Atorvastatin-0.26
40 mg Simvastatin Monotherapy-0.16
100 mg LY2484595 + 40 mg Simvastatin0.00
10 mg Rosuvastatin Monotherapy-0.86
100 mg LY2484595 + 10 mg Rosuvastatin-0.29

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Change From Baseline to 12 Weeks Endpoint in Serum Aldosterone

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionnanogram/deciliter (ng/dL) (Least Squares Mean)
30 mg LY2484595 Monotherapy-0.5
100 mg LY2484595 Monotherapy1.0
500 mg LY2484595 Monotherapy-0.3
Placebo-1.0
20 mg Atorvastatin Monotherapy-1.0
100 mg LY2484595 + 20 mg Atorvastatin0.4
40 mg Simvastatin Monotherapy0.0
100 mg LY2484595 + 40 mg Simvastatin-1.7
10 mg Rosuvastatin Monotherapy-2.5
100 mg LY2484595 + 10 mg Rosuvastatin0.0

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Change From Baseline to 12 Weeks Endpoint in Serum Bicarbonate

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionmilliequivalents/Liter (Least Squares Mean)
30 mg LY2484595 Monotherapy0.40
100 mg LY2484595 Monotherapy0.60
500 mg LY2484595 Monotherapy0.51
Placebo0.27
20 mg Atorvastatin Monotherapy0.10
100 mg LY2484595 + 20 mg Atorvastatin0.58
40 mg Simvastatin Monotherapy1.04
100 mg LY2484595 + 40 mg Simvastatin0.58
10 mg Rosuvastatin Monotherapy0.78
100 mg LY2484595 + 10 mg Rosuvastatin1.25

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Change From Baseline to 12 Weeks Endpoint in Serum Potassium

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionmilliequivalents/Liter (Least Squares Mean)
30 mg LY2484595 Monotherapy-0.04
100 mg LY2484595 Monotherapy0.01
500 mg LY2484595 Monotherapy-0.02
Placebo-0.08
20 mg Atorvastatin Monotherapy0.09
100 mg LY2484595 + 20 mg Atorvastatin0.08
40 mg Simvastatin Monotherapy0.03
100 mg LY2484595 + 40 mg Simvastatin0.02
10 mg Rosuvastatin Monotherapy-0.07
100 mg LY2484595 + 10 mg Rosuvastatin-0.05

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Change From Baseline to 12 Weeks Endpoint in Serum Sodium

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionmilliequivalents/Liter (Least Squares Mean)
30 mg LY2484595 Monotherapy0.3
100 mg LY2484595 Monotherapy0.3
500 mg LY2484595 Monotherapy0.5
Placebo0.1
20 mg Atorvastatin Monotherapy1.3
100 mg LY2484595 + 20 mg Atorvastatin0.6
40 mg Simvastatin Monotherapy0.8
100 mg LY2484595 + 40 mg Simvastatin0.9
10 mg Rosuvastatin Monotherapy0.5
100 mg LY2484595 + 10 mg Rosuvastatin0.3

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Change From Baseline to 18 Weeks Endpoint in EuroQoL Questionnaire - 5 Dimensions (EQ-5D) Score

EQ-5D is a health-related, quality-of-life instrument. It allows participants to rate their health state in 5 domains: mobility, self-care, usual activities, pain/discomfort, and mood. A single score 1 -3 is generated for each domain, with 1=no problem and 3= extreme problems. The outcome ratings on the 5 domains are mapped to a single index through an algorithm. The index ranges 0-1, with the higher score indicating a better health state perceived by the participants. LS Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline up to Week 18

Interventionunits on a scale (Least Squares Mean)
30 mg LY2484595 Monotherapy0.008
100 mg LY2484595 Monotherapy0.002
500 mg LY2484595 Monotherapy0.012
Placebo-0.001
20 mg Atorvastatin Monotherapy-0.002
100 mg LY2484595 + 20 mg Atorvastatin-0.006
40 mg Simvastatin Monotherapy-0.001
100 mg LY2484595 + 40 mg Simvastatin-0.001
10 mg Rosuvastatin Monotherapy0.014
100 mg LY2484595 + 10 mg Rosuvastatin-0.047

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Percent Change From Baseline to 12 Weeks Endpoint in High Density Lipoprotein Cholesterol (HDL-C) With LY2484595 and Placebo

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionpercent change of mg/dL (Least Squares Mean)
30 mg LY2484595 Monotherapy53.6
100 mg LY2484595 Monotherapy94.6
500 mg LY2484595 Monotherapy128.8
Placebo-3.0

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Percent Change From Baseline to 12 Weeks Endpoint in High Density Lipoprotein Cholesterol (HDL-C) With LY2484595 in Combination With Atorvastatin and Atorvastatin Monotherapy

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionpercent change of mg/dL (Least Squares Mean)
20 mg Atorvastatin Monotherapy1.4
100 mg LY2484595 + 20 mg Atorvastatin79.9

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Percent Change From Baseline to 12 Weeks Endpoint in High Density Lipoprotein Cholesterol (HDL-C) With LY2484595 in Combination With Simvastatin or Rosuvastatin and Simvastatin/Rosuvastatin Monotherapy

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionpercent change of mg/dL (Least Squares Mean)
40 mg Simvastatin Monotherapy7.3
100 mg LY2484595 + 40 mg Simvastatin86.6
10 mg Rosuvastatin Monotherapy5.5
100 mg LY2484595 + 10 mg Rosuvastatin94.0

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Percent Change From Baseline to 12 Weeks Endpoint in Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 and Placebo

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionpercent change of mg/dL (Least Squares Mean)
30 mg LY2484595 Monotherapy-13.6
100 mg LY2484595 Monotherapy-22.3
500 mg LY2484595 Monotherapy-35.9
Placebo3.9

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Percent Change From Baseline to 12 Weeks Endpoint in Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 in Combination With Atorvastatin and Atorvastatin Monotherapy

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionpercent change of mg/dL (Least Squares Mean)
20 mg Atorvastatin Monotherapy-33.6
100 mg LY2484595 + 20 mg Atorvastatin-47.6

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Percent Change From Baseline to 12 Weeks Endpoint in Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 in Combination With Simvastatin or Rosuvastatin and Simvastatin/Rosuvastatin Monotherapy

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionpercent change of mg/dL (Least Squares Mean)
40 mg Simvastatin Monotherapy-34.9
100 mg LY2484595 + 40 mg Simvastatin-46.1
10 mg Rosuvastatin Monotherapy-38.8
100 mg LY2484595 + 10 mg Rosuvastatin-52.3

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Percent Change From Baseline to 12 Weeks Endpoint in Plasma Cholesteryl Ester Transfer Protein (CETP) Activity

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionpercent change of picomoles/mL/minute (Least Squares Mean)
30 mg LY2484595 Monotherapy-49.48
100 mg LY2484595 Monotherapy-70.80
500 mg LY2484595 Monotherapy-89.10
Placebo12.12
20 mg Atorvastatin Monotherapy-0.01
100 mg LY2484595 + 20 mg Atorvastatin-72.00
40 mg Simvastatin Monotherapy-2.23
100 mg LY2484595 + 40 mg Simvastatin-64.64
10 mg Rosuvastatin Monotherapy-7.19
100 mg LY2484595 + 10 mg Rosuvastatin-73.24

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Percent Change From Baseline to 12 Weeks Endpoint in Plasma Cholesteryl Ester Transfer Protein (CETP) Mass

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

Interventionpercent change of micrograms/mL (mcg/mL) (Least Squares Mean)
30 mg LY2484595 Monotherapy63.94
100 mg LY2484595 Monotherapy92.27
500 mg LY2484595 Monotherapy136.66
Placebo0.58
20 mg Atorvastatin Monotherapy-11.8
100 mg LY2484595 + 20 mg Atorvastatin62.98
40 mg Simvastatin Monotherapy-11.14
100 mg LY2484595 + 40 mg Simvastatin65.92
10 mg Rosuvastatin Monotherapy-16.58
100 mg LY2484595 + 10 mg Rosuvastatin64.08

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Pharmacokinetics - LY2484595 Area Under the Concentration-Time Curve (AUC) at Steady-State

(NCT01105975)
Timeframe: Baseline up to 12 weeks

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
30 mg LY2484595 Monotherapy2300
100 mg LY2484595 Monotherapy5900
500 mg LY2484595 Monotherapy19700
100 mg LY2484595 + 20 mg Atorvastatin5500
100 mg LY2484595 + 40 mg Simvastatin5620
100 mg LY2484595 + 10 mg Rosuvastatin5960

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Change From Baseline to 12 Weeks Endpoint in Blood Pressure (BP)

Least Squares (LS) Mean values were controlled for region, baseline measurement, treatment, visit, and treatment by visit interaction. (NCT01105975)
Timeframe: Baseline, Week 12

,,,,,,,,,
Interventionmillimeters of mercury (mmHg) (Least Squares Mean)
Diastolic BPSystolic BP
10 mg Rosuvastatin Monotherapy2.20.0
100 mg LY2484595 + 10 mg Rosuvastatin-0.13.8
100 mg LY2484595 + 20 mg Atorvastatin1.22.1
100 mg LY2484595 + 40 mg Simvastatin2.32.3
100 mg LY2484595 Monotherapy0.84.3
20 mg Atorvastatin Monotherapy0.20.2
30 mg LY2484595 Monotherapy1.14.4
40 mg Simvastatin Monotherapy-1.50.0
500 mg LY2484595 Monotherapy1.21.4
Placebo1.62.8

