Page last updated: 2024-11-07

ezetimibe

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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). [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]

Cross-References

ID SourceID
PubMed CID150311
CHEMBL ID1138
CHEBI ID49040
SCHEMBL ID2871
MeSH IDM0422151

Synonyms (119)

Synonym
AC-1057
AKOS005572111
AB00639916-08
1-(4-fluorophenyl)-3(r)-[3-(4-fluorophenyl)-3(s)-hydroxypropyl]-4(s)-(4-hydroxyphenyl)-2-azetidinone
ezetimibe
mk-0653
ezetrol
(3r,4s)-1-(p-fluorophenyl)-3-((3s)-3-(p-fluorophenyl)-3-hydroxypropyl)-4-(p-hydroxyphenyl)-2-azetidinone
ezedoc
sch 58235
(-)-sch 58235
zetia
2-azetidinone, 1-(4-fluorophenyl)-3-((3s)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)-, (3r,4s)-
sch-58235
2-azetidinone, 1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)-, (3r-(3alpha(s*),4beta))-
zient
sch58235
(1-(4-fluorophenyl)-(3r)-(3-(4-fluorophenyl)-(3s)-hydroxypropyl)-(4s)-(4-hydroxyphenyl)-2-azetidinone)
ezetimib
(3r,4s)-1-(4-fluorophenyl)-3-[(3s)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
ezetimiba
ezetimibum
MLS001424125
CHEBI:49040 ,
MLS000759443
smr000466334
DB00973
163222-33-1
D01966
zetia (tn)
ezetimibe (jan/usp/inn)
HMS2051K16
CHEMBL1138
mk0653
nsc-758923
ezetimibe [usan:inn:ban]
unii-eor26lqq24
eor26lqq24 ,
nsc 758923
hsdb 7737
dtxcid9024223
tox21_111443
dtxsid1044223 ,
cas-163222-33-1
HMS2236A04
c24h21f2no3
STK640490
CCG-100884
bdbm50371521
HY-17376
ezetimibe [mart.]
ezetimibe [mi]
ezetimibe [orange book]
nexlizet component ezetimibe
ezetimibe component of roszet
ezetimibe [inn]
ezetimibe [usan]
ezetimibe [who-dd]
ezetimibe [vandf]
ezetimibe [hsdb]
ezetimibe component of nexlizet
roszet component ezetimibe
ezetimibe [usp monograph]
2-azetidinone, 1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)-, (3r-(3.alpha.(s*),4.beta.))-
ezetimibe [usp-rs]
ezetimibe component of vytorin
vytorin component ezetimibe
ezetimibe [jan]
AM84560
S1655
gtpl6816
AB00639916-06
NC00134
SCHEMBL2871
tox21_111443_1
NCGC00263575-01
KS-1170
(3r,4s)-1-(4-fluorophenyl)-3-[(s)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-azetidin-2-one
OLNTVTPDXPETLC-XPWALMASSA-N
(3r,4s)-1-(4-fluorophenyl)-3-[(3 s)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
(3r,4s)-1-(4-fluorophenyl)-3-[(3s)-3-(4-fluorophenyl)-3-hydroxy-propyl]-4-(4-hydroxyphenyl)azetidin-2-one
MLS006011921
ezetimibe, pharmaceutical secondary standard; certified reference material
(3r,4s)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)azetidin-2-one
AB00639916_09
EX-A795
ezetimibe, united states pharmacopeia (usp) reference standard
ezetimibe, >=98% (hplc)
HMS3715D06
NCGC00263575-07
Q417997
Z1541759501
ezetimibe (zetia) ,
(3r,4s)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-
3-hydroxypropyl)-4-(4-hydroxyphenyl)azetidin-2-one
BRD-K42260897-001-09-2
EN300-122361
1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-2-azetidinone
AR-270/43507897
2-azetidinone, 1-(4-fluorophenyl)-3-[(3s)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-, (3r,4s)-
(3r,4s)-1-(4-fluorophenyl)-3-[(3s)-3-(4-fluorophenyl)- 3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
ezetimibe anhydrate
(3~{r},4~{s})-1-(4-fluorophenyl)-3-[(3~{s})-3-(4-fluorophenyl)-3-oxidanyl-propyl]-4-(4-hydroxyphenyl)azetidin-2-one
h56 ,
BE164439
ezetimibe- bio-x
E1449
ezetimibe)
HY-17376R
CS-0694785
ezetimibe (standard)
ezetimibe (usp-rs)
ezetimibe (mart.)
(3r,4s)-1-(p-fluorophenyl)-3-((3s)-3-(p-fluorophenyl)-3- hydroxypropyl)-4-(p-hydroxyphenyl)-2-azetidinone
1-(4-fluorophenyl)-3(r)-(3-(4-fluorophenyl)-3(s)-hydroxypropyl)-4(s)-(4-hydroxyphenyl)-2-azetidinone
2-azetidinone, 1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3- hydroxypropyl)-4-(4-hydroxyphenyl)-, (3r-(3alpha(s*),4beta))-
ezetimibe (usp monograph)
(3r,4s)-1-(4-fluorophenyl)-3-((3s)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)azetidin-2-one
c10ax09

Research Excerpts

Overview

Ezetimibe is a cholesterol-lowering drug having anti-inflammatory and pleiotropic properties. It acts as an antagonist of Niemann-Pick C1-Like 1 receptor required for HCV entry and theoretically can reduce HCV viremia.

ExcerptReferenceRelevance
"Ezetimibe is a potent inhibitor of cholesterol absorption that has been approved for the treatment of hypercholesterolemia, but its molecular target has been elusive. "( The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1).
Altmann, SW; Braun, MP; Bull, HG; Burnett, DA; Chapman, KT; Crona, JH; Davis, HR; Dean, DC; Detmers, PA; Garcia-Calvo, M; Graziano, MP; Hawes, BE; Hughes, M; Iyer, SP; Lisnock, J; Macintyre, DE; Makarewicz, AM; O'neill, KA; Ogawa, A; Shevell, DE; Smith, MM; Tang, YS; Thornberry, NA; Ujjainwalla, F, 2005
)
2.13
"Ezetimibe acts as an antagonist of Niemann-Pick C1-Like 1 receptor required for HCV entry and theoretically can reduce HCV viremia."( Association between ezetimibe usage and hepatitis C RNA levels in uninfected kidney transplant recipients who received hepatitis C infected kidneys.
Azhar, A; Balaraman, V; Bhalla, A; Binari, LA; Concepcion, BP; Eason, JD; Forbes, RC; Hall, IE; Joglekar, K; Molnar, MZ; Rofaiel, G; Shaffer, D; Talwar, M; Tsujita, M, 2021
)
1.67
"Ezetimibe is a widely used medication to reduce the plasma cholesterol level, particularly low-density lipoprotein level. "( Impacts of ezetimibe on risks of various types of cancers: a meta-analysis and systematic review.
Bai, H; Ge, J; He, J; Hu, J; Huang, J; Li, H; Liang, X; Sun, S; Wang, X; Zhao, T, 2023
)
2.74
"Ezetimibe (ETZ) is a hypocholesterolemic agent with limited dissolution, poor water solubility, and subsequently demonstrates low oral bioavailability."( Development of ezetimibe eutectic with improved biopharmaceutical and mechanical properties to design an optimized oral solid dosage formulation.
Ghosh, A; Gour, A; Kumari, N; Nandi, U; Pandey, N; Raj, A; Roy, P; Srividya, B, 2022
)
1.8
"Ezetimibe is a new class of antihyperlipidemic agent indicated for the prevention of atherosclerosis disease and for the treatment of hypercholesterolemia. "( Pharmacokinetics and bioequivalence of Ezetimibe tablet versus Ezetrol®:an open-label, randomized, two-sequence crossover study in healthy Chinese subjects.
Cao, Y; Fu, Y; Gao, X; Jiang, X; Li, T; Li, X; Lin, P; Liu, Y; Ma, Y; Sun, F; Wang, C, 2023
)
2.62
"Ezetimibe is a cholesterol-lowering drug having anti-inflammatory and pleiotropic properties."( Ezetimibe alleviates acetic acid-induced ulcerative colitis in rats: targeting the Akt/NF-κB/STAT3/CXCL10 signaling axis.
Abdel-Rahman, RF; Mostafa, RE, 2023
)
3.07
"Ezetimibe is a lipid-lowering agent that selectively inhibits cholesterol absorption by binding to the Niemann-Pick C1-like 1 (NPC1L1) protein. "( Ezetimibe Induces Vasodilation in Rat Mesenteric Resistance Arteries through Inhibition of Extracellular Ca
Byeon, S; Choi, S; Choi, SK; Haam, CE; Lee, YH; Oh, EY, 2023
)
3.8
"Ezetimibe (EZT) is a selective cholesterol absorption inhibitor with poor aqueous solubility (0.012mg/ml 23oC) and low oral bioavailability (about 35-65% for a once 10mg dose). "( Dissolution rate enhancement of new co-crystals of ezetimibe with maleic acid and isonicotinamide.
Kai, S; Li Na, D; Ling, F; Man, Z; Wen, L; Xiao-Hui, Z; Yan-Jie, H; Yu-Zhen, Y, 2019
)
2.21
"Ezetimibe is a cholesterol-lowering drug that possesses the pharmacophore features to inhibit NTCP."( The effect of twelve weeks of treatment with ezetimibe on HDV RNA level in patients with chronic hepatitis D.
Abbas, M; Abbas, Z; Asim, M; Saad, M; Samejo, SA, 2020
)
1.54
"Ezetimibe is a top-selling hypolipidemic drug for the treatment of cardiovascular diseases. "( Efficient production of an ezetimibe intermediate using carbonyl reductase coupled with glucose dehydrogenase.
Liu, ZQ; Tang, YQ; Wang, MY; Wu, D; Zhang, XJ; Zheng, YG; Zhou, R, 2021
)
2.36
"Ezetimibe is a cholesterol-lowering agent with an oral bioavailability of 50% by virtue of its poor solubility and extensive hepatic and intestinal metabolism."( Amorphous Solid Dispersion Based Oral Disintegrating Film of Ezetimibe: Development and Evaluation.
Narayana, KA; Shrestha, S; Sudheer, P, 2021
)
2.31
"Ezetimibe (EZM) is a selective inhibitor of the sterol transporter Niemann-Pick C1-Like 1 in the small intestine used as an adjunctive therapy to lower cholesterol levels in cases of hyperlipidemia. "( Ezetimibe: A Review of Analytical Methods for the Drug Substance, Pharmaceutical Formulations and Biological Matrices.
Cabral, LM; de Sousa, VP; Pinto, EC; Rocha, LP, 2022
)
3.61
"Ezetimibe is a well-known drug that lowers blood cholesterol levels by reducing its absorption in the small intestine when joining to Niemann-Pick C1-like protein (NPC1L1). "( Synthesis and Modeling of Ezetimibe Analogues.
Díez, D; Garrido, NM; Manchado, A; Nieto, CT; Salgado, MM, 2021
)
2.36
"Ezetimibe is an azetidine derivative which blocks Niemann Pick C1-Like 1 Protein; as its consequence, plasmatic concentration of low density lipoproteins and other apoB-containing lipoproteins, that are the substrate of lysosomal acid lipase, are decreased."( Long term substrate reduction therapy with ezetimibe alone or associated with statins in three adult patients with lysosomal acid lipase deficiency.
Bertamino, M; Bertolini, S; Di Rocco, M; Madeo, A; Pisciotta, L, 2018
)
1.46
"Ezetimibe is a potent cholesterol absorption inhibitor, with an erratic pharmacokinetic (PK) profile, attributed to an extensive enterohepatic recirculation (EHC). "( On the population pharmacokinetics and the enterohepatic recirculation of total ezetimibe.
Karalis, V; Soulele, K, 2019
)
2.18
"Ezetimibe is an FDA-approved drug that reduces cholesterol uptake by inhibiting the endocytosis through Niemman-Pick C1-Like 1 (NPC1L1) receptor, expressed on the membrane of enterocytes and hepatocytes."( Ezetimibe inhibits dengue virus infection in Huh-7 cells by blocking the cholesterol transporter Niemann-Pick C1-like 1 receptor.
Bautista-Carbajal, P; Cervantes-Salazar, M; De Jesús-González, LA; Del Ángel, RM; Farfan-Morales, CN; Hurtado-Monzón, AM; Osuna-Ramos, JF; Reyes-Ruiz, JM, 2018
)
2.64
"Ezetimibe (EZE) is an extensively used antihyperlipidemic drug with an important cholesterol lowering activity. "( Development of a joint population pharmacokinetic model of ezetimibe and its conjugated metabolite.
Karalis, V; Soulele, K, 2019
)
2.2
"Ezetimibe is a selective cholesterol absorption inhibitor, whether it has a positive effect on CVD events remains uncertain."( Ezetimibe for the prevention of cardiovascular disease and all-cause mortality events.
Liu, F; Shu, M; Tang, M; Wu, X; Xia, P; Zhan, S, 2018
)
2.64
"Ezetimibe is an effective lipid-lowering drug, an inhibitor of intestinal absorption of cholesterol, which was investigated in many international and Russian studies, the results of which have demonstrated good tolerability, safety and efficacy (reduction of LDL-C levels by 18% in monotherapy)."( [Possibilities of clinical use of ezetimibe Otrio (JSC "AKRIKHIN", Russia) in patients with high and very high cardiovascular risk who have not reached the target values of lipid metabolism. Conclusion of the Board of experts].
Galyavich, AM; Gurevich, VS; Kaminnyi, AI; Kashtalap, VV; Kobalava, JD; Mareev, VY; Shaposhnik, II; Susekov, AV, 2019
)
1.51
"Ezetimibe is a unique inhibitor of intestinal cholesterol absorption. "( [An inhibitor of intestinal cholesterol transporter].
Sano, M, 2013
)
1.83
"Ezetimibe is a newer lipid-lowering agent, with fewer side effects."( Safety and effectiveness of the association ezetimibe-statin (E-S) versus high dose rosuvastatin after acute coronary syndrome: the SAFE-ES study.
Alessi, MC; Bonnet, G; Bonnet, JL; Cuisset, T; Deharo, P; Grosdidier, C; Morange, P; Pankert, M; Quilici, J; Verdier, V, 2014
)
1.38
"Ezetimibe is a new lipid lowering agent that inhibits cholesterol absorption."( Inhibition of smooth muscle cell proliferation by ezetimibe via the cyclin D1-MAPK pathway.
Gong, YZ; Li, GY; Li, XL; Liao, DF; Luo, HD; Qin, L; Xie, XJ; Yang, YB; Yang, YX; Zheng, XL, 2014
)
1.38
"Ezetimibe is a potent inhibitor of Niemann-Pick type C1-Like 1 and has been approved for the treatment of hypercholesterolemia. "( Ezetimibe-mediated protection of vascular smooth muscle cells from cholesterol accumulation through the regulation of lipid metabolism-related gene expression.
Gong, YZ; Liao, DF; Sun, SW; Tan, X; Tuo, QH; Xie, XJ; Xiong, Y; Yang, XF; Yuan, HY; Zheng, XL, 2014
)
3.29
"Ezetimibe is a novel lipid-lowering agent that inhibits intestinal absorption of dietary and biliary cholesterol. "( Development and validation of a novel stability-indicating HPLC method for the quantitative determination of eleven related substances in ezetimibe drug substance and drug product.
Deng, Z; Hou, C; Liu, Y; Luo, Z; Tang, M; Wang, G; Yang, R; Yang, W; Zhou, H, 2015
)
2.06
"Ezetimibe is a selective inhibitor of Niemann-Pick C1-like 1 (NPC1L1) protein that regulates the cholesterol uptake from the small intestine into the enterocytes."( [Ezetimibe in clinical practice: from laboratory investigations to the IMPROVE-IT trial results].
Borghi, C; Filardi, PP,
)
1.76
"Ezetimibe is a non-statin agent that inhibits intestinal cholesterol absorption, leading to reductions in low-density lipoprotein cholesterol (LDL-C)."( The Role of Ezetimibe in the Treatment of Cardiovascular Disease.
Agarwala, A; Kajani, Z; Miedema, MD; Virani, SS, 2016
)
1.53
"Ezetimibe is a selective cholesterol absorption inhibitor that blocks Niemann Pick C1-like 1 protein, but may exert its effect through suppression of CD36."( The Glucotoxicity Protecting Effect of Ezetimibe in Pancreatic Beta Cells via Inhibition of CD36.
Kim, YW; Lee, HW; Moon, JS; Won, KC; Yoon, JS, 2016
)
1.42
"Ezetimibe, which is a currently marketed drug, could hold promise as an adjunctive, host-directed therapy for TB."( Potential effect of ezetimibe against Mycobacterium tuberculosis infection in type II diabetes.
Chien, MN; Ho, HT; Kuo, CP; Lin, AB; Lu, YT; Tsai, IF; Wei, TY; Wu, CL, 2017
)
2.22
"Ezetimibe is a selective cholesterol absorption inhibitor, which potently inhibits the uptake and absorption of biliary and dietary cholesterol from the small intestine without affecting the absorption of fat-soluble vitamins, triglycerides or bile acids. "( Cholesterol homeostasis by the intestine: lessons from Niemann-Pick C1 Like 1 [NPC1L1).
Altmann, SW; Basso, F; Davis, HR; Hoos, LM; Lally, SM; Tetzloff, G, 2008
)
1.79
"Ezetimibe (EZET) is a cholesterol-lowering agent that specifically inhibits intestinal cholesterol absorption."( Ezetimibe prevents cholesterol gallstone formation in mice.
Amigo, L; Arrese, M; Azocar, L; Jarufe, N; Lammert, F; Miquel, JF; Molina, H; Nervi, F; Pimentel, F; Zúñiga, S, 2008
)
2.51
"Ezetimibe is a new lipid-lowering agent that inhibits intestinal absorption of dietary cholesterol. "( Impact of ezetimibe on atherosclerosis: is the jury still out?
Al Badarin, FJ; Kopecky, SL; Kullo, IJ; Thomas, RJ, 2009
)
2.2
"Ezetimibe is a selective acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor used in hypercholesterolemia. "( Burkholderia cenocepacia: a new biocatalyst for efficient bioreduction of ezetimibe intermediate.
Banerjee, UC; Basit, A; Singh, A, 2009
)
2.03
"Ezetimibe (Zetia) is a potent inhibitor of cholesterol absorption that has been approved for the treatment of hypercholesterolemia. "( Effects of ezetimibe add-on therapy for high-risk patients with dyslipidemia.
Aoyama, N; Hatakeyama, Y; Izumi, T; Kosugi, R; Machida, Y; Masuda, T; Tojo, T; Yamaoka-Tojo, M; Yoshida, Y, 2009
)
2.19
"Ezetimibe is a novel cholesterol absorption inhibitor that reduces the level of low-density lipoprotein (LDL)-cholesterol (C). "( Effects of ezetimibe on remnant-like particle cholesterol, lipoprotein (a), and oxidized low-density lipoprotein in patients with dyslipidemia.
Michishita, I; Mizuguchi, I; Nozue, T, 2010
)
2.19
"Ezetimibe is a drug that inhibits the absorption of both dietary and biliary cholesterol in the small intestine."( Ezetimbe as potential treatment for cholesterol gallstones: the need for clinical trials.
Ahmed, MH, 2010
)
1.08
"Ezetimibe is a lipid lowering medication that is able to inhibit dietary cholesterol. "( Ezetimibe and recent clinical trials: a look on the bright side.
Ahmed, MH, 2010
)
3.25
"Ezetimibe (EZ) is a novel pharmaceutical compound that reduces intestinal cholesterol absorption."( Model of intestinal chylomicron over-production and ezetimibe treatment: impact on the retention of cholesterol in arterial vessels.
Mangat, R; Proctor, SD; Russell, JC; Uwiera, R; Vine, DF; Wang, Y; Warnakula, S, 2010
)
1.33
"Ezetimibe is a potent inhibitor of cholesterol absorption by enterocytes. "( Effect of ezetimibe on incretin secretion in response to the intestinal absorption of a mixed meal.
Howles, PN; Hui, DY; Ji, Y; Kohan, AB; Lai, J; Li, X; Tso, P; Wang, DQ; Yang, L, 2010
)
2.21
"Ezetimibe is a well-tolerated and effective (in terms of achieving LDL-C targets) option inpatients with hyperlipidemia with or without diabetes."( Ezetimibe in diabetes: more than cholesterol lowering?
Katsiki, N; Mikhailidis, DP; Sarigianni, M, 2010
)
2.52
"Ezetimibe is a relatively new drug that inhibits the absorption of dietary cholesterol in the small intestine. "( Potential therapeutic uses for ezetimibe beyond lowering LDL-c to decrease cardiovascular events.
Ahmed, MH; Byrne, CD, 2010
)
2.09
"Ezetimibe is a novel cholesterol absorption inhibitor used in combination with statins."( A randomised placebo-controlled double-blind trial to evaluate lipid-lowering pharmacotherapy on proteolysis and inflammation in abdominal aortic aneurysms.
Choke, E; Cockerill, GW; Dawson, JA; Loftus, IM; Thompson, MM, 2011
)
1.09
"Ezetimibe is a potent inhibitor of cholesterol absorption that has been approved for the treatment of hypercholesterolemia. "( Ezetimibe and reactive oxygen species.
Izumi, T; Masuda, T; Takahira, N; Tojo, T; Yamaoka-Tojo, M, 2011
)
3.25
"Ezetimibe is a new lipid-lowering agent that blocks the intestinal absorption of dietary and biliary cholesterol and reduces LDL-C levels, especially when combined with statins."( Ezetimibe and vascular endothelial function.
Ikeda, S; Maemura, K, 2011
)
2.53
"Ezetimibe is a lipid-lowering agent that inhibits intestinal absorption of dietary cholesterol. "( Role of ezetimibe in the prevention of cardiovascular disease: absence of evidence.
Goldstein, MR; Mascitelli, L; Pezzetta, F, 2010
)
2.24
"Ezetimibe is a lipid-lowering compound that selectively inhibits the absorption of cholesterol and related phytosterols from the intestine. "( Design and characterization of nanocrystal formulations containing ezetimibe.
Gulsun, T; Gursoy, RN; Oner, L, 2011
)
2.05
"Ezetimibe is a hypolipidemic agent acting via inhibition of cholesterol absorption from the small intestine. "( Ezetimibe is effective in the treatment of persistent hyperlipidemia of renal allograft recipients.
Benou, A; Fourtounas, C; Goumenos, D; Kalliakmani, P; Koukoulaki, M; Papachristou, E; Roumeliotou, M; Savvidaki, E; Vlachojannis, JG, 2011
)
3.25
"Ezetimibe is a cholesterol-lowering agent targeting Niemann-Pick C1-like 1, an intestinal cholesterol transporter. "( Chronic administration of ezetimibe increases active glucagon-like peptide-1 and improves glycemic control and pancreatic beta cell mass in a rat model of type 2 diabetes.
Choi, JM; Kim, BJ; Kim, L; Kim, SW; Kim, WJ; Lee, WY; Oh, KW; Park, CY; Park, SE; Park, SW; Rhee, EJ; Sohn, JH; Yang, SJ, 2011
)
2.11
"Ezetimibe glucuronide is a substrate of human MRP2. "( Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells.
Auge, D; Fahrmayr, C; Fromm, MF; König, J; Mieth, M, 2012
)
1.82
"Ezetimibe/simvastatin is an effective and generally well tolerated adjunct to dietary therapy for markedly reducing low-density lipoprotein cholesterol (LDL-C) levels and improving other lipid parameters across diverse patient populations."( Ezetimibe/simvastatin: a guide to its clinical use in hypercholesterolemia.
Lyseng-Williamson, KA, 2012
)
2.54
"Ezetimibe is a cholesterol uptake inhibitor that targets the Niemann-Pick C1-like 1 cholesterol transporter. "( Ezetimibe ameliorates intestinal chylomicron overproduction and improves glucose tolerance in a diet-induced hamster model of insulin resistance.
Adeli, K; Baker, C; Hussain, MM; Iqbal, J; Lino, M; Naples, M, 2012
)
3.26
"Ezetimibe is an inhibitor of cholesterol absorption in the intestine. "( Ezetimibe improves endothelial function and inhibits Rho-kinase activity associated with inhibition of cholesterol absorption in humans.
Fukumoto, Y; Miura, M; Nochioka, K; Shiba, N; Shimokawa, H; Tanaka, S; Zhulanqiqige, do E, 2012
)
3.26
"Ezetimibe is an effective LDL-C lowering agent and is safe and well tolerated."( Ezetimibe therapy: mechanism of action and clinical update.
Dayspring, TD; Phan, BA; Toth, PP, 2012
)
2.54
"Ezetimibe is a lipid-lowering drug that inhibits the intestinal absorption of dietary and biliary cholesterol by blocking passage across the intestinal wall. "( Efficacy and safety of ezetimibe added to ongoing statin therapy for treatment of patients with primary hypercholesterolemia.
Bays, HE; Cho, M; Gagné, C; Gumbiner, B; Mata, P; Melino, M; Musliner, TA; Quinto, K; Weiss, SR, 2002
)
2.07
"Ezetimibe is a cholesterol absorption inhibitor that significantly lowers low- density lipoprotein cholesterol (LDL-C), and favourably affects triglyceride and high-density lipoprotein cholesterol blood levels in monotherapy and in combination with statins. "( Ezetimibe.
Bays, H, 2002
)
3.2
"Ezetimibe is a selective cholesterol absorption inhibitor, with a site of action at the intestinal epithelium."( The future direction of cholesterol-lowering therapy.
Evans, M; Rees, A; Roberts, A, 2002
)
1.04
"Ezetimibe is a novel cholesterol absorption inhibitor that blocks intestinal absorption of dietary and biliary cholesterol. "( Evaluation of the efficacy, safety, and tolerability of ezetimibe in primary hypercholesterolaemia: a pooled analysis from two controlled phase III clinical studies.
Dujovne, CA; Knopp, RH; Le Beaut, A; Lipka, LJ; Suresh, R; Veltri, EP, 2003
)
2.01
"Ezetimibe is a new cholesterol absorption inhibitor that is safe and effective in total cholesterol and LDL-C reduction."( Clinical use of ezetimibe.
Cheng, AY; Leiter, LA, 2003
)
1.39
"Ezetimibe (Zetia) is a novel, selective cholesterol absorption inhibitor. "( Ezetimibe for hypercholesterolemia.
Morris, S; Tiller, R, 2003
)
3.2
"Ezetimibe is an option for monotherapy in patients with mild hypercholesterolemia or in those requiring adjunctive drug therapy for reduction of LDL-C levels. "( Pharmacology and therapeutics of ezetimibe (SCH 58235), a cholesterol-absorption inhibitor.
Cheng, JW; Jeu, L, 2003
)
2.04
"Ezetimibe is an effective treatment option that may enable more patients with hypercholesterolemia to achieve optimal cholesterol levels and reduce their risk for coronary heart disease."( Role of selective cholesterol absorption inhibition in the management of dyslipidemia.
Ballantyne, CM, 2004
)
1.04
"Ezetimibe is a prototype of a new class of agents that specifically block the absorption of cholesterol from the gastrointestinal tract."( Hypolipidemic therapy and cholesterol absorption.
Farmer, JA; Manhas, A, 2004
)
1.04
"Ezetimibe is a cholesterol absorption inhibitor which decreases low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia. "( Effects of ezetimibe on the pharmacodynamics and pharmacokinetics of lovastatin.
Cutler, DL; Kosoglou, T; Maxwell, SE; Meyer, I; Musiol, B; Statkevich, P; Veltri, EP; Yang, B; Zhu, Y, 2004
)
2.16
"Ezetimibe is a lipid-lowering drug indicated for the treatment of hypercholesterolemia as co-administration with HMG-CoA reductase inhibitors (statins) or as monotherapy. "( Pharmacodynamic interaction between ezetimibe and rosuvastatin.
Boutros, T; Cutler, DL; Kosoglou, T; Maxwell, SE; Statkevich, P; Suresh, R; Tiessen, R; Yang, B; Zhu, Y, 2004
)
2.04
"Ezetimibe (Zetia) is a novel inhibitor of intestinal absorption of cholesterol that is approved for the treatment of primary hypercholesterolemia. "( Pharmacokinetic interaction between ezetimibe and lovastatin in healthy volunteers.
Boutros, T; Kosoglou, T; Reyderman, L; Seiberling, M; Statkevich, P, 2004
)
2.04
"Ezetimibe is a US Food and Drug Administration-approved novel drug that targets the absorption of cholesterol in the intestine. "( Ezetimibe: a novel cholesterol-lowering agent that highlights novel physiologic pathways.
Patel, SB, 2004
)
3.21
"Ezetimibe is a novel lipid-lowering drug that prevents intestinal absorption of dietary and biliary cholesterol leading to significant reduction in total-C, LDL-C, Apo B, and TG and increases in HDL-C in patients with hypercholesterolemia. "( Assessment of a multiple-dose drug interaction between ezetimibe, a novel selective cholesterol absorption inhibitor and gemfibrozil.
Affrime, M; Batra, V; Boutros, T; Kosoglou, T; Maxwell, SE; Pember, L; Reyderman, L; Statkevich, P, 2004
)
2.01
"Ezetimibe is a specific inhibitor of intestinal cholesterol absorption recently introduced into medical practice; its mechanism of action, however, is still unknown."( Aminopeptidase N (CD13) is a molecular target of the cholesterol absorption inhibitor ezetimibe in the enterocyte brush border membrane.
Corsiero, D; Frick, W; Girbig, F; Hochleitner, EO; Jähne, G; Kramer, W; Lottspeich, F; Orsó, E; Pfenninger, A; Rhein, M; Schmitz, G; Wendler, W, 2005
)
1.27
"Ezetimibe is a new cholesterol absorption inhibitor that selectively inhibits dietary and biliary cholesterol absorption from the intestine. "( [Ezetimibe (Ezetrol): the statins' partner].
Ducobu, J; Sternon, J, 2004
)
2.68
"Ezetimibe is a newly approved drug that is a potent and highly specific inhibitor of an intestinal sterol permease; in daily doses as low as 10 mg, it suppresses intestinal absorption of cholesterol and decreases serum LDL cholesterol by approximately 18%."( An ezetimibe-policosanol combination has the potential to be an OTC agent that could dramatically lower LDL cholesterol without side effects.
McCarty, MF, 2005
)
1.67
"Ezetimibe is a useful addition to statins in patients with familial hyperlipidaemias but shows a highly variable response profile."( Efficacy of ezetimibe in patients with statin-resistant and statin-intolerant familial hyperlipidaemias.
Chik, G; Crook, MA; Doherty, E; Lumb, PJ; Wierzbicki, AS, 2005
)
2.15
"Ezetimibe (EZE) is a cholesterol-lowering drug that inhibits absorption of dietary and biliary cholesterol across the intestinal wall without affecting absorption of bile acids, fatty acids, fat-soluble vitamins, or triglycerides. "( Long-term safety and, tolerability profiles and lipid-modifying efficacy of ezetimibe coadministered with ongoing simvastatin treatment: a multicenter, randomized, double-blind, placebo-controlled, 48-week extension study.
Cho, M; Gagné, C; Gumbiner, B; Johnson-Levonas, AO; Masana, L; Mata, P; Meehan, A; Sirah, W; Troxell, JK, 2005
)
2
"Ezetimibe is a recently developed compound, which inhibits intestinal cholesterol absorption. "( [Optimization of cholesterol reduction principles and clinical results of dual inhibition].
von Hodenberg, E, 2005
)
1.77
"Ezetimibe is an effective LDL cholesterol-lowering agent in the kidney transplant population. "( Treatment of hypercholesterolemia with ezetimibe in the kidney transplant population.
Keough-Ryan, T; Kiberd, BA; Kiberd, M; Lawen, J; Puthenparumpil, JJ, 2005
)
2.04
"Ezetimibe/simvastatin is a highly efficacious, well-tolerated treatment option for hypercholesterolemic patients."( Dose-comparison study of the combination of ezetimibe and simvastatin (Vytorin) versus atorvastatin in patients with hypercholesterolemia: the Vytorin Versus Atorvastatin (VYVA) study.
Abate, N; Ballantyne, CM; King, TR; Palmisano, J; Yuan, Z, 2005
)
1.31
"Ezetimibe is a novel lipid-lowering agent that inhibits intestinal absorption of dietary and biliary cholesterol. "( Inhibition of intestinal cholesterol absorption by ezetimibe is a novel therapeutic target for fatty liver.
Matsui, T; Nakamura, K; Sato, T; Takeuchi, M; Yamagishi, S, 2006
)
2.03
"Ezetimibe is a new intestinal cholesterol uptake inhibitor, which reduces LDL cholesterol in monotherapy or in combination with statins."( [New results in the management of hypercholesterolemia].
Sármán, B, 2005
)
1.05
"Ezetimibe (Ezetrol) is a novel cholesterol lowering drug which disposition is not fully understood in man. "( A LC-MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1.
Cascorbi, I; Oswald, S; Scheuch, E; Siegmund, W, 2006
)
2.01
"Ezetimibe is an inhibitor of cholesterol absorption that is liver glucuronized after its rapid absorption, and is mobilized to the enterocytes, where together with its metabolites it exerts hypolipidemic effects, avoiding the absorption of cholesterol, through the reduction of specific cholesterol-transporter enzymes in the gut. "( [Ezetimibe--pharmacokinetics and therapeutics].
Araújo, RG; Casella Filho, A; Chagas, AC, 2005
)
2.68
"Ezetimibe seems to be an effective therapy for uncontrolled hypercholesterolemia in renal transplant patients when combined with high-dose statin therapy."( Ezetimibe for the treatment of uncontrolled hypercholesterolemia in patients with high-dose statin therapy after renal transplantation.
Heemann, U; Kohnle, M; Kribben, A; Philipp, T; Pietruck, F; Witzke, O, 2006
)
2.5
"Ezetimibe is a novel cholesterol absorption inhibitor that blocks the translocation of dietary and biliary cholesterol from the gastrointestinal lumen into the intracellular space of jejunal enterocytes."( Cholesterol absorption blockade with ezetimibe.
Davidson, MH; Toth, PP, 2005
)
1.32
"Ezetimibe is an inhibitor of the cholesterol uptake transporter Niemann-Pick C1-like protein (NPC1L1). "( Intestinal expression of P-glycoprotein (ABCB1), multidrug resistance associated protein 2 (ABCC2), and uridine diphosphate-glucuronosyltransferase 1A1 predicts the disposition and modulates the effects of the cholesterol absorption inhibitor ezetimibe in
Adam, U; Cascorbi, I; Dazert, E; Fricke, C; Giessmann, T; Haenisch, S; Jedlitschky, G; Kroemer, HK; Oswald, S; Remmler, C; Siegmund, W; Sudhop, T; von Bergmann, K; Wacke, W; Warzok, R; Weitschies, W, 2006
)
1.96
"Ezetimibe is a highly-selective inhibitor of cholesterol absorption and simvastatin is an evidence-based inhibitor of cholesterol synthesis."( Reaching goal in hypercholesterolaemia: dual inhibition of cholesterol synthesis and absorption with simvastatin plus ezetimibe.
Daskalopoulou, SS; Mikhailidis, DP, 2006
)
1.26
"Ezetimibe (E) is a new cholesterol adsorption inhibitor which prevents the adsorption of dietary and biliary cholesterol by binding to a recently described cholesterol transporter. "( Safety and effects on the lipid and C-reactive protein plasma concentration of the association of ezetimibe plus atorvastatin in renal transplant patients treated by cyclosporine-A: a pilot study.
Barsotti, G; Carpi, A; Consani, C; Manca-Rizza, G; Mantuano, E; Marchetti, V; Panichi, V; Paoletti, S; Sbragia, G; Taccola, D, 2006
)
1.99
"Ezetimibe is a selective inhibitor of intestinal cholesterol absorption that results in an additional 15% to 25% reduction of LDL-C."( Combination of statin and ezetimibe for the treatment of dyslipidemias and the prevention of coronary artery disease.
Genest, J, 2006
)
1.36
"Ezetimibe (EZ) is a selective cholesterol absorption inhibitor approved for use in Canada. "( The clinical effect and tolerability of ezetimibe in high-risk patients managed in a specialty cardiovascular risk reduction clinic.
Francis, GA; Gilchrist, DM; Gyenes, GT; Opgenorth, A; Pearson, GJ; Romney, JS, 2006
)
2.04
"Ezetimibe is a novel CAI that inhibits the absorption of dietary and biliary cholesterol without affecting the absorption of triglycerides or fat-soluble vitamins."( Safety considerations with gastrointestinally active lipid-lowering drugs.
Armani, A; Guyton, JR; Jacobson, TA; McKenney, JM, 2007
)
1.06
"Ezetimibe is a lipid-lowering agent that inhibits the intestinal absorption of cholesterol and other related phytosterols. "( Ezetimibe-induced acute pancreatitis.
Ahmad, I; Hotiana, M; Hussain, M; Rahman, F; Ruby, E; Usman, H, 2007
)
3.23
"Ezetimibe is a novel cholesterol-lowering drug that acts at the brush border of the small intestine."( Ezetimibe: an update on the mechanism of action, pharmacokinetics and recent clinical trials.
Johnson, RR; Sweeney, ME, 2007
)
2.5
"Ezetimibe is a FDA-approved, intestinal cholesterol absorption inhibitor that lowers plasma LDL cholesterol in humans and animals and inhibits aortic root atherosclerosis in apoE KO mice, but has not been proven to reduce CHD."( Inhibition of intestinal absorption of cholesterol by ezetimibe or bile acids by SC-435 alters lipoprotein metabolism and extends the lifespan of SR-BI/apoE double knockout mice.
Acton, S; Braun, A; Broschat, KO; Krieger, M; Krul, ES; Napawan, N; Stagliano, N; Yesilaltay, A, 2008
)
1.32
"Ezetimibe is a drug that impairs intestinal cholesterol absorption and decreases blood cholesterol levels. "( Ezetimibe plus simvastatin cardiovascular outcomes study program.
Padial, LR, 2008
)
3.23
"Ezetimibe is a relatively new lipid lowering agent, which is indicated for the treatment of primary hypercholesterolaemia, either as monotherapy or in combination with other hypolipidaemic drugs. "( Ezetimibe-associated adverse effects: what the clinician needs to know.
Elisaf, MS; Florentin, M; Liberopoulos, EN, 2008
)
3.23
"Ezetimibe is a safe alternative option for hyperlipidaemic patients intolerant to other lipid lowering drugs as well as a beneficial supplementary agent for patients who do not reach the recommended serum cholesterol level with their current hypolipidaemic treatment. "( Ezetimibe-associated adverse effects: what the clinician needs to know.
Elisaf, MS; Florentin, M; Liberopoulos, EN, 2008
)
3.23
"Ezetimibe is a novel cholesterol and plant sterol absorption inhibitor that reduces plasma low-density lipoprotein-cholesterol by selectively binding to the intestinal cholesterol transporter, Niemann-Pick C1-Like 1. "( Ezetimibe improves high fat and cholesterol diet-induced non-alcoholic fatty liver disease in mice.
Cook, J; Davis, H; Hoos, L; Hwa, JJ; Tetzloff, G; van Heek, M; Zheng, S, 2008
)
3.23
"Ezetimibe is a cholesterol absorption inhibitor that blocks the intestinal absorption of both biliary and dietary cholesterol. "( Ezetimibe: cholesterol lowering and beyond.
Bays, HE; Neff, D; Tershakovec, AM; Tomassini, JE, 2008
)
3.23
"Ezetimibe is a novel approach to reduce biliary cholesterol content and a promising strategy for preventing or treating cholesterol gallstones by inhibiting intestinal cholesterol absorption."( Effect of ezetimibe on the prevention and dissolution of cholesterol gallstones.
Mendez-Sanchez, N; Portincasa, P; Uribe, M; Wang, DQ; Wang, HH, 2008
)
2.19
"Ezetimibe is a cholesterol-lowering agent that modulates intestinal absorption of sterols. "( Severe jaundice following treatment with ezetimibe.
Black, PN; Orr, DW; Ritchie, SR, 2008
)
2.05
"Ezetimibe is a novel selective inhibitor of intestinal cholesterol absorption, which has been shown to significantly decrease low-density lipoprotein cholesterol (LDL-C). "( The plasma concentration and LDL-C relationship in patients receiving ezetimibe.
Batra, V; Ezzet, F; Kosoglou, T; Lipka, L; Mellars, L; Patrick, J; Statkevich, P; Veltri, E; Wexler, D, 2001
)
1.99
"Ezetimibe (SCH 58235) is a novel cholesterol absorption inhibitor that selectively and potently blocks intestinal absorption of dietary and biliary cholesterol."( Effectiveness and tolerability of ezetimibe in patients with primary hypercholesterolemia: pooled analysis of two phase II studies.
Bays, HE; Cuffie-Jackson, C; Drehobl, MA; Dujovne, CA; Knopp, RH; Lebeaut, AP; Lipka, LJ; Mellars, LE; Moore, PB; Rosenblatt, S; Toth, PD; Veltri, EP; Yang, B, 2001
)
2.03
"4. Ezetimibe is a potent inhibitor of intestinal free cholesterol absorption that does not require exocrine pancreatic function for activity."( Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function.
Compton, DS; Davis, HR; Farley, C; Hoos, L; van Heek, M, 2001
)
2.27
"Ezetimibe (Sch-58235) is a cholesterol absorption inhibitor being developed by Schering-Plough for the potential treatment of atherosclerosis and hypercholesterolemia. "( Ezetimibe (Schering-Plough).
Meng, CQ, 2001
)
3.2
"Ezetimibe (SCH58235) is a potent, selective, cholesterol absorption inhibitor. "( Ezetimibe, a potent cholesterol absorption inhibitor, inhibits the development of atherosclerosis in ApoE knockout mice.
Compton, DS; Davis, HR; Hoos, L; Tetzloff, G, 2001
)
3.2
"Ezetimibe (Sch-58235) is a cholesterol absorption inhibitor under development by Schering-Plough (SP), in collaboration with Merck, for the potential treatment of hypercholesterolemia. "( Ezetimibe. Schering-Plough.
Meng, CQ, 2002
)
3.2

Effects

Ezetimibe has an antioxidative effect when given as monotherapy or as an add-on to the statin, simvastatin. It also has an adverse-event profile that is similar to placebo when used asmonotherapy or in combination with statins and fenofibrate.

Ezetimibe (EZE) has been reported to have anti-inflammatory and antioxidative properties in hepatology-related diseases. Its potential role in SCI remains unclear. Use has decreased in the US post-ENHANCE, whereas use has gradually but steadily increased in Canada.