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The Number of Episodes of Rashes at Any Time From Baseline Through Week 12

All rash cases were adjudicated by a central dermatologist blinded to treatment assignment according to a study-specific Clinical Events Committee (CEC) charter. Rash events were assessed according to clinical relevance (high risk, low risk, not a relevant dermatosis, or insufficient documentation for determination). A participant could be reported in multiple categories. (NCT01105975)
Timeframe: Baseline through Week 12

,,,,,,,,,
Interventionevents (Number)
High Risk (HR)- AngioedemaHR - Insufficient Documentation for DeterminationLow RiskNot a Relevant DermatosesInsufficient Documentation for Determination
10 mg Rosuvastatin Monotherapy00000
100 mg LY2484595 + 10 mg Rosuvastatin01210
100 mg LY2484595 + 20 mg Atorvastatin00020
100 mg LY2484595 + 40 mg Simvastatin00140
100 mg LY2484595 Monotherapy00050
20 mg Atorvastatin Monotherapy00010
30 mg LY2484595 Monotherapy00040
40 mg Simvastatin Monotherapy10060
500 mg LY2484595 Monotherapy00030
Placebo00000

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Number of Myopathy and Liver Injury Events

Myopathy events were considered muscle-related treatment emergent adverse events (TEAEs) and liver injury events were considered hepatic disorder-related TEAEs reported per Medical Dictionary for Regulatory Activities (MedDRA). An adverse event (AE) was any untoward medical occurrence attributed to study drug in a participant who received study drug. TEAEs were newly occurring AEs or AEs worsening after first dose. (NCT01375075)
Timeframe: Baseline through Week 12

,,,,,
Interventionevents (Number)
Blood creatine phosphokinase increasedMyalgiaHepatic function abnormalGamma-glutamyltransferase increasedAlanine aminotransferase increased
10 mg Atorvastatin11100
100 mg LY248459511010
100 mg LY2484595 + 10 mg Atorvastatin00200
30 mg LY248459500100
500 mg LY248459500100
Placebo00001

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Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) and Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 in Combination With Atorvastatin

Percent change from baseline = 100*(post-baseline assessment - baseline assessment)/baseline assessment. An increase in the percent change from baseline represented an improvement for HDL-C and a decrease in the percent change from baseline represents an improvement for LDL-C. LS mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline, Weeks 2, 4, and 8

,,,,,
Interventionpercent change (Least Squares Mean)
HDL-C, Week 2HDL-C, Week 4HDL-C, Week 8LDL-C, Week 2LDL-C, Week 4LDL-C, Week 8
10 mg Atorvastatin8.8510.8712.98-38.29-42.23-38.97
100 mg LY2484595108.21122.68130.69-27.50-24.43-23.56
100 mg LY2484595 + 10 mg Atorvastatin101.45117.04116.64-55.74-52.62-51.23
30 mg LY248459575.3077.9478.65-17.46-13.32-12.50
500 mg LY2484595122.60147.22169.05-33.19-29.25-25.48
Placebo-0.732.095.19-2.142.840.24

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Percent Change From Baseline in Plasma Cholesteryl Ester Transfer Protein (CETP) Activity

Plasma CETP activity assay employed a fluorometric method to determine the CETP transfer activity. Percent change from baseline = 100*(post-baseline assessment - baseline assessment)/baseline assessment. An increase in the percent change from baseline represented an improvement. LS mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline, Weeks 4, 8, and 12

,,,,,
Interventionpercent change in CETP activity (Least Squares Mean)
4 Weeks8 Weeks12 Weeks
10 mg Atorvastatin-1.33-4.89-5.69
100 mg LY2484595-75.26-76.23-73.86
100 mg LY2484595 + 10 mg Atorvastatin-68.58-79.90-73.38
30 mg LY2484595-41.62-39.91-41.07
500 mg LY2484595-89.14-90.97-85.30
Placebo1.672.709.22

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Percent Change From Baseline to 12 Weeks in High Density Lipoprotein Cholesterol (HDL-C) and Low Density Lipoprotein Cholesterol (LDL-C) With LY2484595 and Placebo

Percent change from baseline = 100*(post-baseline assessment - baseline assessment)/baseline assessment. Higher values in the percent change from baseline represented an improvement for HDL-C and lower values in the percent change from baseline represented an improvement for LDL-C. Least Squares (LS) mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline and Week 12

,,,,,
Interventionpercent change (Least Squares Mean)
HDL-CLDL-C
10 mg Atorvastatin17.35-37.66
100 mg LY2484595123.35-22.13
100 mg LY2484595 + 10 mg Atorvastatin120.60-52.29
30 mg LY248459582.22-14.23
500 mg LY2484595143.56-20.95
Placebo8.001.24

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The Number and Severity of Episodes of Rashes at Any Time From Baseline Through Week 12

All rash cases were adjudicated by a central dermatologist blinded to treatment assignment according to a study-specific Clinical Events Committee (CEC) charter. Rash events were assessed according to clinical relevance (severity). Categories included high risk, low risk, not a relevant dermatosis, or insufficient documentation for determination. High risk rashes included anaphylaxis, toxic epidermal necrolysis, Stevens Johnson Syndrome, Drug Reaction with Eosinophilia and System Symptoms (DRESS), urticaria/angioedema, vasculitis, erythroderma, and lupus-like reaction. All other rashes were considered low risk or not a relevant dermatosis per the Investigator's clinical opinion. A participant could be reported in multiple categories. (NCT01375075)
Timeframe: Baseline through Week 12

,,,,,
Interventionevents (Number)
Low riskHigh riskNot a relevant dermatosisInsufficient documentation for determination
10 mg Atorvastatin0000
100 mg LY24845950000
100 mg LY2484595 + 10 mg Atorvastatin1010
30 mg LY24845950000
500 mg LY24845951100
Placebo0010

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Change From Baseline to 12 Weeks in Blood Pressure

"Blood pressure reported as systolic blood pressure (SBP) and diastolic blood pressure (DBP).~LS mean was adjusted for baseline value of the variable analyzed." (NCT01375075)
Timeframe: Baseline and Week 12

,,,,,
Interventionmillimeters of mercury (mm Hg) (Least Squares Mean)
SBPDBP
10 mg Atorvastatin2.591.49
100 mg LY24845951.440.02
100 mg LY2484595 + 10 mg Atorvastatin2.040.51
30 mg LY24845952.351.46
500 mg LY24845954.512.51
Placebo-1.390.68

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Change From Baseline in Plasma CETP Mass

Plasma CETP mass assay was a solid-phase enzyme-linked immunosorbent assay (ELISA) designated to measure human CETP mass which employed the quantitative enzyme immunoassay principle. An increase in plasma CETP mass represented an improvement. LS mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline, Weeks 4, 8, and 12

,,,,,
Interventionmicrograms per milliliter (µg/mL) (Least Squares Mean)
4 weeks8 weeks12 weeks
10 mg Atorvastatin-0.28-0.21-0.19
100 mg LY24845953.143.092.96
100 mg LY2484595 + 10 mg Atorvastatin1.941.831.95
30 mg LY24845951.881.981.95
500 mg LY24845953.544.023.36
Placebo0.080.100.13

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Pharmacokinetics - Area Under the Curve (AUC) of LY2484595 and Atorvastatin

(NCT01375075)
Timeframe: Weeks 2, 4, 8, 12 (predose and postdose), and Week 16

Interventionnanograms*hours per milliliter (ng*h/mL) (Geometric Mean)
30 mg LY24845953110
100 mg LY24845958690
500 mg LY248459529400
100 mg LY2484595 + 10 mg Atorvastatin8080

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Change From Baseline to 12 Weeks in Serum Sodium

LS mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline and Week 12

Interventionmilliequivalents per liter (mEq/L) (Least Squares Mean)
30 mg LY2484595-0.18
100 mg LY2484595-0.32
500 mg LY2484595-0.07
Placebo-0.32
10 mg Atorvastatin0.35
100 mg LY2484595 + 10 mg Atorvastatin0.53

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Change From Baseline to 12 Weeks in Serum Bicarbonate

LS mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline and Week 12

Interventionmilliequivalents per liter (mEq/L) (Least Squares Mean)
30 mg LY24845950.63
100 mg LY24845950.62
500 mg LY24845950.62
Placebo0.52
10 mg Atorvastatin0.62
100 mg LY2484595 + 10 mg Atorvastatin1.23

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Change From Baseline to 12 Weeks in Plasma Renin Activity

LS mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline and Week 12

Interventionnanograms per milliliter per hour (Least Squares Mean)
30 mg LY2484595-0.32
100 mg LY24845950.01
500 mg LY2484595-0.21
Placebo-0.21
10 mg Atorvastatin-0.01
100 mg LY2484595 + 10 mg Atorvastatin-0.43

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Change From Baseline to 12 Weeks in Aldosterone

LS mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline and Week 12

Interventionnanograms per deciliter (ng/dL) (Least Squares Mean)
30 mg LY2484595-0.40
100 mg LY24845950.37
500 mg LY24845950.59
Placebo0.33
10 mg Atorvastatin0.95
100 mg LY2484595 + 10 mg Atorvastatin0.62

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Change From Baseline to 12 Week Endpoint in Highly-Sensitive C-Reactive Protein (hsCRP)

LS mean was adjusted for baseline value of the variable analyzed. (NCT01375075)
Timeframe: Baseline and Week 12

Interventionmilligrams per deciliter (mg/dL) (Least Squares Mean)
30 mg LY2484595-0.03
100 mg LY24845950.00
500 mg LY24845950.13
Placebo-0.01
10 mg Atorvastatin-0.03
100 mg LY2484595 + 10 mg Atorvastatin0.15

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Pharmacokinetics: Area Under the Concentration-time Curve (AUC) of LY2484595

The geometric least squares (LS) means of area under the concentration-time curve (AUC) from time zero extrapolated to infinity (AUC0-∞) of LY2484595 following administration of LY2484595 alone and with ketoconazole are reported. Least squares means were calculated from an analysis of variance (ANOVA) model with a fixed effect for treatment and a random effect for participant. The LS means for each treatment and the 90% confidence intervals (CI) for the difference in means were back transformed from the log scale to provide estimates of the geometric means and 90% CIs for the ratio of the geometric means (LY2484595 coadministered with ketoconazole and LY2484595 alone). (NCT01448824)
Timeframe: Part 2, Period 1, Day 1 through Day 8: Predose, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168 Hours Post Dose; Period 2, Day 5 through Day 15: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240 Hours Post Dose

InterventionNanograms * hours per milliliter (Geometric Mean)
Part 2, Period 1: 100 mg LY24845955265
Part 2, Period 2: 100 mg LY2484595 + 400 mg Ketoconazole12471

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Pharmacodynamics: Change From Baseline to Day 21 in Cholesteryl Ester Transfer Protein (CETP) Activity

(NCT01448824)
Timeframe: Day 1 (Baseline) and Day 21

InterventionPicomoles per milliliters per minute (Mean)
Part 1 (Cohorts A Through D): Placebo1.3
Part 1, Period 1 (Cohort A): 100 mg LY2484595-0.4
Part 1 (Cohort B): 300 mg LY2484595-0.4
Part 1 (Cohort C): 600 mg LY2484595-9.1
Part 1 (Cohort D): 1200 mg LY2484595-9.5
Part 1, Period 2 (Cohort A): 1800 mg LY2484595-12.9

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Pharmacokinetics: Time of Maximum Observed Plasma Concentration (Tmax) of LY2484595

The times of maximum observed plasma concentrations (tmax) of LY2484595 after a single dose and after once daily (QD) dosing for 14 consecutive days are reported. (NCT01448824)
Timeframe: Part 1, Periods 1 and 2, Day 1: Predose, 1, 2, 3, 4, 6, 8, 12, and 24 Hours Postdose; Day 14 through Day 21: Predose, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 168 Hours Post Dose

,,,,
InterventionHours (h) (Median)
Day 1Day 14
Part 1 (Cohort B): 300 mg LY24845953.002.00
Part 1 (Cohort C): 600 mg LY24845953.002.50
Part 1 (Cohort D): 1200 mg LY24845952.002.00
Part 1, Period 1 (Cohort A): 100 mg LY24845953.004.00
Part 1, Period 2 (Cohort A): 1800 mg LY24845952.003.00

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Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY2484595

The maximum observed plasma concentrations (Cmax) of LY2484595 after a single dose and after once daily (QD) dosing for 14 consecutive days are reported. (NCT01448824)
Timeframe: Part 1, Periods 1 and 2, Day 1: Predose, 1, 2, 3, 4, 6, 8, 12, and 24 Hours Postdose; Day 14 through Day 21: Predose, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 168 Hours Post Dose

,,,,
InterventionNanograms per milliliter (ng/mL) (Geometric Mean)
Day 1Day 14
Part 1 (Cohort B): 300 mg LY248459519901970
Part 1 (Cohort C): 600 mg LY248459527204180
Part 1 (Cohort D): 1200 mg LY248459544505410
Part 1, Period 1 (Cohort A): 100 mg LY2484595628978
Part 1, Period 2 (Cohort A): 1800 mg LY248459535805750

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Pharmacokinetics: Area Under the Concentration-time Curve (AUC) of LY2484595

Exposure to LY2484595 in terms of the area under the concentration-time curves (AUC) after a single dose and after once daily (QD) dosing for 14 consecutive days are reported. (NCT01448824)
Timeframe: Part 1, Periods 1 and 2, Day 1: Predose, 1, 2, 3, 4, 6, 8, 12, and 24 Hours Postdose; Day 14 through Day 21: Predose, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 168 Hours Post Dose

,,,,
InterventionNanograms * hour per milliliter (Geometric Mean)
Day 1Day 14
Part 1 (Cohort B): 300 mg LY24845951450017900
Part 1 (Cohort C): 600 mg LY24845952130036200
Part 1 (Cohort D): 1200 mg LY24845953630046900
Part 1, Period 1 (Cohort A): 100 mg LY248459547808110
Part 1, Period 2 (Cohort A): 1800 mg LY24845953130056600

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Pharmacodynamics: Change From Baseline to Day 21 in High-density Lipoprotein Cholesterol (HDL-C), Low-density Lipoprotein Cholesterol (LDL-C), and Triglycerides (TG)

(NCT01448824)
Timeframe: Day 1 (Baseline) and Day 21

,,,,
InterventionMillimoles per liter (mmol/L) (Mean)
HDL-CLDL-CTG
Part 1 (Cohort B): 300 mg LY24845950.49-0.480.44
Part 1 (Cohort C): 600 mg LY24845950.77-1.150.26
Part 1 (Cohort D): 1200 mg LY24845950.80-1.010.52
Part 1, Period 1 (Cohort A): 100 mg LY24845950.35-0.160.55
Part 1, Period 1 (Cohorts A Through D): Placebo-0.08-0.420.56

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Part 1: Number of Participants With 1 or More Adverse Events (AEs) or Any Serious AEs

The number of participants with 1 or more AEs is summarized cumulatively. In addition, the number of participants with any serious AEs is summarized cumulatively. A serious AE is defined as an event that results in death, initial or prolonged hospitalization, is life-threatening, leads to persistent or significant disability/incapacity, is associated with congenital anomaly/birth defect, or is considered significant by the investigator for any other reason. A summary of serious and other non-serious AEs regardless of causality is located in the Reported Adverse Events module. (NCT01448824)
Timeframe: Part 1: Baseline through ≥14 days after last dose of study drug (≥Day 28)

,,,,,
InterventionParticipants (Number)
AEsSerious AEs
Part 1 (Cohort B): 300 mg LY248459540
Part 1 (Cohort C): 600 mg LY248459520
Part 1 (Cohort D): 1200 mg LY248459560
Part 1 (Cohorts A Through D): Placebo70
Part 1, Period 1 (Cohort A): 100 mg LY248459520
Part 1, Period 2 (Cohort A): 1800 mg LY2484595110

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Pharmacokinetics: Time of Maximum Observed Plasma Concentration (Tmax) of LY2484595

The median times to maximum observed plasma concentration (Tmax) of LY2484595 following administration of LY2484595 alone and with ketoconazole are reported. (NCT01448824)
Timeframe: Part 2, Period 1, Day 1 through Day 8: Predose, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168 Hours Post Dose; Period 2, Day 5 through Day 15: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240 Hours Post Dose

InterventionHours (h) (Median)
Part 2, Period 1: 100 mg LY24845953.00
Part 2, Period 2: 100 mg LY2484595 + 400 mg Ketoconazole3.00

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Pharmacokinetics: Maximum Observed Plasma Concentration (Cmax) of LY2484595

The geometric least squares (LS) means for the maximum observed plasma concentration (Cmax) of LY2484595 following administration of LY2484595 alone and with ketoconazole are reported. Least squares means were calculated from an analysis of variance (ANOVA) model with a fixed effect for treatment and a random effect for participant. The LS means for each treatment and the 90% confidence intervals (CI) for the difference in means were back transformed from the log scale to provide estimates of the geometric means and 90% CIs for the ratio of the geometric means (LY2484595 coadministered with ketoconazole and LY2484595 alone). (NCT01448824)
Timeframe: Part 2, Period 1, Day 1 through Day 8: Predose, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168 Hours Post Dose; Period 2, Day 5 through Day 15: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240 Hours Post Dose

InterventionNanograms per milliliter (ng/mL) (Least Squares Mean)
Part 2, Period 1: 100 mg LY2484595331.83
Part 2, Period 2: 100 mg LY2484595 + 400 mg Ketoconazole643.99

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Pharmacokinetics: Area Under the Plasma Concentration Versus Time Curve (AUC) of LY2484595

Area under the concentration-time curve from time zero to infinity is presented. (NCT01450098)
Timeframe: Predose and 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, and 168 hours postdose

Interventionhours times nanograms per milliliter (Geometric Mean)
LY2484595 200 mg SDSD-PG Fasted12200
LY2484595 200 mg SDSD-PG Low Fat17800
LY2484595 200 mg SDSD-PG High Fat17800

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Pharmacokinetics: Peak Plasma Concentration (Cmax) of LY2484595

(NCT01450098)
Timeframe: Predose and 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, and 168 hours postdose

Interventionnanograms per milliliter (Geometric Mean)
LY2484595 200 mg SDSD-PG Fasted828
LY2484595 200 mg SDSD-PG Low Fat1510
LY2484595 200 mg SDSD-PG High Fat1280

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Pharmacokinetics: Maximum Drug Concentration (Cmax) of LY2484595 During One Dosing Interval at Steady State

(NCT01537887)
Timeframe: Predose, 1, 2, 3, 4, 6, 12, 24, 72, and 168 Hours Postdose

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
LY24845955270

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Pharmacokinetics: Area Under the Concentration Curve (AUC) of LY2484595 During One Dosing Interval at Steady State

(NCT01537887)
Timeframe: Predose, 1, 2, 3, 4, 6, 12, 24, 72, and 168 Hours Postdose