ExcerptReferenceRelevance
"Ezetimibe has an atheroprotective activity through inhibition of the expression of vascular adhesion molecule-I and vascular CD14, a marker of the infiltration of mononuclear leukocytes."( Effects of Ezetimibe, Simvastatin, and their Combination on Inflammatory Parameters in a Rat Model of Adjuvant-Induced Arthritis.
Ames, FQ; Barbosa, CP; Bersani-Amado, CA; Bracht, L; de Souza Silva-Comar, FM; Tronco, RP, 2017
)
1.57
"Ezetimibe has a lipid lowering-independent vascular protective effect in patients with hypercholesterolemia through decreasing oxidative stress."( Ezetimibe monotherapy ameliorates vascular function in patients with hypercholesterolemia through decreasing oxidative stress.
Aihara, K; Akaike, M; Fujimoto, E; Higashida, M; Hirata, Y; Kanbara, T; Kinoshita, H; Kitagawa, T; Kitaichi, T; Kurobe, A; Kurobe, H; Matsumoto, T; Matsuoka, Y; Nakayama, T; Nishiya, M; Sata, M; Sugano, M; Sugasawa, N, 2011
)
3.25
"Ezetimibe also has an adverse-event profile that is similar to placebo when used as monotherapy or in combination with statins and fenofibrate."( Ezetimibe: the first in a novel class of selective cholesterol-absorption inhibitors.
Gupta, EK; Ito, MK,
)
2.3
"Ezetimibe has a relatively flat dose-response curve and titration is not required."( Hypolipidemic therapy and cholesterol absorption.
Farmer, JA; Manhas, A, 2004
)
1.04
"Ezetimibe has a favorable pharmacokinetic profile, which allows it to be administered once daily and to be given in conjunction with statins."( Ezetimibe: a novel option for lowering cholesterol.
Davidson, MH, 2003
)
2.48
"Ezetimibe has an antioxidative effect when given as monotherapy or as an add-on to the statin, simvastatin. "( Ezetimibe's effect on platelet aggregation and LDL tendency to peroxidation in hypercholesterolaemia as monotherapy or in addition to simvastatin.
Hussein, O; Itzkovich, Y; Minasian, L; Shestatski, K; Solomon, L; Zidan, J, 2008
)
3.23
"Ezetimibe (EZE) has been reported to have anti-inflammatory and antioxidative properties in hepatology-related diseases, but its potential role in SCI remains unclear."( Ezetimibe attenuates functional impairment via inhibition of oxidative stress and inflammation in traumatic spinal cord injury.
Deng, J; Li, H; Rong, W; Xiao, S; Yang, H; Yuan, B; Zhang, C; Zhu, J, 2023
)
3.07
"Ezetimibe has unique lipid lowering profile increasing HDL-C concomitant with decreasing LDL-C and TG."( [An inhibitor of intestinal cholesterol transporter].
Sano, M, 2013
)
1.11
"Ezetimibe use has decreased in the US post-ENHANCE, whereas use has gradually but steadily increased in Canada."( Impact of the ENHANCE trial on the use of ezetimibe in the United States and Canada.
Jackevicius, CA; Ko, DT; Krumholz, HM; Lu, L; Ross, JS; Tu, JV, 2014
)
1.39
"Ezetimibe use has steadily increased in Canada during the past decade even in the absence of evidence demonstrating a beneficial effect on clinical outcomes. "( Impact of drug policy on regional trends in ezetimibe use.
Jackevicius, CA; Ko, DT; Krumholz, HM; Lu, L; Ross, JS; Tu, JV, 2014
)
2.11
"Ezetimibe has been reported to provide significant incremental reduction in low-density-lipoprotein cholesterol (LDL-C) when added to a statin; however, its effect on coronary atherosclerosis has not yet been evaluated in detail. "( Effect of combination therapy of ezetimibe and rosuvastatin on regression of coronary atherosclerosis in patients with coronary artery disease.
Dohi, K; Fujimoto, N; Ito, M; Masuda, J; Miyahara, M; Nakamura, M; Nakata, T; Nishikawa, M; Nishimura, Y; Sasou, T; Sawai, T; Tanigawa, T; Yamada, T, 2015
)
2.14
"Ezetimibe has been demonstrated to significantly reduce LDL cholesterol levels in combination with statins and recent trials support its role in reducing the risk of cardiovascular events."( [Ezetimibe in clinical practice: from laboratory investigations to the IMPROVE-IT trial results].
Borghi, C; Filardi, PP,
)
1.76
"Ezetimibe has been reported to inhibit viral entry and to reduce BMI and has been proposed as a novel therapeutic agent for chronic hepatitis C (CHC), potentiating the effects of pegylated interferon and ribavirin (peg-IFN/RBV)."( Coadministration of ezetimibe with pegylated interferon plus ribavirin could improve early virological response in chronic hepatitis C obese Egyptian patients.
Abd-Ellah, MF; Gad, MA; Helal, GK; Mahgoup, EM, 2016
)
2.2
"Ezetimibe use has increased rapidly in Australia since receiving public subsidy. "( Ezetimibe: Use, costs, and adverse events in Australia.
David, MC; Hollingworth, SA; Martin, JH; Ostino, R; Tett, SE, 2017
)
3.34
"Ezetimibe has an atheroprotective activity through inhibition of the expression of vascular adhesion molecule-I and vascular CD14, a marker of the infiltration of mononuclear leukocytes."( Effects of Ezetimibe, Simvastatin, and their Combination on Inflammatory Parameters in a Rat Model of Adjuvant-Induced Arthritis.
Ames, FQ; Barbosa, CP; Bersani-Amado, CA; Bracht, L; de Souza Silva-Comar, FM; Tronco, RP, 2017
)
1.57
"Ezetimibe has been shown to be a selective inhibitor of the Niemann-Pick C1-like 1 (NPC1L1) transporter of cholesterol across the intestinal wall."( Beneficial effects of ezetimibe-based therapy in patients with dyslipidemia.
Miura, S; Saku, K, 2008
)
1.38
"Ezetimibe has been reported to improve lipid control in patients with established cardiovascular disease (CVD)."( Estimating the health benefits and costs associated with ezetimibe coadministered with statin therapy compared with higher dose statin monotherapy in patients with established cardiovascular disease: results of a Markov model for UK costs using data regis
Ara, R; Chilcott, J; Duenas, A; Durrington, P; Paisley, S; Pandor, A; Tumur, I; Wilkinson, A; Williams, R, 2008
)
2.03
"Ezetimibe has proved effective for the treatment of dyslipidemia in these patients."( Treatment with ezetimibe in kidney transplant recipients with uncontrolled dyslipidemia.
Burgos, D; Cabello, M; González Molina, M; Gutiérrez, C; Gutiérrez, E; López, V; Sola, E, 2008
)
1.42
"Ezetimibe has not been associated with serious adverse effects."( Lipid-lowering drugs acting at the level of the gastrointestinal tract.
Filippatos, TD; Mikhailidis, DP, 2009
)
1.07
"Ezetimibe has been reported to reduce LDL-C safely with both monotherapy and combination therapy with statins."( Effects of ezetimibe add-on therapy for high-risk patients with dyslipidemia.
Aoyama, N; Hatakeyama, Y; Izumi, T; Kosugi, R; Machida, Y; Masuda, T; Tojo, T; Yamaoka-Tojo, M; Yoshida, Y, 2009
)
1.46
"Ezetimibe has been more particularly studied in patients with type 2 diabetes whose high cardiovascular risk is well known."( [Ezetimibe (Ezetrol) in patients with diabetes].
Radermecker, RP; Scheen, AJ, 2009
)
1.98
"Ezetimibe therapy has beneficial effects on fibrinolytic activity and homeostasis between oxidant and antioxidant activity in hyperlipidemic patients This may be through lowering lipid levels or other mechanisms such as decreasing insulin resistance and the pleiotropic effects of the drug."( Ezetimibe therapy and its influence on oxidative stress and fibrinolytic activity.
Balci, H; Caner, M; Ercan, MA; Genc, H; Karter, YH; Sipahioglu, F; Turfaner, N; Uzun, H, 2010
)
3.25
"Ezetimibe has been reported to reduce LDL-cholesterol safely with both monotherapy and combination therapy with statins."( Ezetimibe and reactive oxygen species.
Izumi, T; Masuda, T; Takahira, N; Tojo, T; Yamaoka-Tojo, M, 2011
)
2.53
"Ezetimibe has a lipid lowering-independent vascular protective effect in patients with hypercholesterolemia through decreasing oxidative stress."( Ezetimibe monotherapy ameliorates vascular function in patients with hypercholesterolemia through decreasing oxidative stress.
Aihara, K; Akaike, M; Fujimoto, E; Higashida, M; Hirata, Y; Kanbara, T; Kinoshita, H; Kitagawa, T; Kitaichi, T; Kurobe, A; Kurobe, H; Matsumoto, T; Matsuoka, Y; Nakayama, T; Nishiya, M; Sata, M; Sugano, M; Sugasawa, N, 2011
)
3.25
"Ezetimibe treatment has been shown to cause significant decreases in plasma cholesterol levels in patients with hypercholesterolemia and familial hypercholesterolemia."( Ezetimibe ameliorates intestinal chylomicron overproduction and improves glucose tolerance in a diet-induced hamster model of insulin resistance.
Adeli, K; Baker, C; Hussain, MM; Iqbal, J; Lino, M; Naples, M, 2012
)
2.54
"Ezetimibe has been shown to inhibit dietary cholesterol absorption in animal models and humans, but studies on lymphatic lipid transport have not yet been performed. "( Ezetimibe inhibits lymphatic transport of esterified cholesterol but not free cholesterol in thoracic lymph duct-cannulated rats.
Furukawa, Y; Imaizumi, K; Nakamura, Y; Sato, M; Shiraishi, A; Shirouchi, B; Tomoyori, H, 2012
)
3.26
"Ezetimibe has been shown to inhibit cholesterol absorption in animal models, but studies on cholesterol absorption in humans have not been performed thus far."( Inhibition of intestinal cholesterol absorption by ezetimibe in humans.
Igel, M; Kodal, A; Lütjohann, D; Perevozskaya, I; Shah, S; Sudhop, T; Tribble, DL; von Bergmann, K, 2002
)
2.01
"Ezetimibe also has an adverse-event profile that is similar to placebo when used as monotherapy or in combination with statins and fenofibrate."( Ezetimibe: the first in a novel class of selective cholesterol-absorption inhibitors.
Gupta, EK; Ito, MK,
)
2.3
"Ezetimibe has minimal systemic absorption and a metabolic pathway involving enterohepatic circulation that allows for once a day administration due to a prolonged half-life."( Hypolipidemic therapy and cholesterol absorption.
Farmer, JA; Manhas, A, 2004
)
1.04
"Ezetimibe has a favorable pharmacokinetic profile, which allows it to be administered once daily and to be given in conjunction with statins."( Ezetimibe: a novel option for lowering cholesterol.
Davidson, MH, 2003
)
2.48
"Ezetimibe/simvastatin has also been associated with other beneficial effects on lipids, and it achieves greater efficacy than monotherapy with the use of lower, safer doses of the statin."( Enhanced hypercholesterolemia therapy: the ezetimibe/simvastatin tablet.
Cole, P; Rabasseda, X, 2005
)
1.31
"Ezetimibe has no effect on the activity of major drug metabolizing enzymes (CYP450), which reduces any potential drug-drug interactions with other medications."( Zetia: inhibition of Niemann-Pick C1 Like 1 (NPC1L1) to reduce intestinal cholesterol absorption and treat hyperlipidemia.
Davis, HR; Veltri, EP, 2007
)
1.06
"Ezetimibe has shown efficacy in the therapy of hypercholesterolemia in renal transplant patients. "( Ezetimibe treatment in hypercholesterolemic kidney transplant patients is safe and effective and reduces the decline of renal allograft function: a pilot study.
Heemann, U; Kohnle, M; Kribben, A; Nürnberger, J; Philipp, T; Türk, TR; Voropaeva, E; Witzke, O, 2008
)
3.23
"Ezetimibe has an antioxidative effect when given as monotherapy or as an add-on to the statin, simvastatin. "( Ezetimibe's effect on platelet aggregation and LDL tendency to peroxidation in hypercholesterolaemia as monotherapy or in addition to simvastatin.
Hussein, O; Itzkovich, Y; Minasian, L; Shestatski, K; Solomon, L; Zidan, J, 2008
)
3.23

Actions

Ezetimibe can inhibit both hepatic and intestinal NPC1L1. It did not cause side effects on FBG (WMD -0.62, 95% CI: -3.13 to 1.90) and HbA1c.

ExcerptReferenceRelevance
"Ezetimibe may increase the risk of intestine cancer and has a trend of increasing the risk of breast cancer. "( Impacts of ezetimibe on risks of various types of cancers: a meta-analysis and systematic review.
Bai, H; Ge, J; He, J; Hu, J; Huang, J; Li, H; Liang, X; Sun, S; Wang, X; Zhao, T, 2023
)
2.74
"Ezetimibe (EZE) can inhibit both hepatic and intestinal NPC1L1."( FGF15 promotes hepatic NPC1L1 degradation in lithogenic diet-fed mice.
Chen, H; Chen, W; Hu, F; Jiang, X; Li, S; Li, Y; Mo, P; Shan, G; Xu, G; Zhang, F, 2022
)
1.44
"Ezetimibe is known to inhibit cholesterol absorption by blocking the activity of Niemann-Pick C1 like 1 (NPC1L1) protein, and simvastatin is known to enhance NPC1L1 expression in the human body's small intestine."( A prospective mechanism and source of cholesterol uptake by Plasmodium falciparum-infected erythrocytes co-cultured with HepG2 cells.
Hayakawa, EH; Kato, H; Nardone, GA; Usukura, J, 2021
)
1.34
"Ezetimibe did not cause side effects on FBG (WMD -0.62, 95% CI: -3.13 to 1.90) and HbA1c (WMD 0.07, 95% CI: -0.07 to 0.20%)."( Effect of ezetimibe on glycemic control: a systematic review and meta-analysis of randomized controlled trials.
Shang, H; Wu, H; Wu, J, 2018
)
1.6
"Ezetimibe does not increase circulating PCSK9 concentrations while simvastatin does. "( Evidence from a randomized trial that simvastatin, but not ezetimibe, upregulates circulating PCSK9 levels.
Benjannet, S; Berthold, HK; Gouni-Berthold, I; Seidah, NG, 2013
)
2.08
"Ezetimibe-induced increase in cholesterol efflux was approximately 2.5-fold greater in mice having endogenous ATP-binding cassette G5/G8 heterodimer, the major sterol efflux transporter of enterocytes, than the knockout counterparts, suggesting that the heterodimer confers additional rapid BBM-to-lumen cholesterol efflux in response to NPC1L1 inhibition."( Ezetimibe Promotes Brush Border Membrane-to-Lumen Cholesterol Efflux in the Small Intestine.
Awata, T; Inoue, I; Katayama, S; Murakoshi, T; Nakano, T; Ono, H; Takenaka, Y, 2016
)
2.6
"Ezetimibe may increase and stabilize the anticoagulant effect of warfarin, especially in patients taking statins."( Ezetimibe enhances and stabilizes anticoagulant effect of warfarin.
Ako, J; Fujiyoshi, K; Hashikata, T; Hashimoto, T; Ishii, S; Kakizaki, R; Kameda, R; Kitasato, L; Namba, S; Nemoto, T; Shimohama, T; Tojo, T; Yamaoka-Tojo, M, 2017
)
2.62
"Ezetimibe may produce serious toxic hepatitis and prompt withdrawal is mandatory in case of a significant abnormality in liver testing after beginning or during treatment with ezetimibe."( Serious drug-induced liver disease secondary to ezetimibe.
Ariza, J; Castellote, J; Girbau, A; Rota, R; Xiol, X, 2008
)
1.32
"Ezetimibe increase high density lipoprotein (HDL)-cholesterol only in patients with baseline HDL-cholesterol above 1.3 mM/L (p < 0.05)."( Impact of ezetimibe on cholesterol subfractions in dyslipidemic cardiac transplant recipients receiving statin therapy.
Carrier, M; Cossette, M; Le, VV; Pelletier, GB; Racine, N; White, M,
)
1.26
"ezetimibe) plays a pivotal role and is often initiated or modified in rehabilitation centres."( Drug utilization of ezetimibe in rehabilitation centres: registry analysis of factors influencing prescription and effectiveness of treatment.
Benecke, H; Bestehorn, K; Karmann, B; Renner, H; Völler, H; Wegscheider, K, 2006
)
1.38
"Ezetimibe may rarely cause hepatotoxicity, severe cholestatic hepatitis, or acute autoimmune hepatitis."( Severe hepatic side effects of ezetimibe.
Becx, MC; Kuypers, KC; Seldenrijk, CA; Stolk, MF, 2006
)
2.06

Treatment

Oral treatment with ezetimibe, significantly decreased plasma lipid levels and prevented the acceleration of plaque destabilization and rupture induced by dietary oxysterol. Treatment did not affect food intake, body weight gain, adiposity, or blood pressure in mice.

ExcerptReferenceRelevance
"Ezetimibe treatment significantly ameliorated all the aforementioned parameters."( Ezetimibe alleviates acetic acid-induced ulcerative colitis in rats: targeting the Akt/NF-κB/STAT3/CXCL10 signaling axis.
Abdel-Rahman, RF; Mostafa, RE, 2023
)
3.07
"Ezetimibe treatment mitigates UC via downregulation of the Akt/NF-κB/STAT3/CXCL10 signaling axis."( Ezetimibe alleviates acetic acid-induced ulcerative colitis in rats: targeting the Akt/NF-κB/STAT3/CXCL10 signaling axis.
Abdel-Rahman, RF; Mostafa, RE, 2023
)
3.07
"Ezetimibe treatment significantly reduced the apparent absorption of 5β,6β-epoxycholesterol (5,6β-epoxy) and its levels in the proximal intestinal mucosa in OC-fed rats. "( Inhibition of Niemann-Pick C1-Like 1 by Ezetimibe Reduces Dietary 5β,6β-Epoxycholesterol Absorption in Rats.
Furukawa, Y; Imaizumi, K; Kawauchi, A; Nakamura, Y; Oku, H; Sato, M; Shirouchi, B, 2019
)
2.22
"Ezetimibe treatment for 2 weeks completely restored both biliary and fecal excretion of [(3)H]-tracer in the neutral sterol fraction in L1(LivOnly) mice."( Ezetimibe inhibits hepatic Niemann-Pick C1-Like 1 to facilitate macrophage reverse cholesterol transport in mice.
Guo, F; Jia, L; Jiang, XC; Ma, Y; Miao, H; Ou, J; Wang, N; Xie, P; Yazdanyar, A; Yu, L, 2013
)
2.55
"Ezetimibe treatment inhibited intestinal cholesterol absorption by 74% (p < 0.01), but also the bile acid sequestrant cholestyramine decreased cholesterol absorption significantly (24%, p < 0.01)."( rHDL administration increases reverse cholesterol transport in mice, but is not additive on top of ezetimibe or cholestyramine treatment.
Annema, W; Blum, D; Mary, JL; Maugeais, C; Tietge, UJ, 2013
)
1.33
"Ezetimibe/simvastatin treatment (versus atorvastatin) was a significant predictor for change in most efficacy variables."( Age, abdominal obesity, and baseline high-sensitivity C-reactive protein are associated with low-density lipoprotein cholesterol, non-high-density lipoprotein cholesterol, and apolipoprotein B responses to ezetimibe/simvastatin and atorvastatin in patient
Ballantyne, CM; Hsueh, WA; Lin, J; Lowe, RS; Robinson, JG; Rosen, JB; Shah, AK; Tershakovec, AM; Tomassini, JE,
)
1.04
"Ezetimibe/simvastatin treatment was found to be consistently more effective than atorvastatin at the specified dose comparisons across these subgroups."( Age, abdominal obesity, and baseline high-sensitivity C-reactive protein are associated with low-density lipoprotein cholesterol, non-high-density lipoprotein cholesterol, and apolipoprotein B responses to ezetimibe/simvastatin and atorvastatin in patient
Ballantyne, CM; Hsueh, WA; Lin, J; Lowe, RS; Robinson, JG; Rosen, JB; Shah, AK; Tershakovec, AM; Tomassini, JE,
)
1.04
"Ezetimibe treatment approximately doubled the flux of plasma-derived cholesterol into fecal neutral sterols, in association with increases in total fecal neutral sterol excretion, FCR of plasma cholesterol ester, and plasma de novo cholesterol synthesis. "( Inhibition of intestinal cholesterol absorption with ezetimibe increases components of reverse cholesterol transport in humans.
Boban, D; Davidson, MH; Decaris, J; Glass, A; Hellerstein, M; Killion, S; Lu, Y; Luchoomun, J; Mohammad, H; Musliner, T; Neese, R; Neff, D; Tomassini, JE; Turner, S; Villegas, D; Voogt, J, 2013
)
2.08
"Ezetimibe treatment was well tolerated in all patients and resulted in significant reductions in total cholesterol (-11.4%, p = .002), LDL-cholesterol (-20.4%, p = .003), non-HDL-cholesterol (-13.4%, p = .002) and apolipoprotein B (-9.1%, p = .021). "( Effects of ezetimibe on cholesterol metabolism in HIV-infected patients with protease inhibitor-associated dyslipidemia: a single-arm intervention trial.
Cofán, M; Forga, MT; Larrousse, M; Leyes, P; Martínez, E; Pérez-Heras, AM; Ros, E; Trabal, J, 2014
)
2.23
"Ezetimibe treatment virtually reversed all of the transgene-related phenotypes in DKO/L1(IntOnly) mice."( Genetic demonstration of intestinal NPC1L1 as a major determinant of hepatic cholesterol and blood atherogenic lipoprotein levels.
Jia, L; Ma, Y; Shi, H; Tang, W; Wang, Y; Xie, P; Xue, B; Yu, L; Zhu, H, 2014
)
1.12
"Ezetimibe treatment was given to ten patients with diabetes without statin therapy and ten patients with statin therapy. "( Impact of Ezetimibe Alone or in Addition to a Statin on Plasma PCSK9 Concentrations in Patients with Type 2 Diabetes and Hypercholesterolemia: A Pilot Study.
Doi, M; Ito, H; Miyoshi, T; Nakamura, K, 2015
)
2.26
"Ezetimibe treatment for 8weeks attenuated increases in oxycholesterols in the HCD group almost completely in liver, but reduced only levels of 4β-hydroxycholesterol in left ventricular (LV) myocardium."( The pathophysiological role of oxidized cholesterols in epicardial fat accumulation and cardiac dysfunction: a study in swine fed a high caloric diet with an inhibitor of intestinal cholesterol absorption, ezetimibe.
Fukuda, D; Hirata, Y; Kim-Kaneyama, JR; Kitagawa, T; Kurobe, H; Lei, XF; Masuzaki, H; Okawa, C; Sata, M; Sato, M; Shimabukuro, M; Soeki, T; Sugasawa, N; Takao, S; Tanaka, Y; Uematsu, E; Yagi, S; Yamada, H; Yanagi, S, 2016
)
1.34
"Ezetimibe treatment may be a beneficial and effective strategy for preventing progressing stroke."( Effects of ezetimibe and anticoagulant combined therapy on progressing stroke: a randomized, placebo-controlled study.
Shi, L; Wang, J; Wang, X; Yang, L; Zhao, J; Zhao, P, 2016
)
1.55
"Ezetimibe treatment resulted in higher tumor cholesterol."( Evidence for Feedback Regulation Following Cholesterol Lowering Therapy in a Prostate Cancer Xenograft Model.
Alfaqih, MA; Barry, WT; Dambal, SK; Dewhirst, MW; Freedland, AR; Freedland, SJ; Freeman, MR; Macias, E; Masko, EM; Muehlbauer, MJ; Newgard, CB; Phillips, TE; Pizzo, SV; Poulton, SH; Sanders, SE; Solomon, KR; Sun, S; Valilis, NA, 2017
)
1.18
"Ezetimibe treatment (10mg/day) for 6 months significantly decreased circulating levels of LDL-cholesterol, triglycerides and ADMA, while it increased HDL-cholesterol levels."( Ezetimibe decreases serum levels of asymmetric dimethylarginine (ADMA) and ameliorates renal injury in non-diabetic chronic kidney disease patients in a cholesterol-independent manner.
Adachi, H; Fujiwara, N; Kawagoe, Y; Nakamura, T; Okuda, S; Sato, E; Suzuki, T; Ueda, S; Ueda, Y; Yamagishi, S, 2009
)
2.52
"Ezetimibe/simvastatin treatment reduced campesterol levels by 68% and sitosterol levels by 62%; reductions were most pronounced in subjects with the highest cholesterol absorption markers at baseline, the so-called high absorbers (P < 0.001)."( Baseline cholesterol absorption and the response to ezetimibe/simvastatin therapy: a post-hoc analysis of the ENHANCE trial.
Groen, AK; Hutten, BA; Jakulj, L; Kastelein, JJ; Lutjohann, D; Veltri, EP; Vissers, MN, 2010
)
1.33
"Ezetimibe/simvastatin treatment resulted in a significant decrease in ALT (63.78+/-5.12 vs 32.57+/-3.92 U/L; p<0.0001) and AST (50.79+/-3.66 vs 23.68+/-3.42 U/L; p<0.0001). "( Safety and efficacy of combined ezetimibe/simvastatin treatment and simvastatin monotherapy in patients with non-alcoholic fatty liver disease.
Abel, T; Dinya, E; Eldin, MG; Fehér, J; Kovács, A, 2009
)
2.08
"Ezetimibe treatment of db/db mice significantly improved vascular endothelial function, which was associated with the restoration of the decreased phospho-Akt and phospho-endothelial nitric-oxide synthase (eNOS)."( Ezetimibe ameliorates cardiovascular complications and hepatic steatosis in obese and type 2 diabetic db/db mice.
Dong, YF; Fukuda, M; Kataoka, K; Kim-Mitsuyama, S; Nakamura, T; Nako, H; Ogawa, H; Tokutomi, Y; Yasuda, O, 2010
)
2.52
"Ezetimibe treatment decreased "inflammatory" (SAA-containing) HDL3, and may thus have restored the anti-atherogenic function of HDL particles in ESRD patients."( Ezetimibe decreases serum amyloid A levels in HDL3 in hemodialysis patients.
Hirano, T; Hyodo, T; Nakanishi, N; Nohtomi, K; Taira, T; Watanabe, T, 2010
)
3.25
"Ezetimibe treatment also had no impact on NBD-cholesterol absorption by Npc1l1(+/+) mice."( Use of NBD-cholesterol to identify a minor but NPC1L1-independent cholesterol absorption pathway in mouse intestine.
Adams, MR; Cash, JG; Hui, DY; Konaniah, E, 2011
)
1.09
"Ezetimibe treatment for 4 weeks significantly suppressed postprandial elevation in TG (area under the incremental curve, from 1419±594 to 968±32 1 mg h/dl, P<0.05), remnant lipoprotein cholesterol (from 66.9±27.6 to 38.9±15.4 mg h/dl, P<0.01) and apoB-48 (from 58.8±27.5 to 36.2±17.0 μg h/ml, P<0.05) concentrations, and postprandial endothelial dysfunction assessed by %FMD (maximum reduction in %FMD, from -2.6±1.1% to -1.2±0.8%, P<0.05), whereas no significant changes were observed in the control group."( Ezetimibe improves postprandial hyperlipemia and its induced endothelial dysfunction.
Enko, K; Ito, H; Kohno, K; Kusano, KF; Miyoshi, T; Morita, H; Nakamura, K; Yunoki, K, 2011
)
2.53
"Ezetimibe treatment significantly reduced serum levels of low-density lipoprotein cholesterol (LDL-C) and malondialdehyde-modified low-density lipoprotein (MDA-LDL). "( Ezetimibe monotherapy ameliorates vascular function in patients with hypercholesterolemia through decreasing oxidative stress.
Aihara, K; Akaike, M; Fujimoto, E; Higashida, M; Hirata, Y; Kanbara, T; Kinoshita, H; Kitagawa, T; Kitaichi, T; Kurobe, A; Kurobe, H; Matsumoto, T; Matsuoka, Y; Nakayama, T; Nishiya, M; Sata, M; Sugano, M; Sugasawa, N, 2011
)
3.25
"Ezetimibe treatment has been shown to cause significant decreases in plasma cholesterol levels in patients with hypercholesterolemia and familial hypercholesterolemia."( Ezetimibe ameliorates intestinal chylomicron overproduction and improves glucose tolerance in a diet-induced hamster model of insulin resistance.
Adeli, K; Baker, C; Hussain, MM; Iqbal, J; Lino, M; Naples, M, 2012
)
2.54
"Ezetimibe treatment significantly decreased glycated haemoglobin (HbA(1c)), low-density lipoprotein-cholesterol (LDL-C), triglycerides and UAE, and significantly increased high-density lipoprotein-cholesterol and albumin. "( Ezetimibe reduces urinary albumin excretion in hypercholesterolaemic type 2 diabetes patients with microalbuminuria.
Amaha, M; Inoue, H; Kawagoe, Y; Maeda, S; Nakamura, T; Sato, E; Yamagishi, SI, 2012
)
3.26
"Ezetimibe treatment in the high-potency group produced significantly greater reductions from baseline in LDL-C than medium-/low-potency groups (-29.1% vs."( Effects of ezetimibe added to statin therapy on markers of cholesterol absorption and synthesis and LDL-C lowering in hyperlipidemic patients.
Lin, J; Lowe, RS; Schaefer, EJ; Shah, AK; Tershakovec, AM; Thongtang, N; Tomassini, JE, 2012
)
1.49
"Ezetimibe treatment improved other lipid parameters across groups, including triglyceride, high-density lipoprotein cholesterol, non-high-density ilpoprotein cholesterol, and total cholesterol levels."( Effectiveness of ezetimibe added to ongoing statin therapy in modifying lipid profiles and low-density lipoprotein cholesterol goal attainment in patients of different races and ethnicities: a substudy of the Ezetimibe add-on to statin for effectiveness t
Battisti, WP; Brady, WE; Denke, MA; Gazzara, RA; McBride, PE; Palmisano, J; Pearson, TA, 2006
)
1.39
"Ezetimibe treatment significantly reduced aortic root (57%) and coronary arterial (68%) atherosclerosis, cardiomegaly (24%) and cardiac fibrosis (57%), and prolonged the lives of the mice (27%)."( Inhibition of intestinal absorption of cholesterol by ezetimibe or bile acids by SC-435 alters lipoprotein metabolism and extends the lifespan of SR-BI/apoE double knockout mice.
Acton, S; Braun, A; Broschat, KO; Krieger, M; Krul, ES; Napawan, N; Stagliano, N; Yesilaltay, A, 2008
)
1.32
"Treatment with ezetimibe attenuated the IL-1β-induced degradation of the extracellular matrix, including aggrecan and collagen II. "( Ezetimibe Prevents IL-1β-induced Inflammatory Reaction in Mouse Chondrocytes
Han, J; Hu, T; Luo, J; Shen, X; Weng, Q; Zhang, Y, 2022
)
2.52
"Treatment with ezetimibe (2.4%) or PCSK9 inhibitors (0.24%) was rare and 62.6% of the overall cohort had an LDL-C above target at ≥70 mg/dl."( Lipid-lowering treatment among older patients with atherosclerotic cardiovascular disease.
Calvert, SB; Cziraky, MJ; Eapen, Z; Granger, CB; Haynes, K; Nanna, MG; Nelson, AJ; Pagidipati, NJ; Shambhu, S, 2023
)
1.25
"Treatment with ezetimibe, an FDA-approved drug, resulted in decreased levels of free cholesterol and neutral lipids, and a reduction of bacterial growth in vivo."( Early cell-autonomous accumulation of neutral lipids during infection promotes mycobacterial growth.
McClean, CM; Tobin, DM, 2020
)
0.9
"Treatment with ezetimibe resulted in significant FMD changes in MetS patients (from 3.4 to 4.9%, P = 0.002), but not in control patients (from 5.1 to 5.4%, P = 0.216)."( Impact of decreased insulin resistance by ezetimibe on postprandial lipid profiles and endothelial functions in obese, non-diabetic-metabolic syndrome patients with coronary artery disease.
Endo, H; Kanazawa, M; Kondo, M; Nakamura, A; Nozaki, E; Sato, K; Takahashi, T, 2019
)
1.12
"Treatment with ezetimibe reduced hepatic steatosis, insulin levels, and glucose production from pyruvate in mice fed the high-fat diet, suggesting a reduction of insulin resistance in the liver."( Ezetimibe prevents hepatic steatosis induced by a high-fat but not a high-fructose diet.
Kashiwagi, A; Kume, S; Maegawa, H; Maeno, Y; Morino, K; Nagai, Y; Nishio, Y; Sekine, O; Ugi, S; Ushio, M; Yoshizaki, T, 2013
)
2.17
"The treatment of ezetimibe or atorvastatin alone decreased effectively the deposition of lipids in the vascular wall, and a combined dose showed a synergistic effect."( Characterization of the pharmaceutical effect of drugs on atherosclerotic lesions in vivo using integrated fluorescence imaging and Raman spectral measurements.
Chang, WT; Huang, SK; Liau, I; Yang, YC, 2014
)
0.73
"Co-treatment with ezetimibe (3 μmol/L) significantly decreased the cellular levels of TC, CE and FC, which was accompanied by elevation of caveolin-1 expression, and by a reduction of SREBP-1 expression and nuclear translocation."( Ezetimibe suppresses cholesterol accumulation in lipid-loaded vascular smooth muscle cells in vitro via MAPK signaling.
Gong, YZ; Li, SX; Liao, DF; Qin, L; Yang, YB; Yang, YX; Zhang, CP; Zhu, N, 2014
)
2.17
"Treatment with ezetimibe was associated with decreased cholesterol absorption markers (campesterol-to-cholesterol ratio -43.0%, p = .001; sitosterol-to-cholesterol ratio -41.9%, p = .001) and increased synthesis markers (lathosterol-to-cholesterol ratio 53.2%, p = .005)."( Effects of ezetimibe on cholesterol metabolism in HIV-infected patients with protease inhibitor-associated dyslipidemia: a single-arm intervention trial.
Cofán, M; Forga, MT; Larrousse, M; Leyes, P; Martínez, E; Pérez-Heras, AM; Ros, E; Trabal, J, 2014
)
1.13
"Treatment with ezetimibe significantly increased intestinal LDLR (+16.2%; P = .01), 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoAR; +14.0%; P = .04) and acetyl-Coenzyme A acetyltransferase 2 (ACAT-2) mRNA expression (+12.5%; P = .03)."( Ezetimibe increases intestinal expression of the LDL receptor gene in dyslipidaemic men with insulin resistance.
Couture, P; Drouin-Chartier, JP; Lamarche, B; Lemelin, V; Lépine, MC; Tremblay, AJ, 2016
)
2.22
"Co-treatment with ezetimibe significantly reduced plasma cholesterol (by 76%; from 1592 to 381mg/dL) and LDL cholesterol (by 78%; from 1515 to 319mg/dL), and increased HDL cholesterol (by 187%; from 16 to 46mg/dL) in high-fat diet mice."( Vascular protective effects of ezetimibe in ApoE-deficient mice.
Hanayama, R; Hayashi, H; Koriyama, H; Mori, M; Morishita, R; Nakagami, H; Osako, MK; Shimizu, H; Takami, Y, 2009
)
0.96
"Treatment with ezetimibe 10 mg/day led to significant mean percentage reductions from baseline in plasma concentrations of sitosterol (-43.9%; p < 0.001), campesterol (-50.8%; p < 0.001), low-density lipoprotein (LDL) sterols (-13.1%; p < 0.050), total sterols (-10.3%; p < 0.050) and apolipoprotein (apo) B (-10.1%; p < 0.050). "( Long-term efficacy and safety of ezetimibe 10 mg in patients with homozygous sitosterolemia: a 2-year, open-label extension study.
Johnson-Levonas, AO; Lin, J; Lütjohann, D; Macdonell, G; Musliner, T; Sapre, A; Shah, A; Sirah, W; von Bergmann, K, 2008
)
0.98
"Treatment with ezetimibe reduced the fasting serum insulin level (p<0.05) and HbA1c (p<0.05), increased serum adiponectin (p<0.01), and showed a significant decrease of high-sensitive C-reactive protein (hsCRP, p<0.01)."( The effects of ezetimibe on surrogate markers of cholesterol absorption and synthesis in Japanese patients with dyslipidemia.
Hasegawa, K; Hiramitsu, S; Hishida, H; Ishiguro, Y; Kani, A; Kato, K; Matsubara, Y; Matsuyama, H; Noba, M; Ozaki, Y; Uemura, A; Yamada, K; Yoshida, S, 2010
)
1.05
"Treatment with ezetimibe/simvastatine was effective improving the lipid profile as well as the endothelial function of these patients."( Effect of ezetimibe-simvastatine over endothelial dysfunction in dyslipidemic patients: assessment by 13N-ammonia positron emission tomography.
Alexanderson, E; Alexanderson, G; Calleja, R; García-Rojas, L; Jácome, R; Jiménez, M; Martínez, A; Meave, A; Ochoa, JM, 2010
)
1.1
"Treatment with ezetimibe did not change HDL-cholesterol, triglyceride and HbA1c values but caused a significant reduction in remnant like particles-cholesterol (RLP-C, p<0.05) and high-sensitive C-reactive protein (hsCRP, p<0.05)."( Efficacy and safety of ezetimibe in patients undergoing hemodialysis.
Hattori, S; Hattori, Y, 2010
)
1.01
"Treatment with ezetimibe/simvastatin resulted in significantly greater reductions in LDL compared with rosuvastatin or atorvastatin (37 vs 25 and 26 mg/dL, respectively; P <0.05). "( Comparative efficacy of ezetimibe/simvastatin, rosuvastatin, and atorvastatin in uncontrolled hyperlipidemia patients.
Furman, A; Lopez, JR; Malmstrom, RA; Meier, JL; Schaefer, S, 2011
)
1.03
"Men treated with ezetimibe+statin experienced significantly greater changes in LDL-C (p = 0.0066), non-HDL-C, total cholesterol, triglycerides, HDL-C, apolipoprotein A-I (all p < 0.0001) and apolipoprotein B (p = 0.0055) compared with women treated with ezetimibe+statin."( Response by sex to statin plus ezetimibe or statin monotherapy: a pooled analysis of 22,231 hyperlipidemic patients.
Abramson, BL; Benlian, P; Hanson, ME; Lin, J; Shah, A; Tershakovec, AM, 2011
)
0.98
"Dual treatment with ezetimibe/simvastatin is more effective than monotherapy with an HMG-CoA reductase inhibitor (statin), and the addition of ezetimibe to current statin therapy is more effective than doubling the statin dose."( Ezetimibe/simvastatin: a guide to its clinical use in hypercholesterolemia.
Lyseng-Williamson, KA, 2012
)
2.14
"Treatment with ezetimibe in an amount sufficient to block intestinal cholesterol absorption caused small intestinal transit time to return to normal."( Augmented cholesterol absorption and sarcolemmal sterol enrichment slow small intestinal transit in mice, contributing to cholesterol cholelithogenesis.
Andrade, JD; Carey, MC; Fox, JG; Kotecha, VR; Xie, M, 2012
)
0.72
"Treatment with ezetimibe did not affect food intake, body weight gain, adiposity, or blood pressure in db/db mice. "( Ezetimibe ameliorates early diabetic nephropathy in db/db mice.
Arai, H; Matsubara, T; Minami, M; Murayama, T; Tamura, Y; Yokode, M, 2012
)
2.17
"Oral treatment with ezetimibe, significantly decreased plasma lipid levels and prevented the acceleration of plaque destabilization and rupture induced by dietary oxysterol."( Dietary cholesterol oxidation products accelerate plaque destabilization and rupture associated with monocyte infiltration/activation via the MCP-1-CCR2 pathway in mouse brachiocephalic arteries: therapeutic effects of ezetimibe.
Egashira, K; Katsuki, S; Matoba, T; Nakano, K; Osada, K; Sato, K; Sawamura, T; Sunagawa, K, 2012
)
0.88
"Treatment with ezetimibe significantly improved lipid profiles. "( Effects of ezetimibe on visceral fat in the metabolic syndrome: a randomised controlled study.
Dohi, Y; Goto, Y; Hashimoto, T; Kimura, G; Okado, T; Takase, H, 2012
)
1.12
"Treatment with ezetimibe inhibited establishment of intrahepatic cccDNA and expression of viral replication markers when cells were infected with HBV virions, while we observed no effect when the HBV viral genome was transduced via an adenoviral vector."( Ezetimibe blocks hepatitis B virus infection after virus uptake into hepatocytes.
Esser, K; Lucifora, J; Protzer, U, 2013
)
2.17
"Treatment with ezetimibe/simvastatin also led to greater reductions in total cholesterol, triglyceride, non-high-density lipoprotein cholesterol, and apolipoprotein B levels compared with simvastatin alone; both treatments increased high-density lipoprotein cholesterol levels similarly."( Efficacy and safety of ezetimibe coadministered with simvastatin in patients with primary hypercholesterolemia: a randomized, double-blind, placebo-controlled trial.
Capece, R; Goldberg, AC; Liu, J; Mitchel, YB; Sapre, A, 2004
)
0.97
"Treatment with ezetimibe + statin led to significantly greater reductions in low-density lipoprotein cholesterol (LDL-C), total cholesterol, triglycerides, non-high-density lipoprotein cholesterol (non-HDL-C), apolipoprotein B and increases in HDL-C, compared to statin alone."( Efficacy and safety of ezetimibe coadministered with statins: randomised, placebo-controlled, blinded experience in 2382 patients with primary hypercholesterolemia.
Ballantyne, CM; Davidson, MH; Kerzner, B; Lipka, L; Melani, L; Sager, PT; Strony, J; Suresh, R; Veltri, E, 2004
)
0.97
"Treatment with ezetimibe reduced TC, LDL-, and triglycerides, and increased high-density lipoprotein cholesterol (HDL-) significantly from baseline, and to similar extents, in both groups, lowering TC from baseline by 13.7% in APOE3/APOE3 homozygotes compared with 12.1% in epsilon4 allele carriers (p = 0.139); LDL-C by 22.8% (vs. "( Effects of ezetimibe on lipids and lipoproteins in patients with hypercholesterolemia and different apolipoprotein E genotypes.
Dani, G; Fazekas, O; Katona, A; Kovacs, H; Mark, L; Szüle, O, 2007
)
1.08
"Treatment with ezetimibe, simvastatin or their combination does not alter circulating levels of adiponectin, leptin or resistin in adult healthy men."( Short-term treatment with ezetimibe, simvastatin or their combination does not alter circulating adiponectin, resistin or leptin levels in healthy men.
Berthold, HK; Chamberland, JP; Gouni-Berthold, I; Krone, W; Mantzoros, CS, 2008
)
1
"Treatment with ezetimibe in addition to simvastatin has an additive antioxidative effect on LDL."( Ezetimibe's effect on platelet aggregation and LDL tendency to peroxidation in hypercholesterolaemia as monotherapy or in addition to simvastatin.
Hussein, O; Itzkovich, Y; Minasian, L; Shestatski, K; Solomon, L; Zidan, J, 2008
)
2.13
"(2) Treatment with ezetimibe abolishes the increases in serum and liver cholesterol."( Dramatically increased intestinal absorption of cholesterol following hypophysectomy is normalized by thyroid hormone.
Angelin, B; Bonde, Y; Gälman, C; Matasconi, M; Rudling, M, 2008
)
0.66
"Treatment with ezetimibe promoted the dissolution of gallstones by forming an abundance of unsaturated micelles."( Effect of ezetimibe on the prevention and dissolution of cholesterol gallstones.
Mendez-Sanchez, N; Portincasa, P; Uribe, M; Wang, DQ; Wang, HH, 2008
)
1.09

Toxicity

Ezetimibe and simvastatin treatment, either as a single pill or the combined use of the individual compounds, offers limited additional risk compared with statin monotherapy. The combination therapy is safe in a long-term treatment in Japanese patients with combined hyperlipidemia.