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
LY248459548300

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Percentage Change From Baseline to Day 11 in Fasting Lipids and Apolipoproteins

(NCT01537887)
Timeframe: Baseline, Day 11

,
Interventionpercentage change (Mean)
High-density lipoprotein cholesterol (HDL-C)Low-density lipoprotein cholesterol (LDL-C)Apo-A1Apo-B
LY2484595112-3532-24
Placebo-89-98

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Change From Baseline to Day 10 in QT Interval Corrected for Heart Rate (QTc) for LY2484595 Versus Placebo

Data were collected using a 12-lead electrocardiogram (ECG). The QT interval is the time between the start of the Q wave and the end of the T wave in the cardiac electrical cycle and corrected for heart rate. Population-corrected QT interval (QTcP) formula: QTcP = QT / RR^ß, where ß is the population correction factor. (NCT01537887)
Timeframe: Predose of Day 1, Day 10

,
Interventionmilliseconds (msec) (Mean)
4-hour postdose on Day 106-hour postdose on Day 10
LY2484595-4.6-1.1
Placebo-2.7-2.0

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Number of Participants With Composite Endpoint of All-Cause Mortality, MI, Stroke, Coronary Revascularization, or Hospitalization for UA

For component endpoints, the number of participants includes those experiencing fatal events and account for all occurrences regardless of whether or not another component event occurred previously. (NCT01687998)
Timeframe: Baseline through End of Study (Up to 4 years)

InterventionParticipants (Count of Participants)
Evacetrapib857
Placebo867

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Number of Participants With Composite Endpoint of CV Death, MI, or Coronary Revascularization

For component endpoints, the number of participants includes those experiencing fatal events and account for all occurrences regardless of whether or not another component event occurred previously. (NCT01687998)
Timeframe: Baseline through End of Study (Up to 4 years)

InterventionParticipants (Count of Participants)
Evacetrapib690
Placebo691

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Number of Participants With Composite Endpoint of CV Death, MI, Stroke, or Hospitalization for UA

For component endpoints, the number of participants includes those experiencing fatal events and account for all occurrences regardless of whether or not another component event occurred previously. (NCT01687998)
Timeframe: Baseline through End of Study (Up to 4 years)

InterventionParticipants (Count of Participants)
Evacetrapib571
Placebo570

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Number of Participants With Composite Primary Endpoint of Cardiovascular (CV) Death, Myocardial Infarction (MI), Stroke, Coronary Revascularization, or Hospitalization for Unstable Angina (UA)

For component endpoints, the number of participants includes those experiencing fatal events and account for all occurrences regardless of whether or not another component event occurred previously. (NCT01687998)
Timeframe: Baseline to Study Completion (Up to 4 years)

InterventionParticipants (Count of Participants)
Evacetrapib779
Placebo776

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Number of Participants With Triple Composite Endpoint of CV Death, MI, or Stroke

For component endpoints, the number of participants includes those experiencing fatal events and account for all occurrences regardless of whether or not another component event occurred previously. (NCT01687998)
Timeframe: Baseline through End of Study (Up to 4 years)

InterventionParticipants (Count of Participants)
Evacetrapib437
Placebo453

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Mean Percent Change From Baseline to 3 Months in Low-Density (LDL-C) and High-Density Lipoprotein Cholesterol (HDL-C) Levels

(NCT01687998)
Timeframe: Baseline, 3 Months

,
Interventionpercent (Mean)
LDL-CHDL-C
Evacetrapib-31.12133.18
Placebo5.991.63

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Pharmacokinetics (PK): Area Under the Concentration Curve Over a 12 Hour Dosing Interval (AUCτ) of Gemfibrozil

Venous blood samples were taken on Day 1 for PK parameter estimates of gemfibrozil alone and on Day 13 for PK parameter estimates of gemfibrozil when coadministered with evacetrapib. (NCT01736254)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose on Day 1 and Day 13

Interventionng*h/mL (Geometric Mean)
Gemfibrozil55700
Evacetrapib + Gemfibrozil53800

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Pharmacokinetics (PK): Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Evacetrapib

Venous blood samples were taken on Day 11 for PK parameter estimates of evacetrapib alone and on Day 22 for PK parameter estimates of evacetrapib when coadministered with gemfibrozil. (NCT01736254)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours postdose on Day 11 and Day 22

Interventionnanograms*hours/milliliter (ng*h/mL) (Geometric Mean)
Evacetrapib11300
Evacetrapib + Gemfibrozil11400

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib

Venous blood samples were taken on Day 11 for PK parameter estimates of evacetrapib alone and on Day 22 for PK parameter estimates of evacetrapib when coadministered with gemfibrozil. (NCT01736254)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours postdose on Day 11 and Day 22

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
Evacetrapib1270
Evacetrapib + Gemfibrozil1290

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Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Gemfibrozil

Venous blood samples were taken on Day 1 for PK parameter estimates of gemfibrozil alone and on Day 13 for PK parameter estimates of gemfibrozil when coadministered with evacetrapib. (NCT01736254)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose on Day 1 and Day 13

Interventionng/mL (Geometric Mean)
Gemfibrozil17400
Evacetrapib + Gemfibrozil16800

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Pharmacokinetics (PK): Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib

Venous blood samples were taken on Day 11 for PK parameter estimates of evacetrapib alone and on Day 22 for PK parameter estimates of evacetrapib when coadministered with gemfibrozil. (NCT01736254)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours postdose on Day 11 and Day 22

Interventionhours (Median)
Evacetrapib4.00
Evacetrapib + Gemfibrozil3.00

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Pharmacokinetics (PK): Time of Maximum Observed Drug Concentration (Tmax) of Gemfibrozil

Venous blood samples were taken on Day 1 for PK parameter estimates of gemfibrozil alone and on Day 13 for PK parameter estimates of gemfibrozil when coadministered with evacetrapib. (NCT01736254)
Timeframe: Predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose on Day 1 and Day 13

Interventionhours (Median)
Gemfibrozil1.00
Evacetrapib + Gemfibrozil1.08

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Ethinyl Estradiol

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionhour (Median)
Ortho-Cyclen3.00
Ortho-Cyclen + Evacetrapib4.00

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Norelgestromin

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionhour (Median)
Ortho-Cyclen3.53
Ortho-Cyclen + Evacetrapib4.00

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Ethinyl Estradiol

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpicogram per milliliter (pg/ml) (Geometric Mean)
Ortho-Cyclen71.7
Ortho-Cyclen + Evacetrapib70.6

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PK: Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Ethinyl Estradiol

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpicogram x hour per ml (pg*hour/ml) (Geometric Mean)
Ortho-Cyclen907
Ortho-Cyclen + Evacetrapib840

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PK: Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Norelgestromin

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpg*hour/ml (Geometric Mean)
Ortho-Cyclen16200
Ortho-Cyclen + Evacetrapib18100

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PK: Maximum Concentration (Cmax) of Norelgestromin

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpg/ml (Geometric Mean)
Ortho-Cyclen1410
Ortho-Cyclen + Evacetrapib1830

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PK: Minimum Observed Drug Concentration (Cmin) of Ethinyl Estradiol

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpg/ml (Geometric Mean)
Ortho-Cyclen15.9
Ortho-Cyclen + Evacetrapib13.2

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PK: Minimum Observed Drug Concentration (Cmin) of Norelgestromin

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpg/ml (Geometric Mean)
Ortho-Cyclen397
Ortho-Cyclen + Evacetrapib422

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PK: Area Under Concentration Versus Time Curve Over the 24-hour Dosing Interval (AUCτ) of Evacetrapib

(NCT01810432)
Timeframe: Day 10 Periods 1 and 2: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 hours post-dose

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
Evacetrapib (Fasted)9930
Evacetrapib (Fed)14400

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib

(NCT01810432)
Timeframe: Day 10 Periods 1 and 2: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 hours post-dose

Interventionhours (h) (Median)
Evacetrapib (Fasted)3.00
Evacetrapib (Fed)3.00

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib

(NCT01810432)
Timeframe: Day 10 Periods 1 and 2: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 hours post-dose

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
Evacetrapib (Fasted)1140
Evacetrapib (Fed)1720

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Pharmacodynamics (PD): Area Under the International Normalized Ratio Curve (AUCINR) of Warfarin

The INR is a standardized ratio of the prothrombin time (PT), time it takes for blood to clot. AUCINR is the time curve used to measure change in INR over time. (NCT01825876)
Timeframe: Days 1 and 17: 0, 6, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionratio*h (Geometric Mean)
15 mg Warfarin167
130 mg Evacetrapib + 15 mg Warfarin162

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PK: Maximum Observed Concentration (Cmax) of S-Warfarin

(NCT01825876)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
15 mg Warfarin4.69
130 mg Evacetrapib + 15 mg Warfarin4.72

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PK: Cmax of R-Warfarin

(NCT01825876)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionng/mL (Geometric Mean)
15 mg Warfarin6.02
130 mg Evacetrapib + 15 mg Warfarin6.22

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PK: AUC0-∞ of R-Warfarin

(NCT01825876)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionng*h/mL (Geometric Mean)
15 mg Warfarin321
130 mg Evacetrapib + 15 mg Warfarin314

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-∞) of S-Warfarin

(NCT01825876)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
Warfarin132
Evacetrapib + Warfarin126

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PD: Maximum Observed INR Response (INRmax) of Warfarin

The INR is a standardized ratio of the PT, time it takes for blood to clot. (NCT01825876)
Timeframe: 0, 6, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose on Days 1 and 17