ExcerptReferenceRelevance
" Ezetimibe was safe and well tolerated."( Efficacy and safety of ezetimibe coadministered with atorvastatin or simvastatin in patients with homozygous familial hypercholesterolemia.
Bruckert, E; Gagné, C; Gaudet, D, 2002
)
1.54
" Safety evaluations included adverse event (AE) reports and laboratory test results."( Long-term safety and tolerability profile of ezetimibe and atorvastatin coadministration therapy in patients with primary hypercholesterolaemia.
Alizadeh, J; Ballantyne, CM; Lipka, LJ; Sager, PT; Strony, J; Suresh, R; Veltri, EP, 2004
)
0.58
" Ezetimibe plus statin therapy was generally well tolerated, with similar incidence of adverse events, serious adverse events and changes in liver function and muscle enzymes in the given age groups compared with statin therapy alone."( Efficacy and safety of coadministration of ezetimibe and statins in elderly patients with primary hypercholesterolaemia.
Lipka, L; Sager, P; Strony, J; Suresh, R; Veltri, E; Yang, B, 2004
)
1.5
" There were no clinically meaningful differences between the EZE and PBO groups with regard to the incidence of treatment-related adverse events (AEs) (19% vs 17%, respectively), discontinuations due to AEs (7% vs 10%), serious AEs (12% vs 17%), consecutive elevations in liver function tests > or =3 times the upper limit of normal (ULN) (0."( Long-term safety and, tolerability profiles and lipid-modifying efficacy of ezetimibe coadministered with ongoing simvastatin treatment: a multicenter, randomized, double-blind, placebo-controlled, 48-week extension study.
Cho, M; Gagné, C; Gumbiner, B; Johnson-Levonas, AO; Masana, L; Mata, P; Meehan, A; Sirah, W; Troxell, JK, 2005
)
0.56
" There were no serious adverse events caused by study treatment."( The second United Kingdom Heart and Renal Protection (UK-HARP-II) Study: a randomized controlled study of the biochemical safety and efficacy of adding ezetimibe to simvastatin as initial therapy among patients with CKD.
Adu, D; Altmann, P; Armitage, J; Baigent, C; Ball, S; Baxter, A; Blackwell, L; Cairns, HS; Carr, S; Collins, R; Kourellias, K; Landray, M; Leaper, C; Rogerson, M; Scoble, JE; Tomson, CR; Warwick, G; Wheeler, DC, 2006
)
0.53
" Tolerability was assessed by adverse event reports and laboratory and vital signs assessments throughout the study."( Comparison of the lipid-modifying efficacy and safety profiles of ezetimibe coadministered with simvastatin in older versus younger patients with primary hypercholesterolemia: a post Hoc analysis of subpopulations from three pooled clinical trials.
Davidson, M; Feldman, T; Maccubbin, D; Meehan, A; Mitchel, Y; Shah, A; Tribble, D; Veltri, E; Zakson, M, 2006
)
0.57
" Clinical chemistry profiles and proportions of adverse events were similar in both groups at baseline and follow-up."( Efficacy, safety and LDL-C goal attainment of ezetimibe 10 mg-simvastatin 20 mg vs. placebo-simvastatin 20 mg in UK-based adults with coronary heart disease and hypercholesterolaemia.
Hughes, EA; Patel, JV, 2006
)
0.59
" However, case reports and pharmacokinetic data disclose 3 kinds of adverse effects: (1) the decreased absorption of concomitant medications and sometimes of certain vitamins; (2) the physicochemical alteration of intestinal contents leading to constipation and, very rarely, intestinal obstruction; and (3) modest increases in plasma triglyceride levels due to the alteration of hepatic lipid metabolism."( Safety considerations with gastrointestinally active lipid-lowering drugs.
Armani, A; Guyton, JR; Jacobson, TA; McKenney, JM, 2007
)
0.34
" Clinical chemistry profiles and the incidence of adverse events were similar in both groups."( Efficacy and safety of ezetimibe co-administered with atorvastatin in untreated patients with primary hypercholesterolaemia and coronary heart disease.
Blagden, MD; Chipperfield, R, 2007
)
0.65
" Ezetimibe was well tolerated; no hepatic or muscle-related adverse events were observed."( Effectiveness and safety of ezetimibe added to statin therapy in patients with primary dyslipidaemia not achieving the LDL-C treatment goal on statin monotherapy.
Carranza, J; Cervantes, JL; Fernández, P; González, CA; Leyva, JL; Morales, E; Pavía, A; Redding, FJ; Robles, FJ; Rodríguez, L; Rubio-Guerra, AF; Yza, R; Zacarías, JL, 2007
)
1.54
"Addition of ezetimibe to statin treatment was both efficacious and safe when used for further reduction of serum LDL-C in dyslipidaemic patients who had not reached their LDL-C treatment goal while taking statin monotherapy."( Effectiveness and safety of ezetimibe added to statin therapy in patients with primary dyslipidaemia not achieving the LDL-C treatment goal on statin monotherapy.
Carranza, J; Cervantes, JL; Fernández, P; González, CA; Leyva, JL; Morales, E; Pavía, A; Redding, FJ; Robles, FJ; Rodríguez, L; Rubio-Guerra, AF; Yza, R; Zacarías, JL, 2007
)
1.01
" Moreover, we aimed to comment on the possible drug interactions of ezetimibe and present current guidelines regarding its safe use."( Ezetimibe-associated adverse effects: what the clinician needs to know.
Elisaf, MS; Florentin, M; Liberopoulos, EN, 2008
)
2.02
"Compelling evidence from the majority of the data reviewed here showed that adverse effects associated with ezetimibe use are few and mild without having been associated with serious clinical outcomes."( Ezetimibe-associated adverse effects: what the clinician needs to know.
Elisaf, MS; Florentin, M; Liberopoulos, EN, 2008
)
2
"Ezetimibe is a safe alternative option for hyperlipidaemic patients intolerant to other lipid lowering drugs as well as a beneficial supplementary agent for patients who do not reach the recommended serum cholesterol level with their current hypolipidaemic treatment."( Ezetimibe-associated adverse effects: what the clinician needs to know.
Elisaf, MS; Florentin, M; Liberopoulos, EN, 2008
)
3.23
"001) because of clinical adverse experiences (primarily flushing)."( Lipid-altering efficacy and safety of ezetimibe/simvastatin coadministered with extended-release niacin in patients with type IIa or type IIb hyperlipidemia.
Brown, BG; Fazio, S; Guyton, JR; Polis, A; Tershakovec, AM; Tomassini, JE, 2008
)
0.62
" Adverse event (AE) reports for EZE monotherapy-treated patients were summarised for 3-month intervals to allow for comparison with the placebo group of the 3-month base studies."( Safety and efficacy of ezetimibe monotherapy in 1624 primary hypercholesterolaemic patients for up to 2 years.
Dujovne, CA; Maccubbin, D; McCrary Sisk, C; Strony, J; Suresh, R; Veltri, E, 2008
)
0.66
" During the extension study, investigators assessed adverse events (AEs)."( Long-term (48-week) safety of ezetimibe 10 mg/day coadministered with simvastatin compared to simvastatin alone in patients with primary hypercholesterolemia.
Bays, H; Capece, R; Liu, J; Sapre, A; Taggart, W; Tershakovec, A, 2008
)
0.63
" Safety and tolerability were assessed through clinical and laboratory adverse experiences (AEs)."( Long-term safety and tolerability of ezetimibe coadministered with simvastatin in hypercholesterolemic patients: a randomized, 12-month double-blind extension study.
Hanson, ME; Strony, J; Veltri, EP; Yang, B, 2008
)
0.62
" CPK surveillance is recommended because of a slight continued risk of adverse effects."( The efficacy and safety of ezetimibe for treatment of dyslipidemia after heart transplantation.
Castro-Beiras, A; Crespo-Leiro, MG; Flores, X; Franco, R; Grille, Z; Marzoa, R; Mosquera, V; Naya, C; Paniagua, MJ; Rodriguez, JA, 2008
)
0.64
" The incidences of clinical and laboratory adverse experiences were generally similar between groups."( Efficacy and safety of ezetimibe added on to atorvastatin (20 mg) versus uptitration of atorvastatin (to 40 mg) in hypercholesterolemic patients at moderately high risk for coronary heart disease.
Bays, HE; Bird, SR; Conard, SE; Leiter, LA; Lowe, RS; Rubino, J; Tershakovec, AM; Tomassini, JE, 2008
)
0.66
" Safety and tolerability profiles and incidence of liver and muscle adverse experiences were generally similar between groups."( Efficacy and safety of ezetimibe added on to atorvastatin (40 mg) compared with uptitration of atorvastatin (to 80 mg) in hypercholesterolemic patients at high risk of coronary heart disease.
Bays, H; Bird, S; Conard, S; Hanson, ME; Leiter, LA; Rubino, J; Tershakovec, AM; Tomassini, JE, 2008
)
0.66
"These findings indicate that ezetimibe/simvastatin combination therapy is safe and effective in patients with type 2 diabetes and nonalcoholic fatty liver disease."( [Efficacy and safety of ezetimibe/simvastatin combination therapy in patients with type 2 diabetes and nonalcoholic fatty liver disease].
Abel, T; Dinya, E; Fehér, J; Gamal Eldin, M; Kovács, A, 2009
)
0.95
" The incidence of liver, muscle, and gastrointestinal-, hepatitis- and allergic reaction/rash-related adverse events were low and generally similar to those in previous studies of ezetimibe/simvastatin and/or atorvastatin."( Lipid-altering efficacy and safety of ezetimibe/simvastatin versus atorvastatin in patients with hypercholesterolemia and the metabolic syndrome (from the VYMET study).
Adewale, AJ; Ballantyne, CM; Grundy, SM; Hsueh, WA; Parving, HH; Polis, AB; Robinson, JG; Rosen, JB; Tershakovec, AM; Tomassini, JE, 2009
)
0.82
" Efficacy and safety were evaluated using lipid profiles, trough calcineurin inhibitor levels, allograft function, and adverse effects."( The efficacy and safety of ezetimibe and low-dose simvastatin as a primary treatment for dyslipidemia in renal transplant recipients.
Choi, BS; Hwang, HS; Hyoung, BJ; Jeon, YJ; Kim, YS; Lee, SY; Song, JC; Yang, CW; Yoon, HE, 2009
)
0.65
" No significant change in the trough calcineurin inhibitor levels or allograft function occurred, and no serious adverse effects were observed."( The efficacy and safety of ezetimibe and low-dose simvastatin as a primary treatment for dyslipidemia in renal transplant recipients.
Choi, BS; Hwang, HS; Hyoung, BJ; Jeon, YJ; Kim, YS; Lee, SY; Song, JC; Yang, CW; Yoon, HE, 2009
)
0.65
"Ezetimibe and low-dose statin treatment is safe and effective as a primary treatment for dyslipidemia in renal transplant patients."( The efficacy and safety of ezetimibe and low-dose simvastatin as a primary treatment for dyslipidemia in renal transplant recipients.
Choi, BS; Hwang, HS; Hyoung, BJ; Jeon, YJ; Kim, YS; Lee, SY; Song, JC; Yang, CW; Yoon, HE, 2009
)
2.09
"Statins are safe in PBC patients who might benefit from their use."( Statins in primary biliary cirrhosis: are they safe?
Abu Rajab, M; Kaplan, MM, 2010
)
0.36
"These results showed that both the combined ezetimibe/simvastatin treatment and the simvastatin monotherapy proved to be effective and safe in patients with NAFLD and in cases of high cardiovascular risk."( Safety and efficacy of combined ezetimibe/simvastatin treatment and simvastatin monotherapy in patients with non-alcoholic fatty liver disease.
Abel, T; Dinya, E; Eldin, MG; Fehér, J; Kovács, A, 2009
)
0.9
" The primary end point, the safety of E/S plus niacin, included prespecified adverse events (ie, liver, muscle, discontinuations due to flushing, gallbladder-related, cholecystectomy, fasting glucose changes, new-onset diabetes)."( Long-term safety and efficacy of triple combination ezetimibe/simvastatin plus extended-release niacin in patients with hyperlipidemia.
Adewale, AJ; Fazio, S; Guyton, JR; Polis, AB; Ryan, NW; Tershakovec, AM; Tomassini, JE, 2010
)
0.61
" Overall, adverse events were similar in the 2 treatment groups."( Efficacy and safety of fenofibric acid in combination with atorvastatin and ezetimibe in patients with mixed dyslipidemia.
Goldberg, AC; Jones, PH; Kelly, MT; Knapp, HR; Setze, CM; Sleep, DJ; Stolzenbach, JC, 2010
)
0.59
" Incidences of adverse events or creatine kinase elevations were similar between groups."( Lipid-altering efficacy and safety profile of combination therapy with ezetimibe/statin vs. statin monotherapy in patients with and without diabetes: an analysis of pooled data from 27 clinical trials.
Betteridge, DJ; Brudi, P; Farnier, M; Guyton, JR; Johnson-Levonas, AO; Leiter, LA; Lin, J; Shah, A, 2011
)
0.6
"Under standard clinical practice conditions, ezetimibe appears to be effective and safe for the control LDLc, thus making it possible to reach the therapeutic objectives proposed by the ATP-III in a high number of patients, especially when associated to statins."( [Efficacy and safety of ezetimibe in vascular risk units].
Díaz Díaz, JL; Díaz Peromingo, JA; Martínez Ramonde, T; Pena Seijo, M; Pose Reino, A; Suárez Tembra, M, 2011
)
0.94
" Adverse experiences were generally comparable among the groups."( Safety and efficacy of ezetimibe added on to rosuvastatin 5 or 10 mg versus up-titration of rosuvastatin in patients with hypercholesterolemia (the ACTE Study).
Bays, HE; Davidson, MH; Flaim, D; Jones-Burton, C; Lowe, RS; Massaad, R; Tershakovec, AM, 2011
)
0.68
" Both monotherapy and combination therapy groups had similar incidences of all types of adverse events."( Retrospective study on antihyperlipidemic efficacy and safety of simvastatin, ezetimibe and their combination in Korean adults.
Bae, JW; Choi, CI; Jang, CG; Kim, MJ; Lee, SY; Lee, YH, 2011
)
0.6
" The levels of LDL-C in the A+E group were significantly lower than those in the A group at follow-up, whereas there were no differences in major adverse cardiac events, in-stent restenosis, or in-stent % diameter stenosis (DS) between the groups."( Comparison of the efficacy and safety of statin and statin/ezetimibe therapy after coronary stent implantation in patients with stable angina.
Arimura, T; Ike, A; Iwata, A; Kawamura, A; Miura, S; Nishikawa, H; Saku, K; Sugihara, M, 2012
)
0.62
" No treatment-related serious adverse events occurred."( Efficacy, safety, and tolerability of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 in combination with a statin in patients with hypercholesterolaemia (LAPLACE-TIMI 57): a randomised, placebo-controlled, dose-ranging, phase 2 stu
Abrahamsen, TE; Desai, NR; Giugliano, RP; Hoffman, EB; Huang, F; Kohli, P; Liu, T; McDonald, ST; Mohanavelu, S; Rogers, WJ; Sabatine, MS; Scott, R; Somaratne, R; Wasserman, SM, 2012
)
0.38
"63 hyperlipidemic patients with statin induced adverse effects were involved in the study."( Effect of apolipoprotein E genotypes on the efficacy of ezetimibe monotherapy in patients with statin induced adverse effects.
Balogh, I; Harangi, J; Harangi, M; Köbling, T; Márk, L; Paragh, G; Seres, I; Varga, J, 2013
)
0.64
" Reports of adverse experiences were generally similar among groups."( Efficacy and safety of ezetimibe added to atorvastatin versus atorvastatin uptitration or switching to rosuvastatin in patients with primary hypercholesterolemia.
Averna, M; Bays, HE; Brudi, P; De Pellegrin, A; Farnier, M; Giezek, H; Lee, R; Lowe, RS; Majul, C; Muller-Wieland, D; Triscari, J, 2013
)
0.7
" Safety of the combination was examined in terms of the type, onset, and severity of adverse drug reactions (ADRs)."( Safety and efficacy of long-term combination therapy with bezafibrate and ezetimibe in patients with dyslipidemia in the prospective, observational J-COMPATIBLE study.
Abe, K; Taneyama, T; Teramoto, T, 2013
)
0.62
"Bezafibrate in combination with ezetimibe is safe and effective, and is potentially useful for comprehensive management of dyslipidemia."( Safety and efficacy of long-term combination therapy with bezafibrate and ezetimibe in patients with dyslipidemia in the prospective, observational J-COMPATIBLE study.
Abe, K; Taneyama, T; Teramoto, T, 2013
)
0.9
" We aimed to compare the efficacy of and adverse effects from statin uptitration versus statin in combination with ezetimibe since only a few studies have addressed this question."( Comparative efficacy and adverse effects of the addition of ezetimibe to statin versus statin titration in chronic kidney disease patients.
Kumagai, H; Shuto, H; Suzuki, H; Watanabe, Y, 2013
)
0.84
" The observation period was 1 year during which time patients were checked regularly in clinic for adverse effects as well as for usual laboratory examinations."( Comparative efficacy and adverse effects of the addition of ezetimibe to statin versus statin titration in chronic kidney disease patients.
Kumagai, H; Shuto, H; Suzuki, H; Watanabe, Y, 2013
)
0.63
" No serious adverse effects such as rhabdomyolysis were noted in either group."( Comparative efficacy and adverse effects of the addition of ezetimibe to statin versus statin titration in chronic kidney disease patients.
Kumagai, H; Shuto, H; Suzuki, H; Watanabe, Y, 2013
)
0.63
"When statin uptitration produces adverse effects such as myopathy, combination therapy with ezetimibe is recommended instead of statin alone."( Comparative efficacy and adverse effects of the addition of ezetimibe to statin versus statin titration in chronic kidney disease patients.
Kumagai, H; Shuto, H; Suzuki, H; Watanabe, Y, 2013
)
0.85
" However, the ability to detect potentially beneficial changes in other lipoproteins such as lipoprotein (a), triglycerides, high-density lipoprotein cholesterol (HDL-C), and apolipoprotein (Apo) A1, and adverse events (AEs) was limited by sample sizes of individual trials."( Efficacy and safety of evolocumab (AMG 145), a fully human monoclonal antibody to PCSK9, in hyperlipidaemic patients on various background lipid therapies: pooled analysis of 1359 patients in four phase 2 trials.
Albizem, M; Giugliano, RP; Kim, JB; Koren, MJ; Liu, T; Raal, FJ; Roth, EM; Sabatine, MS; Scott, R; Somaratne, R; Stein, EA; Sullivan, D; Wasserman, SM; Weiss, R; Yang, J, 2014
)
0.4
" Adverse events (AEs) and serious AEs with evolocumab were reported in 56."( Efficacy and safety of evolocumab (AMG 145), a fully human monoclonal antibody to PCSK9, in hyperlipidaemic patients on various background lipid therapies: pooled analysis of 1359 patients in four phase 2 trials.
Albizem, M; Giugliano, RP; Kim, JB; Koren, MJ; Liu, T; Raal, FJ; Roth, EM; Sabatine, MS; Scott, R; Somaratne, R; Stein, EA; Sullivan, D; Wasserman, SM; Weiss, R; Yang, J, 2014
)
0.4
" Intolerance was defined as inability to take at least 2 different statins because of muscle-related adverse events (AEs), 1 at the lowest approved starting dose."( Efficacy and safety of alirocumab, a monoclonal antibody to PCSK9, in statin-intolerant patients: design and rationale of ODYSSEY ALTERNATIVE, a randomized phase 3 trial.
Baccara-Dinet, MT; Bruckert, E; Gipe, D; Guyton, JR; Jacobson, TA; Moriarty, PM; Thompson, PD,
)
0.13
" This class side effect appears to be dose dependent, with more lipophilic statin (i."( Risk identification and possible countermeasures for muscle adverse effects during statin therapy.
Macchi, C; Magni, P; Morlotti, B; Ruscica, M; Sirtori, CR, 2015
)
0.42
"The incidence of adverse events was similar between ezetimibe-statin combination therapy and statin monotherapy; thus, we recommend combination therapy for patients with hypercholesterolaemia at high risk for cardiovascular and cerebrovascular disease."( Safety of coadministration of ezetimibe and statins in patients with hypercholesterolaemia: a meta-analysis.
Huang, W; Luo, L; Ren, F; Tang, L; Yuan, X; Zheng, Y; Zhu, H, 2015
)
0.96
" Alirocumab was generally well tolerated, with no evidence of an excess of treatment-emergent adverse events."( Efficacy and safety of alirocumab in high cardiovascular risk patients with inadequately controlled hypercholesterolaemia on maximally tolerated doses of statins: the ODYSSEY COMBO II randomized controlled trial.
Blom, D; Cannon, CP; Cariou, B; Chaudhari, U; Colhoun, HM; Lorenzato, C; McKenney, JM; Pordy, R, 2015
)
0.42
" Two authors independently selected trials fulfilling these criteria: RCTs comparing Ezetimibe±statin or another lipid-lowering drug against placebo, or against the same lipid-lowering drug at the same dosage, with a follow-up at least 24 weeks and one or more of these outcomes: all-cause mortality, cardiovascular (CV) mortality, stroke, myocardial infarction (MI), cancer, serious adverse events (SAEs); we assessed the risk of bias using the Cochrane checklist."( Clinical efficacy and safety of Ezetimibe on major cardiovascular endpoints: systematic review and meta-analysis of randomized controlled trials.
Battaggia, A; Donzelli, A; Font, M; Galvano, A; Molteni, D, 2015
)
0.92
"The addition of ezetimibe to rosuvastatin appears to be safe in patients with HIV."( Lipid lowering efficacy and safety of Ezetimibe combined with rosuvastatin compared with titrating rosuvastatin monotherapy in HIV-positive patients.
Bennett, MT; Bondy, G; Frohlich, J; Johns, K; Saeedi, R, 2015
)
1.03
" Treatment-emergent adverse events occurred in 56."( Efficacy and safety of adding alirocumab to rosuvastatin versus adding ezetimibe or doubling the rosuvastatin dose in high cardiovascular-risk patients: The ODYSSEY OPTIONS II randomized trial.
Averna, M; Colhoun, HM; Donahue, S; Du, Y; Farnier, M; Hanotin, C; Jones, P; Severance, R; Steinhagen-Thiessen, E, 2016
)
0.67
"Alirocumab produced greater LDL-C reductions than ezetimibe in statin-intolerant patients, with fewer skeletal-muscle adverse events vs atorvastatin."( Efficacy and safety of alirocumab vs ezetimibe in statin-intolerant patients, with a statin rechallenge arm: The ODYSSEY ALTERNATIVE randomized trial.
Baccara-Dinet, MT; Bergeron, J; Bruckert, E; Cannon, CP; Du, Y; Gipe, DA; Guyton, JR; Jacobson, TA; Kopecky, SL; Moriarty, PM; Pordy, R; Thompson, PD; Zieve, FJ,
)
0.66
"Ezetimibe and simvastatin treatment, either as a single pill or the combined use of the individual compounds, offers limited additional risk compared with simvastatin monotherapy and comprises a safe and efficient choice for dyslipidemia treatment in high-risk and diabetic patients."( The safety of ezetimibe and simvastatin combination for the treatment of hypercholesterolemia.
Elisaf, MS; Filippatos, TD; Kei, AA, 2016
)
2.24
" Myotoxicity is a frequent side effect of statin therapy and one of the main causes of statin discontinuation, which limits effective treatment of patients at risk of or with cardiovascular disease."( Statin-related myotoxicity.
Fernandes, V; Pérez, A; Santos, MJ, 2016
)
0.43
" Evolocumab was well tolerated, with balanced rates of adverse events leading to discontinuation of evolocumab vs."( Efficacy and Safety of the PCSK9 Inhibitor Evolocumab in Patients with Mixed Hyperlipidemia.
Bridges, I; Dent, R; Djedjos, CS; Jacobson, TA; Miller, M; Preiss, D; Rosenson, RS, 2016
)
0.43
" Fenofibrate use was associated with some changes in laboratory measurements, but there was no differential adverse effect between the combination therapy and fenofibrate monotherapy."( Efficacy and Safety of Long-term Coadministration of Fenofibrate and Ezetimibe in Patients with Combined Hyperlipidemia: Results of the EFECTL Study.
Kono, S; Nakaya, N; Oikawa, S; Sasaki, J; Yamashita, S, 2017
)
0.69
"The combination therapy with fenofibrate and ezetimibe substantially reduces concentrations of LDL cholesterol and triglycerides and is safe in a long-term treatment in Japanese patients with combined hyperlipidemia."( Efficacy and Safety of Long-term Coadministration of Fenofibrate and Ezetimibe in Patients with Combined Hyperlipidemia: Results of the EFECTL Study.
Kono, S; Nakaya, N; Oikawa, S; Sasaki, J; Yamashita, S, 2017
)
0.95
" Treatment-emergent adverse events occurred in 77."( Efficacy and Safety of Alirocumab 150 mg Every 4 Weeks in Patients With Hypercholesterolemia Not on Statin Therapy: The ODYSSEY CHOICE II Study.
Baccara-Dinet, MT; Civeira, F; Farnier, M; Gaudet, D; Guyton, JR; Lecorps, G; Lepor, N; Manvelian, G; Stroes, E; Watts, GF, 2016
)
0.43
"Previous individual trials of alirocumab (a PCSK9 monoclonal antibody) showed significant low-density lipoprotein cholesterol reductions with overall treatment-emergent adverse event (TEAE) rates comparable with controls."( Safety of Alirocumab (A PCSK9 Monoclonal Antibody) from 14 Randomized Trials.
Bays, HE; Chaudhari, U; Jones, PH; Lorenzato, C; Miller, K; Pordy, R; Robinson, JG, 2016
)
0.43
"To analyze the subsidized use and reported adverse events of ezetimibe, used to lower cholesterol, in Australia over the 11 years following its inclusion on the Pharmaceutical Benefits Scheme (PBS) in 2004."( Ezetimibe: Use, costs, and adverse events in Australia.
David, MC; Hollingworth, SA; Martin, JH; Ostino, R; Tett, SE, 2017
)
2.14
" Adverse event data were obtained from the Therapeutic Goods Administration."( Ezetimibe: Use, costs, and adverse events in Australia.
David, MC; Hollingworth, SA; Martin, JH; Ostino, R; Tett, SE, 2017
)
1.9
" The major reported adverse events were musculoskeletal and connective tissue disorders and gastrointestinal disorders."( Ezetimibe: Use, costs, and adverse events in Australia.
David, MC; Hollingworth, SA; Martin, JH; Ostino, R; Tett, SE, 2017
)
1.9
" All patients were assessed for adverse events (AEs), clinical laboratory data, and vital signs."( A Phase III, Multicenter, Randomized, Double-blind, Active Comparator Clinical Trial to Compare the Efficacy and Safety of Combination Therapy With Ezetimibe and Rosuvastatin Versus Rosuvastatin Monotherapy in Patients With Hypercholesterolemia: I-ROSETTE
Ahn, JC; Bae, JH; Cha, DH; Cho, SK; Chung, WS; Han, KR; Hong, SJ; Hyon, MS; Jeon, DW; Jeong, HS; Kim, HS; Kim, SY; Kim, W; Kwan, J; Lee, HC; Rha, SW; Rhee, MY; Shin, JH; Sung, KC; Won, KH; Yoo, BS; Yoo, KD, 2018
)
0.68
" There were no significant differences in the incidence of overall AEs, adverse drug reactions, and serious AEs; laboratory findings, including liver function test results and creatinine kinase levels, were comparable between groups."( A Phase III, Multicenter, Randomized, Double-blind, Active Comparator Clinical Trial to Compare the Efficacy and Safety of Combination Therapy With Ezetimibe and Rosuvastatin Versus Rosuvastatin Monotherapy in Patients With Hypercholesterolemia: I-ROSETTE
Ahn, JC; Bae, JH; Cha, DH; Cho, SK; Chung, WS; Han, KR; Hong, SJ; Hyon, MS; Jeon, DW; Jeong, HS; Kim, HS; Kim, SY; Kim, W; Kwan, J; Lee, HC; Rha, SW; Rhee, MY; Shin, JH; Sung, KC; Won, KH; Yoo, BS; Yoo, KD, 2018
)
0.68
" Safety parameters were assessed by adverse event reports and laboratory assessments throughout the study."( Short-Term Efficacy and Safety of Adding Ezetimibe to Current Regimen of Lipid-Lowering Drugs in Human Immunodeficiency Virus-Infected Thai Patients Treated with Protease Inhibitors.
Boonthos, K; Manosuthi, W; Pengsuparp, T; Puttilerpong, C, 2018
)
0.75
" Bempedoic acid was well tolerated; rates of treatment-emergent adverse events, muscle-related adverse events, and discontinuations were similar in the bempedoic acid and placebo treatment groups."( Efficacy and safety of bempedoic acid added to ezetimibe in statin-intolerant patients with hypercholesterolemia: A randomized, placebo-controlled study.
Ballantyne, CM; Banach, M; Hanselman, JC; Leiter, LA; Lepor, NE; Mancini, GBJ; Zhao, X, 2018
)
0.74
"Recent studies have highlighted the possible risk of neuropsychiatric adverse effects during treatment with lipid-lowering medications."( Risk of Neuropsychiatric Adverse Effects of Lipid-Lowering Drugs: A Mendelian Randomization Study.
Alfadhel, M; Alghamdi, F; Alghamdi, J; Alghamdi, S; Matou-Nasri, S; Padmanabhan, S, 2018
)
0.48
" No significant adverse effects were associated with ezetimibe treatment."( Risk of Neuropsychiatric Adverse Effects of Lipid-Lowering Drugs: A Mendelian Randomization Study.
Alfadhel, M; Alghamdi, F; Alghamdi, J; Alghamdi, S; Matou-Nasri, S; Padmanabhan, S, 2018
)
0.73
"Due to the myopathic adverse events of statins, safer alternatives are being studied."( Safety and efficacy of ETC-1002 in hypercholesterolaemic patients: a meta-analysis of randomised controlled trials.
Gan, X; He, C; Huang, R; Luo, S; Wang, X,
)
0.13
"ETC-1002 is a safe and effective lipid-lowering agent and may be a suitable alternative in statin-intolerant pa-tients."( Safety and efficacy of ETC-1002 in hypercholesterolaemic patients: a meta-analysis of randomised controlled trials.
Gan, X; He, C; Huang, R; Luo, S; Wang, X,
)
0.13
" The primary endpoints included the incidence of adverse cardiovascular events and changed in blood lipids and high-sensitivity C-reactive protein (hs-CRP)."( Efficacy and Safety of Ezetimibe in Combination with Atorvastatin for Acute Coronary Syndrome Patients Accompanied with Type 2 Diabetes: A Single-Center, Non-randomized Cohort Study.
Huang, Z; Li, Q; Li, X; Ye, W; Zhang, Q, 2019
)
0.82
"Statin/ezetimibe fixed-dose combination is often used as statin monotherapy; however, no study has analyzed its adverse effect (AE) signals."( Comparison of signal detection between statin and statin/ezetimibe fixed-dose combination using the Korea Adverse Events Reporting System Database, 2005 - 2016
.
Chun, Y; Ha, D; Lee, YJ; Shin, JY, 2019
)
1.21
"We used data from the Korea Adverse Events Reporting System database from 2005 to 2016."( Comparison of signal detection between statin and statin/ezetimibe fixed-dose combination using the Korea Adverse Events Reporting System Database, 2005 - 2016
.
Chun, Y; Ha, D; Lee, YJ; Shin, JY, 2019
)
0.76
" Treatment-emergent adverse events were similar between alirocumab (68."( Alirocumab efficacy and safety by race and ethnicity: Analysis from 3 ODYSSEY phase 3 trials.
Deedwania, P; Elassal, J; Ferdinand, KC; Jacobson, TA; Koren, A; Thompson, D,
)
0.13
" No significant difference was found in the incidence of laboratory-related adverse events (AEs) between statin combination therapy and monotherapy."( The efficacy and safety of statin in combination with ezetimibe compared with double-dose statin in patients with high cardiovascular risk: A meta-analysis.
Hu, H; Lin, S; Liu, T; Xu, H; Yang, J; Yao, Q; Yu, Y; Zhu, Y, 2020
)
0.81
" Treatment-emergent adverse events occurred in 68."( ODYSSEY EAST: Alirocumab efficacy and safety vs ezetimibe in high cardiovascular risk patients with hypercholesterolemia and on maximally tolerated statin in China, India, and Thailand.
Baccara-Dinet, MT; Chen, J; Chen, R; Chopra, VK; Han, Y; Huang, Z; Kuanprasert, S; Li, J; Ma, C; Ma, Y; Manvelian, G; Su, G; Yao, Z; Yuan, Z; Zhang, S; Zhao, Q,
)
0.39
" However, the onset of adverse events associated with their use prevents to achieve the therapeutic targets recommended by the guidelines (GL) for the management of dyslipidemia."( Effectiveness and Safety of Novel Nutraceutical Formulation Added to Ezetimibe in Statin-Intolerant Hypercholesterolemic Subjects with Moderate-to-High Cardiovascular Risk.
Fratter, A; Lenti, S; Mazza, A; Nicoletti, M; Pellizzato, M; Rigatelli, G; Torin, G, 2021
)
0.86
" It is still controversial whether lower LDL-C levels are associated with significant clinical adverse effects (e."( How low is safe? The frontier of very low (<30 mg/dL) LDL cholesterol.
Blumenthal, RS; Dhindsa, DS; Karagiannis, AD; Mehta, A; Orringer, CE; Sperling, LS; Stone, NJ; Virani, SS, 2021
)
0.62
"00)], and reduced risk of myocardial infarction, cerebrovascular events, revascularization, and major adverse cardiovascular events (MACE)."( Efficacy and safety for the achievement of guideline-recommended lower low-density lipoprotein cholesterol levels: a systematic review and meta-analysis.
Alkhouli, M; Blaha, MJ; Blumenthal, RS; Kalra, A; Khan, MS; Khan, MU; Khan, MZ; Khan, SU; Michos, ED; Rashid, M; Virani, SS, 2022
)
0.72
" We also compared safety based on the adverse events reported for the two groups."( Comparison of Efficacy and Safety of Statin-Ezetimibe Combination Therapy with Statin Monotherapy in Patients with Diabetes: A Meta-Analysis of Randomized Controlled Studies.
Choi, HD; Shin, KH, 2022
)
0.98
" In terms of safety, there were no significant differences in treatment-related adverse events between the two treatments."( Comparison of Efficacy and Safety of Statin-Ezetimibe Combination Therapy with Statin Monotherapy in Patients with Diabetes: A Meta-Analysis of Randomized Controlled Studies.
Choi, HD; Shin, KH, 2022
)
0.98
"Statin-ezetimibe combination therapy enhances levels of LDL-C and other lipids without increasing the risk of adverse events compared with statin monotherapy."( Comparison of Efficacy and Safety of Statin-Ezetimibe Combination Therapy with Statin Monotherapy in Patients with Diabetes: A Meta-Analysis of Randomized Controlled Studies.
Choi, HD; Shin, KH, 2022
)
1.44
" Safety and tolerability were assessed by laboratory values and adverse events."( Efficacy and safety of bempedoic acid in patients not receiving statins in phase 3 clinical trials.
Ballantyne, CM; Banach, M; Bays, H; Bloedon, LT; Catapano, AL; Duell, PB; Goldberg, AC; Gotto, AM; Laufs, U; Leiter, LA; MacDougall, D; Mancini, GBJ; Ray, KK; Zhang, Y,
)
0.13
" Thus, as an alternative to high-intensity statin monotherapy, moderate-intensity statin with ezetimibe combination therapy can lower LDL cholesterol concentrations effectively while reducing adverse effects."( Long-term efficacy and safety of moderate-intensity statin with ezetimibe combination therapy versus high-intensity statin monotherapy in patients with atherosclerotic cardiovascular disease (RACING): a randomised, open-label, non-inferiority trial.
Ahn, CM; Cho, YH; Choi, D; Heo, JH; Hong, BK; Hong, MK; Hong, SJ; Jang, Y; Kim, BK; Kim, JS; Ko, YG; Lee, SJ; Lee, YJ; Rha, SW; Yun, KH, 2022
)
1.18
" Adverse events (AEs), clinical laboratory data, and vital signs were assessed in all patients."( A Multicenter, Randomized, Double-blind, Active-controlled, Factorial Design, Phase III Clinical Trial to Evaluate the Efficacy and Safety of Combination Therapy of Pitavastatin and Ezetimibe Versus Monotherapy of Pitavastatin in Patients With Primary Hyp
Ahn, JC; Cha, DH; Cho, EJ; Cho, JM; Choi, CU; Choi, SY; Gwon, HC; Han, KH; Han, KR; Hong, SJ; Hong, YJ; Jeong, HS; Jeong, YH; Jo, SH; Kang, HJ; Kim, BK; Kim, SH; Kim, WS; Lee, SY; Park, TH; Woo, SI, 2022
)
0.91
" There were no significant differences in the incidence of overall AEs and adverse drug reactions."( A Multicenter, Randomized, Double-blind, Active-controlled, Factorial Design, Phase III Clinical Trial to Evaluate the Efficacy and Safety of Combination Therapy of Pitavastatin and Ezetimibe Versus Monotherapy of Pitavastatin in Patients With Primary Hyp
Ahn, JC; Cha, DH; Cho, EJ; Cho, JM; Choi, CU; Choi, SY; Gwon, HC; Han, KH; Han, KR; Hong, SJ; Hong, YJ; Jeong, HS; Jeong, YH; Jo, SH; Kang, HJ; Kim, BK; Kim, SH; Kim, WS; Lee, SY; Park, TH; Woo, SI, 2022
)
0.91
" The incidence of adverse events and adverse drug reactions was not significantly different between the two groups receiving the fixed-dose combination and monotherapy."( Efficacy and Safety of Pitavastatin/Ezetimibe Fixed-Dose Combination vs. Pitavastatin: Phase III, Double-Blind, Randomized Controlled Trial.
Ako, J; Suganami, H; Tajima, S; Tanigawa, R; Tsujita, K; Yokote, K, 2023
)
1.19
" The numbers of patients with adverse drug reactions (ADRs) were compared as safety variables."( A Randomized, Multicenter, Double-blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of a Quadruple Combination of Amlodipine, Losartan, Rosuvastatin, and Ezetimibe in Patients with Concomitant Essential Hypertension and Dyslipidemia.
Ahn, Y; Chae, IH; Hong, SJ; Hong, TJ; Kang, DH; Kim, BK; Kim, H; Kim, HS; Kim, MC; Kim, MH; Kim, SH; Kim, SY; Kim, W; Rhee, MY, 2023
)
1.1

Pharmacokinetics

The point estimates based on the log-transformed Cmax and AUC values for lovastatin and beta-hydroxylovastatin were 113% and 119%, respectively. Information on the pharmacokinetic profiles of ezetimibe tablet in healthy Chinese volunteers are lacking.

ExcerptReferenceRelevance
"The purpose of this study was to develop a population pharmacokinetic (PPK) model for ezetimibe that incorporates enterohepatic recirculation."( A population pharmacokinetic model that describes multiple peaks due to enterohepatic recirculation of ezetimibe.
Batra, VK; Ezzet, F; Kosoglou, T; Krishna, G; Statkevich, P; Wexler, DB, 2001
)
0.75
" In Study 1, there were no indications of pharmacokinetic interactions between simvastatin and ezetimibe."( Pharmacodynamic interaction between the new selective cholesterol absorption inhibitor ezetimibe and simvastatin.
Affrime, MB; Batra, VK; Cutler, DL; Kosoglou, T; Maxwell, SE; Mellars, L; Meyer, I; Patrick, JE; Statkevich, P; Veltri, EP; Yang, B; Zhu, Y, 2002
)
0.76
" This study investigated the potential for pharmacodynamic and/or pharmacokinetic interactions between ezetimibe and lovastatin."( Effects of ezetimibe on the pharmacodynamics and pharmacokinetics of lovastatin.
Cutler, DL; Kosoglou, T; Maxwell, SE; Meyer, I; Musiol, B; Statkevich, P; Veltri, EP; Yang, B; Zhu, Y, 2004
)
0.93
" The primary objectives of this study were to evaluate the pharmacodynamic effects and safety of the co-administration of ezetimibe and the new statin rosuvastatin."( Pharmacodynamic interaction between ezetimibe and rosuvastatin.
Boutros, T; Cutler, DL; Kosoglou, T; Maxwell, SE; Statkevich, P; Suresh, R; Tiessen, R; Yang, B; Zhu, Y, 2004
)
0.81
" Blood samples were collected for ezetimibe and rosuvastatin pharmacokinetic evaluation prior to the first and last dose and at frequent intervals after the last dose (day 14) of study treatment."( Pharmacodynamic interaction between ezetimibe and rosuvastatin.
Boutros, T; Cutler, DL; Kosoglou, T; Maxwell, SE; Statkevich, P; Suresh, R; Tiessen, R; Yang, B; Zhu, Y, 2004
)
0.88
" There was no significant pharmacokinetic drug interaction between ezetimibe and rosuvastatin."( Pharmacodynamic interaction between ezetimibe and rosuvastatin.
Boutros, T; Cutler, DL; Kosoglou, T; Maxwell, SE; Statkevich, P; Suresh, R; Tiessen, R; Yang, B; Zhu, Y, 2004
)
0.83
" Pharmacokinetic parameters were assessed on day 14."( Pharmacodynamic and pharmacokinetic interaction between fenofibrate and ezetimibe.
Cutler, DL; Fruchart, JC; Guillaume, M; Kosoglou, T; Maxwell, SE; Pember, LJ; Reyderman, L; Statkevich, P; Veltri, EP, 2004
)
0.56
"The primary pharmacodynamic parameter was percentage change from baseline in LDL-C concentration following co-administration of ezetimibe and fenofibrate vs either drug alone, or placebo."( Pharmacodynamic and pharmacokinetic interaction between fenofibrate and ezetimibe.
Cutler, DL; Fruchart, JC; Guillaume, M; Kosoglou, T; Maxwell, SE; Pember, LJ; Reyderman, L; Statkevich, P; Veltri, EP, 2004
)
0.76
" In a separate pilot study, co-administration of ezetimibe and lovastatin resulted in a significant pharmacodynamic interaction, leading to an additive reduction in LDL-C."( Pharmacokinetic interaction between ezetimibe and lovastatin in healthy volunteers.
Boutros, T; Kosoglou, T; Reyderman, L; Seiberling, M; Statkevich, P, 2004
)
0.85
" The point estimates based on the log-transformed Cmax and AUC values for lovastatin and beta-hydroxylovastatin were 113% and 119%, respectively, for co-administration of ezetimibe with lovastatin vs."( Pharmacokinetic interaction between ezetimibe and lovastatin in healthy volunteers.
Boutros, T; Kosoglou, T; Reyderman, L; Seiberling, M; Statkevich, P, 2004
)
0.79
" Co-administration of ezetimibe and lovastatin is unlikely to cause a clinically significant pharmacokinetic drug interaction."( Pharmacokinetic interaction between ezetimibe and lovastatin in healthy volunteers.
Boutros, T; Kosoglou, T; Reyderman, L; Seiberling, M; Statkevich, P, 2004
)
0.91
" The estimated terminal half-life of ezetimibe and ezetimibe-glucuronide is approximately 22 hours."( Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions.
Alton, KB; Bergman, AJ; Johnson-Levonas, AO; Kosoglou, T; Paolini, JF; Statkevich, P, 2005
)
2.04
"The objective of this study was to evaluate the pharmacodynamic effects and safety of the co-administration of ezetimibe and fluvastatin in healthy hypercholesterolemic subjects at clinically-relevant doses and to evaluate the potential for a pharmacokinetic drug interaction between ezetimibe and fluvastatin."( The effect of fluvastatin on the pharmacokinetics and pharmacodynamics of ezetimibe.
Cutler, DL; Kosoglou, T; Maxwell, S; Reyderman, L; Statkevich, P, 2005
)
0.77
" The apparent decrease in fluvastatin exposure on administration with ezetimibe was likely to be due to the parallel study design and two pharmacokinetic outliers and is considered of no clinical significance."( The effect of fluvastatin on the pharmacokinetics and pharmacodynamics of ezetimibe.
Cutler, DL; Kosoglou, T; Maxwell, S; Reyderman, L; Statkevich, P, 2005
)
0.79
"This study was conducted to evaluate the potential for pharmacokinetic interaction between fenofibrate and ezetimibe in healthy subjects."( Evaluation of the potential for pharmacokinetic interaction between fenofibrate and ezetimibe: A phase I, open-label, multiple-dose, three-period crossover study in healthy subjects.
Achari, R; Burt, DA; Chira, T; Edeki, T; Gustavson, LE; Kelly, MT; Rieser, MJ; Schweitzer, SM; Yannicelli, HD, 2006
)
0.77
" The aim of this study was to characterize the pharmacokinetic interactions of mipomersen sodium with simvastatin and ezetimibe."( Lack of pharmacokinetic interaction of mipomersen sodium (ISIS 301012), a 2'-O-methoxyethyl modified antisense oligonucleotide targeting apolipoprotein B-100 messenger RNA, with simvastatin and ezetimibe.
Flaim, JD; Geary, RS; Riley, GC; Tribble, DL; vanVliet, AA; Wedel, MK; Yu, RZ, 2009
)
0.75
" Mipomersen sodium pharmacokinetic profiles were assessed following the first dose (mipomersen sodium alone) and the last dose (mipomersen sodium in combination with simvastatin or ezetimibe)."( Lack of pharmacokinetic interaction of mipomersen sodium (ISIS 301012), a 2'-O-methoxyethyl modified antisense oligonucleotide targeting apolipoprotein B-100 messenger RNA, with simvastatin and ezetimibe.
Flaim, JD; Geary, RS; Riley, GC; Tribble, DL; vanVliet, AA; Wedel, MK; Yu, RZ, 2009
)
0.73
"The area under the plasma concentration-time curve (AUC) from 0 to 24 hours (AUC(24)), maximum plasma concentration and apparent elimination half-life values of mipomersen sodium were similar when administered alone and in combination with oral simvastatin or oral ezetimibe."( Lack of pharmacokinetic interaction of mipomersen sodium (ISIS 301012), a 2'-O-methoxyethyl modified antisense oligonucleotide targeting apolipoprotein B-100 messenger RNA, with simvastatin and ezetimibe.
Flaim, JD; Geary, RS; Riley, GC; Tribble, DL; vanVliet, AA; Wedel, MK; Yu, RZ, 2009
)
0.72
"These data provide evidence that mipomersen sodium exhibits no clinically relevant pharmacokinetic interactions with the disposition and clearance of simvastatin or ezetimibe, and vice versa."( Lack of pharmacokinetic interaction of mipomersen sodium (ISIS 301012), a 2'-O-methoxyethyl modified antisense oligonucleotide targeting apolipoprotein B-100 messenger RNA, with simvastatin and ezetimibe.
Flaim, JD; Geary, RS; Riley, GC; Tribble, DL; vanVliet, AA; Wedel, MK; Yu, RZ, 2009
)
0.74
" Enzyme kinetic parameters (K(m) and V(max)) and pharmacokinetic properties of three probe drugs were compared using wild-type and humanized UGT1 mice that express the Gilbert's UGT1A1*28 allele [Tg(UGT1(A1*28)) Ugt1(-/-) mice]."( A humanized UGT1 mouse model expressing the UGT1A1*28 allele for assessing drug clearance by UGT1A1-dependent glucuronidation.
Cai, H; Chen, S; Hotz, K; La Placa, DB; Nguyen, N; Peterkin, V; Stevens, JC; Tukey, RH; Yang, YS, 2010
)
0.36
" Adverse pharmacokinetic interactions are hypothesized with sirolimus, which is a substrate of OATP1B1 and OATP1B3 and an inhibitor of ABCB1, OATP1B1, and OATP1B3 but not of ABCC2."( Pharmacokinetic and pharmacodynamic interactions between the immunosuppressant sirolimus and the lipid-lowering drug ezetimibe in healthy volunteers.
Engel, A; Hanke, U; Keiser, M; Lütjohann, D; Modess, C; Nassif, A; Oswald, S; Siegmund, W; Weitschies, W, 2010
)
0.57
" Forty-three subjects among them participated in a pharmacokinetic study of ezetimibe."( Effects of UDP-glucuronosyltransferase polymorphisms on the pharmacokinetics of ezetimibe in healthy subjects.
Bae, JW; Choi, CI; Chung, MW; Jang, CG; Lee, JH; Lee, SY, 2011
)
0.83
" Besides the C(max) of unchanged ezetimibe, no significant difference was found in any other pharmacokinetic parameter of unchanged ezetimibe or ezetimibe-glucuronide in the three groups."( Effects of UDP-glucuronosyltransferase polymorphisms on the pharmacokinetics of ezetimibe in healthy subjects.
Bae, JW; Choi, CI; Chung, MW; Jang, CG; Lee, JH; Lee, SY, 2011
)
0.88
"The goals of the current study were to develop and characterize a nanoemulsion of ezetimibe, evaluate its stability, lipid lowering and pharmacokinetic profile."( Nanocarrier for the enhanced bioavailability of a cardiovascular agent: in vitro, pharmacodynamic, pharmacokinetic and stability assessment.
Ali, J; Ali, M; Bali, V, 2011
)
0.59
"This was an open-label, randomized, three-period, multiple-dose crossover study that assessed the potential for pharmacokinetic interaction between extended-release niacin and ezetimibe/simvastatin and their major metabolites."( Assessment of potential pharmacokinetic interactions of ezetimibe/simvastatin and extended-release niacin tablets in healthy subjects.
Cutler, DL; Kim, KT; Kosoglou, T; Statkevich, P; Taggart, W; Triantafyllou, I; Xuan, F; Zhu, Y, 2011
)
0.81
"There is a small pharmacokinetic drug interaction between ER niacin and ezetimibe/simvastatin and although this is not considered to be clinically significant, the concomitant use of these drugs should be appropriately monitored, especially during the niacin titration period."( Assessment of potential pharmacokinetic interactions of ezetimibe/simvastatin and extended-release niacin tablets in healthy subjects.
Cutler, DL; Kim, KT; Kosoglou, T; Statkevich, P; Taggart, W; Triantafyllou, I; Xuan, F; Zhu, Y, 2011
)
0.85
" However, in the presence of raltegravir, ezetimibe AUC0-24 and Ctrough were significantly lower (>20%) and ezetimibe glucuronide Cmax was higher."( Pharmacokinetics and safety of the co-administration of the antiretroviral raltegravir and the lipid-lowering drug ezetimibe in healthy volunteers.
Armenis, K; Back, D; Boffito, M; Bonora, S; D'Avolio, A; Gazzard, B; Jackson, A; Moyle, G; Taylor, J; Watson, V, 2011
)
0.84
" The purposes of this study were to develop a population pharmacodynamic (PPD) model to describe the time course for the LDL-C lowering effects of statins and assess the efficacy of combination therapy based on electronic medical records."( Population pharmacodynamic analysis of LDL-cholesterol lowering effects by statins and co-medications based on electronic medical records.
Fukae, M; Gotanda, K; Hirakawa, M; Hirota, T; Ieiri, I; Kakara, M; Matsubayashi, S; Nomura, H; Shimomura, H, 2014
)
0.4
" In addition, the established framework is expected to be applicable to other drugs without pharmacokinetic data in clinical practice."( Population pharmacodynamic analysis of LDL-cholesterol lowering effects by statins and co-medications based on electronic medical records.
Fukae, M; Gotanda, K; Hirakawa, M; Hirota, T; Ieiri, I; Kakara, M; Matsubayashi, S; Nomura, H; Shimomura, H, 2014
)
0.4
" The optimized nanocrystal formulations were evaluated for in-vitro solubility, dissolution, solid state characters and in-vivo pharmacodynamic performance."( Preparation and pharmacodynamic assessment of ezetimibe nanocrystals: Effect of P-gp inhibitory stabilizer on particle size and oral absorption.
Mishra, B; Srivalli, KMR, 2015
)
0.68
" The method has been successfully applied in clinical pharmacokinetic study in the Indian population."( Development and Validation of an LC-MS-MS Method for the Simultaneous Determination of Simvastatin, Simvastatin Acid and Ezetimibe in Human Plasma and Its Application to Pharmacokinetic Study in the Indian Population.
Bonga, PB; Munaga, SB; Rao, VS; Sharma, HK; Valluru, RK, 2016
)
0.64
" The aim of this study was to compare the pharmacokinetic (PK) profiles of an FDC tablet of rosuvastatin/ezetimibe and co-administration of rosuvastatin and ezetimibe as separate tablets in healthy Korean volunteers."( Comparison of Pharmacokinetics and Safety of a Fixed-dose Combination of Rosuvastatin and Ezetimibe Versus Separate Tablets in Healthy Subjects.
Chang, MJ; Jung, J; Kim, CO; Min, KL; Park, MS, 2017
)
0.89
" However, the pharmacokinetic (PK) interaction was not clear by the coadministration of rosuvastatin and ezetimibe."( Pharmacokinetic and pharmacodynamic interaction between ezetimibe and rosuvastatin in healthy male subjects.
An, H; Kim, CH; Kim, SH; Shin, D, 2017
)
0.92
"Ezetimibe is a potent cholesterol absorption inhibitor, with an erratic pharmacokinetic (PK) profile, attributed to an extensive enterohepatic recirculation (EHC)."( On the population pharmacokinetics and the enterohepatic recirculation of total ezetimibe.
Karalis, V; Soulele, K, 2019
)
2.18
" Both drugs exhibit complex pharmacokinetic profiles attributed mainly to repetitive enterohepatic kinetics."( Development of a joint population pharmacokinetic model of ezetimibe and its conjugated metabolite.
Karalis, V; Soulele, K, 2019
)
0.76
" However, the pharmacokinetic (PK) interaction among these therapeutic drugs has not been clearly reported."( Pharmacokinetic Interaction Between Telmisartan and Rosuvastatin/Ezetimibe After Multiple Oral Administration in Healthy Subjects.
Kang, SI; Kim, CH; Shin, D, 2021
)
0.86
"To evaluate the pharmacokinetic interactions among rosuvastatin, ezetimibe, and telmisartan, a randomized, open-label, 3-period, 6-sequence crossover study was conducted in healthy subjects."( Pharmacokinetic Interaction Among Ezetimibe, Rosuvastatin, and Telmisartan.
Huh, KY; Jang, IJ; Kim, KT; Lee, S; Lee, SB; Lee, SW, 2021
)
1.14
" Thus, the aim of this study is to assess the potential pharmacokinetic DDI between rosuvastatin and ezetimibe in a Chinese population."( Pharmacokinetic Interactions and Tolerability of Rosuvastatin and Ezetimibe: A Randomized, Phase 1, Crossover Study in Healthy Chinese Participants.
Abdel-Moneim, M; Hou, J; Hovsepian, L; Hu, C; Jia, C; Luan, Y; Wang, L; Wang, Q; Xie, F; Xie, X; Yang, N; Zhang, Z; Zhao, Z, 2023
)
1.36
" The plasma concentrations of rosuvastatin and ezetimibe were determined, and the pharmacokinetic parameters were calculated."( Pharmacokinetic Interactions and Tolerability of Rosuvastatin and Ezetimibe: A Randomized, Phase 1, Crossover Study in Healthy Chinese Participants.
Abdel-Moneim, M; Hou, J; Hovsepian, L; Hu, C; Jia, C; Luan, Y; Wang, L; Wang, Q; Xie, F; Xie, X; Yang, N; Zhang, Z; Zhao, Z, 2023
)
1.4
"Co-administration of rosuvastatin and ezetimibe showed no clinically significant pharmacokinetic interactions in a healthy Chinese population."( Pharmacokinetic Interactions and Tolerability of Rosuvastatin and Ezetimibe: A Randomized, Phase 1, Crossover Study in Healthy Chinese Participants.
Abdel-Moneim, M; Hou, J; Hovsepian, L; Hu, C; Jia, C; Luan, Y; Wang, L; Wang, Q; Xie, F; Xie, X; Yang, N; Zhang, Z; Zhao, Z, 2023
)
1.42
" Information on the pharmacokinetic profiles of ezetimibe tablet in healthy Chinese volunteers are lacking, and regulatory requirements necessitate a bioequivalence study of ezetimibe tablet versus Ezetrol® in China."( Pharmacokinetics and bioequivalence of Ezetimibe tablet versus Ezetrol®:an open-label, randomized, two-sequence crossover study in healthy Chinese subjects.
Cao, Y; Fu, Y; Gao, X; Jiang, X; Li, T; Li, X; Lin, P; Liu, Y; Ma, Y; Sun, F; Wang, C, 2023
)
1.44

Compound-Compound Interactions

The aim of this study was to explore the effect of Ezetimibe combined with Simvastatin in the treatment of coronary heart disease (CHD)

ExcerptReferenceRelevance
" Therefore, we determined the effect of SCH 48461 and ezetimibe in combination with 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitors in chow-fed dogs."( The synergistic hypocholesterolemic activity of the potent cholesterol absorption inhibitor, ezetimibe, in combination with 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibitors in dogs.
Alton, KB; Burrier, RE; Davis, HR; Pula, KK; Watkins, RW, 2001
)
0.78
"The purpose of this study was to assess the efficacy and safety of ezetimibe administered with simvastatin in patients with primary hypercholesterolemia."( Ezetimibe coadministered with simvastatin in patients with primary hypercholesterolemia.
Bettis, R; Davidson, MH; LeBeaut, AP; Lipka, LJ; McGarry, T; Melani, L; Sun, S; Suresh, R; Veltri, EP, 2002
)
1.99
"This multicenter, randomized, double-blind, placebo-controlled clinical study assessed the efficacy and safety of ezetimibe administered with lovastatin in primary hypercholesterolemia."( Efficacy and safety of ezetimibe coadministered with lovastatin in primary hypercholesterolemia.
Corbelli, J; Kerzner, B; LeBeaut, A; Lipka, LJ; Melani, L; Mukhopadhyay, P; Sharp, S; Suresh, R; Veltri, EP, 2003
)
0.84
"To evaluate the efficacy and safety of ezetimibe 10 mg administered with pravastatin in patients with primary hypercholesterolemia."( Efficacy and safety of ezetimibe coadministered with pravastatin in patients with primary hypercholesterolemia: a prospective, randomized, double-blind trial.
Hassman, D; LeBeaut, A; Lipetz, R; Lipka, L; Melani, L; Mills, R; Mukhopadhyay, P; Suresh, R; Veltri, E, 2003
)
0.9
" Although statin therapy remains the mainstay of treatment for hyperlipidemia in the elderly, other therapies, including exercise training, plant stanols and sterols, soluble fiber, and drug combinations (especially ezetimibe, niacin, and/or fibrates alone or combined with statins) are also effective and important lipid therapies for the elderly population."( Treatment of hyperlipidemia in elderly persons with exercise training, nonpharmacologic therapy, and drug combinations.
Lavie, CJ,
)
0.32
" Overall, ezetimibe has a favourable drug-drug interaction profile, as evidenced by the lack of clinically relevant interactions between ezetimibe and a variety of drugs commonly used in patients with hypercholesterolaemia."( Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions.
Alton, KB; Bergman, AJ; Johnson-Levonas, AO; Kosoglou, T; Paolini, JF; Statkevich, P, 2005
)
2.17
"To report the case of a patient who underwent orthotopic heart transplant (OHT) and demonstrated a supratherapeutic response to ezetimibe when administered with cyclosporine."( Supratherapeutic response to ezetimibe administered with cyclosporine.
Burton, I; Koshman, SL; Lalonde, LD; Pearson, GJ; Tymchak, WJ, 2005
)
0.83
"To assess whether treatment with insulin-sensitizing agents (ISAs) in combination with ezetimibe and valsartan have greater effect on hepatic fat content and lipid peroxidation compared to monotherapy in the methionine choline-deficient diet (MCDD) rat model of non-alcoholic fatty liver disease (NAFLD)."( Effect of insulin-sensitizing agents in combination with ezetimibe, and valsartan in rats with non-alcoholic fatty liver disease.
Assy, N; Bersudsky, I; Grozovski, M; Hussein, O; Szvalb, S, 2006
)
0.8
"The primary aim of this study was to compare the effect of colesevelam HCl in combination with ezetimibe to ezetimibe monotherapy on low-density lipoprotein cholesterol (LDL-C) levels in subjects with primary hypercholesterolemia."( Lipid-lowering effects of colesevelam HCl in combination with ezetimibe.
Abby, S; Bays, H; Jones, M; Lai, YL; Rhyne, J, 2006
)
0.79
" This study was designed to investigate the efficacy and safety of rosuvastatin 40 mg alone or in combination with ezetimibe 10 mg in patients at high risk of coronary heart disease."( Efficacy and safety of rosuvastatin 40 mg alone or in combination with ezetimibe in patients at high risk of cardiovascular disease (results from the EXPLORER study).
Ballantyne, CM; Duffield, E; Eber, B; Moccetti, T; Sosef, F; Vogt, A; Weiss, R, 2007
)
0.78
" At present a drug combination comprising ezetimibe 10 mg and simvastatin in all doses (10, 20, 40 and 80 mg) is being introduced into our market under the company name Inegy."( [Dual inhibition of cholesterol using the drug combination ezetimibe/simvastatin?].
Vaverková, H, 2007
)
0.85
"This study was undertaken to investigate the effect of ezetimibe (10 mg/day) alone or in combination with atorvastatin (10 mg twice a week) on hypercholesterolemia in 56 high-risk patients intolerant to daily statin use."( Effectiveness of ezetimibe alone or in combination with twice a week Atorvastatin (10 mg) for statin intolerant high-risk patients.
Athyros, VG; Kakafika, AI; Karagiannis, A; Koumaras, H; Mikhailidis, DP; Tziomalos, K, 2008
)
0.93
"The aim of this study was to assess the effects of fluvastatin extended-release (XL) 80 mg/d administered alone or combined with ezetimibe 10 mg/d on plasma lipid levels and inflammatory parameters in patients with primary hypercholesterolemia."( Effects of fluvastatin extended-release (80 mg) alone and in combination with ezetimibe (10 mg) on low-density lipoprotein cholesterol and inflammatory parameters in patients with primary hypercholesterolemia: a 12-week, multicenter, randomized, open-labe
Alvarez-Sala, LA; Cachofeiro, V; Gambus, G; Lahera, V; Masana, L; Moreno, MA; Pinilla, B; Pintó, X; Plana, N; Suarez, C; Trias, F, 2008
)
0.78
"In this multicenter, randomized, open-label, parallel-group study, patients with hypercholesterolemia were randomized in a 1:1 ratio to receive fluvastatin XL 80 mg/d alone or in combination with ezetimibe 10 mg/d for 12 weeks."( Effects of fluvastatin extended-release (80 mg) alone and in combination with ezetimibe (10 mg) on low-density lipoprotein cholesterol and inflammatory parameters in patients with primary hypercholesterolemia: a 12-week, multicenter, randomized, open-labe
Alvarez-Sala, LA; Cachofeiro, V; Gambus, G; Lahera, V; Masana, L; Moreno, MA; Pinilla, B; Pintó, X; Plana, N; Suarez, C; Trias, F, 2008
)
0.76
"Fluvastatin XL in combination with ezetimibe was found to be well-tolerated and effective, allowing the majority (87%) of these patients with primary hypercholesterolemia to achieve current treatment goals, and reduced hs-CRP levels in patients at higher cardiovascular risk."( Effects of fluvastatin extended-release (80 mg) alone and in combination with ezetimibe (10 mg) on low-density lipoprotein cholesterol and inflammatory parameters in patients with primary hypercholesterolemia: a 12-week, multicenter, randomized, open-labe
Alvarez-Sala, LA; Cachofeiro, V; Gambus, G; Lahera, V; Masana, L; Moreno, MA; Pinilla, B; Pintó, X; Plana, N; Suarez, C; Trias, F, 2008
)
0.85
" We established whether ezetimibe combined with simvastatin differently influences post fat load lipid levels and lipoprotein composition as compared to simvastatin 80mg monotherapy in obese male metabolic syndrome patients."( The effect of statin alone or in combination with ezetimibe on postprandial lipoprotein composition in obese metabolic syndrome patients.
Dallinga-Thie, GM; Hajer, GR; van Vark-van der Zee, LC; Visseren, FL, 2009
)
0.91
"Ezetimibe did not alter serum visfatin concentrations, either when administered as monotherapy or combined with a statin."( Effects of ezetimibe, either alone or in combination with atorvastatin, on serum visfatin levels: a pilot study.
Derdemezis, C; Elisaf, M; Filippatos, T; Mikhailidis, D; Tselepis, A, 2008
)
2.18
"The aim of this study was to estimate the potential long-term impact on health status of prescribing ezetimibe in combination with statin therapy in patients with established CVD and evaluate its cost-effectiveness in a health economic model."( Estimating the health benefits and costs associated with ezetimibe coadministered with statin therapy compared with higher dose statin monotherapy in patients with established cardiovascular disease: results of a Markov model for UK costs using data regis
Ara, R; Chilcott, J; Duenas, A; Durrington, P; Paisley, S; Pandor, A; Tumur, I; Wilkinson, A; Williams, R, 2008
)
0.81
"Multicentered double-blind, randomized, placebo-controlled, crossover study to determine the short-term safety, efficacy, and tolerability of ezetimibe in combination with ongoing statin therapy in HIV-infected adults with elevated low-density lipoprotein cholesterol (LDL-C)."( Short-term ezetimibe is well tolerated and effective in combination with statin therapy to treat elevated LDL cholesterol in HIV-infected patients.
Andersen, J; Busti, A; Chen, H; Chow, D; Glesby, MJ; Kohrs, S; Koletar, SL; Souza, S; Wu, J, 2009
)
0.94
" We assessed the effects of rimonabant, alone and in combination with fenofibrate or ezetimibe, on adipokine levels in obese/overweight patients with dyslipidemia."( Effects of rimonabant, as monotherapy and in combination with fenofibrate or ezetimibe, on plasma adipokine levels: a pilot study.
Derdemezis, CS; Elisaf, M; Florentin, M; Liberopoulos, EN; Tellis, CC; Tselepis, A, 2010
)
0.81
" A total of 84 patients were treated with either fluvastatin 80 mg (n = 28) alone or in combination with ezetimibe 10 mg (n = 56) for 12 weeks to determine the effects on lipids, apolipoproteins and LDL subfractions by equilibrium density gradient ultracentrifugation."( Differential effects of fluvastatin alone or in combination with ezetimibe on lipoprotein subfractions in patients at high risk of coronary events.
de Campo, A; März, W; Scharnagl, H; Schmölzer, I; Sourij, H; Stojakovic, T; Wascher, TC, 2010
)
0.81
" This effect was offset when simvastatin was combined with ezetimibe (LDL-IVB +14."( Ezetimibe alone or in combination with simvastatin increases small dense low-density lipoproteins in healthy men: a randomized trial.
Berneis, K; Berthold, HK; Gouni-Berthold, I; Krone, W; Rizzo, M; Spinas, GA, 2010
)
2.05
" We have shown in vitro that ezetimibe and tacrolimus may interact in competition for intestinal UGT1A1 and ABCB1 at concentrations reached in gut lumen after oral administration."( Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers.
Engel, A; Hanke, U; Keiser, M; Lütjohann, D; Modess, C; Nassif, A; Oswald, S; Runge, D; Siegmund, W; Ulrich, A; Weitschies, W, 2011
)
0.88
"We compared the effect of simvastatin versus simvastatin combined with ezetimibe on hemostasis and inflammation after acute coronary events [acute coronary syndromes (ACS)]."( Ezetimibe combined with simvastatin compared with simvastatin alone results in a greater suppression of oxidative stress and enhanced fibrinolysis in patients after acute coronary events.
Machnik, A; Potaczek, DP; Tracz, W; Undas, A; Wypasek, E; Zmudka, K, 2011
)
2.05
"Based on the data of Taiwan's NHIRD, our findings suggest that patients with ACS on ezetimibe combined with statins had a significantly lower risk of rehospitalization due to ACS, percutaneous transluminal coronary angioplasty, and revascularization than those on statins alone."( Impact of ezetimibe coadministered with statins on cardiovascular events following acute coronary syndrome: a 3-year population-based retrospective cohort study in Taiwan.
Bai, CH; Gau, CS; Hsiao, FY; Lin, CF; Shen, LJ; Wu, FL, 2011
)
1
"The incidence of paradoxical HDL-C reductions was low in mixed dyslipidemic patients receiving FENO alone or combined with EZE or EZE/SIMVA."( Low incidence of paradoxical reductions in HDL-C levels in dyslipidemic patients treated with fenofibrate alone or in combination with ezetimibe or ezetimibe/simvastatin.
Brudi, P; Dong, Q; Farnier, M; Johnson-Levonas, AO; Shah, A, 2011
)
0.57
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
"5 mg/day of rosuvastatin combined with 10 mg/day of ezetimibe (R2."( Comparison of anti-inflammatory effects and high-density lipoprotein cholesterol levels between therapy with quadruple-dose rosuvastatin and rosuvastatin combined with ezetimibe.
Iino, K; Ishida, M; Ito, H; Kosaka, T; Koyama, T; Nobori, K; Oguma, Y; Terata, Y; Watanabe, H; Yamazaki, D, 2013
)
0.84
"The aim of this study was to observe the effects of atorvastatin combined with ezetimibe on carotid atherosclerosis in elderly patients with hypercholesterolemia."( Effects of atorvastatin in combination with ezetimibe on carotid atherosclerosis in elderly patients with hypercholesterolemia.
Du, S; Han, YG; Li, L; Luo, P; Wang, GG; Wang, LX; Wu, SL; Zhu, HH, 2014
)
0.89
" Fifty-one in each group were given placebo, ezetimibe 10mg combined with simvastatin 10mg (Vyto10), ezetimibe 10mg combined with simvastatin 20mg (Vyto20), or simvastatin 20mg alone (Simva20) daily for 2months."( Vascular and metabolic effects of ezetimibe combined with simvastatin in patients with hypercholesterolemia.
Han, SH; Hayashi, T; Kim, EY; Koh, KK; Lee, Y; Oh, PC; Park, YM; Sakuma, I; Shin, EK, 2015
)
0.96
"To compare 2 doses of ETC-1002, alone or combined with ezetimibe 10 mg (EZE), vs EZE monotherapy for lowering low-density lipoprotein cholesterol (LDL-C)."( Treatment with ETC-1002 alone and in combination with ezetimibe lowers LDL cholesterol in hypercholesterolemic patients with or without statin intolerance.
Ballantyne, CM; Hanselman, JC; MacDougall, DE; Margulies, JR; McKenney, JM; Newton, RS; Orloff, DG; Thompson, PD,
)
0.63
" ETC-1002 alone or combined with EZE also reduced non-high-density lipoprotein cholesterol, total cholesterol, apolipoprotein B, LDL particle number, and high-sensitivity C-reactive protein compared with EZE alone."( Treatment with ETC-1002 alone and in combination with ezetimibe lowers LDL cholesterol in hypercholesterolemic patients with or without statin intolerance.
Ballantyne, CM; Hanselman, JC; MacDougall, DE; Margulies, JR; McKenney, JM; Newton, RS; Orloff, DG; Thompson, PD,
)
0.38
"We sought to investigate whether treatment with ezetimibe in combination with statins improves coronary endothelial function in target vessels in coronary artery disease patients after coronary stenting."( Ezetimibe in Combination With Statins Ameliorates Endothelial Dysfunction in Coronary Arteries After Stenting: The CuVIC Trial (Effect of Cholesterol Absorption Inhibitor Usage on Target Vessel Dysfunction After Coronary Stenting), a Multicenter Randomize
Egashira, K; Eshima, K; Higo, T; Hironaga, K; Ichi, I; Inoue, S; Kadokami, T; Katsuki, S; Kishimoto, J; Matoba, T; Miyata, K; Mukai, Y; Nakashiro, S; Oi, K; Sadamatsu, K; Satoh, S; Suematsu, N; Sunagawa, K; Takase, S; Takemoto, M; Todaka, K; Usui, M; Yamamoto, M, 2017
)
2.15
"The aim of this study was to evaluate the efficacy of ezetimibe combined with atorvastatin in treatment of carotid artery plaque in patients with type 2 diabetes mellitus complicated with coronary heart disease (CHD)."( Efficacy of ezetimibe combined with atorvastatin in the treatment of carotid artery plaque in patients with type 2 diabetes mellitus complicated with coronary heart disease.
Ai, XB; Li, L; Wang, F; Wang, J; Yi, XL; Zou, YW, 2017
)
1.08
" To explore the efficacy and safety of ezetimibe in combination with atorvastatin for the treatment of patients with T2DM and acute coronary syndrome (ACS)."( Efficacy and Safety of Ezetimibe in Combination with Atorvastatin for Acute Coronary Syndrome Patients Accompanied with Type 2 Diabetes: A Single-Center, Non-randomized Cohort Study.
Huang, Z; Li, Q; Li, X; Ye, W; Zhang, Q, 2019
)
1.09
" Overall, ezetimibe and statin combination therapy significantly decreased LDL-C, non-HDL-C, and TC levels in patients with high cardiovascular risk, among which ezetimibe combined with atorvastatin had the best therapeutic effect."( The efficacy and safety of statin in combination with ezetimibe compared with double-dose statin in patients with high cardiovascular risk: A meta-analysis.
Hu, H; Lin, S; Liu, T; Xu, H; Yang, J; Yao, Q; Yu, Y; Zhu, Y, 2020
)
1.21
"The results mentioned above suggested that pitavastatin combined with ezetimibe was an effective approach for STEMI patients with non-IRA disease undergoing primary PCI."( Pitavastatin Combined with Ezetimibe Treatment was an Effective Approach to Non-IRA Lesion of ST-segment Elevation Myocardial Infarction Patients with Primary Percutaneous Coronary Intervention.
Lei, LC; Li, GP; Peng, JJ; Ren, LH; Wang, ZY; Ye, HM; Zhao, B; Zhao, S, 2021
)
1.15
" The present study aimed to compare mean LDL cholesterol reduction and its variability achieved with different doses of the three statins most frequently used in monotherapy or combined with ezetimibe in a real clinical setting."( LDL Cholesterol Reduction Variability with Different Types and Doses of Statins in Monotherapy or Combined with Ezetimibe. Results from the Spanish Arteriosclerosis Society Dyslipidaemia Registry.
Bea, AM; Benaiges, D; Blanco-Vaca, F; Brea-Hernando, Á; Climent, E; Pedro-Botet, J; Perea, V; Pintó, X; Plana, N; Suárez-Tembra, M, 2022
)
1.12
" As to combined treatment, the lowest and highest mean percentage LDL cholesterol reductions were obtained with simvastatin 10 mg combined with ezetimibe (50."( LDL Cholesterol Reduction Variability with Different Types and Doses of Statins in Monotherapy or Combined with Ezetimibe. Results from the Spanish Arteriosclerosis Society Dyslipidaemia Registry.
Bea, AM; Benaiges, D; Blanco-Vaca, F; Brea-Hernando, Á; Climent, E; Pedro-Botet, J; Perea, V; Pintó, X; Plana, N; Suárez-Tembra, M, 2022
)
1.13
"In a real clinical setting, rosuvastatin was superior to the other statins in lowering LDL cholesterol, both as monotherapy or combined with ezetimibe."( LDL Cholesterol Reduction Variability with Different Types and Doses of Statins in Monotherapy or Combined with Ezetimibe. Results from the Spanish Arteriosclerosis Society Dyslipidaemia Registry.
Bea, AM; Benaiges, D; Blanco-Vaca, F; Brea-Hernando, Á; Climent, E; Pedro-Botet, J; Perea, V; Pintó, X; Plana, N; Suárez-Tembra, M, 2022
)
1.13
"To assess the cost effectiveness of icosapent ethyl, fenofibrate, ezetimibe, evolocumab, and alirocumab in combination with statins compared to statin monotherapy for cardiovascular prevention from the perspective of UK's National Health Service."( Cost-Effectiveness of Icosapent Ethyl, Evolocumab, Alirocumab, Ezetimibe, or Fenofibrate in Combination with Statins Compared to Statin Monotherapy.
Boch, T; Michaeli, DT; Michaeli, JC; Michaeli, T, 2022
)
1.2
"To analyze the significance of ezetimibe in combination with low- to moderate-intensity atorvastatin adjuvant aspirin therapy for cerebrovascular disease."( Implications of Ezetimibe in Combination with Low- to Moderate-Intensity Atorvastatin Adjuvant Aspirin Therapy for Cerebrovascular Disease.
Tang, X; Wang, L, 2022
)
1.35
"Ezetimibe combined with medium- and low-intensity atorvastatin with aspirin in the treatment of cerebrovascular diseases can effectively improve the coagulation function of patients, reduce the level of inflammatory factors in patients, and improve the level of blood lipids in patients, with high safety and worthy of clinical application."( Implications of Ezetimibe in Combination with Low- to Moderate-Intensity Atorvastatin Adjuvant Aspirin Therapy for Cerebrovascular Disease.
Tang, X; Wang, L, 2022
)
2.51
" However, the results of individual studies on the effect of statin therapy in combination with ezetimibe on C-reactive protein (CRP) and high-sensitivity CRP (hs-CRP) levels have not been clear."( The effect of statin therapy in combination with ezetimibe on circulating C-reactive protein levels: a systematic review and meta-analysis of randomized controlled trials.
Arabi, SM; Bahrami, LS; Chambari, M; Hadi, V; Malek-Ahmadi, M; Rizzo, M; Sahebkar, A, 2022
)
1.19
" Statin therapy in combination with ezetimibe significantly reduced the serum levels of hs-CRP (WMD - 0."( The effect of statin therapy in combination with ezetimibe on circulating C-reactive protein levels: a systematic review and meta-analysis of randomized controlled trials.
Arabi, SM; Bahrami, LS; Chambari, M; Hadi, V; Malek-Ahmadi, M; Rizzo, M; Sahebkar, A, 2022
)
1.25
"The current study showed that statin therapy in combination with ezetimibe could be effective in reducing the levels of hs-CRP and overall CRP."( The effect of statin therapy in combination with ezetimibe on circulating C-reactive protein levels: a systematic review and meta-analysis of randomized controlled trials.
Arabi, SM; Bahrami, LS; Chambari, M; Hadi, V; Malek-Ahmadi, M; Rizzo, M; Sahebkar, A, 2022
)
1.21
"To investigate the application of atorvastatin (AT) combined with ezetimibe (EZ) in elderly patients with hypertension (HY) combined with type 2 diabetes mellitus (T2DM) and the significance analysis of changes in serum bilirubin levels during treatment."( Application of Atorvastatin Combined with Ezetimibe in Elderly Patients with Hypertension Combined with T2DM and Analysis of Significance of Changes in Serum Bilirubin Levels During Treatment.
Du, M; Wang, Q; Wang, T; Zhu, S, 2023
)
1.41
"One hundred and twelve elderly patients with HY combined with T2DM admitted to our hospital from September 2019 to March 2022 were selected and divided into a control group (AT) and a combined group (AT + EZ) according to the random number table method, with 56 cases in each group."( Application of Atorvastatin Combined with Ezetimibe in Elderly Patients with Hypertension Combined with T2DM and Analysis of Significance of Changes in Serum Bilirubin Levels During Treatment.
Du, M; Wang, Q; Wang, T; Zhu, S, 2023
)
1.17
"AT combined with EZ can effectively improve glucose, lipids, inflammation and upregulate serum bilirubin in patients with HY combined with T2DM."( Application of Atorvastatin Combined with Ezetimibe in Elderly Patients with Hypertension Combined with T2DM and Analysis of Significance of Changes in Serum Bilirubin Levels During Treatment.
Du, M; Wang, Q; Wang, T; Zhu, S, 2023
)
1.17
" In total, we have retrospectively examined 1275 patients with CAD from January 2009 to April 2019 and divided them into two groups: intensive statin group and conventional-dose statins combined with ezetimibe group."( Variability in Plasma Lipids Between Intensive Statin Therapy and Conventional-Dose Statins Combined with Ezetimibe Therapy in Patients with Coronary Atherosclerosis Disease.
Chen, Z; Jin, J; Li, D; Li, Y; Liu, L; Liu, X; Shan, L; Wang, M; Xu, T; Zhang, W, 2023
)
1.31
"The aim of this study was to explore the effect of Ezetimibe combined with Simvastatin in the treatment of coronary heart disease (CHD)."( Effect of Ezetimibe combined with Simvastatin in the treatment of coronary heart disease: a retrospective analysis.
Li, B; Li, Y; Liu, YQ; Peng, WZ; Wen, JK; Xu, ZS, 2023
)
1.56

Bioavailability

The study aimed to overcome low bioavailability issues of ezetimibe by formulating an oral disintegrating film. The study compared the physicochemical characteristics, solubility, dissolution, and oral bioavailability of an ezatimibe-loaded solid self-nanoemulsifying drug delivery system (SNEDDS)

ExcerptReferenceRelevance
" The intersubject coefficient of variation was 46% to 80% in the absorption rate constant, 27% in the distribution phase, and approximately 50% in the volume of distribution."( A population pharmacokinetic model that describes multiple peaks due to enterohepatic recirculation of ezetimibe.
Batra, VK; Ezzet, F; Kosoglou, T; Krishna, G; Statkevich, P; Wexler, DB, 2001
)
0.53
" On average, about half of all cholesterol entering the intestine is absorbed, but the fractional absorption rate varies greatly among individuals."( Cholesterol metabolism and therapeutic targets: rationale for targeting multiple metabolic pathways.
Turley, SD, 2004
)
0.32
" The oral bioavailability of ezetimibe coadministered with gemfibrozil relative to each drug administered alone was evaluated with an analysis-of-variance model."( Assessment of a multiple-dose drug interaction between ezetimibe, a novel selective cholesterol absorption inhibitor and gemfibrozil.
Affrime, M; Batra, V; Boutros, T; Kosoglou, T; Maxwell, SE; Pember, L; Reyderman, L; Statkevich, P, 2004
)
0.86
" Ezetimibe did not alter the bioavailability (based on AUC) of gemfibrozil."( Assessment of a multiple-dose drug interaction between ezetimibe, a novel selective cholesterol absorption inhibitor and gemfibrozil.
Affrime, M; Batra, V; Boutros, T; Kosoglou, T; Maxwell, SE; Pember, L; Reyderman, L; Statkevich, P, 2004
)
1.48
"Plant sterols are widely distributed in human diet but are poorly absorbed so that their plasma levels are very low."( Effect of high plant sterol-enriched diet and cholesterol absorption inhibitor, SCH 58235, on plant sterol absorption and plasma concentrations in hypercholesterolemic wild-type Kyoto rats.
Batta, AK; Bollineni, JS; Salen, G; Shefer, S; Xu, G, 2005
)
0.33
" Although coadministration with gemfibrozil and fenofibrate increased the bioavailability of ezetimibe, the clinical significance is thought to be minor considering the relatively flat dose-response curve of ezetimibe and the lack of dose-related increase in adverse events."( Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions.
Alton, KB; Bergman, AJ; Johnson-Levonas, AO; Kosoglou, T; Paolini, JF; Statkevich, P, 2005
)
1.99
" Studying the rate of absorption and synthesis has come only recently into the foreground of interest."( [Change in the cholesterol metabolism associated with the combined inhibition of synthesis and absorption].
Márk, L; Paragh, G, 2007
)
0.34
"Hypercholesterolemia is associated with decreased vascular nitric oxide bioavailability and deletion of endothelial nitric oxide synthase (eNOS) markedly accelerates atherosclerosis development in apolipoprotein E knockout (apoE ko) mice."( Ezetimibe potently reduces vascular inflammation and arteriosclerosis in eNOS-deficient ApoE ko mice.
Bauersachs, J; Ertl, G; Hu, K; Huang, PL; Kuhlencordt, PJ; Padmapriya, P; Rützel, S; Schäfer, A; Schödel, J, 2009
)
1.8
"Self-nanoemulsifying granules (SNGs) were formulated with the objective of enhancing the bioavailability of the ezetimibe."( Self-nanoemulsifying granules of ezetimibe: design, optimization and evaluation.
Dixit, RP; Nagarsenker, MS, 2008
)
0.84
"Self-nanoemulsifying granules were formulated with the objective of improving the bioavailability of the ezetimibe and simvastatin when administered together."( Formulation and in vivo evaluation of self-nanoemulsifying granules for oral delivery of a combination of ezetimibe and simvastatin.
Dixit, RP; Nagarsenker, MS, 2008
)
0.77
" The formulation used for assessment of lipid lowering potential and bioavailability contained Capryol 90 (10%, v/v), Tween 20 (33."( Study of surfactant combinations and development of a novel nanoemulsion for minimising variations in bioavailability of ezetimibe.
Ali, J; Ali, M; Bali, V, 2010
)
0.57
" The present study established nanoemulsion to be a possible alternative for minimizing variation in bioavailability of ezetimibe."( Novel nanoemulsion for minimizing variations in bioavailability of ezetimibe.
Ali, J; Ali, M; Bali, V, 2010
)
0.81
"Ezetimibe ameliorated the status of metabolic syndrome and microalbuminuria, reduced inflammation and oxidative stress, and increased nitric oxide bioavailability in a LDL-chol reduction-dependent and -independent manner."( Ezetimibe ameliorates metabolic disorders and microalbuminuria in patients with hypercholesterolemia.
Aihara, K; Akaike, M; Dagvasumberel, M; Hirata, Y; Ishikawa, K; Iwase, T; Koshiba, K; Kusunose, K; Matsumoto, T; Niki, T; Sata, M; Soeki, T; Sumitomo-Ueda, Y; Taketani, Y; Tomita, N; Wakatsuki, T; Yagi, S; Yamada, H; Yamaguchi, K; Yoshida, S, 2010
)
3.25
"Carotenoid bioavailability is influenced by a number of factors including the presence of other carotenoids, which may enhance or inhibit the transport of one another by intestinal cells."( Investigation of beta-carotene and lutein transport in Caco-2 cells: carotenoid-carotenoid interactions and transport inhibition by ezetimibe.
Aisling, SA; O'Brien, NM; O'Sullivan, L, 2009
)
0.56
" The formulation selected for bioavailability estimation contained Capryol 90 (10%, v/v), Crempophor EL (11."( Nanocarrier for the enhanced bioavailability of a cardiovascular agent: in vitro, pharmacodynamic, pharmacokinetic and stability assessment.
Ali, J; Ali, M; Bali, V, 2011
)
0.37
" As ezetimibe is almost insoluble in water, its bioavailability is too low to be detected."( Design and characterization of nanocrystal formulations containing ezetimibe.
Gulsun, T; Gursoy, RN; Oner, L, 2011
)
1.16
"The aim of this study was to investigate the bioavailability enhancement of the biopharmaceutics classification system class II compound ezetimibe loaded in ordered mesoporous silica (OMS) in dogs."( Use of ordered mesoporous silica to enhance the oral bioavailability of ezetimibe in dogs.
Daems, T; Eelen, S; Kiekens, F; Martens, J; Van Den Mooter, G; Verheyden, L, 2012
)
0.81
"The aim of this work was to compare the intestinal absorption kinetics and the bioavailability of γ-tocotrienol (γ-T3) and α-tocopherol (α-Tph) administered separately as oil solutions to rats in vivo."( Comparison of the intestinal absorption and bioavailability of γ-tocotrienol and α-tocopherol: in vitro, in situ and in vivo studies.
Abuasal, BS; Kaddoumi, A; Qosa, H; Sylvester, PW, 2012
)
0.38
" The studies, therefore, indicate the successful formulation development of self-nanoemulsifying systems with distinctly improved bioavailability potential of ezetimibe."( Optimized self nano-emulsifying systems of ezetimibe with enhanced bioavailability potential using long chain and medium chain triglycerides.
Bandyopadhyay, S; Katare, OP; Singh, B, 2012
)
0.84
"The oral bioavailability of poorly water-soluble drugs (PWSD) is often significantly enhanced by coadministration with lipids in food or lipid-based oral formulations."( Intestinal bile secretion promotes drug absorption from lipid colloidal phases via induction of supersaturation.
Charman, WN; Porter, CJ; Quach, T; Trevaskis, NL; Tso, P; Yeap, YY, 2013
)
0.39
"The purpose of this research was to evaluate the effect of the HPC (hydroxypropylcellulose) and Tween 80 on the physicochemical properties and oral bioavailability of ezetimibe-loaded solid dispersions."( Effect of hydroxypropylcellulose and Tween 80 on physicochemical properties and bioavailability of ezetimibe-loaded solid dispersion.
Choi, HG; Din, FU; Kim, DW; Kim, JO; Mustapha, O; Park, JH; Rashid, R; Yong, CS; Yousaf, AM, 2015
)
0.83
"Drug nanocrystals have been widely accepted as potent formulations to overcome poor solubility, dissolution and bioavailability problems of hydrophobic drugs."( Preparation and pharmacodynamic assessment of ezetimibe nanocrystals: Effect of P-gp inhibitory stabilizer on particle size and oral absorption.
Mishra, B; Srivalli, KMR, 2015
)
0.68
"The objective of this study was to compare the physicochemical characteristics, solubility, dissolution, and oral bioavailability of an ezetimibe-loaded solid self-nanoemulsifying drug delivery system (SNEDDS), surface modified solid dispersion (SMSD), and solvent evaporated solid dispersion (SESD) to identify the best drug delivery system with the highest oral bioavailability."( Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe.
Choi, HG; Kim, DW; Kim, JO; Mustapha, O; Oh, YK; Park, JH; Rashid, R; Yong, CS; Youn, YS; Yousaf, AM, 2015
)
0.82
" We also examined an approach to improve intestinal absorption of a poorly absorbed water-insoluble component, coenzyme Q10 (CoQ10), by this mechanism."( An Approach to Improve Intestinal Absorption of Poorly Absorbed Water-Insoluble Components via Niemann-Pick C1-Like 1.
Imai, M; Iseki, K; Noto, K; Sato, Y; Sugawara, M; Sumi, M; Takekawa, Y; Takekuma, Y; Yamaki, Y, 2016
)
0.43
" The PK time course data were well described by a two compartment PK model with first order absorption, and covariates identified for PK parameters included weight on both clearance (CL) and central volume (V2), dose on CL, race on bioavailability (F), and age on V2."( Population Pharmacokinetics (PK) and Pharmacodynamics (PD) Analysis of LY3015014, a Monoclonal Antibody to Protein Convertase Subtilisin/Kexin Type 9 (PCSK9) in Healthy Subjects and Hypercholesterolemia Patients.
James, DE; Krueger, KA; Shen, T, 2017
)
0.46
"We propose that the specific intestinal Niemann-Pick C1-like 1 protein inhibitor ezetimibe is a potential agent for preventing gallstone formation by reducing bioavailability of intestine- derived cholesterol to the liver for biliary secretion and desaturating bile through the inhibition of intestinal absorption of cholesterol."( Effect of Inhibition of Intestinal Cholesterol Absorption on the Prevention of Cholesterol Gallstone Formation.
Portincasa, P; Wang, DQ, 2017
)
0.68
" There were no significant differences in the absorption rate of the drug, even at high concentrations on the apical side."( Investigation of supersaturation and in vitro permeation of the poorly water soluble drug ezetimibe.
Alhayali, A; Ehrhardt, C; Selo, MA; Velaga, S, 2018
)
0.7
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"012mg/ml 23oC) and low oral bioavailability (about 35-65% for a once 10mg dose)."( Dissolution rate enhancement of new co-crystals of ezetimibe with maleic acid and isonicotinamide.
Kai, S; Li Na, D; Ling, F; Man, Z; Wen, L; Xiao-Hui, Z; Yan-Jie, H; Yu-Zhen, Y, 2019
)
0.77
"Ezetimibe is a cholesterol-lowering agent with an oral bioavailability of 50% by virtue of its poor solubility and extensive hepatic and intestinal metabolism."( Amorphous Solid Dispersion Based Oral Disintegrating Film of Ezetimibe: Development and Evaluation.
Narayana, KA; Shrestha, S; Sudheer, P, 2021
)
2.31
"The study aimed to overcome low bioavailability issues of ezetimibe by formulating an oral disintegrating film."( Amorphous Solid Dispersion Based Oral Disintegrating Film of Ezetimibe: Development and Evaluation.
Narayana, KA; Shrestha, S; Sudheer, P, 2021
)
1.11
"The study revealed that the formulation approach could overcome the biopharmaceutical challenge of solubility as well as low bioavailability issues of ezetimibe."( Amorphous Solid Dispersion Based Oral Disintegrating Film of Ezetimibe: Development and Evaluation.
Narayana, KA; Shrestha, S; Sudheer, P, 2021
)
1.06
" Eight different scenarios were performed with changes in the rate of absorption of EZE and EZEG."( Investigation of the discriminatory ability of analytes for the bioequivalence assessment of ezetimibe: Parent drug, metabolite, total form, and combination of parent drug and total form.
Hsieh, CM; Hsu, LF, 2022
)
0.94
"Understanding the solid-state transitions of active pharmaceutical ingredients (APIs) is essential for quality control since differences in their forms affect the bioavailability of APIs."( Study on Hydration and Dehydration of Ezetimibe by Terahertz Spectroscopy with Humidity-Controlled Measurements and Theoretical Analysis.
Aiko, K; Davis, MP; Korter, TM; Mohara, M; Ono, T; Shimura, K, 2022
)
0.99
"36 ng*h/mL), indicating improved oral bioavailability for eutectics."( Development of ezetimibe eutectic with improved biopharmaceutical and mechanical properties to design an optimized oral solid dosage formulation.
Ghosh, A; Gour, A; Kumari, N; Nandi, U; Pandey, N; Raj, A; Roy, P; Srividya, B, 2022
)
1.07
" PK and bioavailability parameters were estimated via non-compartmental methods."( Pharmacokinetics and bioequivalence of Ezetimibe tablet versus Ezetrol®:an open-label, randomized, two-sequence crossover study in healthy Chinese subjects.
Cao, Y; Fu, Y; Gao, X; Jiang, X; Li, T; Li, X; Lin, P; Liu, Y; Ma, Y; Sun, F; Wang, C, 2023
)
1.18

Dosage Studied

In an open-label clinical trial, 54 hypercholesterolemic patients included in the study underwent 12 months of treatment with ezetimibe at a dosage of 10 mg/d. Blood samples were collected for up to 24 hours after dosing on study day 1 and up to 120 hours afterwards for determination of plasma concentrations of fenofibric acid.