Interventionratio (Geometric Mean)
15 mg Warfarin1.36
130 mg Evacetrapib + 15 mg Warfarin1.25

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Pharmacokinetics (PK): Observed Maximum Concentration (Cmax) of Evacetrapib

(NCT01825889)
Timeframe: Predose and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours postdose

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
Evacetrapib (Participants With Renal Impairment)969
Evacetrapib (Healthy Participants)1140

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Pharmacokinetics (PK): Area Under The Concentration Versus Time Curve From Time Zero To Time Tlast, Where Tlast is the Last Time Point With a Measurable Concentration (AUC[0-Tlast]) of Evacetrapib

(NCT01825889)
Timeframe: Predose and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours postdose

Interventionnanograms*hours/milliliter (ng*h/mL) (Geometric Mean)
Evacetrapib (Participants With Renal Impairment)15200
Evacetrapib (Healthy Participants)16000

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Pharmacokinetics (PK): Area Under the Concentration Time Curve From Time Zero to Infinity (AUC[0-∞]) of Evacetrapib

(NCT01825889)
Timeframe: Predose and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours postdose

Interventionng*h/mL (Geometric Mean)
Evacetrapib (Participants With Renal Impairment)15500
Evacetrapib (Healthy Participants)16300

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib

(NCT01836185)
Timeframe: Predose on Day 1, and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours after the Day 1 dose

Interventionh (Mean)
Evacetrapib (Healthy)3
Evacetrapib (Hepatic, Mild)3
Evacetrapib (Hepatic, Moderate)3
Evacetrapib (Hepatic, Severe)3

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PK: Maximum Observed Concentration (Cmax) of Evacetrapib

(NCT01836185)
Timeframe: Predose on Day 1, and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours after the Day 1 dose

Interventionng/mL (Geometric Mean)
Evacetrapib (Healthy)605
Evacetrapib (Hepatic, Mild)609
Evacetrapib (Hepatic, Moderate)591
Evacetrapib (Hepatic, Severe)478

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Time Tlast (AUC0-tlast) of Evacetrapib

tlast is defined as the last time point with a measurable concentration of Evacetrapib. (NCT01836185)
Timeframe: Predose on Day 1, and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, 264, 312, and 336 hours after the Day 1 dose

Interventionnanograms*hour per milliliter (ng*h/mL) (Geometric Mean)
Evacetrapib (Healthy)10700
Evacetrapib (Hepatic, Mild)10500
Evacetrapib (Hepatic, Moderate)13200
Evacetrapib (Hepatic, Severe)15800

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Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Digoxin

(NCT01897493)
Timeframe: Periods 1 and 2: digoxin predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, and 96 hours after administration of digoxin

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
Period 1-Digoxin1.75
Period 2-Evacetrapib + Digoxin2.15

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PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-∞) of Digoxin

(NCT01897493)
Timeframe: Periods 1 and 2: digoxin predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, and 96 hours after administration of digoxin

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
Period 1-Digoxin31.3
Period 2-Evacetrapib + Digoxin33.5

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Digoxin

(NCT01897493)
Timeframe: Periods 1 and 2: digoxin predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, and 96 hours after administration of digoxin

Interventionhours (Median)
Period 1-Digoxin2.00
Period 2-Evacetrapib + Digoxin2.00

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Renal Clearance (CLr) of Digoxin

CLr was defined as the volume of serum cleared of digoxin per unit of time after a single dose of digoxin. (NCT01897493)
Timeframe: Periods 1 and 2: digoxin predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, and 96 hours after administration of digoxin

Interventionliters/hour (L/h) (Geometric Mean)
Period 1-Digoxin9.43
Period 2-Evacetrapib + Digoxin8.10

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib (LY2484595)

Evacetrapib exposure in terms of Area Under the Concentration Versus Time Curve from time 0 extrapolated to infinity (AUC[0-∞]) is summarized for each solid fraction control (Reference and Test). (NCT01903434)
Timeframe: Predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose in each period

Interventionnanograms times hours per milliliter (Geometric Mean)
Reference10400
Test10300

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib (LY2484595)

The maximum observed drug concentration (Cmax) of evacetrapib is summarized for each solid fraction control (Reference and Test). (NCT01903434)
Timeframe: Predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose in each period

Interventionnanograms per milliliter (Geometric Mean)
Reference604
Test597

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib

(NCT01908582)
Timeframe: Day 1 and Day 16, predose of evacetrapib and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Evacetrapib599
Evacetrapib + Rifampin269

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Pharmacokinetics (PK): Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib

(NCT01908582)
Timeframe: Day 1 and Day 16, predose of evacetrapib and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Interventionhours (Median)
Evacetrapib2.00
Evacetrapib + Rifampin2.00

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Pharmacokinetics, Area Under the Plasma Concentration-Time Curve From Time 0 Hour (h) to Infinity (AUC0-∞) of Evacetrapib

(NCT01908582)
Timeframe: Day 1 and Day 16, predose of evacetrapib and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Interventionnanograms * hours per milliliter (Geometric Mean)
Evacetrapib9810
Evacetrapib + Rifampin2070

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Pravastatin

(NCT01958489)
Timeframe: Day 1 and Day 11: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 10, 12 and 24 hours postdose

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
Pravastatin (Period 1)142
Evacetrapib + Pravastatin (Period 2)128

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PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity [AUC(0-∞)] of Pravastatin

(NCT01958489)
Timeframe: Day 1 and Day 11: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 10, 12 and 24 hours postdose

Interventionnanograms*hours/milliliters (ng*h/mL) (Geometric Mean)
Pravastatin (Period 1)257
Evacetrapib + Pravastatin (Period 2)229

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PK: Time of Maximum Observed Concentration (Tmax) of Pravastatin

(NCT01958489)
Timeframe: Day 1 and Day 11: Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 7, 8, 10, 12 and 24 hours postdose

Interventionhours (Median)
Pravastatin (Period 1)1.00
Evacetrapib + Pravastatin (Period 2)0.75

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PK: Cmax of Evacetrapib Alone and With Simvastatin or Atorvastatin

Pharmacokinetic parameter estimates of evacetrapib following 130 mg evacetrapib daily alone or with 40 mg simvastatin or 20 mg atorvastatin daily. (NCT02156492)
Timeframe: Part 2: Day 14 and 22 Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 hours Postdose.

,
Interventionng/mL (Geometric Mean)
Days 5-14Days 15- 22
Evacetrapib Daily and Simvastatin11801020
Evactrapib Daily and Atorvastatin11201000

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PK: AUC of Evacetrapib Alone and With Simvastatin or Atorvastatin

Pharmacokinetic parameter estimates of evacetrapib following 130 mg evacetrapib daily alone or with 40 mg simvastatin or 20 mg atorvastatin daily AUC (0-24). (NCT02156492)
Timeframe: Part 2: Day 14 and 22 Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 hours Postdose

,
Interventionng*h/mL (Geometric Mean)
Days 5-14Days 15-22
Evacetrapib Daily and Atorvastatin106009480
Evacetrapib Daily and Simvastatin107009640

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Pharmacokinetics (PK): Area Under Curve (AUC 0-inf) of Evacetrapib

Pharmacokinetic (PK) parameter estimates from evacetrapib concentrations following single dose and daily dose of 130 mg evacetrapib. (NCT02156492)
Timeframe: Part 1: Day 1 Predose 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 144, and 168 hours Postdose; Part 2 Day 14 Predose 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24 hours Postdose

Interventionnanogram * hour per milliliter (ng*h/mL) (Geometric Mean)
Day 1Day 14
Evacetrapib Single and Multiple Dose770023600

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Effect of Evacetrapib Single and Multiple Doses on High Density Lipoprotein Cholesterol (HDL-C), Low Density Lipoprotein Cholesterol (LDL-C), and Triglycerides (TG)

(NCT02156492)
Timeframe: Single Dose Day 2 and Multiple Dose Day 22

,
Interventionmillimoles per liter (mmol/L) (Mean)
HDL-CLDL-CTG
Evacetrapib Multiple Dose Day 222.6761.2411.221
Evacetrapib Single Dose Day 21.6412.2890.984

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PK: Tmax of Evacetrapib Alone and With Simvastatin or Atorvastatin

Pharmacokinetic parameter estimates of Tmax of evacetrapib following 130 mg daily dose alone or with 40 mg Simvastatin or 20 mg Atorvastatin. Tmax of simvastatin and atorvastatin. (NCT02156492)
Timeframe: Part 2: Predose on Day 14 and 22 and at 0.5, 1, 2, 3, 4, 6, 8, 12, and 24 hours postdose.

,
Interventionh (Median)
Days 5-14Days 15- 22
Evacetrapib Daily and Atrovastatin3.003.00
Evacetrapib Daily and Simvastatin3.003.00

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PK: Maximum Concentration (Cmax) of Evacetrapib

Pharmacokinetic parameter estimates from evacetrapib following single dose and daily doses of 130 mg. (NCT02156492)
Timeframe: Part 1: Day 1 and Day 14 Predose 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 144, and 168 hours Postdose; Part 2 Day 14: Predose 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours Postdose

Interventionng/mL (Geometric Mean)
Single Dose Day 1Multiple Dose Day 14
Evacetrapib Single and Multiple Dose418954

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PK: Time to Maximum Concentration (Tmax) of Evacetrapib

Pharmacokinetic parameter estimates of evacetrapib following single and daily doses of 130 mg evacetrapib. (NCT02156492)
Timeframe: Part 1: Day 1 Predose on Day 1 or Day 14 and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 144, and 168 hours postdose. Part 2: Predose on Day 14 at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose.