ExcerptRelevanceReference
" Additional dose-scheduling studies demonstrated that evening dosing was only slightly more effective than morning dosing, and that the drug could be taken with or without food without any impairment in efficacy."( An investigative look: selective cholesterol absorption inhibitors--embarking on a new standard of care.
Stein, EA, 2002
)
0.31
" Optimum doses of statins, which have demonstrated undisputed efficacy in the treatment of hypercholesterolaemia in clinical trials, are seldom used; the inconvenience of dosage adjustments and safety concerns, particularly myalgia, may constitute obstacles to their optimal use for LDL-C reduction in clinical practice."( Selective cholesterol absorption inhibition: a novel strategy in lipid-lowering management.
Leitersdorf, E, 2002
)
0.31
" To determine whether this class of intestinal cholesterol absorption inhibitors could discriminate between newly synthesized cholesterol in the intestine versus exogenously administered cholesterol, rats were intraduodenally dosed with (14)C-cholesterol and (3)H-mevalonate, and mesenteric lymph was analyzed for radiolabeled cholesterol and cholesteryl ester content."( Ezetimibe potently inhibits cholesterol absorption but does not affect acute hepatic or intestinal cholesterol synthesis in rats.
Compton, DS; Davis, HR; Farley, C; Hoos, LM; Smith-Torhan, A; van Heek, M, 2003
)
1.76
" The maximum mean reduction of LDL cholesterol is approximately 20-25% in small studies at the maximal dose tested of 40 mg/day and the reduction is usually in the 16-20% range at the dosage of 10 mg/day."( Ezetimibe.
Brown, WV; Davis, W; Harris, M, 2003
)
1.76
" Other possible roles for ezetimibe include its concurrent use with a statin to permit a lowering of statin dosage to avoid statin-related complications or its use as monotherapy to treat hypercholesterolemia when statin use cannot be tolerated or is contraindicated."( Ezetimibe for management of hypercholesterolemia.
Mauro, VF; Tuckerman, CE, 2003
)
2.06
" Ezetimibe has a relatively flat dose-response curve and titration is not required."( Hypolipidemic therapy and cholesterol absorption.
Farmer, JA; Manhas, A, 2004
)
1.23
" If the desired effect is not achieved with the starting dose of statins, a doubling of dosage only leads to 6% additional LDL-cholesterol level decrease."( [New treatment option for decreasing blood cholesterol level--clinical significance of inhibition of both, cholesterol absorption and synthesis].
Czine, Z; Márk, L; Paragh, G, 2004
)
0.32
" However, based on the established safety profile and flat dose-response of ezetimibe, this effect is not considered to be clinically significant."( Pharmacodynamic and pharmacokinetic interaction between fenofibrate and ezetimibe.
Cutler, DL; Fruchart, JC; Guillaume, M; Kosoglou, T; Maxwell, SE; Pember, LJ; Reyderman, L; Statkevich, P; Veltri, EP, 2004
)
0.79
" 10/10 mg, 10/20 mg, 10/40 mg, and 10/80 mg) and hence, the dosage may be adjusted to suit the individual patient's needs."( Ezetimibe/Simvastatin: a review of its use in the management of hypercholesterolemia.
Murdoch, D; Scott, LJ, 2004
)
1.77
" There are no clinically significant effects of age, sex or race on ezetimibe pharmacokinetics and no dosage adjustment is necessary in patients with mild hepatic impairment or mild-to-severe renal insufficiency."( Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions.
Alton, KB; Bergman, AJ; Johnson-Levonas, AO; Kosoglou, T; Paolini, JF; Statkevich, P, 2005
)
2.01
" A rapid, specific reversed-phase HPLC method has been developed for assaying ezetimibe in pharmaceutical dosage forms."( Development and validation of a reversed-phase HPLC method for the determination of ezetimibe in pharmaceutical dosage forms.
Chandrasekar, D; Diwan, PV; Kashyap, YV; Sistla, R; Tata, VS, 2005
)
0.78
" The implications for chronic EZE dosing within the usual clinical paradigm of chronic CyA dosing have not been established; caution is recommended when using these agents concomitantly."( Effects of ezetimibe on cyclosporine pharmacokinetics in healthy subjects.
Bergman, AJ; Burke, J; Frick, G; Gottesdiener, K; Greenberg, HE; Johnson-Levonas, AO; Kosoglou, T; Kraft, WK; Larson, P; Murphy, G; Paolini, JF; Reyderman, L; Statkevich, P, 2006
)
0.72
"This open-label, single-period study evaluated the single-dose pharmacokinetics of ezetimibe (EZE) 10 mg in the setting of steady-state cyclosporine (CyA) dosing in renal transplant patients."( Interaction of single-dose ezetimibe and steady-state cyclosporine in renal transplant patients.
Bergman, AJ; Burke, J; Gottesdiener, K; Johnson-Levonas, AO; Kosoglou, T; Larson, P; Maxwell, SE; Murphy, G; Paolini, JF; Reyderman, L; Robson, R; Statkevich, P, 2006
)
0.86
"The lowest and highest dosage strengths of EZE/SIMVA tablet were bioequivalent to the individual drug components administered together."( Bioequivalence of an ezetimibe/simvastatin combination tablet and coadministration of ezetimibe and simvastatin as separate tablets in healthy subjects.
Bergman, A; Gambale, J; Gottesdiener, K; Groff, M; Hreniuk, D; Johnson-Levonas, AO; Kosoglou, T; Lasseter, KC; Laurent, A; Liu, L; Matthews, N; Migoya, EM; Murphy, G; Musson, DG; Paolini, JF; Riffel, K; Roadcap, B; Statkevich, P; Valesky, R; Yi, B; Zhao, JJ, 2006
)
0.65
" Blood samples were collected for up to 24 hours after dosing on study day 1 and up to 120 hours after dosing on study day 10 for determination of plasma concentrations of fenofibric acid, unconjugated (free) ezetimibe, and total (conjugated and unconjugated) ezetimibe using validated high-performance liquid chromatography methods with mass-spectrometric detection."( Evaluation of the potential for pharmacokinetic interaction between fenofibrate and ezetimibe: A phase I, open-label, multiple-dose, three-period crossover study in healthy subjects.
Achari, R; Burt, DA; Chira, T; Edeki, T; Gustavson, LE; Kelly, MT; Rieser, MJ; Schweitzer, SM; Yannicelli, HD, 2006
)
0.75
"Ezetimibe added to atorvastatin therapy compared with treatment with the most common fixed atorvastatin daily dosage (10 mg) or with common atorvastatin titration strategies (up to 20 mg daily; up to 40 mg daily) resulted in cost per QALY estimates ranging from 25,344 to 44,332 Canadian dollars."( Cost effectiveness of adding ezetimibe to atorvastatin therapy in patients not at cholesterol treatment goal in Canada.
Alemao, E; Attard, C; Bourgault, C; Cook, J; Huse, D; Kohli, M; Lam, A; Marentette, M; Yin, D, 2006
)
2.07
" The recommended dosage is 10 mg once daily; it is safe and well tolerated."( Combination of statin and ezetimibe for the treatment of dyslipidemias and the prevention of coronary artery disease.
Genest, J, 2006
)
0.63
"We sought to test the platelet inhibitory and anti-inflammatory effects of a higher statin dosage compared with combined treatment with ezetimibe plus a low statin dose."( Treatment with ezetimibe plus low-dose atorvastatin compared with higher-dose atorvastatin alone: is sufficient cholesterol-lowering enough to inhibit platelets?
Fischer, S; Jaster, M; Martus, P; Morguet, AJ; Piorkowski, M; Rauch, U; Schultheiss, HP; Stellbaum, C, 2007
)
0.9
" An excellent safety and tolerability profile combined with once-daily dosing make this attractive adjunct therapy for the treatment of hypercholesterolemia."( Ezetimibe: an update on the mechanism of action, pharmacokinetics and recent clinical trials.
Johnson, RR; Sweeney, ME, 2007
)
1.78
" This has lead to a series of international and national recommendations for a further reduction in target values for LDL-cholesterol, which is often difficult to achieve with the usual dosage of statins."( [Dual inhibition of cholesterol using the drug combination ezetimibe/simvastatin?].
Vaverková, H, 2007
)
0.58
" The proposed method can be useful in the quality control of bulk manufacturing and pharmaceutical dosage forms."( Stability-indicating reversed-phase liquid chromatographic method for simultaneous determination of simvastatin and ezetimibe from their combination drug products.
Chaudhari, BG; Patel, NM; Shah, PB,
)
0.34
" The proposed method can be useful in the quality control of bulk manufacturing and pharmaceutical dosage forms."( Stability-indicating reversed-phase liquid chromatographic method for simultaneous determination of atorvastatin and ezetimibe from their combination drug products.
Chaudhari, BG; Patel, LJ; Patel, NM; Patel, VP; Shah, PB,
)
0.34
"A reversed-phase liquid chromatographic (LC) method was developed and validated for the simultaneous determination of ezetimibe and simvastatin in pharmaceutical dosage forms."( Simultaneous liquid chromatographic determination of ezetimibe and simvastatin in pharmaceutical products.
Barth, T; Dalmora, SL; Oliveira, PR; Todeschini, V,
)
0.59
" The primary end-point for this analysis was the evaluation of the long-term safety and tolerability of EZE 10 mg monotherapy dosed daily for up to 24 months."( Safety and efficacy of ezetimibe monotherapy in 1624 primary hypercholesterolaemic patients for up to 2 years.
Dujovne, CA; Maccubbin, D; McCrary Sisk, C; Strony, J; Suresh, R; Veltri, E, 2008
)
0.66
"Poor results from lipid-lowering therapy are mainly due to inadequate dosing and increased adverse effects with high-dose statin monotherapy or drug combinations."( Statin plus ezetimibe treatment in clinical practice: the SI-SPECT (Slovenia (SI) Statin Plus Ezetimibe in Cholesterol Treatment) monitoring of clinical practice study.
Fras, Z; Mikhailidis, DP, 2008
)
0.72
"The authors conducted a prospective, controlled, open-label trial examining the effectiveness and safety of high-dose fluvastatin or a standard dosage of simvastatin plus ezetimibe, both with an intensive guideline-oriented cardiac rehabilitation program, in achieving the new ATP III LDL-C targets in patients with proven coronary artery disease."( Simvastatin and ezetimibe in addition to nonpharmacological risk factor modification for achieving new low-density lipoprotein cholesterol targets.
Abdel-Wahab, M; Geist, V; Herrmann, L; Khattab, AA; Liska, B; Richardt, G; Tölg, R; Westphal, R, 2008
)
0.89
" The direct application of study observations to clinical practice is limited by patient selection criteria and dosage regime, which randomly applied relatively high doses rather than titration which often occurs in clinical practice."( Long-term (48-week) safety of ezetimibe 10 mg/day coadministered with simvastatin compared to simvastatin alone in patients with primary hypercholesterolemia.
Bays, H; Capece, R; Liu, J; Sapre, A; Taggart, W; Tershakovec, A, 2008
)
0.63
"The impact of the 2 ezetimibe dosing strategies on percent lowering of low-density lipoprotein cholesterol (LDL-C) and achievement of National Cholesterol Education Program Adult Treatment Panel III (ATP III) goals was assessed in all patients prescribed ezetimibe 5 or 10 mg."( Ezetimibe 5 and 10 mg for lowering LDL-C: potential billion-dollar savings with improved tolerability.
Agarwal, S; Baruch, L; Eng, C; Gupta, B; Lieberman-Blum, SS, 2008
)
2.11
" The initial dose administered to patients in the extension was ezetimibe 10 mg coadministered with simvastatin 10 mg with the option to up-titrate statin dosage if LDL-C goals were not met."( Long-term safety and tolerability of ezetimibe coadministered with simvastatin in hypercholesterolemic patients: a randomized, 12-month double-blind extension study.
Hanson, ME; Strony, J; Veltri, EP; Yang, B, 2008
)
0.86
"Ezetimibe is usually dosed daily, but its 22-hour elimination half-life permits significant cholesterol reduction with less frequent dosing."( Effectiveness of thrice weekly ezetimibe.
Seip, RL; Thompson, PD; Venero, CV; Venero, JV, 2008
)
2.07
" The impact of the 2 ezetimibe dosing strategies on LDL and the achievement of the Adult Treatment Panel III LDL goal was evaluated."( Effect on serum lipid levels of switching dose of ezetimibe from 10 to 5 mg.
Agarwal, S; Baruch, L; Eng, C; Gupta, B; Haynos, A, 2009
)
0.92
"In an open-label clinical trial, 54 hypercholesterolemic patients included in the study underwent 12 months of treatment with ezetimibe at a dosage of 10 mg/d."( Ezetimibe effect on bone mineral density and markers of bone formation and resorption.
Ayter, M; Ersoy, U; Gultekin Tirtil, F; Kucukkaya, B; Sertbas, Y, 2010
)
2.01
"Two spectrophotometric methods are presented for the simultaneous determination of ezetimibe/simvastatin and ezetimibe/atorvastatin binary mixtures in combined pharmaceutical dosage forms without prior separation."( Enhanced spectrophotometric determination of two antihyperlipidemic mixtures containing ezetimibe in pharmaceutical preparations.
Barary, MA; El-Kimary, EI; Hassan, EM; Maher, HM; Youssef, RM, 2011
)
0.82
"This paper describes validated HPLC and HPTLC methods for the simultaneous determination of rosuvastatin (ROS) and ezetimibe (EZE) in a combined tablet dosage form."( Determination of rosuvastatin and ezetimibe in a combined tablet dosage form using high-performance column liquid chromatography and high-performance thin-layer chromatography.
Ravi, TK; Varghese, SJ,
)
0.62
"Simple, accurate, sensitive, and precise UV spectrophotometric, chemometric, and HPLC methods were developed for simultaneous determination of a two-component drug mixture of ezetimibe (EZ) and simvastatin (SM) in laboratory-prepared mixtures and a combined tablet dosage form."( Quantitative analysis of the cholesterol-lowering drugs ezetimibe and simvastatin in pure powder, binary mixtures, and a combined dosage form by spectrophotometry, chemometry, and high-performance column liquid chromatography.
Aboul Alamein, AM; Hegazy, MA; Lotfy, HM,
)
0.57
" Simvastatin was discontinued and dosage of cholinesterase inhibitor was temporarily increased."( Statin-associated myasthenic weakness.
Pasutharnchat, N; Phanthumchinda, K, 2011
)
0.37
" The incidence ofstatin-associated myasthenic weakness should be clearly investigated Challenge with other brands of statin or with reduced dosage is not beneficial in these patients."( Statin-associated myasthenic weakness.
Pasutharnchat, N; Phanthumchinda, K, 2011
)
0.37
" Dalcetrapib did not change plasma (3)H-cholesterol level but increased (3)H-cholesterol in plasma HDL vs non-HDL, after oral dosing of labeled cholesterol."( Effect of dalcetrapib, a CETP modulator, on non-cholesterol sterol markers of cholesterol homeostasis in healthy subjects.
Blum, D; Chaput, E; Derks, M; Kallend, D; Niesor, EJ; Staempfli, A, 2011
)
0.37
" The sinusoidal transporter Abcc3 was induced in MCD rats, which correlated with increased plasma concentrations of EZE-GLUC, regardless of dosing method."( Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
Canet, MJ; Cherrington, NJ; Fisher, CD; Hardwick, RN; Street, SM, 2012
)
0.66
" We assessed the efficacy and safety of various doses and dosing intervals of REGN727, a monoclonal antibody to PCSK9, added to statins, to further lower LDL-C in patients with heterozygous familial hypercholesterolaemia."( Effect of a monoclonal antibody to PCSK9, REGN727/SAR236553, to reduce low-density lipoprotein cholesterol in patients with heterozygous familial hypercholesterolaemia on stable statin dose with or without ezetimibe therapy: a phase 2 randomised controlle
Bergeron, J; Dufour, R; Gaudet, D; Gipe, D; Pordy, R; Stein, EA; Weiss, R; Wu, R, 2012
)
0.57
" At the end of the dosing interval at week 12, the mean LDL-C concentrations were reduced generally dose dependently by AMG 145 every 2 weeks (ranging from 41·8% to 66·1%; p<0·0001 for each dose vs placebo) and AMG 145 every 4 weeks (ranging from 41·8% to 50·3%; p<0·0001)."( Efficacy, safety, and tolerability of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 in combination with a statin in patients with hypercholesterolaemia (LAPLACE-TIMI 57): a randomised, placebo-controlled, dose-ranging, phase 2 stu
Abrahamsen, TE; Desai, NR; Giugliano, RP; Hoffman, EB; Huang, F; Kohli, P; Liu, T; McDonald, ST; Mohanavelu, S; Rogers, WJ; Sabatine, MS; Scott, R; Somaratne, R; Wasserman, SM, 2012
)
0.38
" Pharmacy data and drug dosage information were used to estimate a moving window of ezetimibe and statin exposure for each day of study follow-up."( Effect of ezetimibe on major atherosclerotic disease events and all-cause mortality.
Ahmedani, BK; Canepa Escaro, F; Divine, G; Gamalski, S; Hayek, S; Lanfear, DE; Pladevall, M; Sattar, A; Wells, KE; Williams, LK, 2013
)
1.02
" The validated LC/ESI-MS method can be used to study pharmacokinetics, bioavailability, and bioequivalence of combined dosage forms of ROS and EZE."( Development and validation of a liquid chromatography/ mass spectrometry method for the simultaneous quantitation of rosuvastatin and ezetimibe in human plasma.
Ravi, TK; Varghese, SJ,
)
0.33
"To assess the lipid-lowering efficacy of ezetimibe in dyslipidemic cynomolgus monkeys comparing two dosing methods, and to evaluate PCSK9 plasma levels during dyslipidemia induction by feeding a high-fat/high-cholesterol diet (HFD), ezetimibe (Zetia(®), Ezetrol(®)) treatment, ezetimibe washout, and HFD washout."( Inverse relationship between LDL cholesterol and PCSK9 plasma levels in dyslipidemic cynomolgus monkeys: effects of LDL lowering by ezetimibe in the absence of statins.
Chia, SM; Davis, HR; Hentze, H; Jensen, KK; Johns, DG; Shaw, RJ; Shih, SJ; Wong, KK, 2013
)
0.86
" No difference between 20-mg and 10-mg dosing was seen among patients not receiving statins."( Incremental lowering of low-density lipoprotein cholesterol with ezetimibe 20 mg vs 10 mg daily in patients receiving concomitant statin therapy.
Ban, MR; DeGorter, MK; Hegele, RA; Kim, RB; Schwarz, UI; Tirona, RG; Ziada, A, 2013
)
0.63
" Using a retrospective cohort design, we collected lipid profile data from patients who had been treated with hypolipidemic agents at a stable dosage for at least 12 weeks."( Second-line treatments for dyslipidemia in patients at risk of cardiovascular disease.
Hamai, J; Kamiko, K; Kawasaki, S; Kondo, Y; Nezu, U; Shigematsu, E; Takahashi, M; Takano, T; Terauchi, Y; Yamada, M; Yamakawa, T; Yamazaki, S; Yoshii, T, 2014
)
0.4
"In addition to LDL-C reduction, evolocumab, dosed either Q2W or Q4W, demonstrated significant and favourable changes in other atherogenic and anti-atherogenic lipoproteins, and was well tolerated over the 12-week treatment period."( Efficacy and safety of evolocumab (AMG 145), a fully human monoclonal antibody to PCSK9, in hyperlipidaemic patients on various background lipid therapies: pooled analysis of 1359 patients in four phase 2 trials.
Albizem, M; Giugliano, RP; Kim, JB; Koren, MJ; Liu, T; Raal, FJ; Roth, EM; Sabatine, MS; Scott, R; Somaratne, R; Stein, EA; Sullivan, D; Wasserman, SM; Weiss, R; Yang, J, 2014
)
0.4
" These data suggest that modeling of dose-response relationships may be useful in predicting clinical equivalence, lowering cost/timelines through effective powering of studies, and predicting the effectiveness of new dosage formulations without the need for additional clinical efficacy trials in regulatory settings."( Prediction of clinical irrelevance of PK differences in atorvastatin using PK/PD models derived from literature-based meta-analyses.
Adewale, A; Behm, MO; Kerbusch, T; Mandema, J; Vargo, R, 2014
)
0.4
" Expected differences between FDC and the corresponding co-administered doses were predicted from a dose-response relationship model; sample size was estimated given the expected difference and equivalence margins (±4%)."( Fixed-dose combination ezetimibe+atorvastatin lowers LDL-C equivalent to co-administered components in randomized trials: use of a dose-response model.
Bays, HE; Chen, E; McPeters, G; Polis, AB; Tomassini, JE; Triscari, J, 2015
)
0.73
"This paper describes a new RP-HPLC method for simultaneous quantification of these compounds in the bulk sample drug as well as in tablet dosage forms."( New Validated RP-HPLC Analytical Method for Simultaneous Estimation of Atorvastatin and Ezetimibe in Bulk Samples as Well in Tablet Dosage Forms by Using PDA Detector.
Debnath, M; Kumar, SA; Seshagiri Rao, JV, 2014
)
0.62
" The dosage of atorvastatin will be increased by titration within the usual dose range with a treatment goal of lowering LDL-C below 70 mg/dL based on consecutive measures of LDL-C at follow-up visits."( Plaque REgression with Cholesterol absorption Inhibitor or Synthesis inhibitor Evaluated by IntraVascular UltraSound (PRECISE-IVUS Trial): Study protocol for a randomized controlled trial.
Fujimoto, K; Hokimoto, S; Ishihara, M; Kaikita, K; Koide, S; Komura, N; Matsui, K; Matsumura, T; Matsuyama, K; Morikami, Y; Nakamura, N; Nakamura, S; Nakao, K; Ogawa, H; Oka, H; Ono, T; Oshima, S; Sakaino, N; Sakamoto, K; Shimomura, H; Sugiyama, S; Sumida, H; Tsujita, K; Tsunoda, R; Yamamoto, N; Yamanaga, K; Yamashita, T, 2015
)
0.42
" Afterwards, clinicians have several options to treat dyslipidemia, including the use of a lower dose of the same statin, intermittent non-daily dosing of statin, initiation of a different statin, alone or in combination with nonstatin lipid-lowering agents, and substitution with red yeast rice."( Risk identification and possible countermeasures for muscle adverse effects during statin therapy.
Macchi, C; Magni, P; Morlotti, B; Ruscica, M; Sirtori, CR, 2015
)
0.42
" Thus, the management of patients intolerant to statins, particularly those at high or very high cardiovascular risk, involves alternative therapies, including the switch to another statin or the use of intermittent dosage statin regimens, as well as nonstatin lipid lowering drugs (ezetimibe and fibrates) or new hypolipidemic drugs such as PCSK9 monoclonal antibodies, the antisense oligonucleotide against the coding region of human apolipoprotein B mRNA (mipomersen), and microsomal triglyceride transfer protein inhibitor lomitapide."( Statin intolerance: diagnosis and remedies.
Catapano, AL; Pirillo, A, 2015
)
0.59
" The proposed methods were successfully applied for the determination of the investigated drugs in pure form, dosage form and in synthetic mixtures with good recovery and the results obtained were favorably compared to those obtained with a reference method."( Application of new spectrofluorometric techniques for determination of atorvastatin and ezetimibe in combined tablet dosage form.
Ayad, MF; Magdy, N, 2015
)
0.64
"Evolocumab (Repatha(®)) is a monoclonal antibody targeting proprotein convertase subtilisin/kexin type 9 (PCSK9) that is administered subcutaneously at a dosage of 140 mg every 2 weeks or 420 mg once monthly."( Evolocumab: A Review in Hyperlipidemia.
Keating, GM, 2016
)
0.43
" Every-4-weeks dosing of alirocumab may be appropriate for some patients in absence of background statin but is not yet approved."( Relationship Between Low-Density Lipoprotein Cholesterol, Free Proprotein Convertase Subtilisin/Kexin Type 9, and Alirocumab Levels After Different Lipid-Lowering Strategies.
Brunet, A; Cannon, CP; DiCioccio, AT; Hanotin, C; Paehler, T; Pinquier, JL; Poitiers, F; Rey, J; Sasiela, WJ; Surks, HK, 2016
)
0.43
" The dosage of atorvastatin was uptitrated with a treatment goal of lowering low-density lipoprotein cholesterol to below 70 mg/dl in both groups."( Synergistic effect of ezetimibe addition on coronary atheroma regression in patients with prior statin therapy: Subanalysis of PRECISE-IVUS trial.
Fujimoto, K; Hokimoto, S; Ishihara, M; Kaikita, K; Koide, S; Komura, N; Matsui, K; Matsumura, T; Matsuyama, K; Morikami, Y; Nakamura, N; Nakamura, S; Nakao, K; Ogawa, H; Oka, H; Oshima, S; Sakaino, N; Sakamoto, K; Shimomura, H; Sugiyama, S; Sumida, H; Tsujita, K; Tsunoda, R; Yamamoto, N; Yamanaga, K; Yamashita, T, 2016
)
0.75
" Because the option of a monthly dosing regimen is convenient, ODYSSEY CHOICE II evaluated alirocumab 150 mg Q4W in patients with inadequately controlled hypercholesterolemia and not on statin (majority with statin-associated muscle symptoms), receiving treatment with fenofibrate, ezetimibe, or diet alone."( Efficacy and Safety of Alirocumab 150 mg Every 4 Weeks in Patients With Hypercholesterolemia Not on Statin Therapy: The ODYSSEY CHOICE II Study.
Baccara-Dinet, MT; Civeira, F; Farnier, M; Gaudet, D; Guyton, JR; Lecorps, G; Lepor, N; Manvelian, G; Stroes, E; Watts, GF, 2016
)
0.61
" Identification of clinically significant covariates will support the design and dose selection for the pivotal registration studies, ensuring that patients are dosed appropriately."( Population Pharmacokinetics (PK) and Pharmacodynamics (PD) Analysis of LY3015014, a Monoclonal Antibody to Protein Convertase Subtilisin/Kexin Type 9 (PCSK9) in Healthy Subjects and Hypercholesterolemia Patients.
James, DE; Krueger, KA; Shen, T, 2017
)
0.46
" In vivo, low continuous dosing of ezetimibe, delivered by food, or simvastatin, delivered via an osmotic pump had no effect on tumor growth compared to control mice."( Evidence for Feedback Regulation Following Cholesterol Lowering Therapy in a Prostate Cancer Xenograft Model.
Alfaqih, MA; Barry, WT; Dambal, SK; Dewhirst, MW; Freedland, AR; Freedland, SJ; Freeman, MR; Macias, E; Masko, EM; Muehlbauer, MJ; Newgard, CB; Phillips, TE; Pizzo, SV; Poulton, SH; Sanders, SE; Solomon, KR; Sun, S; Valilis, NA, 2017
)
0.73
" Preventive effect of high-dose statin treatment is without doubt, although administration of such high dosage might require special precautions for patients with prior intracerebral hemorrhage and it also risks development of incident diabetes."( [Lipids and cerebrovascular disease - New therapeutic options in lowering LDL-cholesterol].
Csécsei, P; Karádi, Z; Lovadi, E; Lovig, C; Szapáry, L, 2016
)
0.43
" Finally, poor adherence was slightly more prevalent among patients treated with less effective statins, and at both low and maximal dosage regimens."( Effectiveness of adherence to lipid lowering therapy on LDL-cholesterol in patients with very high cardiovascular risk: A real-world evidence study in primary care.
Bellia, A; Cricelli, C; Cricelli, I; Della-Morte, D; Guglielmi, V; Lapi, F; Lauro, D; Medea, G; Parretti, D; Pecchioli, S; Sbraccia, P, 2017
)
0.46
" Metformin hydrochloride (MTF), sitagliptin phosphate (SIT), simvastatin (SIM) and ezetimibe (EZB) were simultaneously determined with a simple reversed-phase LC method in which a SIT-SIM binary mixture, present in a dosage form brand, was considered central for its development."( A Versatile Liquid Chromatographic Method for the Simultaneous Determination of Metformin, Sitagliptin, Simvastatin, and Ezetimibe in Different Dosage Forms.
El-Zaher, AA; Elkady, EF; Elwy, HM; Saleh, MAEM, 2018
)
0.91
" There is a clear dose-response effect of statin treatment on PCSK9 level, as increasing doses of statins also increase the level of circulating PCSK9."( Lipid Lowering Therapy and Circulating PCSK9 Concentration.
Nozue, T, 2017
)
0.46
" Areas covered: The efficacy and safety of alirocumab has been initially evaluated in a comprehensive phase 3 program conducted in more than 6 000 patients with primary non-familial and heterozygous familial hypercholesterolemia: alirocumab reduced LDL-cholesterol up to 62% in phase 3 with every 2-week dosing compared with placebo, and up to 36% compared with ezetimibe, with an excellent safety and tolerability profile."( Alirocumab for the treatment of hyperlipidemia in high-risk patients: an updated review.
Farnier, M, 2017
)
0.62
"Changes in low-density lipoprotein cholesterol (LDL-C) and other lipids from baseline to Week 24 were analysed (intention-to-treat) in four pools by alirocumab dosage (150 mg every 2 weeks [150] or 75 mg with possible increase to 150 mg every 2 weeks [75/150]), control (placebo/ezetimibe) and background statin usage (yes/no)."( Efficacy and safety of alirocumab among individuals with diabetes mellitus and atherosclerotic cardiovascular disease in the ODYSSEY phase 3 trials.
Bujas-Bobanovic, M; Ganda, OP; Koren, A; Leiter, LA; Letierce, A; Mandel, J; Plutzky, J; Sanganalmath, SK, 2018
)
0.66
" The increased dosage of rosuvastatin was also well tolerated in the combination treatment."( Efficacy and Safety of Ezetimibe and Rosuvastatin Combination Therapy Versus Those of Rosuvastatin Monotherapy in Patients With Primary Hypercholesterolemia.
Bae, JW; Han, SH; Hong, BK; Hong, SJ; Hwang, GS; Hyon, MS; Kim, JY; Kim, MK; Kim, SH; Kim, SW; Kim, W; Lee, SE; Park, CG; Park, JH; Rhee, MY; Shin, JH; Shin, SH; Son, JW; Sung, KC; Yoon, YE, 2018
)
0.79
"In the prospective, randomized, controlled, multicenter PRECISE-IVUS trial, 246 patients undergoing intravascular ultrasound (IVUS)-guided PCI were randomly assigned to receive atorvastatin/ezetimibe combination or atorvastatin alone (the dosage of atorvastatin was up-titrated to achieve the level of low-density lipoprotein cholesterol < 70 mg/dL)."( Impact of statin-ezetimibe combination on coronary atheroma plaque in patients with and without chronic kidney disease - Sub-analysis of PRECISE-IVUS trial.
Fujimoto, K; Fujisue, K; Hokimoto, S; Ishihara, M; Izumiya, Y; Kaikita, K; Koide, S; Matsui, K; Matsumura, T; Matsuyama, K; Morikami, Y; Nagamatsu, S; Nakamura, S; Nakao, K; Ogawa, H; Oshima, S; Sakamoto, K; Shimomura, H; Tsujita, K; Tsunoda, R; Yamamoto, N; Yamashita, T, 2018
)
1.01
" The method is suitable for both drug substance and oral solid dosage form."( Development of a Simple, Highly Selective RP-LC Method for the Quantification of Diastereomers and Other Related Substances of Ezetimibe Using Multivariate Analysis.
Anireddy, JS; Balasubramanian, H; Kumar, RS; Rao, DV, 2019
)
0.72
" The aim of this study was to evaluate the efficacy of adding ezetimibe to simvastatin, atorvastatin, or rosuvastatin monotherapy versus doubling the dosage or switching to a higher-potency statin in a population of patients with hypocholesterolemia at high risk of cardiovascular disease (CVD) and who had been previously treated with a statin."( Ezetimibe in high-risk, previously treated statin patients: a systematic review and network meta-analysis of lipid efficacy.
Ambegaonkar, B; Baxter, CA; Davies, G; Jansen, J; Lorenzi, M; Zoratti, MJ, 2019
)
2.2
" Indeed, a significant number of patients resulted intolerants, especially when the dosage increased."( Current Drugs and Nutraceuticals for the Treatment of Patients with Dyslipidemias.
Costa, D; Napoli, C; Scognamiglio, M; Sorriento, A, 2019
)
0.51
" To increase adherence and prevent worse outcomes, a combination therapy with lower dosage of statins and new lipid-lowering drugs may be used."( An expert opinion paper on statin adherence and implementation of new lipid-lowering medications by the ESC Working Group on Cardiovascular Pharmacotherapy: Barriers to be overcome.
Bilato, C; Coats, AJS; Drexel, H; Mollace, V; Perrone Filardi, P; Rosano, GMC; Spoletini, I, 2020
)
0.56
" To achieve these goals, investigators used the statin and dosage of their choice and added ezetimibe as needed."( Carotid Atherosclerosis Evolution When Targeting a Low-Density Lipoprotein Cholesterol Concentration <70 mg/dL After an Ischemic Stroke of Atherosclerotic Origin.
Amarenco, P; Bruckert, E; Charles, H; Gabriel Steg, P; Giroud, M; Hobeanu, C; Labreuche, J; Lavallée, PC; Meseguer, E; Touboul, PJ; Vicaut, É, 2020
)
0.78
" After a 5-week run-in period of treatment with atorvastatin 10 or 20 mg/d (cohorts A and B, respectively), or a bioequivalent dosage of another statin, patients were randomized in a 1:1 ratio within each cohort to receive EZ/AS 10/10 mg FDC (EZ10/AS10) or atorvastatin 20 mg (AS20), once daily (cohort A); or EZ/AS 10/20 mg FDC (EZ10/AS20) or atorvastatin 40 mg (AS40), once daily (cohort B)."( Efficacy and Tolerability of Ezetimibe/Atorvastatin Fixed-dose Combination Versus Atorvastatin Monotherapy in Hypercholesterolemia: A Phase III, Randomized, Active-controlled Study in Chinese Patients.
Chen, J; Ding, C; Ge, J; Li, Z; Liu, Y; Qian, J; Ren, X; Shi, M; Yang, P; Zhang, X, 2022
)
1.01
" Additionally, ETZ exhibits poor mechanical properties, leading to difficulties in developing dosage forms through direct compression."( Development of ezetimibe eutectic with improved biopharmaceutical and mechanical properties to design an optimized oral solid dosage formulation.
Ghosh, A; Gour, A; Kumari, N; Nandi, U; Pandey, N; Raj, A; Roy, P; Srividya, B, 2022
)
1.07
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
anticholesteremic drugA substance used to lower plasma cholesterol levels.
antilipemic drugA substance used to treat hyperlipidemia (an excess of lipids in the blood).
antimetaboliteA substance which is structurally similar to a metabolite but which competes with it or replaces it, and so prevents or reduces its normal utilization.
[role 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]

Drug Classes (3)

ClassDescription
azetidines
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
beta-lactamA lactam in which the amide bond is contained within a four-membered ring, which includes the amide nitrogen and the carbonyl carbon.
[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]

Pathways (1)

PathwayProteinsCompounds
Drug induction of bile acid pathway025

Protein Targets (37)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency29.84930.006038.004119,952.5996AID1159523
TDP1 proteinHomo sapiens (human)Potency33.49830.000811.382244.6684AID686979
GLI family zinc finger 3Homo sapiens (human)Potency31.61800.000714.592883.7951AID1259392
AR proteinHomo sapiens (human)Potency19.28800.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency9.43920.000657.913322,387.1992AID1259378
progesterone receptorHomo sapiens (human)Potency25.15670.000417.946075.1148AID1346784; AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.56510.01237.983543.2770AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency13.33320.003041.611522,387.1992AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency27.13040.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency29.84930.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency29.84930.000229.305416,493.5996AID1259244
GVesicular stomatitis virusPotency8.22000.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency12.50460.00108.379861.1304AID1645840
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency29.84700.001019.414170.9645AID743191
aryl hydrocarbon receptorHomo sapiens (human)Potency21.59130.000723.06741,258.9301AID743085; AID743122
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency22.38720.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.60320.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency25.15470.000627.21521,122.0200AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency13.51610.00798.23321,122.0200AID2546; AID2551
neuropeptide S receptor isoform AHomo sapiens (human)Potency5.01190.015812.3113615.5000AID1461
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency29.84930.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency8.22000.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.22000.01238.964839.8107AID1645842
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency29.84930.001551.739315,848.9004AID1259244
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency12.58930.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.22000.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.22000.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)56.00000.11007.190310.0000AID1473738
NPC1-like intracellular cholesterol transporter 1Rattus norvegicus (Norway rat)Ki0.20000.18000.19000.2000AID315718
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
NPC1-like intracellular cholesterol transporter 1Homo sapiens (human)IC50 (µMol)0.37000.30000.32330.3700AID1872307
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km64.00004.49006.51339.0000AID624630
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km42.00007.34007.34007.3400AID624632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (121)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
androgen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B7Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
bile acid secretionUDP-glucuronosyltransferase 1A3Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A3Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A3Homo sapiens (human)
sodium ion transportSodium/bile acid cotransporterHomo sapiens (human)
response to organic cyclic compoundSodium/bile acid cotransporterHomo sapiens (human)
bile acid and bile salt transportSodium/bile acid cotransporterHomo sapiens (human)
response to nutrient levelsSodium/bile acid cotransporterHomo sapiens (human)
bile acid signaling pathwaySodium/bile acid cotransporterHomo sapiens (human)
response to estrogenSodium/bile acid cotransporterHomo sapiens (human)
response to ethanolSodium/bile acid cotransporterHomo sapiens (human)
symbiont entry into host cellSodium/bile acid cotransporterHomo sapiens (human)
transmembrane transportSodium/bile acid cotransporterHomo sapiens (human)
cellular response to xenobiotic stimulusSodium/bile acid cotransporterHomo sapiens (human)
regulation of bile acid secretionSodium/bile acid cotransporterHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cholesterol biosynthetic processNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
intestinal cholesterol absorptionNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
cholesterol transportNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
lipoprotein metabolic processNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
vitamin E metabolic processNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
vitamin transportNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
cellular response to sterol depletionNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
cholesterol homeostasisNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (53)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A3Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A3Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A3Homo sapiens (human)
virus receptor activitySodium/bile acid cotransporterHomo sapiens (human)
protein bindingSodium/bile acid cotransporterHomo sapiens (human)
bile acid:sodium symporter activitySodium/bile acid cotransporterHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
vitamin E bindingNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
cholesterol bindingNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
small GTPase bindingNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
myosin V bindingNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
protein homodimerization activityNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (38)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A3Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A3Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A3Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneSodium/bile acid cotransporterHomo sapiens (human)
basolateral plasma membraneSodium/bile acid cotransporterHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
plasma membraneNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
apical plasma membraneNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
cytoplasmic vesicle membraneNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
plasma membraneNPC1-like intracellular cholesterol transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (255)

Assay IDTitleYearJournalArticle
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211319Drug level in methionine and choline deficient fed Sprague-Dawley rat bile at 10 mg/kg, iv after 30 to 90 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1567204Chaperone activity at GALNS p.R61W/p.W405_T406 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in p62 level at 0.001 to 0.01 uM measured after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1168723Cytotoxicity against human HepG2 cells after 4 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID178717Compound was tested for the change in serum cholesterol (SC) level in cholesterol fed rat2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
The discovery of ezetimibe: a view from outside the receptor.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1896147Antiviral activity against hepatitis D virus infected in human Huh-7 cells overexpressing NTCP assessed as reduction in intracellular HDV RNA for 20 hrs followed by viral infection further compound washout and measured after 6 days post infection by RT-qP2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
AID1275465Decrease in free fatty acid level in serum of cholesterol fed hamster model at 50 mg/kg/day, po administered for 7 days measured on day 7 post last dose2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID24830Percent negation of rise in total serum cholesterol relative to control-fed 0.5% cholesterol for 7 days, At a dose of 0.1 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211292Drug metabolism in human intestinal microsomes assessed as UGT1A1-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID289523Decrease in LDL-cholesterol levels in high-cholesterol diet fed Wistar rat at 4 mg/kg/day2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Ezetimibe analogs with a reorganized azetidinone ring: Design, synthesis, and evaluation of cholesterol absorption inhibitions.
AID1758168Inhibition of PTL (unknown origin) at 50 uM relative to control2021European journal of medicinal chemistry, Apr-15, Volume: 216One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.
AID1567208Chaperone activity at GALNS p.R61W/p.W405_T406 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in LC3B-2 level at 0.001 to 0.01 uM measured after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID624630Drug glucuronidation reaction catalyzed by human recombinant UGT1A12005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID547673Antidyslipidemic activity in cholesterol-fed rhesus monkey assessed as reduction in plasma cholesterol2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
2-Azetidinone--a new profile of various pharmacological activities.
AID548191Inhibition of [3H]cholesterol absorption in C57BL/6 mouse plasma at 1 mg/kg, po after 1.5 hrs2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Spiroimidazolidinone NPC1L1 inhibitors. Part 2: structure-activity studies and in vivo efficacy.
AID24836Percent negation of rise in total serum cholesterol relative to control-fed 0.5% cholesterol for 7 days, at a dose of 0.03 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID1599411Antiviral activity against DENV2 New Guinea infected in human Huh7 cells assessed as reduction in viral yield after 48 hrs by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Recent update on anti-dengue drug discovery.
AID1195465Inhibition of [3H]cholesterol uptake in C57BL/6 mouse duodenum at 20 mg/kg/day, po for 2 days measured 4 hrs post last dose on day 22015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID624640Drug glucuronidation reaction catalyzed by human recombinant UGT2B72005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1195467Inhibition of [3H]cholesterol uptake in C57BL/6 mouse ileum at 20 mg/kg/day, po for 2 days measured 4 hrs post last dose on day 22015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID1389994Antiinflammatory activity against mouse RAW264.7 cells assessed as decrease in cholesterol-methyl-beta-cyclodextrin-induced TNFalpha release at 30 uM relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1567190Chaperone activity at GALNS p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in enzyme activity at 0.001 to 0.01 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 48 hrs by2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID86018Compound was tested for percent reduction of liver cholesterol esters absorption in cholesterol fed hamster model at a dose of 3 mg/kg/day1998Bioorganic & medicinal chemistry letters, Feb-03, Volume: 8, Issue:3
Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: enhanced potency by modification of the sugar.
AID1567199Chaperone activity at GALNS p.R386C/p.F285 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as decrease in lysosomal mass measured after 48 hrs by LysoTracker Red DND-99/hoechst dye based fluorescence assay2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1211216Unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1211221Ratio of unbound intrinsic glucuronidation clearance in human kidney microsomes in presence of 2% bovine serum albumin to unbound intrinsic glucuronidation clearance in human kidney microsomes in absence of bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID89949Compound was tested for the reduction in low density lipoprotein cholesterol2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
The discovery of ezetimibe: a view from outside the receptor.
AID1567206Chaperone activity at GALNS p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in p62 level at 0.001 to 0.01 uM measured after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1567196Chaperone activity at GALNS p.R61W/p.W405_T406 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as decrease in lysosomal mass measured after 48 hrs by LysoTracker Red DND-99/hoechst dye based fluorescence assay2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1567178Inhibition of recombinant human GALNS expressed in Pichia pastoris at 10 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 18 hrs by fluorescence assay relative to control2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID315718Displacement of [3H]ezetimibe-glucuronide from NPC1L1 in Sprague-Dawley rat brush border membrane2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption.
AID1195461Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID1211252Drug metabolism in human intestinal microsomes assessed as UGT2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 1% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1211201Drug metabolism in human liver microsomes assessed as UGT1A1-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1473762Ratio of drug concentration at steady state in human at 10 mg, po after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1567188Chaperone activity at GALNS p.R61W/p.W405_T406 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in enzyme activity at 0.001 to 0.01 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate meas2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1567189Chaperone activity at GALNS p.R94C/p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in enzyme activity at 0.001 to 0.01 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 482019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID24838The pharmacokinetics property percent negation of rise in liver cholesterol esters relative to control-fed 0.5% cholesterol for 7 days, At a dose of 0.03 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID1567191Chaperone activity at GALNS p.R386C/p.F285 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in enzyme activity at 0.001 to 0.01 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1211237Fraction unbound in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID547674Antidyslipidemic activity in cholesterol-fed hamster model assessed as reduction in liver cholesteryl esters2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
2-Azetidinone--a new profile of various pharmacological activities.
AID289522Decrease in total cholesterol levels in high-cholesterol diet fed Wistar rat at 4 mg/kg/day2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Ezetimibe analogs with a reorganized azetidinone ring: Design, synthesis, and evaluation of cholesterol absorption inhibitions.
AID547675Antidyslipidemic activity in cholesterol-fed Dog assessed as reduction in plasma cholesterol level2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
2-Azetidinone--a new profile of various pharmacological activities.
AID422543Reduction in human pancreatic recombinant 1B PLA2 activity expressed in Escherichia coli assessed as hydrolysis of 1,2-dimyristoyl-sn-3-glycerophosphocholine vesicles at 0.03 mol fraction relative to cholate2009Journal of natural products, Jan, Volume: 72, Issue:1
Effect of guggulsterone and cembranoids of Commiphora mukul on pancreatic phospholipase A(2): role in hypocholesterolemia.
AID1567213Chaperone activity at GALNS p.R94C/p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as decrease in lysosomal mass at 0.001 uM measured after 72 hrs in presence of recombinant human GALNS expressed in Pichia pastoris by LysoTrac2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1567187Chaperone activity at recombinant human GALNS expressed in HEK293 cells assessed as increase in GALNs level at 0.001 mM measured after 48 hrs by LysoTracker Green DND-26/DAPI staining based immunofluorescence assay2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1567185Chaperone activity at recombinant human GALNS expressed in HEK293 cells assessed as increase in intracellular enzyme activity at 0.001 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 48 hrs by fluorescence assa2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1211225Drug metabolism in human liver microsomes assessed as UGT1A1-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1211194Ratio of UGT1A1-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A1-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1567181Chaperone activity at recombinant human GALNS expressed in Escherichia coli BL21 (DE3) assessed as increase in extracellular enzyme activity at 0.001 to 1 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 24 hrs 2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID315720Half life in rat hepatocytes2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption.
AID1211251Unbound intrinsic glucuronidation clearance in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID315719Inhibition of cholesterol absorption in chow fed hamster at 3 mg/kg, po2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1211272Ratio of UGT1A1-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A1-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM in presence of 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID374274Hypocholesterolemic effect in high cholesterol-fed hamster assessed as reduction in plasma total cholesterol at 50 mg/kg, po for 7 days2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
2-Azetidinone derivatives: design, synthesis and evaluation of cholesterol absorption inhibitors.
AID59638Compound was tested for the change in serum cholesterol (SC) levels in cholesterol fed dog2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
The discovery of ezetimibe: a view from outside the receptor.
AID1195464Inhibition of [3H]cholesterol uptake in C57BL/6 mouse liver at 20 mg/kg/day, po for 2 days measured 4 hrs post last dose on day 22015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID1896146Binding affinity to NTCP (unknown origin)2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
AID1599410Antiviral activity against DENV1 infected in human Huh7 cells assessed as reduction in viral yield after 48 hrs by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Recent update on anti-dengue drug discovery.
AID1211333Drug level in methionine and choline deficient fed Sprague-Dawley rat plasma at 10 mg/kg, po after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1275467Increase in proportion of high density lipoprotein cholesterol to total cholesterol in serum of cholesterol fed hamster at 50 mg/kg/day, po administered for 7 days measured on day 7 post last dose2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID1211334Drug metabolism in methionine and choline deficient fed Sprague-Dawley rat plasma assessed as ezetimibe glucuronide formation at 10 mg/kg, po after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1211340Drug metabolism in methionine and choline deficient fed Sprague-Dawley rat plasma assessed as ezetimibe glucuronide formation at 10 mg/kg, iv after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1211258Ratio of UGT1A1-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A1-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM in presence of 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1211211Unbound intrinsic glucuronidation clearance in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1758176Inhibition of PTL mRNA expression in human Caco-2 cells at 100 uM incubated for 24 hrs by qRT-PCR analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211325Drug level in methionine and choline deficient fed Sprague-Dawley rat urine at 10 mg/kg, iv after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1168724Inhibition of cholesterol uptake in MDCK2 cells at 20 to 100 uM after 1 hr by liquid scintillation counting2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID24833Percent negation of rise in total serum cholesterol relative to control-fed 0.5% cholesterol for 7 days, At a dose of 1 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID1567211Chaperone activity at GALNS p.R386C/p.F285 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in LC3B-2 level at 0.001 to 0.01 uM measured after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID182776Compound was tested for cholesterol absorption inhibition in rats by bolus injection 1 mL) via the intestinal catheter into the small intestine, by cholesterol absorption assay2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis of fluorescent biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1211336Drug level in methionine and choline deficient fed Sprague-Dawley rat plasma at 10 mg/kg, iv after 40 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1168733In vivo inhibition of acute [3H]cholesterol absorption in C57BL/6 mouse ileum at 10 mg/kg/day, po for 2 days before cholesterol administration measured 4 hrs post cholesterol administration relative to vehicle-treated control2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID422555Antagonist activity at human FXR transfected in human HuH7 cells co-transfected with human BSEP promoter reporter plasmid at 10 uM after 30 hrs by dual-luciferase reporter assay relative to chenodeoxycholate2009Journal of natural products, Jan, Volume: 72, Issue:1
Effect of guggulsterone and cembranoids of Commiphora mukul on pancreatic phospholipase A(2): role in hypocholesterolemia.
AID1567193Chaperone activity at GALNS p.R94C/p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in protein expression at 0.001 to 0.01 uM after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID86158Compound was tested for percent reduction of serum cholesterol absorption in cholesterol fed hamster model at a dose of 3 mg/kg/day1998Bioorganic & medicinal chemistry letters, Feb-03, Volume: 8, Issue:3
Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: enhanced potency by modification of the sugar.
AID1211329Effect on total bile acid levels in Sprague-Dawley rat nonalcoholic steatohepatitis model at 10 mg/kg, iv after 120 mins by spectrophotometry2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1758179Inhibition of NPC1L1 expression in human Caco-2 cells at 0.1 to 100 uM incubated for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.
AID84698Compound was tested for the change in liver cholesterol (CE) levels in hamster2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
The discovery of ezetimibe: a view from outside the receptor.
AID1567205Chaperone activity at GALNS p.R94C/p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in p62 level at 0.001 to 0.01 uM measured after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211219Ratio of unbound intrinsic glucuronidation clearance in human liver microsomes in presence of 2% bovine serum albumin to unbound intrinsic glucuronidation clearance in human liver microsomes in absence of bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1567210Chaperone activity at GALNS p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in LC3B-2 level at 0.001 to 0.01 uM measured after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID374275Hypocholesterolemic effect in high cholesterol-fed hamster assessed as increase in HDL-cholesterol at 50 mg/kg, po for 7 days2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
2-Azetidinone derivatives: design, synthesis and evaluation of cholesterol absorption inhibitors.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211249Unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1389991Inhibition of NPC1L1-mediated cholesterol-methyl-beta-cyclodextrin accumulation in mouse RAW264.7 cells incubated for 72 hrs by Oil Red O/hematoxyline staining based microscopic analysis2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1211326Drug metabolism in methionine and choline deficient fed Sprague-Dawley rat urine assessed as ezetimibe glucuronide formation at 10 mg/kg, iv after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1567180Chaperone activity at recombinant human GALNS expressed in Escherichia coli BL21 (DE3) assessed as increase in intracellular enzyme activity at 0.001 to 1 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 24 hrs 2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1567207Chaperone activity at GALNS p.R386C/p.F285 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in p62 level at 0.001 to 0.01 uM measured after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1211187Ratio of UGT1A1-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes to UGT1A1-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID711532Inhibition of cholesterol absorption in syrian golden hamster2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1211265Ratio of UGT1A1-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes to UGT1A1-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM in presence of 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID422544Reduction in human pancreatic recombinant 1B PLA2 activity expressed in Escherichia coli assessed as hydrolysis of 1,2-dimyristoyl-sn-3-glycerophosphocholine vesicles at 0.007 mol fraction relative to cholate2009Journal of natural products, Jan, Volume: 72, Issue:1
Effect of guggulsterone and cembranoids of Commiphora mukul on pancreatic phospholipase A(2): role in hypocholesterolemia.
AID1195459Cytotoxicity against MDCK2 cells after 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1168722Cytotoxicity against MDCK2 cells after 4 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID1275466Decrease in triglyceride level in serum of cholesterol fed hamster model at 50 mg/kg/day, po administered for 7 days measured on day 7 post last dose2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID1211342Drug level in methionine and choline deficient fed Sprague-Dawley rat bile at 10 mg/kg, po after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1389993Inhibition of NPC1L1-mediated cholesterol-methyl-beta-cyclodextrin accumulation in mouse RAW264.7 cells assessed as decrease in foam cell formation by measuring decrease in MDA level at 30 uM relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID422554Agonist activity at human FXR transfected in human HuH7 cells co-transfected with human BSEP promoter reporter plasmid at 10 uM after 30 hrs by dual-luciferase reporter assay relative to control2009Journal of natural products, Jan, Volume: 72, Issue:1
Effect of guggulsterone and cembranoids of Commiphora mukul on pancreatic phospholipase A(2): role in hypocholesterolemia.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID24840The pharmacokinetics property percent negation of rise in liver cholesterol esters relative to control-fed 0.5% cholesterol for 7 days, At a dose of 0.3 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID24835Percent negation of rise in total serum cholesterol relative to control-fed 0.5% cholesterol for 7 days, At a dose of 3 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID1168737Inhibition of cholesterol uptake in MDCK2 cells expressing human NPC1L1 at 20 to 100 uM after 1 hr by liquid scintillation counting2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1567194Chaperone activity at GALNS p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in protein expression at 0.001 to 0.01 uM after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID89950Compound was tested for the reduction in total cholesterol2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
The discovery of ezetimibe: a view from outside the receptor.
AID89951Compound was tested for the reduction in triglycerides2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
The discovery of ezetimibe: a view from outside the receptor.
AID1168735In vivo inhibition of acute [3H]cholesterol absorption in C57BL/6 mouse liver at 10 mg/kg/day, po for 2 days before cholesterol administration measured 4 hrs post cholesterol administration relative to vehicle-treated control2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID1567184Chaperone activity at recombinant human GALNS expressed in HEK293 cells assessed as increase in extracellular enzyme activity at 0.01 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 48 hrs by fluorescence assay2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1389987Cytotoxicity against mouse RAW264.7 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID1431667Antagonist activity at Myc-tagged RXRalpha (unknown origin) expressed in human MCF-7 cells assessed as inhibition of 9-cis-RA induced receptor transactivation at 10 uM after 24 hrs by luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Virtual screening and experimental validation identify novel modulators of nuclear receptor RXRα from Drugbank database.
AID1211241Fraction unbound in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1567214Chaperone activity at GALNS p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as decrease in lysosomal mass at 0.001 uM measured after 72 hrs in presence of recombinant human GALNS expressed in Pichia pastoris by LysoTracker Red2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID86163In vivo activity in a cholesterol-fed hamster assay was determined at 1 mg/kg/day2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
AID1567195Chaperone activity at GALNS p.R386C/p.F285 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in protein expression at 0.001 to 0.01 uM after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID24831Percent negation of rise in total serum cholesterol relative to control-fed 0.5% cholesterol for 7 days, At a dose of 0.3 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1567197Chaperone activity at GALNS p.R94C/p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as decrease in lysosomal mass measured after 48 hrs by LysoTracker Red DND-99/hoechst dye based fluorescence assay2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID768314Competitive binding affinity to human GFP-tagged NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as localization to endoplasmic reticulum and plasma membrane at 0.01 to 10 uM after 24 hrs by fluorescence microscopic analysis in presence of 2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Structure-activity relationship studies of Niemann-Pick type C1-like 1 (NPC1L1) ligands identified by screening assay monitoring pharmacological chaperone effect.
AID89948Compound was tested for the reduction in high density lipoprotein cholesterol2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
The discovery of ezetimibe: a view from outside the receptor.
AID1567216Chaperone activity at recombinant human GALNS expressed in Pichia pastoris assessed as increase in extracellular enzyme level by bioreactor-based assay2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1195469Cytotoxicity against MDCK2 cells expressing human NPC1L1 dosed with micelles after 1 hr2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID1275458Octanol-water partition coefficient, logP of the compound by HPLC analysis2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID84866Evaluated for its ability to reduce liver cholesterol esters(LCE) in cholesterol-fed hamsters.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID1473761Drug concentration at steady state in human at 10 mg, po after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1168731In vivo inhibition of acute [3H]cholesterol absorption in C57BL/6 mouse jejunum at 10 mg/kg/day, po for 2 days before cholesterol administration measured 4 hrs post cholesterol administration relative to vehicle-treated control2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID1567220Half life in po dosed human2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID126335Compound was tested for the change in serum cholesterol (SC) levels in cholesterol fed monkey2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
The discovery of ezetimibe: a view from outside the receptor.
AID181919Percent inhibition of 14C]cholesterol absorption into plasma using cholesterol absorption assay in rats at the dose of 10 ug/Kg2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis of fluorescent biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
AID1389988Inhibition of NPC1L1 in human Caco2 cells assessed as decrease in cholesterol uptake at 100 uM preincubated for 24 hrs followed by stigmosterol substrate addition measured after 24 hrs by HPLC method relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID1758178Inhibition of PTL expression in human Caco-2 cells at 0.1 to 100 uM incubated for 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.
AID1275464Decrease in low density lipoprotein cholesterol level in serum of cholesterol fed hamster model at 50 mg/kg/day, po administered for 7 days measured on day 7 post last dose2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID1567183Chaperone activity at recombinant human GALNS expressed in HEK293 cells assessed as increase in intracellular enzyme activity at 0.01 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 48 hrs by fluorescence assay2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1567215Chaperone activity at GALNS p.R386C/p.F285 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as decrease in lysosomal mass at 0.001 uM measured after 72 hrs in presence of recombinant human GALNS expressed in Pichia pastoris by2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1872307Inhibition of NPC1L1 (unknown origin) assessed as inhibition of cholesterol cellular uptake by BCA colorimetric assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Niemann-Pick C1-Like 1 inhibitors for reducing cholesterol absorption.
AID1275461Cytotoxicity against human GES-1 cells assessed as cell viability after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID1168720Cytotoxicity against MDCK2 cells expressing human NPC1L1 after 4 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID84707Dose required to inhibit cholesterol absorption in cholesterol fed hamster model1998Bioorganic & medicinal chemistry letters, Feb-03, Volume: 8, Issue:3
Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: enhanced potency by modification of the sugar.
AID1211245Unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1211213Unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1567192Chaperone activity at GALNS p.R61W/p.W405_T406 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in protein expression at 0.001 to 0.01 uM after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID315721Metabolic stability assessed as half life in rat liver microsomes2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption.
AID1275472Toxicity in cholesterol fed hamster model assessed as decrease in body weight at 50 mg/kg/day, po administered for 7 days measured for 3 days during compound dosing2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID1389992Inhibition of NPC1L1-mediated cholesterol-methyl-beta-cyclodextrin accumulation in mouse RAW264.7 cells assessed as decrease in foam cell formation by measuring decrease in LDH level at 30 uM relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID1211232Drug metabolism in human kidney microsomes assessed as UGT1A1-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1211320Drug metabolism in methionine and choline deficient fed Sprague-Dawley rat bile assessed as ezetimibe glucuronide formation at 10 mg/kg, iv after 30 to 90 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1211339Drug level in methionine and choline deficient fed Sprague-Dawley rat plasma at 10 mg/kg, iv after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID181923Percent inhibition of 14C]cholesterol absorption into plasma using cholesterol absorption assay in rats at the dose of 3 ug/Kg2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis of fluorescent biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
AID256344Percent inhibition against cholesterol absorption in brush border membrane vesicle using rabbit small intestine at concentration of 6 uM2005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Synthesis and in vitro evaluation of inhibitors of intestinal cholesterol absorption.
AID1567198Chaperone activity at GALNS p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as decrease in lysosomal mass measured after 48 hrs by LysoTracker Red DND-99/hoechst dye based fluorescence assay2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1211322Drug level in methionine and choline deficient fed Sprague-Dawley rat urine at 10 mg/kg, po after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1211330Drug level in methionine and choline deficient fed Sprague-Dawley rat plasma at 10 mg/kg, po after 40 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1389986Cytotoxicity against HEK293 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID84842Effective dose required to produe activity in cholesterol hamster assay was determined2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
AID1211180Ratio of UGT1A1-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A1-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID768317Binding affinity to human GFP-tagged NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as localization to endoplasmic reticulum and plasma membrane at 10 uM after 24 hrs by fluorescence microscopic analysis2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Structure-activity relationship studies of Niemann-Pick type C1-like 1 (NPC1L1) ligands identified by screening assay monitoring pharmacological chaperone effect.
AID1758177Inhibition of NPC1L1 mRNA expression in human Caco-2 cells at 100 uM incubated for 24 hrs by qRT-PCR analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.
AID1567186Chaperone activity at recombinant human GALNS expressed in HEK293 cells assessed as increase in extracellular enzyme activity at 0.001 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate measured after 48 hrs by fluorescence assa2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1389995Antiinflammatory activity against mouse RAW264.7 cells assessed as decrease in cholesterol-methyl-beta-cyclodextrin-induced ROS level at 30 uM relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID1211337Drug metabolism in methionine and choline deficient fed Sprague-Dawley rat plasma assessed as ezetimibe glucuronide formation at 10 mg/kg, iv after 40 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1168727In vivo inhibition of acute [3H]cholesterol absorption in C57BL/6 mouse plasma at 10 mg/kg/day, po for 2 days before cholesterol administration measured 4 hrs post cholesterol administration relative to vehicle-treated control2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID255693Effective dose required for reduction of liver cholesterol ester using 7-day cholesterol-fed hamster model2005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Synthesis and in vitro evaluation of inhibitors of intestinal cholesterol absorption.
AID1567182Chaperone activity at recombinant human GALNS expressed in Pichia pastoris assessed as increase in extracellular enzyme activity at 0.001 uM using 4-methylumbelliferyl-beta-D-galactopyranoside-6-sulfate as substrate treated every 24 hrs for 96 hrs by fluo2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1567209Chaperone activity at GALNS p.R94C/p.A393S mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as increase in LC3B-2 level at 0.001 to 0.01 uM measured after 48 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1275462Cytotoxicity against human HEK293 cells assessed as cell viability after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID1567179Stabilization of recombinant human GALNS expressed in Pichia pastoris assessed as melting temperature at 1 uM by SYPRO orange dye based fluorescence assay (Rvb = 62.8 degC)2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1211343Drug metabolism in methionine and choline deficient fed Sprague-Dawley rat bile assessed as ezetimibe glucuronide formation at 10 mg/kg, po after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1211323Drug metabolism in methionine and choline deficient fed Sprague-Dawley rat urine assessed as ezetimibe glucuronide formation at 10 mg/kg, po after 120 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID1211208Drug metabolism in human kidney microsomes assessed as UGT1A1-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1195460Cytotoxicity against MDCK2 cells expressing human NPC1L1 after 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID1389989Inhibition of NPC1L1 in mouse RAW264.7 cells assessed as decrease in choleserol-D7 absorption at 30 uM after 72 hrs by LC-MS/MS analysis relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response.
AID1195463Inhibition of human NPC1L1 transfected in MDCK2 cells assessed as [3H]cholesterol uptake at 60 uM after 1 hr by liquid scintillation counting analysis2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID624632Drug glucuronidation reaction catalyzed by human recombinant UGT1A32005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1599413Antiviral activity against DENV2 H241 infected in human Huh7 cells assessed as reduction in viral yield after 48 hrs by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Recent update on anti-dengue drug discovery.
AID1211244Fraction unbound in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 2% bovine serum albumin2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID24842The pharmacokinetics property percent negation of rise in liver cholesterol esters relative to control-fed 0.5% cholesterol for 7 days, At a dose of 1 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID1599412Antiviral activity against DENV3 infected in human Huh7 cells assessed as reduction in viral yield after 48 hrs by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Recent update on anti-dengue drug discovery.
AID1567212Chaperone activity at GALNS p.R61W/p.W405_T406 deletion mutant in mucopolysaccharidosis patient-derived fibroblasts assessed as decrease in lysosomal mass at 0.001 uM measured after 72 hrs in presence of recombinant human GALNS expressed in Pichia pastori2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211173Drug metabolism in human intestinal microsomes assessed as UGT1A1-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID24843The pharmacokinetics property percent negation of rise in liver cholesterol esters relative to control-fed 0.5% cholesterol for 7 days, At a dose of 3 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID1473760AUC in human at 10 mg, po after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1211328Effect on total bile acid levels in Sprague-Dawley rat nonalcoholic steatohepatitis model at 10 mg/kg, po after 120 mins by spectrophotometry2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID24839The pharmacokinetics property percent negation of rise in liver cholesterol esters relative to control-fed 0.5% cholesterol for 7 days, At a dose of 0.1 mg/kg/day1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
AID1195468Cytotoxicity against MDCK2 cells dosed with micelles after 1 hr2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID548195Inhibition of [3H]cholesterol absorption in C57BL/6 mouse plasma at 1 mg/kg, po after 5 hrs2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Spiroimidazolidinone NPC1L1 inhibitors. Part 2: structure-activity studies and in vivo efficacy.
AID1168729In vivo inhibition of acute [3H]cholesterol absorption in C57BL/6 mouse duodenum at 10 mg/kg/day, po for 2 days before cholesterol administration measured 4 hrs post cholesterol administration relative to vehicle-treated control2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors.
AID1758174Inhibition of NPC1L1 in human Caco-2 cells assessed as decrease in uptake of cholesterol-d6 at 50 uM by HPLC-MS analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.
AID1211239Fraction unbound in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin.
AID1275463Decrease in total cholesterol level in serum of cholesterol fed hamster model at 50 mg/kg/day, po administered for 7 days measured on day 7 post last dose2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors.
AID1195466Inhibition of [3H]cholesterol uptake in C57BL/6 mouse jejunum at 20 mg/kg/day, po for 2 days measured 4 hrs post last dose on day 22015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
AID1211331Drug metabolism in methionine and choline deficient fed Sprague-Dawley rat plasma assessed as ezetimibe glucuronide formation at 10 mg/kg, po after 40 mins by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1346036Human NPC1 like intracellular cholesterol transporter 1 (Patched family)2005Proceedings of the National Academy of Sciences of the United States of America, Jun-07, Volume: 102, Issue:23
The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,314)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (0.17)18.2507
2000's697 (30.12)29.6817
2010's1185 (51.21)24.3611
2020's428 (18.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 112.94