Interventionhours (h) (Median)
Single Dose Day 1Daily Dose Day 14
Evacetrapib Single and Multiple Dose3.003.00

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PK: Maximum Observed Concentration (Cmax) of S-warfarin

(NCT02161731)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Warfarin4.20
Evacetrapib + Warfarin4.34

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PK: Cmax of R-warfarin

(NCT02161731)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionng/mL (Geometric Mean)
Warfarin5.03
Evacetrapib + Warfarin5.27

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PK: AUC[0-∞] of R-warfarin

(NCT02161731)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionng*h/mL (Geometric Mean)
Warfarin287
Evacetrapib + Warfarin271

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of S-Warfarin

(NCT02161731)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionnanogram*hour/milliliter (ng*h/mL) (Geometric Mean)
Warfarin128
Evacetrapib + Warfarin114

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Pharmacodynamics (PD): Area Under the International Normalized Ratio Curve (AUC[INR]) of Warfarin

The INR is a standardized ratio of the prothrombin time (PT), time it takes for blood to clot. AUC[INR] is the time curve used to measure change in INR over time. (NCT02161731)
Timeframe: Days 1 and 17: 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionratio times hour (ratio*h) (Geometric Mean)
Warfarin174
Evacetrapib + Warfarin165

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PD: Maximum Observed International Normalized Ratio Response (INRmax) of Warfarin

(NCT02161731)
Timeframe: Days 1 and 17: 0, 6, 12, 24, 36, 48, 72, 96, 120, and 144 hours following warfarin dose

Interventionratio (Geometric Mean)
Warfarin1.47
Evacetrapib + Warfarin1.34

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PD Parameters of Evacetrapib: Triglyceride Level

(NCT02168803)
Timeframe: Day -1, Day 8

,,
Interventionmmol (Mean)
Single-Dose Phase Day -1Single-Dose Phase Day 8
Evacetrapib: Multiple Dose 12 Weeks1.4741.482
Evacetrapib: Multiple Dose 24 Weeks1.3111.309
Evacetrapib: Multiple Dose 52 Weeks1.4851.419

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PD Parameters of Evacetrapib: Total Cholesterol Level

(NCT02168803)
Timeframe: Day -1, Day 8

,,
Interventionmmol (Mean)
Single-Dose Phase Day -1Single-Dose Phase Day 8
Evacetrapib: Multiple Dose 12 Weeks5.9225.577
Evacetrapib: Multiple Dose 24 Weeks5.5235.531
Evacetrapib: Multiple Dose 52 Weeks6.0155.715

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PD Parameters of Evacetrapib: Low-Density Lipoprotein Cholesterol (LDL-C) Level

(NCT02168803)
Timeframe: Day -1, Day 8

,,
Interventionmmol/L (Mean)
Single-Dose Phase Day -1Single-Dose Phase Day 8
Evacetrapib: Multiple Dose 12 Weeks3.7113.173
Evacetrapib: Multiple Dose 24 Weeks3.3593.152
Evacetrapib: Multiple Dose 52 Weeks3.6623.293

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PD Parameters of Evacetrapib: High Density Lipoprotein Cholesterol (HDL-C) Level

(NCT02168803)
Timeframe: Day -1, Day 8

,,
Interventionmillimole/Liter (mmol/L) (Mean)
Single-Dose Phase Day -1Single-dose Phase Day 8
Evacetrapib: Multiple Dose 12 Weeks1.5381.724
Evacetrapib: Multiple Dose 24 Weeks1.5621.777
Evacetrapib: Multiple Dose 52 Weeks1.6701.772

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PK Parameters of Evacetrapib: Terminal Half-life

(NCT02168803)
Timeframe: Single-Dose: 1,2,3,4,6,8,12,24,36,48,72,120,168 Hours Postdose; Multiple Dose: Predose, 1,2,3,4,6,8,12,24,36,48,72,120,168 hours; 10,13,17,20,24,29,36,43,50,57, and 71 Days Post Dose

InterventionDays (Number)
Evacetrapib: Single, Multiple Dose 12, 24, and 52 Weeks52.5

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PK Parameters of Evacetrapib: Maximum Concentration (Cmax)

(NCT02168803)
Timeframe: Single-Dose: 1,2,3,4,6,8,12,24,36,48,72,120,168 Hours Postdose; Multiple Dose: Predose, 1,2,3,4,6,8,12,24,36,48,72,120,168 hours; 10,13,17,20,24,29,36,43,50,57, and 71 Days Post Dose

Interventionnanogram/milliliter (ng/mL) (Geometric Mean)
Evacetrapib: Single Dose, All Participants1020
Evacetrapib: Multiple Dose 12 Weeks1690
Evacetrapib: Multiple Dose 24 Weeks1770
Evacetrapib: Multiple Dose 52 Weeks1850

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Pharmacokinetics (PK) Parameters of Evacetrapib: Area Under the Concentration Versus Time Curve From Time Zero to the Last Time Point With a Measurable Concentration (AUC[0-tlast])

(NCT02168803)
Timeframe: Single-Dose: 1,2,3,4,6,8,12,24,36,48,72,120,168 Hours Postdose; Multiple Dose: Predose, 1,2,3,4,6,8,12,24,36,48,72,120,168 hours; 10,13,17,20,24,29,36,43,50,57, and 71 Days Post Dose

Interventionnanogram∙hour/mililliter (ng∙h/mL) (Geometric Mean)
Evacetrapib: Single Dose, All Participants14200
Evacetrapib: Multiple Dose 12 Weeks37400
Evacetrapib: Multiple Dose 24 Weeks36900
Evacetrapib: Multiple Dose 52 Weeks44400

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Pharmacokinetics (PK): Area Under the Concentration Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib (Fasted)

(NCT02226653)
Timeframe: Pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 Hours Post-dose in Periods 1,2,3, and 4

Interventionnanogram·hour/milliliter (ng·h/mL) (Geometric Mean)
Reference (Fasted)14600
Test (Fasted)14600

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PK: AUC(0-∞)of Evacetrapib (Fasted and Fed)

(NCT02226653)
Timeframe: Pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 Hours Post-dose in Periods 2,4, and 5

Interventionng·h/mL (Geometric Mean)
Reference (Fasted)14800
Reference (Fed)18900
Test (Fasted)14600
Test (Fed)18600

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PK: Cmax of Evacetrapib (Fasted and Fed)

(NCT02226653)
Timeframe: Pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 Hours Post-dose in Periods 2,4, and 5

Interventionng/ml (Geometric Mean)
Reference (Fasted)1100
Reference (Fed)1450
Test (Fasted)1090
Test (Fed)1480

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PK: Maximum Concentration (Cmax) of Evacetrapib (Fasted)

(NCT02226653)
Timeframe: Pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 Hours Post-dose in Periods 1,2,3, and 4

Interventionnanogram/milliliter (ng/ml) (Geometric Mean)
Reference (Fasted)1130
Test (Fasted)1100

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib (Fasted and Fed)

(NCT02226653)
Timeframe: Pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168 Hours Post-dose in Periods 2,4, and 5

Interventionhour (h) (Median)
Reference (Fasted)3.75
Reference (Fed)2.50
Test (Fasted)3.50
Test (Fed)2.75

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Percent Change From Baseline to 3 Months in Apolipoprotein B (apoB)

Change in apoB levels from baseline to the 3-month visit expressed as a percentage of the baseline levels. Statistics are from analysis of covariance with log baseline measurement and treatment is included in the model. LS means and median differences were analyzed in log units and converted to standard units. Log Percent change from baseline response is the dependent variable. (NCT02227784)
Timeframe: Baseline, 3 Months

Interventionpercent (Median)
Atorvastatin + Evacetrapib-22.96
Atorvastatin 40 mg0.21
Atorvastatin 80 mg-6.54
Atorvastatin + Ezetimibe-18.84

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Percent Change From Baseline to 3 Months in Cholesterol Efflux Capacity

Change in cholesterol efflux capacity from baseline to the 3-month visit expressed as a percentage of the baseline levels. Statistics are from analysis of covariance with log baseline measurement and treatment is included in the model. LS means and median differences were analyzed in log units and converted to standard units. Log Percent change from baseline response is the dependent variable. (NCT02227784)
Timeframe: Baseline, 3 Months

Interventionpercent (Median)
Atorvastatin + Evacetrapib35.09
Atorvastatin 40 mg-2.96
Atorvastatin + Ezetimibe-7.03
Atorvastatin 80 mg-4.55

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Percent Change From Baseline to 3 Months in High-Density Lipoprotein Cholesterol (HDL-C)

Change in HDL-C levels from baseline to the 3-month visit expressed as a percentage of the baseline levels. LS medians and median differences were analyzed in log units and converted to standard units. Statistics are from mixed model repeated measures analysis with log baseline measurement, treatment, visit, and treatment by visit interaction included in the model. Log percent change from baseline response is the dependent variable. Within-participant repeated measures at multiple visits are modeled by a compound symmetry covariance structure. (NCT02227784)
Timeframe: Baseline, 3 Months

Interventionpercent (Median)
Atorvastatin + Evacetrapib125.39
Atorvastatin 40 mg0.11
Atorvastatin 80 mg-6.10
Atorvastatin + Ezetimibe-2.18

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Percent Change From Baseline to 3 Months in Lipoprotein(a) (Lp[a])

Change in Lp(a) levels from baseline to the 3-month visit expressed as a percentage of the baseline levels. Statistics are from analysis of covariance with log baseline measurement and treatment is included in the model. LS means and median differences were analyzed in log units and converted to standard units. Log Percent change from baseline response is the dependent variable. (NCT02227784)
Timeframe: Baseline, 3 Months

Interventionpercent (Median)
Atorvastatin + Evacetrapib-28.73
Atorvastatin 40 mg4.45
Atorvastatin 80 mg3.90
Atorvastatin + Ezetimibe13.42

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Percent Change From Baseline to 3 Months in Low-Density Lipoprotein Cholesterol (LDL-C)

Change in LDL-C levels from baseline to the 3-month visit expressed as a percentage of the baseline levels. LDL-C was measured by beta quantification. Statistics are from analysis of covariance with log baseline measurement and treatment is included in the model. Least Square Means (LS means) and median differences were analyzed in log units and converted to standard units. Log Percent change from baseline response is the dependent variable. (NCT02227784)
Timeframe: Baseline, 3 Months

Interventionpercent (Median)
Atorvastatin + Evacetrapib-33.44
Atorvastatin 40 mg0.04
Atorvastatin 80 mg-6.19
Atorvastatin + Ezetimibe-27.30

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Percent Change From Baseline to 3 Months in Non-HDL-C

Change in Non-HDL-C levels from baseline to the 3-month visit expressed as a percentage of the baseline levels. LS medians and median differences were analyzed in log units and converted to standard units. Statistics are from mixed model repeated measures analysis with log baseline measurement, treatment, visit, and treatment by visit interaction included in the model. Log percent change from baseline response is the dependent variable. Within-participant repeated measures at multiple visits are modeled by a compound symmetry covariance structure. (NCT02227784)
Timeframe: Baseline, 3 Months

Interventionpercent (Median)
Atorvastatin + Evacetrapib-31.42
Atorvastatin 40 mg-4.95
Atorvastatin 80 mg-9.40
Atorvastatin + Ezetimibe-24.37

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Percent Change From Baseline to 3 Months in Apolipoprotein AI (apoAI)

Change in apoAI levels from baseline to the 3-month visit expressed as a percentage of the baseline levels. Statistics are from analysis of covariance with log baseline measurement and treatment is included in the model. LS means and median differences were analyzed in log units and converted to standard units. Log Percent change from baseline response is the dependent variable. (NCT02227784)
Timeframe: Baseline, 3 Months

Interventionpercent (Median)
Atorvastatin + Evacetrapib46.08
Atorvastatin 40 mg-0.27
Atorvastatin 80 mg-6.14
Atorvastatin + Ezetimibe-2.36

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Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C)

LS mean using MMRM adjusted for baseline, treatment, visit , and treatment*visit, where the participant is a random effect. (NCT02260635)
Timeframe: Baseline, Week 12

Interventionpercent change of HDL-C (Least Squares Mean)
Evacetrapib123.57
Placebo-0.45

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Percent Change From Baseline in LDL-C (Direct)

LS mean using MMRM adjusted for baseline, treatment, visit , and treatment*visit, where the participant is a random effect. (NCT02260635)
Timeframe: Baseline, Week 12

Interventionpercent change of LDL-C direct (Least Squares Mean)
Evacetrapib-33.86
Placebo0.22

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Percent Change From Baseline in Non HDL-C

LS mean using MMRM adjusted for baseline, treatment, visit , and treatment*visit, where the participant is a random effect. (NCT02260635)
Timeframe: Baseline, Week 12

Interventionpercent change in non HDL-C (Least Squares Mean)
Evacetrapib-26.48
Placebo-0.03

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Percent Change From Baseline to Week 12 in Low-Density Lipoprotein Cholesterol (LDL-C) Measured by Beta Quantification

Least Square Mean (LS mean) using mixed model repeated measures (MMRM) adjusted for baseline, treatment, visit , and treatment*visit, where the participant is a random effect. (NCT02260635)
Timeframe: Baseline, Week 12

Interventionpercent change in LDL-C (Least Squares Mean)
Evacetrapib-34.27
Placebo0.00

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Percent Change From Baseline in Apolipoprotein A-I

LS Mean from ANCOVA model adjusted for baseline and treatment. (NCT02260635)
Timeframe: Baseline, Week 12, Week 52

,
Interventionpercent change in Apolipoprotein A-I (Least Squares Mean)
Week 12Week 52
Evacetrapib49.1NA
Placebo-2.5NA

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Percent Change From Baseline in Apolipoprotein B

LS Mean from ANCOVA model adjusted for baseline and treatment. (NCT02260635)
Timeframe: Baseline, Week 12, Week 52

,
Interventionpercent change in Apolipoprotein B (Least Squares Mean)
Week 12Week 52
Evacetrapib-29.0NA
Placebo-1.3NA

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Percent Change From Baseline in Lipoprotein-a

LS Mean from analysis of covariance (ANCOVA) model adjusted for baseline and treatment. (NCT02260635)
Timeframe: Baseline, Week 12, Week 52

,
Interventionpercent change in Lipoprotein-a (Least Squares Mean)
Week 12Week 52
Evacetrapib-35.71NA
Placebo3.54NA

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Percent Change From Baseline to Week 12 in Apolipoprotein B

The ANCOVA model using last observation carried forward (LOCF) was applied to analyze percent changes from baseline. (NCT02260648)
Timeframe: Baseline, Week 12

Interventionpercent change in Apolipoprotien B (Least Squares Mean)
Evacetrapib-20.4
Placebo-3.0
Ezetimibe-20.4

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Percent Change From Baseline to Week 12 in Non HDL-C

The MMRM was used for the LS Mean estimates at Week 12 for Non HDL-C adjusting for baseline as response variables, baseline measurement as a covariate, treatment, visit, and treatment-by-visit interaction as fixed effects, and participant as a random effect. (NCT02260648)
Timeframe: Baseline, Week 12

Interventionpercent change in non HDL-C (Least Squares Mean)
Evacetrapib-22.01
Placebo-6.42
Ezetimibe-27.35

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Percent Change From Baseline to Week 12 in Low-Density Lipoprotein Cholesterol (LDL-C) Measured by Beta Quantification

The mixed-effects model for repeated measures (MMRM) was used for the Least Squares Mean (LS Mean) estimates at Week 12 for LDL-C adjusting for baseline as response variables, baseline measurement as a covariate, treatment, Visit (4,5,6, or 7), and treatment-by-visit interaction as fixed effects, and participant as a random effect. (NCT02260648)
Timeframe: Baseline, Week 12

Interventionpercent change in LDL-C (Least Squares Mean)
Evacetrapib-26.37
Placebo-3.75
Ezetimibe-27.31

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Percent Change From Baseline to Week 12 in Lipoprotein-a

The analysis of covariance (ANCOVA) model using last observation carried forward (LOCF) was applied to analyze percent changes from baseline. (NCT02260648)
Timeframe: Baseline, Week 12

Interventionpercent change in Lipoprotein-a (Least Squares Mean)
Evacetrapib-33.17
Placebo7.78
Ezetimibe0.68

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Percent Change From Baseline to Week 12 in LDL-C (Direct)

The MMRM was used for the LS Mean estimates at Week 12 for LDL-C (direct) adjusting for baseline as response variables, baseline measurement as a covariate, treatment, visit, and treatment-by-visit interaction as fixed effects, and participant as a random effect. (NCT02260648)
Timeframe: Baseline, Week 12

Interventionpercent change in LDL-C (Direct) (Least Squares Mean)
Evacetrapib-27.17
Placebo-3.40
Ezetimibe-28.96

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Percent Change From Baseline to Week 12 in High-Density Lipoprotein Cholesterol (HDL-C)

The MMRM was used for the LS Mean estimates at Week 12 for HDL-C adjusting for baseline as response variables, baseline measurement as a covariate, treatment, visit, and treatment-by-visit interaction as fixed effects, and participant as a random effect, and treatment-by-visit interaction as fixed effects, and participant as a random effect. (NCT02260648)
Timeframe: Baseline, Week 12

Interventionpercent change in HDL-C (Least Squares Mean)
Evacetrapib108.96
Placebo-0.90
Ezetimibe-3.12

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Percent Change From Baseline to Week 12 in Apolipoprotein A-I

The ANCOVA model using last observation carried forward (LOCF) was applied to analyze percent changes from baseline. (NCT02260648)
Timeframe: Baseline, Week 12

Interventionpercent change in Apolipoprotein A-I (Least Squares Mean)
Evacetrapib42.8
Placebo0.6
Ezetimibe-0.6

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Pharmacokinetics (PK): Dose Normalized Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib

(NCT02271425)
Timeframe: Day 1:Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.25, 4.5, 5, 5.5, 6, 6.5, 8, 10, 12, Day 2; 24, 36 Day 3; 48 Day 4; 72 Day 5; 96 Day 6; 120 Day 7; 144 and Day 8; 168 hours post-dose

Interventionnanogramxhour/milliliter/mg (ngxh/ml/mg) (Geometric Mean)
Evacetrapib: Tablet111
Evacetrapib: Intravenous248

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Pharmacokinetics (PK): Time of Maximum Observed Concentration (Tmax) of Evacetrapib

(NCT02365558)
Timeframe: Day 1 and Day 14 at 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 Hours Postdose

InterventionHours (Median)
Evacetrapib3.00
Evacetrapib + Omeprazole3.00

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞])

(NCT02365558)
Timeframe: Day 1 and Day 14 at 0, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 Hours Postdose