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index112.94 (24.57)
Research Supply Index8.02 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index207.31 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (112.94)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials563 (22.67%)5.53%
Reviews504 (20.29%)6.00%
Case Studies103 (4.15%)4.05%
Observational38 (1.53%)0.25%
Other1,276 (51.37%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (342)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Kidney Fat in Type 2 Diabetes & Diabetic Kidney Disease and the Effects of Ezetimibe: A Cross-Sectional Study and Randomized, Placebo-Controlled Trial [NCT04589351]Phase 360 participants (Anticipated)Interventional2020-10-01Active, not recruiting
Retrospective Observational Study of the Efficacy and Safety of Statin Monotherapy or Statins in Combination With Ezetimibe in Patients Receiving Lipid-lowering Therapy in Both Primary and Secondary Prevention of CVD [NCT04895098]1,000 participants (Actual)Observational2021-06-23Completed
A Single Center, Open Label, Randomized Study to Compare the Effect of Vytorin (Simvastatin/Ezetimibe) 10/20mg Versus Atorvastatin 20mg on ApoB/ApoA1 Ratio in Subjects With Diabetes [NCT01185236]Phase 4132 participants (Anticipated)Interventional2010-09-30Not yet recruiting
A Randomized, Double-Blind, Placebo-Controlled, Multicenter Study to Evaluate Efficacy, Safety, and Tolerability of Ezetimibe 10 mg or Placebo Added to Existing Atorvastatin 10 mg or 20 mg in Attaining Low-Density Lipoprotein Cholesterol Target Levels in [NCT00092638]Phase 3450 participants (Actual)Interventional2003-05-31Completed
Evaluation of the Efficacy and Safety of Fenofibrate and Ezetimibe Coadministration in Patients With Mixed Hyperlipidemia [NCT00092560]Phase 3587 participants (Actual)Interventional2002-12-31Completed
A Multicenter, Randomized, Double-Blind Study to Evaluate the Lipid-Altering Efficacy and Safety of the Ezetimibe/Simvastatin Combination Tablet Versus Rosuvastatin in Patients With Primary Hypercholesterolemia [NCT00090298]Phase 32,815 participants (Actual)Interventional2004-04-30Completed
Begin With The Right Patients With Dual-Inhibition Action Therapy Through Vytorin for Newly Diagnosed Dyslipidemia Patients [NCT00654628]Phase 4173 participants (Actual)Interventional2007-08-01Completed
A Multicenter, Randomized, Open-label Study to Evaluate the Lipid-Altering Efficacy and Safety of Ezetimibe (+) Simvastatin Versus Atorvastatin in Patients With Primary Hypercholesterolemia [NCT00166504]Phase 4203 participants (Actual)Interventional2005-10-31Completed
Non-Interventional Study On The Treatment With Bempedoic Acid And/Or Its Fixed-dose Combination With Ezetimibe in Routine Clinical Practice in Patients With Primary Hypercholesterolemia Or Mixed Dyslipidemia [NCT05798390]0 participants (Actual)Observational2023-09-01Withdrawn(stopped due to Due to patient availability)
Comparison of Efficacy and Safety of High-Intensity Statin and Ezetimibe Combination Versus StanDard carE in AsymptomatiC PatIentS wIth Presence of COroNary Artery CALCIUM (DECISION-CAL) [NCT05845424]Phase 46,000 participants (Anticipated)Interventional2023-06-01Not yet recruiting
A Randomized, Double-Blind, Placebo-Controlled Study Followed by an Open Label Treatment Period to Evaluate the Efficacy and Safety of Alirocumab in Children and Adolescents With Heterozygous Familial Hypercholesterolemia [NCT03510884]Phase 3153 participants (Actual)Interventional2018-05-31Completed
Designated Drug Use Investigation (12 Weeks) of Zetia 10mg Tablets - A 12-Week Designated Drug Use Investigation of Zetia Monotherapy and Combination Therapy [NCT00704444]11,332 participants (Actual)Observational2007-06-30Completed
A Randomized, Double-blind, Active-controlled, Multicenter Phase3 Trial to Evaluate the Efficacy and Safety of Co-administrated Rosuvastatin/Ezetimibe and Telmisartan in Patients With Primary Hypercholesterolemia and Essential Hypertension [NCT03872232]Phase 3180 participants (Actual)Interventional2019-02-26Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study to Evaluate the Efficacy and Safety of Triplet Therapy With Bempedoic Acid (ETC 1002) 180 mg, Ezetimibe 10 mg, and Atorvastatin 20 mg in Patients With Elevated LDL C [NCT03051100]Phase 263 participants (Actual)Interventional2017-01-19Completed
A Randomized, Double-Blind, Parallel Group Study to Evaluate the Efficacy and Safety of Bempedoic Acid 180 Mg + Ezetimibe 10 Mg Fixed-Dose Combination Compared to Bempedoic Acid, Ezetimibe, and Placebo Alone in Patients Treated With Maximally Tolerated St [NCT03337308]Phase 3382 participants (Actual)Interventional2017-10-23Completed
Analysis of Changes in Intestinal Flora of Hyperlipidemia by Ezetimibe and Orlistat. [NCT03884127]58 participants (Anticipated)Observational2019-04-01Not yet recruiting
Prospective German Very High Cardiovascular Risk Patients Dyslipidemia Treatment Indication Registry [NCT03110432]1,713 participants (Actual)Observational2017-05-18Active, not recruiting
A Phase 1 Feasibility Study of Cholesterol Metabolism Reprogramming (Evolocumab, Atorvastatin and Ezetimibe) in Combination With the Standard of Care in Patients With Advanced or Metastatic Pancreatic Adenocarcinoma [NCT04862260]Early Phase 112 participants (Anticipated)Interventional2021-10-04Recruiting
A Multicentre, Open-Label, Observational Local Study to Evaluate the LDL-C Lowering Effect of Ezetimibe as Prescribed in Daily Routine Practice in the South African Population [NCT00457275]Phase 3440 participants Interventional2005-04-30Completed
A Randomized, Double-Blind, Placebo-Controlled, Multicenter Study to Evaluate Efficacy, Safety, and Tolerability of Ezetimibe 10 mg or Placebo Added to Existing Atorvastatin 10 mg or 20 mg in Attaining Low-Density Lipoprotein Cholesterol Target Levels in [NCT00092625]Phase 3442 participants (Actual)Interventional2003-03-31Completed
A Multicenter, Randomized, Parallel-Groups, Double-Blind Placebo-Controlled Study Comparing the Efficacy, Safety, and Tolerability of Administration of Ezetimibe/Simvastatin Tablet 10/20 mg Versus Doubling the Dose of Simvastatin 20 mg [Simvastatin 40 mg] [NCT00423579]Phase 4120 participants (Actual)Interventional2006-07-01Completed
A Multicenter, Randomized, Double-blind, Active-controlled, Parallel Design, Phase III Clinical Trial to Evaluate the Efficacy and Safety of DP-R207 (Rosuvastatin /Ezetimibe Combination) and Rosuvastatin Monotherapy in Patients With Primary Hypercholester [NCT02445352]Phase 3379 participants (Actual)Interventional2014-07-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel Group, Multicenter Study to Evaluate the Efficacy and Safety of Bempedoic Acid (ETC 1002) 180 mg/Day as Add-on to Ezetimibe Therapy in Patients With Elevated LDL-C [NCT03001076]Phase 3269 participants (Actual)Interventional2016-11-29Completed
A Randomized Study to Evaluate the Efficacy and Safety of Bempedoic Acid 180 + Ezetimibe 10 Fixed-Dose Combination Compared to Ezetimibe and Placebo In Subjects With T2DM and Elevated LDL-Cholesterol [NCT03531905]Phase 2242 participants (Actual)Interventional2018-05-09Completed
Pegylated Interferon Alone or in Combination With Ezetimibe for Patients With Chronic Hepatitis D [NCT03105310]Phase 220 participants (Anticipated)Interventional2016-01-31Active, not recruiting
A Randomized, Open-label, Blinded Intravascular Ultrasound Analysis, Parallel Group, Multicenter Study to Evaluate the Effect of Praluent® (Alirocumab) on Coronary Atheroma Volume in Japanese Patients Hospitalized for Acute Coronary Syndrome With Hypercho [NCT02984982]Phase 4206 participants (Actual)Interventional2016-11-15Completed
A Randomized, Double-Blind, Placebo-Controlled, Multicenter Study to Evaluate Efficacy, Safety, and Tolerability of Ezetimibe 10 mg or Placebo Co-administered With Existing Simvastatin 10 mg or 20 mg in Attaining Low-Density Lipoprotein Cholesterol Target [NCT00092599]Phase 3410 participants (Actual)Interventional2003-02-28Completed
A Randomized, Double-Blind, Active-Controlled, Multicenter, Crossover Study to Evaluate the Efficacy and Safety of Ezetimibe/Atorvastatin 10 mg/20 mg Fixed-Dose Combination Tablet Compared to Co-administration of Marketed Ezetimibe 10 mg and Atorvastatin [NCT01370590]Phase 3406 participants (Actual)Interventional2011-09-30Completed
"A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Factorial Design Study to Evaluate the Lipid-Altering Efficacy and Safety of Ezetimibe/Simvastatin Combination Tablet in Patients With Primary Hypercholesterolemia" [NCT00092651]Phase 31,398 participants (Actual)Interventional2002-09-30Completed
Evaluation of the Efficacy and Safety of Fenofibrate and Ezetimibe Coadministration in Patients With Mixed Hyperlipidemia [NCT00092573]Phase 3576 participants (Actual)Interventional2003-04-30Completed
Ezetimibe Phase IV Clinical Study in Patients With Hypercholesterolemia [NCT00871351]Phase 4125 participants (Actual)Interventional2009-02-01Completed
Evaluate The Lipid-Lowering Efficacy and Safety of Vytorin in Comparison With Atorvastatin in Hypercholesterolaemic Patients With Coronary Artery Disease [NCT00442897]Phase 4229 participants (Actual)Interventional2006-09-30Completed
A Randomized, Open Label Crossover Study to Investigate the Pharmacokinetic Drug Interactions Between Rosuvastatin and Ezetimibe in Healthy Male Subjects [NCT02127320]Phase 124 participants (Actual)Interventional2014-06-30Completed
A Placebo-Controlled, Double-Blind, Randomized, Phase 2 Study to Evaluate the Effect of Obicetrapib 10 mg Daily in Combination With Ezetimibe 10 mg Daily as an Adjunct to High-Intensity Statin Therapy: The ROSE 2 Study [NCT05266586]Phase 2119 participants (Actual)Interventional2022-03-09Completed
Efficacy, Safety, and Tolerability of Ezetimibe in Coadministration With Simvastatin in the Therapy of Adolescents With Heterozygous Familial Hypercholesterolemia [NCT00129402]Phase 3248 participants (Actual)Interventional2005-08-31Completed
A Randomized, Double-Blind, Parallel-Group, Placebo-Controlled Efficacy and Safety Study of Ezetimibe Monotherapy in Children (Ages 6 to 10 Years) With Primary Hypercholesterolemia (Heterozygous Familial and Nonfamilial) (Phase 3, Protocol No. P05522) [NCT00867165]Phase 3138 participants (Actual)Interventional2009-05-21Completed
Early Alirocumab to Reduce LDL-C in Myocardial Infarction [NCT03750760]Phase 40 participants (Actual)Interventional2020-01-31Withdrawn(stopped due to Changes in funding decision)
Same Lipid Lowering by Atorvastatin Versus Atorvastatin Plus Ezetimibe on Coronary Plaque Progression [NCT01086020]Phase 4400 participants (Anticipated)Interventional2010-01-31Recruiting
A Multicenter, Double-Blind, Randomized, Placebo-Controlled Study to Evaluate the Effects of Ezetimibe + Simvastatin on Clinical Outcomes in Patients With Aortic Stenosis [NCT00092677]Phase 31,873 participants (Actual)Interventional2001-01-31Completed
Assessment of Sterol Metabolism in Sitosterolemia: A Pilot Study of Patients Treated With Ezetimibe [NCT01584206]8 participants (Actual)Interventional2012-04-30Completed
Synergistic Effect of Simvastatin and Ezetimibe on Lipid and Pro-inflammatory Profiles in Pre-diabetic Subjects [NCT01103648]50 participants (Actual)Interventional2005-06-30Completed
A Randomized, Double-Blind, Placebo-Controlled, 2-Period, Crossover Study to Evaluate the Effects of Ezetimibe on the Postprandial Lipoprotein Response in Patients With Primary Hypercholesterolemia [NCT00101439]Phase 358 participants (Actual)Interventional2005-11-10Completed
Effect of High-intensity Statin With Ezetimibe COmbination theRapy Versus High-intensity sTatin Monotherapy After Percutaneous Coronary Intervention With Drug-eluting Stents; the ESCORT Trial [NCT05782777]4,310 participants (Anticipated)Interventional2023-03-31Not yet recruiting
Clinical Trial to Assess the Pharmacokinetic Characteristics and Safety/Tolerability of CKD-391 in Healthy Male Subjects [NCT02461004]Phase 152 participants (Actual)Interventional2015-07-31Completed
A Multi-center, Randomized, Double-blind, Phase III Clinical Trial to Evaluate the Efficacy and Safety of Combination Therapy of Rosuvastatin and Ezetimibe and Rosuvastatin Monotherapy in Patients With Primary Hypercholesterolemia [NCT03288038]Phase 3382 participants (Actual)Interventional2014-10-13Completed
A Multicenter, Randomized, Double-blind, Active-controlled, Parallel Group, Factorial Design, Phase III Clinical Trial To Evaluate the Efficacy and Safety of Atorvastatin+Ezetimibe Combination Therapy and Atorvastatin Monotherapy in Patients With Primary [NCT02451098]Phase 3385 participants (Actual)Interventional2015-03-31Completed
A Post-marketing, Long-term, Observational, Descriptive Study to Assess the Risk of Pregnancy and Maternal Complications and Adverse Effects on the Developing Fetus, Neonate, and Infant Among Women Exposed to Bempedoic Acid or Bempedoic Acid/Ezetimibe Fix [NCT05103254]20 participants (Anticipated)Observational2021-09-01Recruiting
Comparison of High-dose Rosuvastatin Versus Low-dose Rosuvastatin Plus Ezetimibe on Carotid Plaque Inflammation in Patients With Acute Coronary Syndrome [NCT04056169]Phase 450 participants (Actual)Interventional2017-06-29Completed
A Randomized, Prospective, Open Label, Active Control, Phase IV Study to Evaluate the Effects of Statin Monotherapy or Statin / Ezetimibe Combination Therapy on Hepatic Steatosis in Patients With Hyperlipidemia and Nonalcoholic Fatty Liver Disease [NCT03434613]Phase 464 participants (Actual)Interventional2018-05-14Completed
A Multi-country, Multicenter, Single-arm, Open-label Study to Document the Safety, Tolerability and Effect of Alirocumab on Atherogenic Lipoproteins in High Cardio-vascular Risk Patients With Severe Hypercholesterolemia Not Adequately Controlled With Conv [NCT02476006]Phase 3998 participants (Actual)Interventional2015-06-23Completed
A Randomized, Double-Blind, Active-Controlled Study of Patients With Cardiovascular Disease and Diabetes Mellitus Not Adequately Controlled With Simvastatin or Atorvastatin: Comparison of Switching to Combination Tablet Ezetimibe/Simvastatin Versus Switch [NCT00862251]Phase 3808 participants (Actual)Interventional2009-04-30Completed
A Multicenter, Randomized, Double-Blind, Parallel Arm, 6-Week Study to Evaluate the Efficacy and Safety of Ezetimibe/Simvastatin Versus Atorvastatin in Patients With Metabolic Syndrome and Hypercholesterolemia at High Risk for Coronary Heart Disease [NCT00409773]Phase 31,143 participants (Actual)Interventional2007-01-31Completed
A Multicenter Prospective Randomized-controlled Interventional Study to Evaluate the Effect of High Dose Rosuvastatin Versus High Dose Rosuvastatin and Ezetimibe in Acute Ischemic Stroke Patients [NCT05884502]Phase 4330 participants (Anticipated)Interventional2022-09-01Recruiting
A Phase III Efficacy And Safety Study of Ezetimibe (SCH58235) 10 mg in Addition to Atorvastatin or Simvastatin in the Therapy of Homozygous Familial Hypercholesterolemia [NCT03884452]Phase 350 participants (Actual)Interventional2000-05-03Completed
Long-Term, Safety and Tolerability Study of SCH 58235 or Placebo in Addition to Atorvastatin in Subjects With Primary Hypercholesterolemia [NCT03882892]Phase 3400 participants (Anticipated)Interventional2001-02-02Completed
Lipid-lowering Regimes Improve Oxidative Stress, Tryptophan Degradation in Hypercholesterolemia Chronic Kidney Disease Patients [NCT03543774]Phase 430 participants (Anticipated)Interventional2018-06-15Recruiting
A Double-blind, Randomized, Multicenter Study to Evaluate the Safety and Efficacy of Evolocumab, Compared With Ezetimibe, in Hypercholesterolemic Japanese Subjects Unable to Tolerate an Effective Dose of a HMG-CoA Reductase Inhibitor Due to Muscle Related [NCT02634580]Phase 361 participants (Actual)Interventional2016-02-27Completed
A Randomized, Open-label, Multiple-dose, Crossover Clinical Trial to Evaluate the Safety/Tolerability and Pharmacokinetic Drug-drug Interaction Between LGEV1801 and LGEV1802 in Healthy Korean Male Volunteers [NCT03532854]Phase 142 participants (Actual)Interventional2018-05-28Completed
A Phase III, Open-label, Clinical Trial to Assess the Long Term Safety and Tolerability of MK-0653H in Japanese Patients With Hypercholesterolemia Who Have Inadequate LDL-C Control on Ezetimibe or Rosuvastatin Monotherapy [NCT02748057]Phase 3135 participants (Actual)Interventional2016-05-18Completed
Estudo clínico Randomizado, Controlado e Duplo-cego do Impacto da inibição de um Transportador de Membrana do Colesterol na absorção da Vitamina D [NCT02234544]Phase 452 participants (Actual)Interventional2014-10-31Completed
A Multicenter, Randomized, Open Label Study to Evaluate the Lipid Lowering Efficacy and Safety of Vytorin® 10/20 vs. Atorvastatin 10mg in Hypercholesterolemia Patients With Metabolic Syndrome in Korea [NCT00496730]Phase 3256 participants (Actual)Interventional2007-07-31Completed
A Double-blind, Randomized, Placebo and Ezetimibe Controlled, Multicenter Study to Evaluate Safety, Tolerability and Efficacy of AMG 145 on LDL-C in Combination With Statin Therapy in Subjects With Primary Hypercholesterolemia and Mixed Dyslipidemia [NCT01763866]Phase 32,067 participants (Actual)Interventional2013-01-15Completed
A Multicenter, Double-Blind, Randomized Study to Establish the Clinical Benefit and Safety of Vytorin (Ezetimibe/Simvastatin Tablet) vs Simvastatin Monotherapy in High-Risk Subjects Presenting With Acute Coronary Syndrome (IMProved Reduction of Outcomes: [NCT00202878]Phase 318,144 participants (Actual)Interventional2005-10-17Completed
SurveY Followed by a Retrospective Chart Review to Describe the Key Factors Leading to Physician's Decision to Treat Patients at High and Very High Cardiovascular Risk With hyperchOlesterolemia or Mixed Dyslipidemia With NUSTENDI® (Fixed Dose Combination [NCT05546398]500 participants (Actual)Observational2022-04-22Completed
The Effect of Simvastatin on Bone Density in Postmenopausal Women With Type 2 Diabetes: a Double-blind, Randomized Active-comparator (Ezetimibe) Controlled Clinical Trial [NCT05613400]Phase 4240 participants (Anticipated)Interventional2022-04-13Enrolling by invitation
A Multicenter, Double-Blind, Randomized, Parallel Group, 6-Week Study to Evaluate the Efficacy and Safety of Ezetimibe/Simvastatin Combination Tablet Versus Atorvastatin in Patients With Hypercholesterolemia [NCT00092690]Phase 31,902 participants (Actual)Interventional2003-06-30Completed
A Randomized, Double-Blind, Placebo-Controlled, Multicenter Study to Evaluate Efficacy, Safety, and Tolerability of Ezetimibe 10 mg or Placebo Co-administered With Existing Simvastatin 10 mg or 20 mg in Attaining Low-Density Lipoprotein Cholesterol Target [NCT00092612]Phase 3372 participants (Actual)Interventional2003-05-31Completed
Drugs in Breast Milk [NCT05543122]304 participants (Anticipated)Observational2022-03-09Recruiting
Effects of High-dose StAtin Versus Low-dose Statin Plus Ezetimibe on Statin-Associated Muscle Symptoms & on Reaching Target LDL-C Levels Among Elderly Patients With Atherosclerotic Cardiovascular Disease [NCT04826354]Phase 4582 participants (Actual)Interventional2021-08-11Completed
CKD-391 in Healthy Volunteers to Investigate the Pharmacokinetic Drug Interaction Between Atorvastatin an Ezetimibe After Oral Administration [NCT02288338]Phase 136 participants (Actual)Interventional2014-11-30Completed
A Phase I Clinical Trial to Investigate the Pharmacokinetic Interactions and Safety Between Rosuvastatin and Ezetimibe in Healthy Male Volunteers [NCT02289430]Phase 159 participants (Actual)Interventional2014-12-31Completed
A Double-blind, Randomized, Placebo and Ezetimibe-controlled, Multicenter Study to Evaluate Safety and Efficacy of Lipid Lowering Monotherapy With AMG 145 in Subjects With a 10-Year Framingham Risk Score of 10% or Less [NCT01763827]Phase 3615 participants (Actual)Interventional2013-01-21Completed
A Randomized, Placebo- and Ezetimibe-controlled, Dose-ranging Study to Evaluate Tolerability and Efficacy of AMG 145 on LDL-C in Hypercholesterolemic Subjects With a 10-year Framingham Risk Score of 10% or Less [NCT01375777]Phase 2411 participants (Actual)Interventional2011-07-06Completed
A Randomized Double-blinded, Double Dummy, Active-controlled, Parallel Design, Phase 3 Clinical Trial to Evaluate the Efficacy and the Safety of Single Pill Combination (SPC) Ezetimibe/Rosuvastatin in Chinese Adult Patients With Primary Hypercholesterolem [NCT04669041]Phase 3305 participants (Actual)Interventional2020-12-08Completed
Study on the Bioavailability and Bioequivalence of Ezetimibe Tablets in Healthy Subjects [NCT05681247]Phase 159 participants (Actual)Interventional2017-12-17Completed
The Effect of Ezetimibe 10 mg, Simvastatin 20 mg and the Combination of Simvastatin 20 mg Plus 10 mg Ezetimibe on Low Density Lipoprotein (LDL)-Subfractions in Patients With Type 2 Diabetes [NCT01384058]Phase 441 participants (Actual)Interventional2007-11-30Completed
An 8-Week Open-Label, Sequential, Repeated Dose-Finding Study to Evaluate the Efficacy and Safety of Alirocumab in Children and Adolescents With Heterozygous Familial Hypercholesterolemia Followed by an Extension Phase [NCT02890992]Phase 242 participants (Actual)Interventional2016-09-15Completed
A MC, DB, Rand, Study to Evaluate Efficacy, Safety and Tolerability of Eze/Simva 10/40 mg, Atorva 40 mg, Rosuva 10 mg in Achieving LDL-C <2 mmol/l in Pts With CVD...on Simva 40 mg With LDL-C ³2 mmol/l [NCT00462748]Phase 3786 participants (Actual)Interventional2007-03-31Completed
A Multicenter, Randomized, Double-Blind, Parallel Arm, 12-Week Study to Evaluate the Efficacy and Safety of Ezetimibe 10 mg When Added to Atorvastatin 10 mg Versus Titration to Atorvastatin 20 mg and to 40 mg in Elderly Patients With Hypercholesterolemia [NCT00418834]Phase 31,053 participants (Actual)Interventional2007-01-31Completed
Clinical Trial to Assess the Pharmacokinetic Characteristics and Safety/Tolerability of CKD-391 in Healthy Male Subjects [NCT02501200]Phase 146 participants (Actual)Interventional2015-08-31Completed
An Open-Label Study to Evaluate the Efficacy and Safety of Alirocumab in Children and Adolescents With Homozygous Familial Hypercholesterolemia [NCT03510715]Phase 318 participants (Actual)Interventional2018-08-31Completed
"A Multicenter, Randomized, Double-Blind, Placebo-Controlled Factorial Design Study to Evaluate the Lipid-Altering Efficacy and Safety of Ezetimibe/Simvastatin Combination Tablet in Patients With Primary Hypercholesterolemia" [NCT00092664]Phase 31,104 participants (Actual)Interventional2003-01-31Completed
A Multi-center, Double-Blind, Randomized, Placebo-Controlled, Parallel Group, 6-Week Study to Evaluate the Efficacy and Safety of Ezetimibe 10 mg/Day When Added to Ongoing Therapy With a Statin Versus Statin Therapy Alone, in Patients With Hypercholestero [NCT00092586]Phase 32,904 participants (Actual)Interventional2002-09-30Completed
A Multicenter Study to Assess the Cholesterol Lowering Level of Switching to an Investigational Drug Compared to Doubling the Dose of an Investigational Drug in Patients With Hypercholesterolemia and Atherosclerotic or Coronary Vascular Disease [NCT00090168]Phase 3435 participants (Actual)Interventional2004-01-27Completed
Intravascular Ultrasound Evaluation of the Intervention Effect of Simvastatin Combined With Ezetimibe on Coronary Borderline Lesion in Patients With Stable Angina Pectoris and Diabetes Mellitus Compared With Simvastatin Alone [NCT03771053]240 participants (Anticipated)Interventional2018-01-01Recruiting
Pharmacokinetic Drug Interaction Between Ezetimibe and Tacrolimus After Single Dose Administration in Healthy Subjects [NCT00621699]Phase 124 participants (Actual)Interventional2007-09-30Completed
Efficacy of Ezetimibe/Simvastatin 10/20 mg and MK0524A (1-2 g/Day) in Patients With Mixed Hyperlipidemia and Two or More Risk Factors to Cardiovascular Disease. [NCT00738985]Phase 40 participants (Actual)Interventional2009-11-30Withdrawn(stopped due to The study was cancelled due to budget limitations)
Observational Study of Approaches to Lipid-lowering Therapy in Russian Patients With Coronary Heart Disease (<>) [NCT00730132]712 participants (Actual)Observational2008-01-31Completed
A Randomized, Open-Labeled, Parallel Group Comparison Study to Evaluate the Efficacy, Safety of Ezetimibe Alone Versus Statin in the Treatment of Hypercholesterolemia [NCT00753883]Phase 440 participants (Actual)Interventional2006-07-31Completed
Efficacy and Safety of Combination Therapy of Moderate-intensity Statin and Ezetimibe Compared to High-intensity Statin: Study Protocol for a Randomized Controlled Trial [NCT04080310]Phase 4270 participants (Actual)Interventional2018-03-15Completed
Comparison of Low-Intensity Statin Plus Ezetimibe Versus High-Intensity Statin Therapy on Risk of New-Onset Diabetes Mellitus in Prediabetic Patients With Atherosclerotic Cardiovascular Disease [NCT05579626]4,000 participants (Anticipated)Interventional2023-03-14Recruiting
A Multicenter, Randomized, Open-labeled, Parallel Group Comparison Study to Evaluate the Efficacy, Safety and Tolerability of Ezetimibe Added to Ongoing Statin Therapy Versus Doubling the Dose of Ongoing Statin in the Treatment of Hypercholesterolemia. [NCT00652327]Phase 483 participants (Actual)Interventional2005-12-31Completed
Fluvastatin 80 mg Ret. vs Combination With Ezetimibe 10 mg in Patients With High Cardiovascular Risk [NCT00814723]Phase 490 participants (Actual)Interventional2005-09-30Completed
Coadministration of Ezetimibe With Fenofibrate Versus Pravastatin Monotherapy for the Treatment of Hyperlipidaemia in HIV-infected Patients Receiving Protease Inhibitors: a Randomized, Prospective, Controlled Pilot Study. [NCT00843661]Phase 460 participants (Anticipated)Interventional2009-03-31Recruiting
A Multicenter, Randomized, Parallel Groups, Placebo-Controlled Study Comparing the Efficacy, Safety, and Tolerability of the Daily Co-Administration of Ezetimibe 10 mg or Ezetimibe Placebo to Ongoing Treatment With Atorvastatin 10 mg in Subjects With Prim [NCT00202904]Phase 481 participants (Actual)Interventional2005-05-31Completed
Te Influence of Ezetimibe on Gallbladder Function [NCT00634140]0 participants (Actual)Interventional2009-08-31Withdrawn(stopped due to Study was never initiated due to lack of funding support.)
A Randomized, Double-blind, Multi-center Clinical Trial to Evaluate Efficacy and Safety of Ezetimibe/Rosuvastatin Combination Tablets and Candesartan Cilexetil/Amlodipine Besylate Combination Tablets [NCT03847506]Phase 4127 participants (Actual)Interventional2018-07-05Completed
A Randomized, Double-Blind, Active-Controlled, Multicenter Study to Assess the LDL-C Lowering of Switching to a Combo Tab Ezetimibe/Simvastatin (10 mg/20 mg) Compared to Rosuvastatin 10 mg in Patients With Primary High Cholesterol and High Cardiovascular [NCT00479713]Phase 3618 participants (Actual)Interventional2007-02-01Completed
Rosuvastatin for Reduction of Myocardial Damage and Systemic Inflammation During Coronary Angioplasty - The REMEDY Study [NCT02205775]Phase 3280 participants (Actual)Interventional2010-05-31Terminated(stopped due to difficult recruitment)
A Randomized, Double-Blind, Placebo-Controlled, 2-Period, Crossover Study to Evaluate the Effects of Ezetimibe on the Plasma Appearance of 7-Ketocholesterol After an Oral Bolus in Patients With Primary Hypercholesterolemia [NCT00794677]Phase 426 participants (Actual)Interventional2006-06-30Completed
Post-marketing Surveillance of the Safety, Tolerability and Efficacy of Ezetimibe Among Filipino Patients [NCT00704535]4,105 participants (Actual)Observational2006-03-31Completed
A Phase 3, Double-Blind Efficacy and Safety Study of Ezetimibe (SCH 58235) 10 mg in Addition to Atorvastatin Compared to Placebo in Subjects With Primary Hypercholesterolemia (Protocol P00692) [NCT03867110]Phase 3628 participants (Actual)Interventional2000-03-06Completed
A Multicenter, Randomized, Parallel Groups, Placebo-Controlled Study Comparing The Efficacy, Safety, And Tolerability Of The Daily Co-administration Of Ezetimibe 10 mg Or Ezetimibe Placebo To Ongoing Treatment With Atorvastatin 10 mg In Subjects With Prim [NCT00651404]Phase 3137 participants (Actual)Interventional2004-01-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Multicenter Study to Evaluate the Efficacy, Safety, and Tolerability of Ezetimibe 10 mg or Placebo Co-administered With Existing Simvastatin 10mg or 20mg in Attaining Low-Density Lipoprotein Cholesterol Targ [NCT00651014]Phase 482 participants (Actual)Interventional2004-01-31Terminated(stopped due to slow subject recruitment and lack of medical and scientific merit due to change in new standard of therapy during that same period.)
A Randomized Open Label Trial to Assess the Effect of Plant Sterols Associated With Ezetimibe in LDL-cholesterol Levels in Coronary Patients Previously on Statin Therapy [NCT02089867]Phase 2/Phase 347 participants (Actual)Interventional2006-10-31Completed
Ezetimibe Reverse Cholesterol Transport (RCT) Pilot Study [NCT00701727]Phase 431 participants (Actual)Interventional2008-06-30Completed
The Impact of Ezetimibe on Biochemical Markers of Cardiovascular Risk in Kidney Transplant Patients [NCT02103049]Phase 480 participants (Actual)Interventional2014-04-30Completed
Ezetimibe for Patients With Chronic Hepatitis D [NCT03099278]Phase 220 participants (Anticipated)Interventional2017-01-31Recruiting
A Pilot Study of the Effect of Ezetimibe in Patients With Chronic Hepatitis C Infection [NCT02126137]Phase 120 participants (Anticipated)Interventional2013-10-31Recruiting
A Randomized, Double-Blind, Active-Controlled, Multicenter, Crossover Study to Evaluate the Efficacy of Ezetimibe/Atorvastatin 10 mg/40 mg Fixed-Dose Combination Tablet Compared to Co-Administration of Marketed Ezetimibe 10 mg and Atorvastatin 40 mg in Pa [NCT01370603]Phase 3328 participants (Actual)Interventional2011-09-30Completed
Antilipidemic Ezetimibe Induces Regression of Endometriotic Explants in a Rat Model of Endometriosis [NCT04844996]Early Phase 118 participants (Actual)Interventional2019-09-01Completed
[NCT02251847]Phase 3400 participants (Anticipated)Interventional2014-07-31Recruiting
Ezetimibe/Simvastatin and Rosuvastatin for Oxidative Stress and Mitochondrial Function in Diabetic Polyneuropathy: a Randomized, Double Blinded, Placebo Controlled Clinical Trial [NCT02129231]Phase 274 participants (Actual)Interventional2012-02-29Completed
Effects of Ezetimibe, Simvastatin, and Vytorin on Reducing L5 in Patients With Metabolic Syndrome [NCT00988364]Phase 430 participants (Actual)Interventional2007-03-31Completed
A Placebo-Controlled, Double-Blind, Randomized, Phase 3 Study to Evaluate the Effect of Obicetrapib 10 mg and Ezetimibe 10 mg Fixed Dose Combination Daily on Top of Maximally Tolerated Lipid-Modifying Therapy in Participants With Heterozygous Familial Hyp [NCT06005597]Phase 3400 participants (Anticipated)Interventional2024-01-31Not yet recruiting
Effect of Ezetimibe on Oxidized LDL Cholesterol [NCT01008345]Phase 4100 participants (Actual)Interventional2008-09-30Completed
Plaque REgression With Cholesterol Absorption Inhibitor or Synthesis Inhibitor Evaluated by IntraVascular UltraSound [NCT01043380]Phase 4245 participants (Actual)Interventional2010-01-31Completed
Open-label, Long-term Study of Coadministration of Ezetimibe and Atorvastatin in Patients With Primary Hypercholesterolemia Who Have Not Reached LDL-cholesterol Target With HMG-CoA Reductase Inhibitors [NCT00654095]Phase 3146 participants (Actual)Interventional2007-12-01Completed
Effect of Ezetimibe on Flow-mediated Brachial Artery Reactivity in Healthy Subjects [NCT00376246]Phase 428 participants (Actual)Interventional2006-09-30Completed
A Prospective, Non-Intervention, Multi-Center Observational Study to Evaluate the Efficacy and Safety of CREZET Tablet in Patients With Dyslipidemia [NCT05889143]15,000 participants (Anticipated)Observational2023-05-24Recruiting
Evaluating the Anti-Proliferative Effects of Atorvastatin on the Endometrium of Endometrial Cancer Patients: A Pre-Operative Window Study [NCT02767362]Early Phase 124 participants (Actual)Interventional2015-11-30Completed
Additive Effect of Ezetimibe Upon Simvastatin Treatment on Systemic Inflammatory Activity and Endothelial Function During Myocardial Infarction [NCT00905905]Phase 440 participants (Anticipated)Interventional2009-05-31Completed
Orient Pharma Co., Ltd. [NCT04643093]Phase 3390 participants (Actual)Interventional2020-08-01Completed
[NCT02749994]Phase 3396 participants (Actual)Interventional2016-04-30Completed
A Multicenter., Rand., Double-Blind, Titration Study to Evaluate & Compare the Efficacy & Safety of Ezetimibe Plus Atorvastatin Vs Atorvastatin in Hypercholesterolemic Pts. at Moderately High Risk for CHD Not Adequately Controlled on Atorvastatin 20 Mg [NCT00276458]Phase 3196 participants (Actual)Interventional2006-02-28Completed
Post - Marketing Surveillance of the Safety, Tolerability and Efficacy of Vytorin (Ezetimibe + Simvastatin) Tablet Among Filipino Patients [NCT00909389]4,748 participants (Actual)Observational2006-11-30Completed
A 6wk Open-Label, Randomised, Multicentre, Phase IIIb, Parallel Group Study to Compare the Safety & Efficacy of Rosuvastatin 40mg in Comb.With Ezetimibe 10mg in Subjects With Hypercholesterolaemia & CHD or Atherosclerosis or a CHD Risk Equiv. (10 yr Risk [NCT00653445]Phase 30 participants Interventional2004-06-30Completed
Cholesterol Lowering Via Bempedoic Acid/Ezetimibe, an ACL-Inhibiting Regimen in Acute Coronary Syndrome (CLEAR ACS) Study [NCT05263778]Phase 4500 participants (Anticipated)Interventional2022-03-31Not yet recruiting
A Multicenter, Double-blind, Randomized, Active-controlled Parallel Groups Study Comparing The Efficacy and Safety of The Daily Co-Administration of Ezetimibe 10 mg With Simvastatin 20 mg Vs Simvastatin Or Ezetimibe Alone in Subjects With Primary Hypercho [NCT00650819]Phase 3240 participants (Actual)Interventional2004-06-01Completed
A Multicenter, Randomized, Double-blind, Parallel Group, 6-Week Study to Evaluate the Efficacy and Safety of Ezetimibe/Simvastatin Combination Tablet Versus Atorvastatin in Patients With Type 2 Diabetes Mellitus (T2DM) and Hypercholesterolemia [NCT00110435]Phase 31,229 participants (Actual)Interventional2005-05-31Completed
A Study to Evaluate the Efficacy and Safety of Ezetimibe/Simvastatin and Fenofibrate Coadministration in Patients With Mixed Hyperlipidemia [NCT00093899]Phase 3611 participants (Actual)Interventional2004-11-30Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of MK0653 When Added to Current Regimen in Patients With Homozygous Sitosterolemia - 1 Year Open-Label Extension [NCT00092807]Phase 337 participants (Actual)Interventional2001-02-12Completed
[NCT00681525]Phase 118 participants (Actual)Interventional2008-04-30Completed
Goal Achievement of A1c and LDL in a Randomized Trial Comparing Colesevelam vs. Ezetimibe as Add-on to Baseline Statin Therapy: The GOAL-RCT Trial [NCT02682680]Phase 4200 participants (Actual)Interventional2016-01-11Completed
[NCT00972829]Phase 430 participants (Anticipated)Interventional2009-09-30Recruiting
A 12-week Open-label, Randomised, Parallel-group, Multicentre, Phase IIIb Study to Compare the Efficacy and Safety of Rosuvastatin (CRESTOR™) in Combination With Ezetimibe and Simvastatin in Patients With Hypercholesterolaemia and CHD [NCT00525824]Phase 31,743 participants (Actual)Interventional2007-08-31Completed
A Double-blind, Randomized, Placebo- and Active-Comparator Controlled Study to Evaluate the Efficacy of Inclisiran as Monotherapy in Patients With Primary Hypercholesterolemia Not Receiving Lipid-Lowering Therapy (VictORION-Mono) [NCT05763875]Phase 3300 participants (Anticipated)Interventional2023-03-15Recruiting
[NCT00810303]Phase 112 participants (Actual)Interventional2009-03-31Completed
Efficacy and Safety of Simvastatin-ezetimibe Combination Therapy in Reduction of Progression of Atherosclerosis Among Patients With Systemic Lupus Erythematosus: A Randomized Single-Blind Trial [NCT02548936]Early Phase 130 participants (Actual)Interventional2015-04-30Enrolling by invitation
Pharmacokinetic Drug Interaction Between Ezetimibe and Sirolimus After Single Dose Administration in Healthy Subjects [NCT00621101]Phase 124 participants (Actual)Interventional2007-04-30Completed
Effects of Ezetimibe in Association With Statins on Postprandial Lipemia in Type 2 Diabetic Patients [NCT00699023]Phase 413 participants (Anticipated)Interventional2008-06-30Completed
Randomized Trial of Ezetimibe Versus nutraCeuticals in Statin-intoLerant patIents Treated With PercutaneouS Coronary Intervention [NCT01490229]Phase 4100 participants (Anticipated)Interventional2013-01-31Recruiting
INdians Followed for INtensive Lipid Lowering Treatment and Its safetY: To Assess The Safety And Effectiveness Of Ezetimibe Co-Administered With Any Statin Compared To Doubling Of Current Statin Daily Dose In South Asian Canadians [NCT00664469]Phase 364 participants (Actual)Interventional2007-08-31Terminated(stopped due to Poor enrollment)
Transplantation Using Hepatitis C Positive Donors to Hepatitis C Negative Recipients: A Safety Trial [NCT04017338]Phase 340 participants (Anticipated)Interventional2018-08-06Recruiting
Effects of Simvastatin Versus Simvastatin Combined With Ezetimibe on Blood Coagulation in Patients With Acute Coronary Events: Relationship With Cholesterol-Lowering and Anti-Inflammatory Properties [NCT00725829]100 participants (Anticipated)Interventional2008-06-30Recruiting
Regulation of Cholesterol Absorption: LDL Cholesterol Response to a Combination of Phytosterols and Ezetimibe (Phyto-3) [NCT00863265]Early Phase 122 participants (Actual)Interventional2009-06-30Completed
Evaluation of the Pharmacokinetics and Safety of Raltegravir and Ezetimibe When Co-administered to Male and Female Healthy Volunteers [NCT00772551]Phase 126 participants (Actual)Interventional2008-06-30Completed
SCH 58235: A Multicentre, Randomised, Parallel Group, Placebo-Controlled Study Comparing the Efficacy, Safety, And Tolerability of the Daily Co-Administration of Ezetimibe 10 mg With Atorvastatin 10 mg vs. Ezetimibe Placebo With Atorvastatin 10 mg in Untr [NCT00653796]Phase 4148 participants (Actual)Interventional2003-09-01Completed
Evaluation of Long-term Lipid-lowering Therapy on Myocardial Electrical Heterogeneity, Myocardial Deformation, Arterial Stiffness and Quality of Life in Patients With Primary STEMI/NSTEMI With Coronavirus Infection COVID-19 [NCT04900155]45 participants (Actual)Interventional2020-11-20Active, not recruiting
Assessment of the Effects of Long-term Lipid-lowering Therapy on Parameters of Electrical Myocardial Heterogeneity, Myocardial Deformation Characteristics, Vascular Rigidity, and Quality of Life in Patients With Primary STEMI or NSTEMI [NCT04347434]Phase 4300 participants (Anticipated)Interventional2020-02-12Recruiting
The Effect of Usual Dose Rosuvastatin Plue Ezetimibe Versus High-dose Rosuvastatin on Coronary Atherosclerotic Plaque: A Randomized Controlled Trial [NCT03169985]Phase 4280 participants (Anticipated)Interventional2017-07-12Recruiting
A Retrospective Survey to Evaluate the Effectiveness and Safety of Dual Inhibition Lipid-lowering Regimen in the Treatment of Dyslipidemic Patients in Normal Practice [NCT00726856]1,200 participants (Anticipated)Observational2007-05-31Completed
A Multicenter, Randomized, Parallel Groups, Placebo-Controlled Study Comparing The Efficacy, Safety, And Tolerability Of The Daily Co-administration Of Ezetimibe 10 Mg Or Ezetimibe Placebo To Ongoing Treatment With Simvastatin 20 Mg In Subjects With Prima [NCT00651274]Phase 4144 participants (Actual)Interventional2003-04-01Completed
A Randomized, Double-Blind, Active Controlled, Parallel-Group Study to Evaluate the Safety and Efficacy of the Combination BMS-201038 (AEGR-733) and Ezetimibe vs. Monotherapy in Subjects With Moderate Hypercholesterolemia [NCT00405067]Phase 260 participants (Actual)Interventional2006-05-31Completed
A Multi-center, Randomized, Double-Blind, Phase III Clinical Trial to Evaluate the Efficacy and Safety of DWJ1451 in Patients With Hypertension and Dyslipidemia [NCT04161001]Phase 3237 participants (Anticipated)Interventional2019-11-20Recruiting
The Impact of the Time of Drug Administration on the Effectiveness of Combined Treatment of Hypercholesterolemia With ROSuvastatin and EZEtimibe (ROSEZE) - A Single-center, Crossover, Open-label Study [NCT02772640]Phase 483 participants (Actual)Interventional2016-03-31Completed
Retrospective Study to Evaluate the Safety of the Fixed-dose Combination Rosuvastatin / Ezetimibe as a Treatment for Patients With Dyslipidaemia in Usual Medical Practice. [NCT04862962]120 participants (Actual)Observational2021-09-30Completed
Vytorin on Carotid Intima-media Thickness and Overall Rigidity [NCT00738296]Phase 490 participants (Actual)Interventional2005-04-30Completed
A Randomized, Double-Blind, Parallel Group, Multicenter Study to Evaluate the Efficacy and Safety of ETC-1002, Ezetimibe, and the Combination in Hypercholesterolemic Patients With or Without Statin Intolerance [NCT01941836]Phase 2349 participants (Actual)Interventional2013-09-30Completed
The Effect Of Ezetimibe In Addition To Optimal Cholesterol-Lowering Statin Therapy On The Plaque Composition In Patients With Acute Myocardial Infarction - Assessed By Optical Coherence Tomography And Intravascular Ultrasound. [NCT01385631]Phase 487 participants (Actual)Interventional2011-06-30Completed
A Phase II, Fixed-sequenced, Open- Label, Research Study to Assess Pharmacokinetic Drug Interactions of AEGR-733 on Lipid-lowering Therapies in Healthy Volunteers [NCT00359281]Phase 2125 participants (Actual)Interventional2006-03-31Completed
A Randomized, Double-blinded, Multi-center, Phase III Study to Compare The Efficacy and Safety of Co-administered HGP0608, HGP0904 and HCP1306 Versus HCP1701 in Patients With Hypertension and Dyslipidemia [NCT04074551]Phase 3145 participants (Actual)Interventional2019-07-16Completed
Evaluation of Potential for Pharmacokinetic Drug Interaction Between SCH 58235 and Pitavastatin [NCT00653913]Phase 118 participants (Actual)Interventional2004-03-31Completed
SCH 465981: Assessment of Bi-Directional Interaction Between Components of Vytorin® (Ezetimibe and Simvastatin) and Niaspan® (Niacin Extended-Release Tablets) in Healthy Subjects [NCT00652431]Phase 118 participants (Actual)Interventional2007-05-31Completed
A Double-Blind, Randomized, Multicenter, Active-Comparative, 12-Week Study to Assess the Efficacy and Safety of the Drug in Conjunction With Another Drug in Korean Patients With Primary Hypercholesterolemia [NCT00157911]Phase 3136 participants (Actual)Interventional2002-12-31Completed
An Open-Label, Multicenter Study to Assess the Efficacy of Switching to a Combination Tablet Ezetimibe/Simvastatin 10mg/40mg, Compared to Doubling the Dose of Statin in Patients Hospitalized With a Coronary Event [NCT00132717]Phase 3450 participants (Actual)Interventional2005-01-01Completed
Effects on Atherosclerosis Regression of Ezetimibe Monotherapy or Ezetimibe Plus Simvastatin Combination Therapy: Evaluation by Fluorodeoxyglucose Positron Emission Tomography [NCT00926055]0 participants (Actual)Interventional2011-09-30Withdrawn
Prospective Evaluation of LDL Levels in Patients Converted From Zetia (Ezetimibe)10 mg to 5 mg [NCT00762229]39 participants (Actual)Interventional2007-07-31Completed
"An Open-Label, Randomized, Parallel-Group, Multicenter Study to Compare the Efficacy and Safety of Switching to Rosuvastatin 10 mg Daily Versus Atorvastatin 10 mg Daily With Ezetimibe 10 mg Daily Versus Doubling the Dose of Atorvastatin to 20 mg Daily in [NCT00651378]Phase 487 participants (Actual)Interventional2004-09-01Terminated(stopped due to Slow enrollment [HIGH SCREEN FAILURE RATE])
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate Efficacy and Safety of Adding Ezetimibe 30 mg to An Ongoing Regimen of Ezetimibe 10 mg in Patients Homozygous Sitosterolemia [NCT00092898]Phase 330 participants (Actual)Interventional2004-10-31Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of MK0653 When Added to Current Regimen in Patients With Homozygous Sitosterolemia [NCT00092820]Phase 358 participants (Actual)Interventional2001-02-12Completed
A Pilot Study of the Safety, Efficacy, and Tolerability of Ezetimibe (Zetia) in Combination With Statin Therapy for the Treatment of Elevated LDL Cholesterol in HIV-Infected Subjects [NCT00099684]44 participants (Actual)Interventional2005-11-30Completed
An Open-label Exploratory Study of the Pharmacokinetic Interaction of CXA-10 Administered to Steady State With Pravastatin and Vytorin® (Simvastatin and Ezetimibe) in Healthy Males [NCT02547402]Phase 110 participants (Actual)Interventional2015-12-31Completed
Can Cholesterol Lowering Drugs Influence Circulating Omega-3 Fatty Acid Levels [NCT00955227]60 participants (Actual)Interventional2009-07-31Completed
[NCT00548145]38 participants (Actual)Interventional2007-11-30Terminated
[NCT02942602]58 participants (Actual)Interventional2014-04-03Completed
Efficacy and Safety Study of Fluvastatin and Ezetimibe Combined Versus Fluvastatin Alone [NCT00171288]Phase 383 participants (Actual)Interventional2003-08-31Completed
A Randomized Trial of the Long-term Clinical Effects of Raising HDL Cholesterol With Extended Release Niacin/Laropiprant [NCT00461630]Phase 325,673 participants (Actual)Interventional2007-01-31Completed
A Single Center, Randomized, Parallel Groups, Placebo-Controlled Study Comparing The Efficacy, Safety, And Tolerability Of The Daily Co-administration Of Ezetimibe 10 Mg Or Ezetimibe Placebo To Ongoing Treatment With Atorvastatin 10 Mg In Subjects With Pr [NCT00319449]Phase 422 participants (Actual)Interventional2005-09-30Completed
A Multicenter, Rand., Double-Blind, Titration Study to Evaluate & Compare the Efficacy & Safety of Ezetimibe Plus Atorvastatin Vs Atorvastatin in Hypercholesterolemic Pts. at High Risk for CHD Not Adequately Controlled on Atorvastatin 40 Mg [NCT00276484]Phase 3579 participants (Actual)Interventional2006-02-28Completed
A Multicenter, Double-blind, Randomized, Placebo-controlled Parallel Groups Study Comparing the Efficacy and Safety of Vytorin Versus Placebo in Subjects With Primary Hypercholesterolemia [NCT00413972]Phase 3392 participants (Actual)Interventional2006-04-30Completed
Assessment of the Effects of Ezetimibe on Coronary Plaque Volume in Patients With Acute Coronary Syndrome [NCT01068093]Phase 4120 participants (Anticipated)Interventional2010-10-31Recruiting
A Multicenter, Randomized, Parallel-Groups, Double-Blind Placebo Controlled Study Comparing the Efficacy, Safety, and Tolerability of Co-administration of Ezetimibe 10 mg With Ongoing Treatment With Simvastatin 20 mg Versus Doubling the Dose of Simvastati [NCT00423488]Phase 393 participants (Actual)Interventional2005-07-12Completed
Platelet Function in Diabetic Patients With and Without Renal Impairment, and the Effects of Lipid Lowering Treatment [NCT01035320]Phase 439 participants (Actual)Interventional2006-01-31Completed
A Prospective, Open Label Comparison of Ezetimibe, Niacin, and Colestipol as Adjunct Therapy in Lipid Reduction [NCT00203476]Phase 430 participants (Actual)Interventional2005-05-31Completed
Moderate-intensity Rosuvastatin Plus Ezetimibe Versus High-intensity Rosuvastatin for Target LDL-C Goal Achievement in Patients With Recent Ischemic Stroke: a Randomized Clinical Trial [NCT03993236]Phase 4584 participants (Anticipated)Interventional2019-09-09Recruiting
A Randomized, Double-blind, Multi-center, Phase III Trial to Evaluate the Efficacy and Safety of BR1017A and BR1017B Combination Therapy in Essential Hypertension Patients With Primary Hypercholesterolemia [NCT05930028]Phase 3156 participants (Anticipated)Interventional2023-07-13Recruiting
A Phase III, Randomized, Active Comparator-controlled, Clinical Trial to Study the Efficacy and Safety of MK-0653H in Japanese Patients With Hypercholesterolemia. [NCT02741245]Phase 3321 participants (Actual)Interventional2016-06-09Completed
A Randomised Controlled Trial of Lifestyle Versus Ezetimibe Plus Lifestyle in Patients With Non-alcoholic Steatohepatitis [NCT01950884]Phase 445 participants (Anticipated)Interventional2013-10-31Enrolling by invitation
Effects of Ezetimibe Combination Therapy for Patients With Atherosclerotic Cardiovascular Disease; Randomized Comparison of LDL-cholesterol Targeting <70 Versus <55mg/dL; Ez-PAVE Trial [NCT04626973]3,048 participants (Anticipated)Interventional2021-01-15Recruiting
To Evaluate the Efficacy and Safety of Combination Therapy of Pitavastatin and Ezetimibe Versus Monotherapy of Pitavastatin in Patients With Primary Hypercholesterolemia [NCT04584736]Phase 3283 participants (Actual)Interventional2019-06-11Completed
A Randomized, Double Blind, Parallel, Multi-center, Phase 3 Clinical Trial to Evaluate the Efficacy and Safety of DW1125 and DW1125A in Patient With Primary Hypercholesterolemia or Mixed Dyslipidemia [NCT05970679]Phase 3252 participants (Actual)Interventional2022-08-17Completed
A Clinical Trial to Compare the Pharmacokinetics and Safety of NVP-1205 and Coadministration of Rosuvastatin and Ezetimibe in Healthy Male Volunteers [NCT02029625]Phase 141 participants (Actual)Interventional2014-02-28Completed
Clinical Comparison of Low-dose Rosuvastatin Plus Ezetimibe Combination Therapy and High-dose Rosuvastatin Monotherapy in Patients With Minimal to Intermediate Coronary Artery Disease Without Percutaneous Coronary Intervention : A Prospective, Multicenter [NCT06186037]Phase 46,356 participants (Anticipated)Interventional2024-01-01Not yet recruiting
A Randomized, Double-Blinded Study of Simvastatin 20 mg/Day Versus Vytorin 10/20 in Subjects With Lipid Profiles Not Meeting Current NCEP Guidelines, Following a Low-Carbohydrate Diet [NCT00566267]Phase 2/Phase 358 participants (Actual)Interventional2006-04-30Completed
Reverse Cholesterol Transport in Humans [NCT01603758]Phase 1132 participants (Actual)Interventional2014-01-31Completed
Impact of Combined Ezetimibe and Atorvastatin Therapy on Coronary Thin-cap Fibroatheroma As Assessed by Optical Coherence Tomography [NCT02588235]Phase 4100 participants (Anticipated)Interventional2015-10-31Recruiting
Open-label, Long-term Study of Coadministration of Ezetimibe and Simvastatin in Patients With Primary Hypercholesterolemia Who Have Not Reached LDL-cholesterol Target With HMG-CoA Reductase Inhibitors [NCT00653523]Phase 3151 participants (Actual)Interventional2007-12-01Completed
A Randomized, Single-dose, Open, Crossover Clinical Trial to Compare the Pharmacokinetics of DP-R207 in Comparison to Each Component Administered Alone in Healthy Male Volunteers [NCT02730689]Phase 166 participants (Actual)Interventional2014-12-31Completed
A Double-Blind, Double-Dummy, Randomized, Parallel Group, Multicenter, Phase 3 Study to Evaluate the Efficacy and Safety of Lapaquistat Acetate 100 mg and Lapaquistat Acetate 100 mg Administered in Combination With Ezetimibe 10 mg vs Ezetimibe 10 mg in Su [NCT00268697]Phase 31,267 participants (Actual)Interventional2005-10-31Completed
Effect of Diabetes Mellitus on Cholesterol Absorption, Synthesis and Statin Efficacy [NCT00879710]57 participants (Actual)Interventional2008-08-31Completed
In Silico Non Interventional Secondary Use of Data Study Assessing the Impact of Inclisiran on Major Adverse Cardiovascular Events in Patients With Established Cardiovascular Disease [NCT05974345]204,691 participants (Actual)Observational2023-11-03Active, not recruiting
Pilot Study of Ezetimibe for Chronic Hepatitis C Virus (HCV) Infection in Liver Transplant Candidates (EZE-2) [NCT02768545]Phase 412 participants (Anticipated)Interventional2013-06-30Recruiting
A Study to Evaluate the Definitive Bioequivalence of SCH 900068 With Marketed Products (Protocol No. P07551) [NCT01236430]Phase 1200 participants (Actual)Interventional2011-02-28Completed
A Multicenter, Randomized, Open-label Study to Evaluate the Lipid-Altering Efficacy and Safety of Ezetimibe (+) Simvastatin Versus Atorvastatin in Hypercholesterolemic Patients With Diabetes Mellitus or Metabolic Syndrome [NCT00157924]Phase 4190 participants (Actual)Interventional2005-11-30Completed
Risk Reduction in Coronary Heart Disease - a Prospective Randomized Study [NCT00679237]1,600 participants (Actual)Interventional2007-09-30Completed
A Randomized, Double-Blind, Active-Controlled, Multicenter Study of Patients With Primary Hypercholesterolemia and High Cardiovascular Risk Who Are Not Adequately Controlled With Atorvastatin 10 mg: A Comparison of the Efficacy and Safety of Switching to [NCT01154036]Phase 31,547 participants (Actual)Interventional2010-07-31Completed
A Prospective, Randomized Study to Determine the Effect of Ezetimibe in Addition to Rosuvastatin on Lipids in Participants With the Hypercholesterolemia Associated With HIV Antiretroviral Therapy [NCT00908011]43 participants (Actual)Interventional2009-06-30Completed
A Randomized, Double-blind, Active-controlled, Multicenter Phase III Trial to Evaluate the Efficacy and Safety of Co-administrated AD-2071 and AD-2073 in Patients With Primary Hypercholesterolemia and Essential Hypertension [NCT04158076]Phase 3131 participants (Actual)Interventional2020-01-23Completed
Designated Drug Use Investigation (Long-Term Administration) of Zetia 10-mg Tablets - A 52-Week Long-Term Designated Drug Use Investigation of Zetia Monotherapy and Combination Therapy [NCT00705211]1,794 participants (Actual)Observational2007-06-30Completed
A Phase II, Placebo-Controlled, Double-Blind, Randomised, 10-Week, Parallel-Group Study to Assess the Efficacy of Different Doses of KB2115 as Add on to Ezetimibe Treatment in Patients With Primary Hypercholesterolemia [NCT00677248]Phase 2120 participants (Anticipated)Interventional2008-04-30Completed
Randomized Comparison of the CHOlesterol-lowering Effects of nutraceuticaLs Versus Ezetimibe in Statin-intolerant patientS - The CHOLESS Trial [NCT01807078]Phase 4200 participants (Anticipated)Interventional2014-01-31Not yet recruiting
Phase IV Study for Efficacy and Safety of Evolocumab Added to Ezetimibe (Standard of Care) in High Cardiovascular Risk Haemodialized Statin Intolerant Patients With Hypercholesterolemia [NCT04659525]Phase 450 participants (Anticipated)Interventional2020-11-01Recruiting
Long-Term, Open-Label, Safety and Tolerability Study of SCH 58235 in Addition to Atorvastatin or Simvastatin in the Therapy of Homozygous Familial Hypercholesterolemia [NCT03885921]Phase 344 participants (Actual)Interventional2000-10-25Completed
A Multicenter, Randomized, Double-blind, Active-controlled, Phase 3 Trial to Evaluate the Efficacy and Safety of Co-administrated Ezetimibe/Rosuvastatin and Telmisartan in Patients With Essential Hypertension and Primary Hypercholesterolemia [NCT04659070]Phase 3156 participants (Anticipated)Interventional2020-07-15Recruiting
Rho-kinase in Patients With Atherosclerosis: Effects of Statins A Randomized Clinical Trial Comparing Ezetimibe/Simvastatin and Simvastatin [NCT00560170]Phase 440 participants (Actual)Interventional2007-09-30Completed
A Randomized, Double-Blind, Active-Controlled, Parallel-Group Study to Evaluate the Efficacy And Safety of SAR236553/REGN727 Over 24 Weeks in Patients With Hypercholesterolemia [NCT01644474]Phase 3103 participants (Actual)Interventional2012-07-31Completed
[NCT01857843]Phase 4160 participants (Actual)Interventional2009-11-30Completed
Long-Term, Open-Label, Safety and Tolerability Study of Ezetimibe (SCH 58235) in Addition to Atorvastatin in Subjects With Coronary Heart Disease or Multiple Risk Factors and With Primary Hypercholesterolemia Not Controlled by a Starting Dose (10 mg) of A [NCT03882996]Phase 3432 participants (Actual)Interventional2000-10-06Completed
Austrian Cholesterol Screening And Treatment II (ACT II) [NCT01381679]1,682 participants (Actual)Observational2009-05-31Completed
Left Ventricular Hypertrophy Reduction With Statins in Hypertensives Patients. [NCT00738972]Phase 312 participants (Actual)Interventional2008-01-31Terminated(stopped due to Study terminated early due to sample size, not possible to perform further statistical analysis.)
A Randomized, Double-blind, Placebo-controlled, Parallel-group Study to Evaluate Low Doses of the MTP-Inhibitor AEGR-733 on Hepatic Fat Accumulation as Measured by Magnetic Resonance Spectroscopy [NCT00559962]Phase 2260 participants (Actual)Interventional2007-10-31Completed
Phase 4 Study on Effect of Ezetimibe on Platelet Aggregation and LDL Tendency to Peroxidation In Hypercholesterolemic Patients on Simvastatin [NCT00466401]Phase 420 participants Interventional2005-02-28Completed
A Multicenter, Open Labeled, Cross-Over Designed Prospective Study Evaluating the Effects of Lipid Lowering Treatment on Steroid Synthesis [NCT00433823]Phase 40 participants Interventional2007-01-31Recruiting
"Ezetimibe Utilization Early After Acute Myocardial Infarction. EzAMI Trial" [NCT04701242]500 participants (Anticipated)Interventional2021-03-24Recruiting
A Randomized, Double-Blind, Parallel-Group, Placebo-Controlled,Ezetimibe-Calibrated, Multicenter Study Evaluating the Safety and Efficacy of Four Doses and Two Dose-Regimens of AVE5530 Over 4 Weeks in Patients With Mild to Moderate Primary Hypercholestero [NCT00440154]Phase 2206 participants (Actual)Interventional2007-02-28Completed