Interventionnanogram*hour per milliliter (ng·h/mL) (Geometric Mean)
Evacetrapib12400
Evacetrapib + Omeprazole14100

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Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Evacetrapib

(NCT02365558)
Timeframe: Day 1 and Day 14 at 0, 1, 2, 3, 4, 6, 8,12, 24, 36, 48, 72, 96, 120, 144 and 168 Hours Postdose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Evacetrapib748
Evacetrapib + Omeprazole959

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Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Evacetrapib

(NCT02497391)
Timeframe: Predose on Day 1,and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 Hours Postdose

Interventionnangram/milliliter (ng/mL) (Geometric Mean)
Evacetrapib Reference (R)983
Evacetrapib Test 1 (T1)1170
Evacetrapib Test 2 (T2)1120

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PK: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of Evacetrapib

(NCT02497391)
Timeframe: Predose on Day 1,and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 Hours Postdose

Interventionnanogram·hour/milliter (ng·h/mL) (Geometric Mean)
Evacetrapib Reference (R)14700
Evacetrapib Test 1 (T1)16100
Evacetrapib Test 2 (T2)15500

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SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		2.13106-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
niacin
Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.		3.8730pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3		antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
midazolam
Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.		3.511imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
probucol
Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood.		3.2710dithioketal;
polyphenol		anti-inflammatory drug;
anticholesteremic drug;
antilipemic drug;
antioxidant;
cardiovascular drug
tolbutamide
Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.		3.511N-sulfonylureahuman metabolite;
hypoglycemic agent;
insulin secretagogue;
potassium channel blocker
aldosterone
[no description available]		9.822111beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde		human metabolite;
mouse metabolite
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		5.3522pyrrole;
secondary amine
fluorobenzenes
Fluorobenzenes: Derivatives of BENZENE that contain FLUORINE.. monofluorobenzene : The simplest member of the class of monofluorobenzenes that is benzene carrying a single fluoro substituent.. fluorobenzenes : Any fluoroarene that is a benzene or a substituted benzene carrying at least one fluoro group.		4.3711monofluorobenzenesNMR chemical shift reference compound
oleanolic acid
[no description available]		2.1510hydroxy monocarboxylic acid;
pentacyclic triterpenoid		plant metabolite
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		5.3522delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
atorvastatin
[no description available]		7.5565aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
ursolic acid
[no description available]		2.1510hydroxy monocarboxylic acid;
pentacyclic triterpenoid		geroprotector;
plant metabolite
betulinic acid
[no description available]		2.1510hydroxy monocarboxylic acid;
pentacyclic triterpenoid		anti-HIV agent;
anti-inflammatory agent;
antimalarial;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
plant metabolite
oxazolidin-2-one
Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.		8.13240carbamate ester;
oxazolidinone		metabolite
ezetimibe
Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).		6.8132azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
oleanolic acid 3-acetate
oleanolic acid 3-acetate: from Gardenia jasminoides; RN given for (3beta)-isomer		2.1510
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		3.4811aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
torcetrapib
[no description available]		7.6200(trifluoromethyl)benzenes;
carbamate ester;
quinolines		anticholesteremic drug;
CETP inhibitor
lignans
Lignans: A class of dibenzylbutane derivatives which occurs in higher plants and in fluids (bile, serum, urine, etc.) in man and other animals. These compounds, which have a potential anti-cancer role, can be synthesized in vitro by human fecal flora. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)		3.2710
dalcetrapib
dalcetrapib: inhibits cholesteryl ester transfer protein (CETP)		7.6200anilide
bms201038
BMS201038: an anticholesteremic agent and microsomal triglycide transfer protein inhibitor. lomitapide : A member of the class of benzamides obtained by formal condensation of the carboxy group of 4'-(trifluoromethyl)biphenyl-2-carboxylic acid with the primary amino group of 9-[4-(4-aminopiperidin-1-yl)butyl]-N-(2,2,2-trifluoroethyl)-9H-fluorene-9-carboxamide. Used (as its mesylate salt) as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia.		4.120(trifluoromethyl)benzenes;
benzamides;
fluorenes;
piperidines		anticholesteremic drug;
MTP inhibitor
etc-1002
8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid: inhibits ATP citrate lyase (ACL); has anti-atherosclerotic activity. bempedoic acid : An alpha,omega-dicarboxylic acid that is pentadecanedioic acid which is substituted by methyl groups groups at positions 2 and 14, and by a hydroxy group at position 8. It is a drug used for the treatment of high LDL cholesterol, which is sometimes referred to as 'bad cholesterol'.		3.1810alpha,omega-dicarboxylic acidantilipemic drug;
EC 2.3.3.8 (ATP citrate synthase) inhibitor;
prodrug
ta-8995
TA-8995: inhibits cholesteryl ester transfer protein		4.1520
anacetrapib
[no description available]		8.31290
oligonucleotides
[no description available]		4.120
pci 32765
ibrutinib: a Btk protein inhibitor. ibrutinib : A member of the class of acrylamides that is (3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine in which the piperidine nitrogen is replaced by an acryloyl group. A selective and covalent inhibitor of the enzyme Bruton's tyrosine kinase, it is used for treatment of B-cell malignancies.		2.1310acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
piperidines
Piperidines: A family of hexahydropyridines.		2.1310
leoligin
leoligin: inhibits intimal hyperplasia of venous bypass grafts; isolated from Edelweiss; structure in first source		3.2710
ConditionIndicatedRelationship StrengthStudiesTrials
Hypertriglyceridemia
A condition of elevated levels of TRIGLYCERIDES in the blood.		02.1510
Coronary Heart Disease
[description not available]		06.561
Coronary Disease
An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.		06.561
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		011.64196
Hyperlipemia
[description not available]		03.811
Hyperlipidemias
Conditions with excess LIPIDS in the blood.		03.811
Colorectal Cancer
[description not available]		07.4110
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		02.4110
Vascular Diseases
Pathological processes involving any of the BLOOD VESSELS in the cardiac or peripheral circulation. They include diseases of ARTERIES; VEINS; and rest of the vasculature system in the body.		05.441
Complications of Diabetes Mellitus
[description not available]		03.6411
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		010.7532
Elevated Cholesterol
[description not available]		05.8241
Hypercholesterolemia
A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.		05.8241
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.5520
Delayed Effects, Prenatal Exposure
[description not available]		02.5520
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.5520
Dyslipidemia
[description not available]		015.11114
Atherogenesis
[description not available]		07.2351
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		010.11114
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		07.2351
Diseases, Peripheral Vascular
[description not available]		05.422
Heart Disease, Ischemic
[description not available]		04.4511
Cerebral Arteriosclerosis
[description not available]		04.4511
Intracranial Arteriosclerosis
Vascular diseases characterized by thickening and hardening of the walls of ARTERIES inside the SKULL. There are three subtypes: (1) atherosclerosis with fatty deposits in the ARTERIAL INTIMA; (2) Monckeberg's sclerosis with calcium deposits in the media and (3) arteriolosclerosis involving the small caliber arteries. Clinical signs include HEADACHE; CONFUSION; transient blindness (AMAUROSIS FUGAX); speech impairment; and HEMIPARESIS.		04.4511
Peripheral Vascular Diseases
Pathological processes involving any one of the BLOOD VESSELS in the vasculature outside the HEART.		05.422
Myocardial Ischemia
A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).		04.4511
Arteriosclerosis, Coronary
[description not available]		03.8921
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		03.8921
Atrioventricular Nodal Re-Entrant Tachycardia
[description not available]		03.4811
Tachycardia, Ventricular
An abnormally rapid ventricular rhythm usually in excess of 150 beats per minute. It is generated within the ventricle below the BUNDLE OF HIS, either as autonomic impulse formation or reentrant impulse conduction. Depending on the etiology, onset of ventricular tachycardia can be paroxysmal (sudden) or nonparoxysmal, its wide QRS complexes can be uniform or polymorphic, and the ventricular beating may be independent of the atrial beating (AV dissociation).		03.4811
Apolipoprotein B-100, Familial Defective
[description not available]		03.0110
Hyperlipoproteinemia Type II
A group of familial disorders characterized by elevated circulating cholesterol contained in either LOW-DENSITY LIPOPROTEINS alone or also in VERY-LOW-DENSITY LIPOPROTEINS (pre-beta lipoproteins).		03.0110
Cardiac Diseases
[description not available]		03.0110
Hyperlipoproteinemia
[description not available]		03.0110
Heart Diseases
Pathological conditions involving the HEART including its structural and functional abnormalities.		03.0110
Hyperlipoproteinemias
Conditions with abnormally elevated levels of LIPOPROTEINS in the blood. They may be inherited, acquired, primary, or secondary. Hyperlipoproteinemias are classified according to the pattern of lipoproteins on electrophoresis or ultracentrifugation.		03.0110
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		03.0110
Lipid Metabolism, Inborn Error
[description not available]		03.7130
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.8130
Brain Vascular Disorders
[description not available]		03.511
Cerebrovascular Disorders
A spectrum of pathological conditions of impaired blood flow in the brain. They can involve vessels (ARTERIES or VEINS) in the CEREBRUM, the CEREBELLUM, and the BRAIN STEM. Major categories include INTRACRANIAL ARTERIOVENOUS MALFORMATIONS; BRAIN ISCHEMIA; CEREBRAL HEMORRHAGE; and others.		03.511
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		03.5111
Liver Dysfunction
[description not available]		03.5111
Liver Diseases
Pathological processes of the LIVER.		03.5111
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		03.5111
Genetic Predisposition
[description not available]		02.1510
Acute Coronary Syndrome
An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION.		02.0610