A Multi-center, Randomized, Open-label, Active-controlled, Phase IV Clinical Trial to Evaluate the Efficacy and Safety of EzetimiBe/Rosuvastatin Diabetic Dislipidemia With Hypertriglyceridaemia [NCT04700436]Phase 4240 participants (Anticipated)Interventional2020-01-03Recruiting
Effects of Ezetimibe Add-On to Statin Therapy on Adipokine Production in Obese and Metabolic Syndrome Patients With Atherosclerosis [NCT00485121]50 participants (Anticipated)Interventional2007-04-30Completed
A Randomized, Double-blind, Active-controlled, Multicenter Phase 3 Trial to Evaluate the Efficacy and Safety of Administrated AD-221 and AD-221A in Patients With Primary Hypercholesterolemia [NCT05131997]Phase 3290 participants (Actual)Interventional2021-11-16Completed
An Open-Label Postmarking Milk-Only Lactation Study to Evaluate the Concentration of Bempedoic Acid and Bempedoic Acid and Ezetimibe in the Breast Milk of Healthy Lactating Women Administered Therapeutic Doses of Bempedoic Acid or Bempedoic Acid/Ezetimibe [NCT06021951]Phase 416 participants (Anticipated)Interventional2023-08-04Recruiting
Low Dose Statins, Ezetimibe and Nutraceuticals in Coronary Artery Disease Patients Intolerant to High Intensity Statin Treatment (TArget ChOlesterol) [NCT03277079]Phase 4100 participants (Anticipated)Interventional2017-10-01Not yet recruiting
Phase IV Study for Efficacy and Safety of Evolocumab Added to Ezetimibe (Standard of Care) in High Cardiovascular Risk Haemodialized Statin Intolerant Patients With Hypercholesterolemia [NCT04397653]Phase 450 participants (Anticipated)Interventional2020-05-04Recruiting
A Phase III Double-Blind Efficacy and Safety of Ezetimibe (SCH 58235) 10 MG in Addition to Atorvastatin in Subjects With Coronary Heart Disease or Multiple Cardiovascular Risk Factors and With Primary Hypercholesterolemia Not Controlled by a Starting Dose [NCT03867318]Phase 3621 participants (Actual)Interventional2000-04-24Completed
SCH 058235: Assessment of a Multiple-Dose Drug Interaction Between Ezetimibe and Rosuvastatin in Healthy Hypercholesterolemic Subjects [NCT00651144]Phase 140 participants (Actual)Interventional2003-03-31Completed
A Study to Assess Adding Ezetimibe 30 mg to Ongoing Treatment With Ezetimibe 10 mg in Patients With Homozygous Sitosterolemia [NCT00099996]Phase 33 participants Interventional2004-12-31Completed
The Comparison of the Efficacy of Ezetimibe and Fenofibrate Versus Atorvastatin Alone in the Lowering of LDL Cholesterol [NCT00299884]45 participants (Actual)Observational2005-01-31Completed
A Randomized, Multicenter Study to Evaluate Tolerability and Efficacy of AMG 145 on LDL-C, Compared With Ezetimibe, in Hypercholesterolemic Subjects Unable to Tolerate an Effective Dose of a HMG-CoA Reductase Inhibitor [NCT01375764]Phase 2160 participants (Actual)Interventional2011-07-28Completed
Silent Cerebrovascular Lesion and Cognitive Decline Prevention in Atrial Fibrillation by Intensive Cholesterol Lowering in Elderly Patients [NCT00449410]Phase 435 participants Interventional2005-05-31Completed
Genetic Determinanats of Cardiovascular Risk Factors: Comparison of Efficacy and Safety of Ezetimibe or Statin Monotherapy to Co-Administration of Both [NCT00461968]240 participants Interventional2005-02-28Completed
A Randomized, Prospective, Double-Blind Study to Evaluate the Effects on Lipid Profile of Combined Ezetimibe and Simvastatin Therapy as Compared to Simvastatin Alone in People With Type 2 Diabetes [NCT00157482]Phase 2108 participants Interventional2005-01-31Completed
Clinical Trial of Zocor and Vytorin in Adolescents With Type 1 Diabetes [NCT00477204]Phase 29 participants (Actual)Interventional2007-05-31Completed
A Prospective Randomized Open Label Blinded Endpoint Multicenter Study in Patients With Coronary Artery Disease to Assess the LDL Lowering Effect of Switching to Ezetimibe (+) Simvastatin for Cholesterol Lowering, Compared the Dose of the Statin Used. [NCT00166530]Phase 4367 participants (Actual)Interventional2005-11-30Completed
"Effect of Lipid Modification on Peripheral Arterial Disease After Endovascular Intervention (The ELIMIT Trial)" [NCT00687076]Phase 4102 participants (Actual)Interventional2004-04-30Completed
A Study to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Administering Multiple Oral Doses of GSK1292263 Alone and With Atorvastatin [NCT01218204]Phase 2287 participants (Actual)Interventional2010-09-14Completed
Evaluation of Chylomicrons Metabolism in Sub-Clinical Atherosclerosis in Patients Whit Heterozigous Familial Hypercholesterolemia (FH) Treated With Statin Plus Ezetimibe [NCT00475826]0 participants Interventional2007-04-30Recruiting
Comparison of the Effect on Endothelial Function of Statin Therapy in High Dose Versus Low Dose Combined With Ezetimibe [NCT01241097]60 participants (Anticipated)Interventional2010-03-31Recruiting
A Double-blinded, Placebo-controlled Randomized Trial Assessing the Extent to Which Consumption of Two Different Amounts of a Non-Pharmaceutical Food Supplement Can Improve Cardiovascular Health [NCT01890889]150 participants (Anticipated)Interventional2013-07-31Recruiting
ARBITER 6: ARterial Biology for the Investigation of the Treatment Effects of Reducing Cholesterol 6 - HDL and LDL Treatment Strategies in Atherosclerosis (HALTS) [NCT00397657]Phase 4400 participants (Anticipated)Interventional2006-11-30Terminated(stopped due to Independent steering committee has stopped the trial based on results of a prespecified, blinded interim analysis. It was not stopped due to safety concerns.)
Effect of Early Initiation of Evolocumab and Combination Lipid-lowering Agent on Lipid Profiles Changes in Patients With Acute Coronary Syndrome Undergoing percuTAneous coronaRy Intervention: a Prospective, Randomized Controlled Trial [NCT05661552]Phase 4102 participants (Anticipated)Interventional2022-12-01Recruiting
A RANDOMIZED, BALANCED, OPEN LABEL, CROSSOVER, TWO PERIOD, TWO TREATMENT, TWO SEQUENCE, SINGLE DOSE, BIOEQUIVALENCE STUDY OF ACOTRAL® EZETIMIBE 10 MG TABLETS CONTAINING EZETIMIBE MANUFACTURED BY LABORATORIOS PHOENIX S.A.I.C.F, ARGENTINA AND ZETIA® EZETIMI [NCT01597700]Phase 152 participants (Actual)Interventional2012-01-13Completed
Comparison of Antiplatelet and Anti-inflammatory Effects of High Dose Statin Monotherapy Versus Moderate Dose Statin Plus Ezetimibe [NCT00474123]78 participants (Actual)Interventional2006-01-31Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Study to Evaluate SCH-58235 in Homozygous Sitosterolemia [NCT00045812]Phase 25 participants Interventional2001-03-31Completed
Comparative Efficacy Evaluation of Lipid Levels When Treated With Niaspan and Statin or Other Lipid-Modifying Therapies [NCT00079638]Phase 4300 participants Interventional2004-04-30Completed
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study of the Efficacy and Safety of WelChol® in Combination With Zetia® Compared to Zetia® Alone in Patients With Primary Hypercholesterolemia [NCT00185107]Phase 445 participants Interventional2005-03-31Completed
The Effects of Ezetimibe on Postprandial Hyperlipidemia and Endothelial Dysfunction in Patients With the Metabolic Syndrome. [NCT00189085]Phase 420 participants Interventional2004-12-31Completed
A Multicenter, Randomized, Double-Blind, Prospective, Parallel Study to Compare the Safety and Efficacy of Fenofibrate or Ezetimibe as Add-On Therapy to Atorvastatin in Subjects With Combined Hyperlipidemia, Typical of the Metabolic Syndrome [NCT00195793]Phase 3174 participants (Actual)Interventional2004-08-31Completed
CHORD1 - CHOlesterol Lowering and Residual Risk in Diabetes, Type 1 [NCT05641753]Phase 4125 participants (Anticipated)Interventional2022-12-06Recruiting
Effects of Statin and Ezetimibe Association on Kinetics of Artificial Chilomicrons in Men With Stable Coronary Heart Disease. [NCT00481351]Phase 425 participants (Actual)Interventional2007-06-30Completed
A Multicenter, Open-label, 6 Week Study to Evaluate the Efficacy and Safety of Algorithm Based Intensive Treatment With Vytorin Versus Standard Treatment of Other Statins in Moderate, Moderately High and High Risk Patients. [NCT01587235]Phase 40 participants (Actual)Interventional2013-03-31Withdrawn
A Multicenter, Open Study To Evaluate The Efficacy Of Ezetimibe 10 Mg Added On Statin Therapy, In Reducing LDL Cholesterol To Target Levels In Patients After Acute Coronary Syndrome [NCT00652717]Phase 4280 participants (Actual)Interventional2005-02-01Completed
Ezetimibe Added to Statin Therapy [NCT00395473]Phase 3141 participants (Actual)Interventional2005-03-31Completed
An Open-Label, Worldwide, Treatment Use Study to Provide Ezetimibe 10 Mg/Day to Patients With Homozygous Familial Hypercholesterolemia or Homozygous Sitosterolemia [NCT00092833]Phase 349 participants (Actual)Interventional2002-07-31Terminated
Randomized Parallel Group Trial Of The Efficacy And Safety Of Ezetimibe With A Statin Versus Statin Dose Doubling In Patients With Persistent Primary Hypercholesterolemia [NCT00652847]Phase 41,140 participants (Actual)Interventional2005-05-31Completed
A Randomized, Double-Blind, Placebo-Controlled,4-Period, Crossover Study to Evaluate the Effects of Ezetimibe and Simvastatin, Coadministered and Alone, on Intestinal Absorption of Cholesterol [NCT00652301]Phase 340 participants (Actual)Interventional2003-07-31Completed
A Comparison of Treatment With Ezetimibe (SCH 58235) and Simvastatin Coadministration Versus Simvastatin in Attaining the National Cholesterol Education Program (NCEP) Adult Treatment Panel (ATP) III Coronary Heart Disease (CHD) or CHD Risk Equivalent Str [NCT00551447]Phase 3616 participants (Actual)Interventional2002-01-31Completed
A Double-Blind, Multicenter Study to Assess the LDL-C Lowering of Combination Tablets Ezetimibe/Simvastatin (10mg/20mg) and Ezetimibe/Simvastatin (10mg/40mg) Compared to Atorvastatin 20mg in Patients With Type II Diabetes. [NCT00541697]Phase 3648 participants (Actual)Interventional2005-01-19Completed
Compare Ezetimibe 10mg and Simvastatin 40mg vs Atorvastatin 80mg Daily in Subjects With Cardiovascular Heart Disease and/or Diabetes Mellitus With Uncontrolled Lipids on Statin Therapy [NCT00395603]Phase 3550 participants (Anticipated)Interventional2006-09-30Terminated(stopped due to This study was terminated early due to poor recruitment.)
Ezetimibe Together With Any Statin Cholesterol Enhancement [NCT00328523]Phase 31,496 participants (Actual)Interventional2004-06-30Completed
Multicenter,Double Blind,Randomized, 2-period, Crossover Study to Compare Ezetimibe/Simvastatin (10mg/10 mg) Combination Tablet Versus Simvastatin 80mg Tablet on Postprandial Arterial Endothelial Function in Patients With Metabolic Syndrome [NCT00817843]Phase 4100 participants (Actual)Interventional2009-04-30Completed
The Effects of Ezetimibe/Simvastatin Versus Simvastatin Alone on Platelet and Inflammatory Biomarkers in Patients With the Metabolic Syndrome [NCT00819403]Phase 415 participants (Actual)Interventional2009-01-31Completed
A Randomized, Partial Blind, 3 Parallel Groups Study of the Pharmacodynamic Profile of SAR236553 (REGN727) Administered as Multiple Subcutaneous Doses, Either Alone or on Top of Ezetimibe or Fenofibrate Administered as Multiple Oral Doses in Healthy Subje [NCT01723735]Phase 179 participants (Actual)Interventional2012-11-30Completed
Effects of Selective Inhibition of Cholesterol Absorption With Ezetimibe on Intestinal Cholesterol Homeostasis in Dyslipidemic Men With Insulin-resistance - a Pilot Study [NCT01849068]Phase 320 participants (Actual)Interventional2013-06-30Completed
Phase 0 Trial of Presurgical Cholesterol-lowering on Prostate Cancer Cell Growth [NCT02534376]Early Phase 163 participants (Actual)Interventional2015-09-30Completed
Phase 3, Open-Label, Multi-Center, Double-Blind, Randomized, Parallel Group Study Efficacy and Safety of Fixed Combination Torcetrapib/Atorvastatin, Administered Once Daily (QD) Compared to Fixed Combination Ezetimibe/Simvastatin for 6 Weeks in Subjects W [NCT00267267]Phase 31,784 participants Interventional2006-01-31Terminated
A Phase 2 ,Multicentre, Randomised, Double Blind Double Simulation, Placebo and Positive Controlled Study to Evaluate the Efficacy and Safety of HSK31679 in Patients With Hypercholesterolemia With Non-alcoholic Fatty Liver Disease [NCT05795517]Phase 2200 participants (Anticipated)Interventional2023-04-26Active, not recruiting
Effect of PCSK9 Inhibitors on Calcific Aortic Valve Disease: a Prospective Randomized Controlled Trial [NCT04968509]Phase 3160 participants (Anticipated)Interventional2024-01-31Not yet recruiting
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.)
Ezetimibe Versus Placebo in the Treatment of Non-alcoholic Steatohepatitis [NCT01766713]Phase 250 participants (Actual)Interventional2013-01-31Completed
A Randomized, Double-Blind Study of the Efficacy and Safety of Alirocumab Added on to Atorvastatin Versus Ezetimibe Added on to Atorvastatin Versus Atorvastatin Dose Increase Versus Switch to Rosuvastatin in Patients Who Are Not Controlled on Atorvastatin [NCT01730040]Phase 3355 participants (Actual)Interventional2012-10-31Completed
Atorvastatin vs. Atorvastatin/Ezetimibe in Patients With Hypo-response to Initial Dose Statin Therapy [NCT00965055]Phase 32 participants (Actual)Interventional2009-09-30Terminated(stopped due to The study was terminated due to inability to recruit subjects. A total of 2/100 anticipated were radomized.)
Examination of the Effect of Ezetimibe on Glucose Metabolism - Randomized, Double-blind, Placebo-controlled Study in Type 2 Diabetes Mellitus Patients With Hypercholesterolemia - Phase 4, Protocol No. 367 (Also Known as SCH 58235, P06541) [NCT01611883]Phase 4152 participants (Actual)Interventional2012-07-02Completed
A Phase III, Randomized, Active Comparator-controlled Clinical Trial to Study the Efficacy and Safety of MK-0653C in Japanese Patients With Hypercholesterolemia [NCT02550288]Phase 3309 participants (Actual)Interventional2015-09-29Completed
A Multicenter, Randomized, Double-Blind, Titration Study to Evaluate the Efficacy and Safety of Ezetimibe Added On to Rosuvastatin Versus Up Titration of Rosuvastatin in Patients With Hypercholesterolemia at Risk for Coronary Heart Disease [NCT00783263]Phase 3440 participants (Actual)Interventional2008-11-30Completed
A Randomized comparaTive Study Of Rosuvastatin/Ezetimibe 20/10mg and Atorvastatin/Ezetimibe 40/10mg in Patients With Coronary Artery Drug eLuting stEnt Implantation Requiring High-dose stAtin/Ezetimibe combiNaTion Therapy: TOLERANT Trial [NCT05910476]Phase 4200 participants (Anticipated)Interventional2023-05-03Recruiting
A Placebo-Controlled, Double-Blind, Randomized Phase 2 Study to Evaluate the Effect of Obicetrapib in Combination With Ezetimibe in Participants With Mild Dyslipidemia [NCT04770389]Phase 2112 participants (Actual)Interventional2021-02-23Completed
Effect of Combination Ezetimibe and High-Dose Simvastatin vs Simvastatin Alone on the Atherosclerotic Process in Subjects With Heterozygous Familial Hypercholesterolemia (The ENHANCE Trial) [NCT00552097]Phase 3720 participants (Actual)Interventional2002-06-01Completed
Study of Heart and Renal Protection (SHARP): The Effects of Lowering LDL-cholesterol With Simvastatin 20mg Plus Ezetimibe 10mg in Patients With Chronic Kidney Disease: a Randomized Placebo-controlled Trial [NCT00125593]Phase 49,438 participants (Actual)Interventional2003-06-30Completed
Study of no Pharmacokinetic Interaction Between Rosuvastatin 20 mg and Ezetimibe 10 mg, Open Design, Randomized, Single Dose, 3x6, Crossove, Healthy Volunteers in Fasting, in Fixed Combination Against Individuals Components Managed [NCT04895059]Phase 136 participants (Actual)Interventional2017-04-30Completed
RAndomized Comparison of Efficacy and Safety of Lipid-lowerING With Statin Monotherapy Versus Statin/Ezetimibe Combination for High-risk Cardiovascular Diseases (RACING Trial) [NCT03044665]3,780 participants (Anticipated)Interventional2017-03-15Recruiting
Real World Data Observational Study to Evaluate the Management Status of Dyslipidemia Following Administration of Statin and Ezetimibe Complex Treatment Patient in the Medical Situation by Classification of Medical Institutions in KOREA [NCT05614765]18,000 participants (Anticipated)Observational2022-07-08Recruiting
A Multicenter Clinical Trial to Compare the Efficacy and Safety Between Rosuvastatin/Ezetimibe Combination and Monotherapy of Rosuvastatin in Patients With Diabetes Mellitus and Hypercholesterolemia [NCT03217409]Phase 485 participants (Actual)Interventional2017-08-10Completed
A Randomised, Double-Blind Study Comparing the Efficacy and Safety of 145 mg Fenofibrate, 10 mg Ezetimibe and Their Combination in Patients With Type IIb Dyslipidemia and Features of the Metabolic Syndrome [NCT00349284]Phase 3181 participants Interventional2005-01-31Completed
Effects of Ezetimibe and Simvastatin on LDL Receptor Protein Expression and on LDL Receptor and HMG-CoA Reductase mRNA Expression in Mononuclear Cells: a Randomized Controlled Study in Healthy Men [NCT00317993]Phase 460 participants Interventional2004-04-30Completed
A Randomized, Double-Blind, Active-Controlled Study of Patients With Primary Hypercholesterolemia and High Cardiovascular Risk and Not Adequately Controlled With Atorvastatin: A Comparison of Switching to a Combination Tablet Ezetimibe/Simvastatin Versus [NCT00782184]Phase 3250 participants (Actual)Interventional2008-11-30Completed
A Double-blind, Randomized, Placebo-controlled, Multicenter Phase II Study of AK102 in the Treatment of Hypercholesterolemia Patients at Very High or High Risk of Cardiovascular Disease [NCT04358432]Phase 2262 participants (Actual)Interventional2020-05-13Completed
A 16-week Multicenter, 2-period Study to Investigate the Effect of the Combination of Fluvastatin ER 80mg and Fenofibrate 200mg on HDL-C in Comparison to the Combination of Simvastatin 20mg and Ezetimibe 10mg in Patients With Metabolic Syndrome [NCT00385658]Phase 475 participants (Actual)Interventional2006-08-31Completed
A Double-blind, Randomized, Placebo-controlled, Multicenter Study to Evaluate the Safety and Efficacy of AK102 in Patients With Heterozygous Familial Hypercholesterolemia [NCT04173793]Phase 2109 participants (Actual)Interventional2019-11-18Completed
A Randomized, Double-Blind, Parallel Group Study to Evaluate the Efficacy and Safety of SAR236553/REGN727 Versus Ezetimibe in High Cardiovascular Risk Patients With Hypercholesterolemia Not Adequately Controlled With Their Statin Therapy [NCT01644188]Phase 3720 participants (Actual)Interventional2012-08-31Completed
A Phase 2 Study to Evaluate the Safety and Efficacy of PCSK9 Inhibitor AK102 in Patients With Homozygous Familial Hypercholesterolemia (HoFH) [NCT03933293]Phase 210 participants (Actual)Interventional2019-05-13Completed
Intensive Lipid-lowering Therapy for Early Achievement of Guideline-recommended LDL Cholesterol Levels in Patients With ST-elevation Myocardial Infarctions [NCT05587621]1,000 participants (Anticipated)Observational [Patient Registry]2022-08-23Recruiting
Ezetimibe as a Safe and Efficacious Treatment for Chronic Hepatitis C [NCT02971033]Phase 22 participants (Actual)Interventional2018-04-16Terminated(stopped due to Study Funding ended)
CHOlesterol Lowering and Residual Risk in Type 2 Diabetes [NCT04369664]Phase 4151 participants (Actual)Interventional2020-08-12Completed
A Double-Blind, Randomized, Placebo-controlled, Multicenter Study to Evaluate Long-Term Tolerability and Durable Efficacy of AMG 145 (Evolocumab) on LDL-C in Hyperlipidemic Subjects [NCT01516879]Phase 3905 participants (Actual)Interventional2012-01-05Completed
Metagenomic Analysis of Human Gut Microbiota in Patients With Metabolic Diseases Including Diabetes. [NCT03204799]150 participants (Anticipated)Observational2016-12-17Recruiting
Bioequivalence of Ezetimibe Tablets in Healthy Subjects: A Single-dose and Two-period Crossover Study [NCT04814589]Phase 196 participants (Anticipated)Interventional2021-03-13Recruiting
A Phase 2 Double Blind, Parallel Group, Placebo Controlled, Randomized, Dose Ranging Study To Assess The Efficacy, Safety And Tolerability Of Pf-04950615 Following Twice Monthly Subcutaneous Doses In Hypercholesterolemic Japanese Subjects Who Are Receivin [NCT02055976]Phase 2218 participants (Actual)Interventional2014-03-31Completed
A Long-term Study to Evaluate the Efficacy and Safety of AK102 in Combination With Lipid-lowering Therapy in Patients With Hypercholesterolemia [NCT04173403]Phase 2796 participants (Actual)Interventional2019-11-04Completed
A Randomized, Open-Label, Parallel Group Study to Evaluate the Efficacy and Safety of Alirocumab Versus Usual Care in Patients With Type 2 Diabetes and Mixed Dyslipidemia at High Cardiovascular Risk With Non-HDL-C Not Adequately Controlled With Maximally [NCT02642159]Phase 4413 participants (Actual)Interventional2016-03-15Completed
A Multicenter, Double-Blind, Randomized, Placebo-Controlled Study to Evaluate the Lipid-Altering Efficacy, Safety, and Tolerability of SCH 58235 When Added to Ongoing Therapy With an HMG-CoA Reductase Inhibitor (Statin) in Patients With Primary Hyperchole [NCT03882905]Phase 3769 participants (Actual)Interventional2001-01-31Completed
A Multicenter, Double-Blind, Randomized Study to Evaluate the Lipid-Altering Efficacy, Safety, and Tolerability of Ezetimibe Coadministered With Simvastatin Versus Simvastatin Monotherapy in African-American Subjects With Primary Hypercholesterolemia [NCT00650663]Phase 4247 participants (Actual)Interventional2003-10-01Completed
Comparison of Effects of Simvastatin Versus Ezetimibe on Intracellular Lipid and Inflammation in Obese Subjects [NCT04638400]Phase 410 participants (Actual)Interventional2017-05-01Terminated(stopped due to Lack of recruitment- Fellow responsible for study graduated)
Phase III, Multicenter, Randomized, Open-label, Comparative Study to Evaluate Efficacy and Safety of Rosuvastatin + Ezetimibe Versus Simvastatin + Ezetimibe in High Risk Patients With Primary Hypercholesterolemia or Mixed Dyslipidemia [NCT01420549]Phase 3129 participants (Actual)Interventional2013-03-31Completed
Open Label Study Evaluating The Use Of Combination Therapy Of Ezetimibe And Statins In Patients With Dyslipidemia In Colombia [NCT00651963]Phase 480 participants (Actual)Interventional2004-09-30Completed
Investigate the Effect of Ezetimibe, Simvastatin, and Omega 3- Fatty Acids on Dyslipidemia Patients: a Pharmacokinetics Based Study [NCT05080140]3 participants (Anticipated)Observational2019-06-01Active, not recruiting
A Phase 2 Efficacy and Safety Dose-Ranging Study of LY3015014 in Patients With Primary Hypercholesterolemia [NCT01890967]Phase 2527 participants (Actual)Interventional2013-06-30Completed
Effect Of Ezetimibe Coadministration With Simvastatin In A Middle Eastern Population: A Prospective, Multicentre, Randomized, Double-Blind, Placebo-Controlled Trial [NCT00652444]Phase 4120 participants (Actual)Interventional2003-09-30Completed
A Multicenter, Double-Blind, Randomized, Parallel Group, 28-Week Study to Evaluate the Efficacy and Safety of Ezetimibe and Simvastatin Co-administration Versus Atorvastatin in Patients With Hypercholesteremia [NCT00092716]Phase 3655 participants (Actual)Interventional2002-05-31Completed
A Double-blind, Randomized, Multicenter Study to Evaluate Safety and Efficacy of AMG 145, Compared With Ezetimibe, in Hypercholesterolemic Subjects Unable to Tolerate an Effective Dose of a HMG-CoA Reductase Inhibitor [NCT01763905]Phase 3307 participants (Actual)Interventional2013-01-24Completed
A Randomized, Double-Blind Study of the Efficacy and Safety of REGN727 Added-on to Rosuvastatin Versus Ezetimibe Added-on to Rosuvastatin Versus Rosuvastatin Dose Increase in Patients Who Are Not Controlled on Rosuvastatin [NCT01730053]Phase 3305 participants (Actual)Interventional2012-11-30Completed
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.)
Observational Study Evaluating the LDL-C Lowering Effects of Ezetimibe With a Statin as Prescribed in Daily Routine Practice in an Indonesian Population [NCT00705081]453 participants (Actual)Observational2006-01-31Completed
THE EFFECT OF SIMVASTATIN VERSUS COMBINED SIMVASTATIN/EZETIMIBE TREATMENT ON THE CONCENTRATION OF SMALL DENSE LOW-DENSITY LIPOPROTEIN PARTICLES IN PATIENTS WITH PRIMARY HYPERCHOLESTEROLEMIA [NCT00932620]Phase 4100 participants (Actual)Interventional2009-06-30Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study of the Effect of Ezetimibe Plus Simvastatin Compared With Simvastatin Alone on Flow-Mediated Brachial Artery Vasoactivity in Subjects With Primary Hypercholesterolemia (The EFFECTS Trial) [NCT00651391]Phase 328 participants (Actual)Interventional2003-10-01Terminated(stopped due to Slow enrollment)
A Multicenter, Randomized, Parallel Groups, Placebo-controlled Study Comparing the Efficacy, Safety, and Tolerability of the Daily Coadministration of Ezetimibe 10 mg With Atorvastatin 10 mg in Untreated Subjects With Primary Hypercholesterolemia and Coro [NCT00650689]Phase 3122 participants (Actual)Interventional2003-05-31Completed
Comprehensive Magnetic Resonance of Peripheral Arterial Disease [NCT00587678]85 participants (Actual)Interventional2006-01-31Completed
An Open-Label, 2-Period, Crossover Study to Determine the Effect of Multiple Oral Doses of Ezetimibe 20 mg on the Pharmacokinetics of a Single Oral Dose of Cyclosporine in Young, Healthy, Normal, Male and Female Subjects [NCT00653276]Phase 113 participants (Actual)Interventional2003-11-30Completed
Vytorin As Strategy To Reduce Dislipidemia In Adults [NCT00651560]Phase 3167 participants (Actual)Interventional2005-11-01Completed
A Randomized, Double-Blind, Parallel, Multicenter Study to Evaluate the Efficacy and Safety of Simvastatin Monotherapy Compared With Simvastatin Plus Ezetimibe (SCH 58235) in Type 2 Diabetic Patients Treated With Thiazolidinediones [NCT00551876]Phase 3214 participants (Actual)Interventional2001-12-31Completed
A Multicenter, Randomized, Double-Blind, Prospective Study Comparing the Safety and Efficacy of ABT-335 in Combination With Atorvastatin and Ezetimibe to Atorvastatin in Combination With Ezetimibe in Subjects With Combined (Atherogenic) Dyslipidemia [NCT00639158]Phase 3543 participants (Actual)Interventional2008-02-29Completed
Effect of Atorvastatin and Omega 3 Combination Therapy on Carotid Atherosclerosis Estimated by 3D Ultrasound in Patients With Type 2 Diabetes and Combined Dyslipidemia [NCT05365438]Phase 4105 participants (Anticipated)Interventional2022-10-01Recruiting
Non-interventional Study on the Treatment With Bempedoic Acid and/or Its Fixed-dose Combination With Ezetimibe in Routine Clinical Practice in Patients With Primary Hypercholesterolemia or Mixed Dyslipidemia (MILOS) [NCT04579367]5,000 participants (Anticipated)Observational2021-01-15Recruiting
A Randomized, Double-blind, Parallel Group Study to Evaluate the Efficacy and Safety of Alirocumab (SAR236553/REGN727) Versus Ezetimibe in Asia in High Cardiovascular Risk Patients With Hypercholesterolemia Not Adequately Controlled With Their Statin Ther [NCT02715726]Phase 3615 participants (Actual)Interventional2016-07-27Completed
A Multicenter, Randomized, Double-Blind, Parallel, 12-Week Study to Evaluate the Efficacy and Safety of Ezetimibe/Simvastatin Combination Tablet Versus Atorvastatin in Elderly Patients With Hypercholesterolemia at High or Moderately High Risk for Coronary [NCT00535405]Phase 31,289 participants (Actual)Interventional2007-11-30Completed
Multicenter, Randomized, Double-Blind Study to Evaluate the Efficacy and Safety of Ezetimibe/Simvastatin and Niacin (Extended Release Tablet) Co-Administered in Patients With Type IIa or Type IIb Hyperlipidemia [NCT00271817]Phase 31,220 participants (Actual)Interventional2005-12-31Completed
INvestigating the Lowest Threshold of Vascular bENefits From LDL Cholesterol Lowering With a PCSK9 mAb InhibiTor (Alirocumab) in Patients With Stable Cardiovascular Disease (INTENSITY-HIGH) [NCT03355027]60 participants (Actual)Interventional2017-11-30Active, not recruiting
A Prospective, Multicenter, Randomized, Open-label Trial to Compare Low-dose ROSUvastatin Plus eZETimibe Versus High-dose Rosuvastatin in Patients With Acute Myocardial Infarction Undergoing Percutaneous Coronary Intervention [NCT04499859]Phase 43,548 participants (Anticipated)Interventional2020-10-01Recruiting
A Double-blind, Randomized, Multicenter Study to Evaluate the Safety and Efficacy of Evolocumab, Compared With Ezetimibe, in Hypercholesterolemic Subjects Unable to Tolerate an Effective Dose of a HMG-CoA Reductase Inhibitor Due to Muscle Related Side Eff [NCT01984424]Phase 3511 participants (Actual)Interventional2013-12-10Completed
SCH 58235: A Multicenter, Randomised, Parallel Groups, Placebo-Controlled Study Comparing The Efficacy, Safety, and Tolerability Of The Daily Co-Administration of Ezetimibe 10 mg With Simvastatin 20 mg vs Ezetimibe Placebo With Simvastatin 20 mg in Untrea [NCT00653835]Phase 4153 participants (Actual)Interventional2003-09-01Completed
"An Open Label, One-sequence, 3-period Study to Evaluate Drug-drug Interactions and Safety Between BR1017-1 and BR1017-2 in Healthy Volunteers" [NCT05372380]Phase 132 participants (Actual)Interventional2022-05-09Completed
A Randomized, Double-Blind, Double-Dummy, Active-Controlled Study to Evaluate the Efficacy and Safety of REGN727/SAR236553 in Patients With Primary Hypercholesterolemia Who Are Intolerant to Statins [NCT01709513]Phase 3314 participants (Actual)Interventional2012-09-30Completed
Study of Lipoprotein Subfractions, Inflammation, Oxidative Stress and Endothelial Function After Treatment With Simvastatin and Ezetimibe Administered Alone and in Combination in Hyperlipidemic Patients [NCT02304926]42 participants (Actual)Interventional2009-01-31Completed
The Effect of Ezetimibe-Ursodiol Combination Therapy on Biomarkers of Liver Function and Sterol Balance in Subjects With NAFLD [NCT02244944]Phase 22 participants (Actual)Interventional2014-09-30Terminated(stopped due to Failure to recruit)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00092677 (19) [back to overview]Number of Participants That Experienced One or More Components of the Composite Clinical Endpoint of AVE (Aortic Valve Events)
NCT00092677 (19) [back to overview]Incident Cancer
NCT00092677 (19) [back to overview]Nonfatal Myocardial Infarction (MI)
NCT00092677 (19) [back to overview]Nonhemorrhagic Stroke
NCT00092677 (19) [back to overview]Percutaneous Coronary Intervention (PCI)
NCT00092677 (19) [back to overview]Percent Change in Time Weighted Average Triglycerides From Baseline to End of Follow-up
NCT00092677 (19) [back to overview]Percent Change in Time Weighted Average Total Cholesterol From Baseline to End of Follow-up
NCT00092677 (19) [back to overview]Percent Change in Time Weighted Average Low-density Lipoprotein Cholesterol (LDL-C) From Baseline to End of Follow-up
NCT00092677 (19) [back to overview]Percent Change in Time Weighted Average High-density Lipoprotein Cholesterol (HDL-C) From Baseline to End of Follow-up
NCT00092677 (19) [back to overview]Aortic Valve Replacement (AVR)
NCT00092677 (19) [back to overview]Number of Participants That Experienced One or More Components of the Composite Clinical Endpoint of ICE (Ischemic Cardiovascular Events)
NCT00092677 (19) [back to overview]Number of Participants That Experienced One or More Components of the Composite Clinical Endpoint of MCE (Major Cardiovascular Events)
NCT00092677 (19) [back to overview]Cardiovascular Death
NCT00092677 (19) [back to overview]Change From Baseline in Peak Transaortic Jet Velocity
NCT00092677 (19) [back to overview]Congestive Heart Failure (CHF) Due to Progression of Aortic Stenosis (AS)
NCT00092677 (19) [back to overview]Hospitalization for Unstable Angina
NCT00092677 (19) [back to overview]Death Due to Cancer
NCT00092677 (19) [back to overview]Death (Any Cause)
NCT00092677 (19) [back to overview]Coronary Artery Bypass Grafting (CABG)
NCT00101439 (2) [back to overview]Total Cholesterol Concentration of Chylomicron-remnant (Sf 60-400) Subfractions After a Cholesterol-Rich Test Meal
NCT00101439 (2) [back to overview]Total Cholesterol Concentration of Chylomicron (Sf≥400) Fractions After a Cholesterol-Rich Test Meal
NCT00125593 (7) [back to overview]Major Vascular Events Analyzed Among All Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo
NCT00125593 (7) [back to overview]Major Vascular Events Analyzed Amongst Patients Initially Randomized to Simvastatin Plus Ezetimibe Versus Placebo (Original Protocol-defined Primary Outcome)
NCT00125593 (7) [back to overview]Non-hemorrhagic Stroke Among All of Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo
NCT00125593 (7) [back to overview]Key Outcome as Per Statistical Analysis Plan = Major Atherosclerotic Events Among All Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo
NCT00125593 (7) [back to overview]Coronary or Non-coronary Revascularization Among All Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo
NCT00125593 (7) [back to overview]End-stage Renal Disease Among All Patients Not on Dialysis at the Time of Randomization to Simvastatin Plus Ezetimibe Versus Placebo
NCT00125593 (7) [back to overview]Major Coronary Events Among All Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo
NCT00129402 (6) [back to overview]Percent Change From Baseline in Total Cholesterol (TC)
NCT00129402 (6) [back to overview]Percent Change From Baseline in Non High-density Lipoprotein Cholesterol (Non HDL-C)
NCT00129402 (6) [back to overview]Percent Change From Baseline in Triglycerides (TG)
NCT00129402 (6) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)
NCT00129402 (6) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo B)
NCT00129402 (6) [back to overview]Percent Change From Baseline in HDL-C
NCT00166504 (1) [back to overview]LDL-C Lowering Efficacy
NCT00202878 (4) [back to overview]Time to First Occurrence of CV Death, Nonfatal MI, UA With Hospitalization, All Revascularization Occurring ≥30 Days After Randomization, and Non-fatal Stroke (Kaplan-Meier Estimate of Percentage of Participants Experiencing a Qualifying Event)
NCT00202878 (4) [back to overview]Time to First Occurrence of Death From Any Cause, Major Coronary Event, or Non-fatal Stroke (Kaplan-Meier Estimate of Percentage of Participants Experiencing a Qualifying Event)
NCT00202878 (4) [back to overview]Time to First Occurrence of Cardiovascular Death, Major Coronary Event, or Non-fatal Stroke (Kaplan-Meier Estimate of Percentage of Participants Experiencing a Qualifying Event)
NCT00202878 (4) [back to overview]Time to First Occurrence of Coronary Heart Disease (CHD) Death, Non-fatal MI, or Urgent Coronary Revascularization With PCI or CABG ≥ 30 Days After Randomization (Kaplan-Meier Estimate of Percentage of Participants Experiencing a Qualifying Event)
NCT00203476 (4) [back to overview]LFT Elevation
NCT00203476 (4) [back to overview]LDL Goal Attainment
NCT00203476 (4) [back to overview]Incidents of Rhabdomyolysis
NCT00203476 (4) [back to overview]Change in HDL From Baseline to 12 Weeks.
NCT00271817 (10) [back to overview]Percent Change From Baseline in Non-High-Density Lipoprotein-Cholesterol (Non-HDL-C)
NCT00271817 (10) [back to overview]Percent Change From Baseline in Non-High-Density Lipoprotein-Cholesterol (Non-HDL-C)
NCT00271817 (10) [back to overview]Percent Change From Baseline in Triglycerides (TG)
NCT00271817 (10) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C)
NCT00271817 (10) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C)
NCT00271817 (10) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C)
NCT00271817 (10) [back to overview]Percent Change From Baseline in Non-High-Density Lipoprotein-Cholesterol (Non-HDL-C)
NCT00271817 (10) [back to overview]Percent Change From Baseline in High-Density Lipoprotein-Cholesterol (HDL-C)
NCT00271817 (10) [back to overview]Percent Change From Baseline in High-Density Lipoprotein-Cholesterol (HDL-C)
NCT00271817 (10) [back to overview]Percent Change From Baseline in Triglycerides (TG)
NCT00276458 (14) [back to overview]Percent Change in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in Apolipoprotein B: Apolipoprotein A-I Ratio at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in C-Reactive Protein (CRP) at Week 6
NCT00276458 (14) [back to overview]Number of Participants Who Attained Target LDL-C <100 mg/dL at Week 6
NCT00276458 (14) [back to overview]Percent Change in High Density Lipoprotein -Cholesterol (HDL-C)at Week 6
NCT00276458 (14) [back to overview]Percent Change in C-Reactive Protein (CRP) at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in Total-Cholesterol:High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6
NCT00276458 (14) [back to overview]Percent Change in Apolipoprotein A-I at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in Triglycerides (TG) at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in Total-Cholesterol at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (HDL-C):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6
NCT00276458 (14) [back to overview]Percent Change From Baseline in Low Density Lipoprotein-Cholesterol (LDL-C) at Week 6
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Apolipoprotein B (Apo B)
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Apolipoprotein A-I (Apo A-I)
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Apolipoprotein B:Apolipoprotein A-I (Apo B:Apo A-I) Ratio
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in C Reactive Protein (CRP)
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Non-High-Density Lipoprotein-Cholesterol:High-Density Lipoprotein-Cholesterol (Non-HDL-C:HDL-C) Ratio
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Total-Cholesterol
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Triglycerides (TG)
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C)
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Low-Density Lipoprotein-Cholesterol:High-Density Lipoprotein-Cholesterol (LDL-C:HDL-C) Ratio
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Low-Density Lipoprotein (LDL)-C
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in High-Density Lipoprotein Cholesterol (HDL-C)
NCT00276484 (13) [back to overview]Percent Change From Baseline to Week 6 in Total-Cholesterol (TC):High-Density Lipoprotein Cholesterol (HDL-C) Ratio
NCT00276484 (13) [back to overview]Number of Patients Who Attained Target Low-Density Lipoprotein Cholesterol (LDL-C) <70 mg/dL at Week 6
NCT00319449 (3) [back to overview]Number of Participants Who Achieve the Target LDL-C Concentration of < 3.3 mmol/L (130 mg/dL)
NCT00319449 (3) [back to overview]High Density Lipoprotein-cholesterol (HDL-C), Total Cholesterol and Triglycerides at Baseline and After 6 Weeks of Treatment With Ezetimibe 10 mg Added to Atorvastatin 10 mg Versus Placebo Added to Atorvastatin 10 mg
NCT00319449 (3) [back to overview]Low Density Lipoprotein-cholesterol (LDL-C) at Baseline and After 6 Weeks of Treatment With Ezetimibe 10 mg Added to Atorvastatin 10 mg Versus Placebo Added to Atorvastatin 10 mg
NCT00359281 (11) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)
NCT00359281 (11) [back to overview]AUC0-t Rosuvastatin (Lomitapide 60 mg)
NCT00359281 (11) [back to overview]AUC0-t Atorvastatin Acid (Lomitapide 60 mg)
NCT00359281 (11) [back to overview]AUC0-t Fenofibric Acid
NCT00359281 (11) [back to overview]AUC0-t Nicotinic Acid
NCT00359281 (11) [back to overview]AUC0-t Nicotinuric Acid
NCT00359281 (11) [back to overview]AUC0-t Rosuvastatin (Lomitapide 10 mg)
NCT00359281 (11) [back to overview]AUC0-t Simvastatin
NCT00359281 (11) [back to overview]AUC0-t Simvastatin Acid
NCT00359281 (11) [back to overview]AUC0-t Total Ezetimibe
NCT00359281 (11) [back to overview]Area Under Concentration-time Curve From 0 to Last Measureable Concentration (AUC0-t) Atorvastatin Acid (Lomitapide 10 mg)
NCT00376246 (2) [back to overview]Percent Change in Flow Mediated Dilation
NCT00376246 (2) [back to overview]Lipid Profile- Change in LDL(Low Density Lipoprotein)
NCT00405067 (10) [back to overview]Percent Change in Apolipoprotein A1 (Apo A1) at 12 Weeks as Compared to Baseline
NCT00405067 (10) [back to overview]Percent Change in Apolipoprotein B (Apo B) at 12 Weeks as Compared to Baseline
NCT00405067 (10) [back to overview]Percent Change in Body Weight at 12 Weeks as Compared to Baseline
NCT00405067 (10) [back to overview]Percent Change in HDL-C at 12 Weeks Compared to Baseline
NCT00405067 (10) [back to overview]Percent Change in High-sensitivity C-reactive Protein (Hs-CRP) at 12 Weeks as Compared to Baseline
NCT00405067 (10) [back to overview]Percent Change in LDL-C at 12 Weeks Therapy Compared to Baseline Between Treatments
NCT00405067 (10) [back to overview]Percent Change in Lipoprotein(a)[Lp(a)]at 12 Weeks as Compared to Baseline
NCT00405067 (10) [back to overview]Percent Change in Tryglycerides (TGs) at 12 Weeks Compared to Baseline
NCT00405067 (10) [back to overview]Percent of Change at 12 Weeks Therapy Compared to Baseline Between Treatments for the Following Parameters: Total Cholesterol (TC)
NCT00405067 (10) [back to overview]Percent Change in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at 12 Weeks as Compared to Baseline.
NCT00409773 (15) [back to overview]Percent Change From Baseline in Low Density Lipoprotein Cholesterol: High Density Lipoprotein Cholesterol (LDL-C: HDL-C) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 6 in Patients With Atherosclerotic Vascular Disease (AVD)
NCT00409773 (15) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Low Density Lipoprotein (LDL-C) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Very Low Density Lipoprotein Cholesterol (VLDL-C) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Triglyceride (TG) (mg/dL) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 6 in Patients Without Atherosclerotic Vascular Disease (AVD)
NCT00409773 (15) [back to overview]Percent Change From Baseline in Total-Cholesterol: High Density Lipoprotein-Cholesterol (Total-C:HDL- C) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Total Cholesterol(mg/dL) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol: High Density Lipoprotein Cholesterol (Non-HDL-C:HDL-C) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in High-Sensitivity C-reactive (Hs-CRP) (mg/dL) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Apolipoprotein-B: Apolipoprotein-A1 (Apo-B:Apo-A1) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Apolipoprotein-A1 (Apo-A1) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Apolipoprotein- B (Apo-B) at Week 6
NCT00409773 (15) [back to overview]Percent Change From Baseline in Non- High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 6
NCT00413972 (1) [back to overview]Percent Change in Low-density Lipoprotein Cholesterol (LDL-C) From Baseline to Endpoint After 8 Weeks of Treatment
NCT00418834 (28) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in LDL-C at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Ratio of Highly Selective C-Reactive Protein (Hs-CRP) at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Ratio of Highly Selective C-Reactive Protein (Hs-CRP) at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Total Cholesterol (TC): High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Total Cholesterol (TC):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Triglycerides (TG) at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Triglycerides (TG) at Week 6
NCT00418834 (28) [back to overview]Number of Patients Who Achieved LDL-C <100 mg/dL for Patients Without Atherosclerotic Vascular Disease (AVD) and LDL-C <70 mg/dL for Patients With Atherosclerotic Vascular Disease (AVD) at Week 6
NCT00418834 (28) [back to overview]Number of Patients Who Achieved LDL-C<100 mg/dL for Patients Without AVD and LDL-C<70 mg/dL for Patients With AVD at Week 12
NCT00418834 (28) [back to overview]Number of Patients Who Achieved Low Density Lipoprotein Cholesterol (LDL-C) <70 mg/dL at Week 12
NCT00418834 (28) [back to overview]Number of Patients Who Achieved Low Density Lipoprotein Cholesterol (LDL-C) <70 mg/dL at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Apo Lipoprotein B (Apo B):Apo Lipoprotein A-I (Apo A-I) Ratio at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Apo Lipoprotein A-I (Apo A-I) at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Apo Lipoprotein A-I (Apo A-I) at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Apo Lipoprotein B (Apo B) at Week 12
NCT00418834 (28) [back to overview]Percent Change From Baseline in Apo Lipoprotein B (Apo B) at Week 6
NCT00418834 (28) [back to overview]Percent Change From Baseline in Apo Lipoprotein B (Apo B):Apo Lipoprotein A-I (Apo A-I) Ratio at Week 6
NCT00423488 (1) [back to overview]Percent Change in Low-Density Lipoprotein Cholesterol (LDL-C) From Baseline to Endpoint, After 6 Weeks of Treatment
NCT00423579 (1) [back to overview]Change in Low-density-lipoprotein Cholesterol (LDL-C) at 6 Weeks
NCT00442897 (2) [back to overview]Number of Participants Reaching the LDL-C (Low Density Lipoprotein-Cholesterol) Goal (< 100 mg/dl) After 6 Weeks of Treatment
NCT00442897 (2) [back to overview]Number of Participants Reaching the LDL-C Goal (< 100 mg/dl) After 12 Weeks of Treatment
NCT00461630 (5) [back to overview]Stroke
NCT00461630 (5) [back to overview]Coronary or Non-coronary Revascularisation
NCT00461630 (5) [back to overview]Major Coronary Events
NCT00461630 (5) [back to overview]Major Vascular Event
NCT00461630 (5) [back to overview]Mortality
NCT00462748 (1) [back to overview]Percentage of Patients Achieving a Target of Fasting LDL-C of <2mmol/l at Study End
NCT00474123 (10) [back to overview]Interleukin-6
NCT00474123 (10) [back to overview]Monocyte Chemoattractant Protein (MCP)-1
NCT00474123 (10) [back to overview]Oxidized Low-Density Lipoprotein Cholesterol
NCT00474123 (10) [back to overview]Platelet Function Analyzer [PFA]-100
NCT00474123 (10) [back to overview]Soluble CD40 Ligand
NCT00474123 (10) [back to overview]Soluble Intercellular Adhesion Molecule (sICAM)-1
NCT00474123 (10) [back to overview]C-reactive Protein
NCT00474123 (10) [back to overview]Endothelial Progenitor Cells
NCT00474123 (10) [back to overview]Triglyceride
NCT00474123 (10) [back to overview]LDL Cholesterol
NCT00477204 (1) [back to overview]Change in LDL-c From Baseline to 6 Months in Subjects With Type 1 Diabetes Taking Vytorin or Zocor.
NCT00479713 (10) [back to overview]Percent Change in Low Density Lipoprotein-Cholesterol (LDL-C) at Study Endpoint After Six Weeks of Treatment
NCT00479713 (10) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein-Cholesterol (Non-HDL-C)
NCT00479713 (10) [back to overview]Percent Change From Baseline in High-sensitivity C (Hs-C) Reactive Protein
NCT00479713 (10) [back to overview]Percent Change From Baseline in Triglycerides.
NCT00479713 (10) [back to overview]The Percentage of Participants Achieving Designated Low Density Lipoprotein-Cholesterol (LDL-C) Levels After 6 Weeks of Treatment
NCT00479713 (10) [back to overview]Percent Change From Baseline in Apolipoprotein B
NCT00479713 (10) [back to overview]Percent Change From Baseline in Total Cholesterol/High Density Lipoprotein-Cholesterol (HDL-C) Ratio
NCT00479713 (10) [back to overview]Percent Change From Baseline in Low Density Lipoprotein-Cholesterol (LDL-C)/High Density Lipoprotein-Cholesterol (HDL-C) Ratio
NCT00479713 (10) [back to overview]Percent Change From Baseline in High Density Lipoprotein-Cholesterol (HDL-C)
NCT00479713 (10) [back to overview]Percent Change From Baseline in Total Cholesterol
NCT00481351 (5) [back to overview]CPK
NCT00481351 (5) [back to overview]High Density Lipoprotein
NCT00481351 (5) [back to overview]Low Density Lipoprotein
NCT00481351 (5) [back to overview]Total Cholesterol
NCT00481351 (5) [back to overview]Alanine Aminotransferase
NCT00496730 (3) [back to overview]Change in Lower Density Lipoprotein Cholesterol From Baseline After 8 Weeks.
NCT00496730 (3) [back to overview]Mean Percent Change of Low Density Lipoprotein-Cholesterol (LDL-C) From Baseline After 8 Weeks.
NCT00496730 (3) [back to overview]Number of Patients Attaining LDL-C Goal After 8 Weeks Treatment.
NCT00525824 (13) [back to overview]Percent Change in Apolipoprotein A1 (ApoA-1) After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in Apolipoprotein B (ApoB) After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in ApoB/ApoA-1 After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in Triglycerides (TG) After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in Total Cholesterol (TC) After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in TC/HDL-C After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in Non-high-density Lipoprotein Cholesterol (nonHDL-C) After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in Non-HDL-C/HDL-C After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in LDL-C/HDL-C After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in LDL-C After 6 Weeks Monotherapy
NCT00525824 (13) [back to overview]Percent Change in High-sensitivity C-reactive Protein (Hs-CRP) After 6 Weeks Combination Treatment
NCT00525824 (13) [back to overview]Percent Change in High-density Lipoprotein Cholesterol (HDL-C) After 6 Weeks Combination Treatment
NCT00535405 (6) [back to overview]Percentage of Patients Who Achieved LDL-C <100 mg/dL at Week 12
NCT00535405 (6) [back to overview]Percent Change From Baseline in Low Density Lipoprotein (LDL-C) at Week 12
NCT00535405 (6) [back to overview]Percentage of Patients Who Achieved LDL-C <70 mg/dL at Week 12
NCT00535405 (6) [back to overview]Percentage of Patients Without Atherosclerosis Vascular Disease (AVD) Who Achieved LDL-C <100 mg/dL or Patients With AVD Who Achieved LDL-C <70 mg/dL at Week 12
NCT00535405 (6) [back to overview]Percentage of Patients With High Risk for CHD Who Achieved LDL-C <70 mg/dL at Week 12
NCT00535405 (6) [back to overview]Percentage of Patients With AVD Who Achieved LDL-C <70 mg/dL at Week 12
NCT00548145 (1) [back to overview]Alzheimer's Disease Assessment Scale-cognitive Component-Japanese Version(ADAS-Jcog)
NCT00559962 (1) [back to overview]Absolute Change From Baseline in Percent Hepatic Fat
NCT00587678 (11) [back to overview]Plaque Volume
NCT00587678 (11) [back to overview]Triglycerides
NCT00587678 (11) [back to overview]V02 - Maximal Oxygen Consumption
NCT00587678 (11) [back to overview]Total Cholesterol
NCT00587678 (11) [back to overview]6-minute Walk Distance
NCT00587678 (11) [back to overview]High Density Lipoprotein Cholesterol
NCT00587678 (11) [back to overview]Log Treadmill Exercise Time
NCT00587678 (11) [back to overview]Low Density Lipoprotein Cholesterol
NCT00587678 (11) [back to overview]Magnetic Resonance Angiographic Index
NCT00587678 (11) [back to overview]Perfusion Index
NCT00587678 (11) [back to overview]Phosphocreatine Recovery Time Constant - the Time it Takes for Phosphocreatine Levels to Recover to Plateau.
NCT00639158 (8) [back to overview]Mean Percent Change in Apolipoprotein AI (apoAI) From Baseline to Final Visit
NCT00639158 (8) [back to overview]Mean Percent Change in Apolipoprotein B (apoB) From Baseline to Final Visit
NCT00639158 (8) [back to overview]Mean Percent Change in Apolipoprotein CIII (apoCIII) From Baseline to Final Visit
NCT00639158 (8) [back to overview]Mean Percent Change in High-Density Lipoprotein Cholesterol (HDL-C) From Baseline to Final Visit
NCT00639158 (8) [back to overview]Mean Percent Change in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) From Baseline to Final Visit
NCT00639158 (8) [back to overview]Median Percent Change in High-Sensitivity C-Reactive Protein (hsCRP) From Baseline to Final Visit
NCT00639158 (8) [back to overview]Median Percent Change in Triglycerides From Baseline to Final Visit
NCT00639158 (8) [back to overview]Mean Percent Change in Very Low-Density Lipoprotein Cholesterol (VLDL-C) From Baseline to Final Visit
NCT00652327 (1) [back to overview]Percentage Change in Low Density Lipoprotein-Cholesterol (LDL-C) From Baseline at Study Endpoint, After 8 Weeks of Treatment
NCT00653523 (1) [back to overview]Number of Participants With Adverse Events and Adverse Reactions
NCT00654095 (1) [back to overview]Number of Participants With Adverse Events and Adverse Reactions
NCT00654628 (12) [back to overview]Mean Change From Baseline of Low Density Lipoprotein-Cholesterol (LDL-C) at Week 6
NCT00654628 (12) [back to overview]Mean Percent Change From Baseline of High Density Lipoprotein-C (HDL-C) at Week 12
NCT00654628 (12) [back to overview]Mean Percent Change From Baseline of High Density Lipoprotein-C (HDL-C) at Week 6
NCT00654628 (12) [back to overview]Mean Percent Change From Baseline of Low Density Lipoprotein-Cholesterol (LDL-C) at Week 12
NCT00654628 (12) [back to overview]Mean Percent Change From Baseline of Low Density Lipoprotein-Cholesterol (LDL-C) at Week 6
NCT00654628 (12) [back to overview]Mean Percent Change From Baseline of Total-Cholesterol (TC) at Week 12
NCT00654628 (12) [back to overview]Mean Percent Change From Baseline of Total-Cholesterol (TC) at Week 6
NCT00654628 (12) [back to overview]Mean Percent Change of Triglycerides From Baseline at Week 12
NCT00654628 (12) [back to overview]Mean Percent Change of Triglycerides From Baseline at Week 6
NCT00654628 (12) [back to overview]The Percentage of Participants Achieving Low Density Lipoprotein-C (LDL-C) Treatment Goal After 12-week Treatment.
NCT00654628 (12) [back to overview]The Percentage of Participants Achieving Low Density Lipoprotein-C (LDL-C) Treatment Goal After 6-week Treatment.
NCT00654628 (12) [back to overview]Mean Change From Baseline of Low Density Lipoprotein-Cholesterol (LDL-C) at Week 12
NCT00687076 (2) [back to overview]Effect of Intensive Lipid Modification Medication Therapy on Progression of Atherosclerosis and Restenosis of Femoral Arteries Measured Using High Resolution Magnetic Resonance Imaging (MRI) to Examine the Femoral Artery for Progression of Atherosclerosis
NCT00687076 (2) [back to overview]Change in Total Cholesterol (mg/dl) From Baseline to Month 12
NCT00701727 (7) [back to overview]Change From Baseline in Total Cholesterol, From Fasting Plasma Samples
NCT00701727 (7) [back to overview]Low-density Lipoprotein (LDL);
NCT00701727 (7) [back to overview]Cholesterol Efflux Rate (Ra Cholesterol)
NCT00701727 (7) [back to overview]de Novo Cholesterol Synthesis (DNC)
NCT00701727 (7) [back to overview]Fecal Excretion of Plasma-derived Cholesterol
NCT00701727 (7) [back to overview]High-density Lipoprotein (HDL)
NCT00701727 (7) [back to overview]Triglycerides (TG)
NCT00704535 (8) [back to overview]Safety as Measured by Number of Subjects With at Least One Adverse Event
NCT00704535 (8) [back to overview]To Evaluate the Efficacy of Ezetimibe in Lowering Serum Cholesterol Levels 28 Days After Visit 1 (Baseline)
NCT00704535 (8) [back to overview]Safety as Measured by Adverse Event Relatedness to Study Drug as Reported by the Investigator.
NCT00704535 (8) [back to overview]Safety as Measured by Severity of Adverse Events as Determined by the Investigator
NCT00704535 (8) [back to overview]Safety as Measured by Dose Adjustment Upon Incidence of an Adverse Event
NCT00704535 (8) [back to overview]Safety as Measured by Outcome of Adverse Events
NCT00704535 (8) [back to overview]Tolerability as Measured by Subject Self-assessment
NCT00704535 (8) [back to overview]Safety as Measured by Number and Type of Adverse Events.
NCT00705081 (3) [back to overview]Number of Participants Reporting Adverse Events
NCT00705081 (3) [back to overview]Intensity of Adverse Events Reported
NCT00705081 (3) [back to overview]Participants Achieving Low-density Lipoprotein-cholesterol (LDL-C) Target Levels With Co-administration Therapy
NCT00730132 (5) [back to overview]Percentage of Patients Per Group Who Reach Goal for Total Cholesterol (TC) (< 4.5 mmol/L) According to All-Russian Scientific Cardiologists Society (ARSCS) Recommendations by End of Observation
NCT00730132 (5) [back to overview]Percentage of Patients Per Group Who Reached Goal for Low Density Lipoprotein (LDL-C) (< 2.6 mmol/L) According to ARSCS Recommendations by End of Observation
NCT00730132 (5) [back to overview]Percentage of Relative Change of LDL-C Level Measured on Visit 2 Compared With the Baseline (Visit 1) in Each of the Three Therapy Groups
NCT00730132 (5) [back to overview]Percentage of Relative Change of Total Cholesterol (TC) Level Measured on Visit 2 Compared With the Baseline (Visit 1) in Each of the Three Therapy Groups
NCT00730132 (5) [back to overview]Percentage of Patients Receiving Each Variant of Modified Lipid-lowering Therapy: Statin Dose Titration, Administration of a New Statin, Administration of a Ezetimibe in Addition to a Current Statin.
NCT00762229 (2) [back to overview]Total Cholesterol
NCT00762229 (2) [back to overview]LDL Cholesterol
NCT00782184 (15) [back to overview]Percent Change From Baseline in LDL-Cholesterol/HDL-Cholesterol Ratio
NCT00782184 (15) [back to overview]Percent Change From Baseline in Low Density Lipoprotein (LDL)-C
NCT00782184 (15) [back to overview]Percent Change From Baseline in Non-HDL Cholesterol
NCT00782184 (15) [back to overview]Percent Change From Baseline in Non-HDL Cholesterol/HDL-Cholesterol Ratio
NCT00782184 (15) [back to overview]Percent Change From Baseline in Total Cholesterol
NCT00782184 (15) [back to overview]Percent Change From Baseline in Total Cholesterol/HDL-Cholesterol Ratio
NCT00782184 (15) [back to overview]Percent Change From Baseline in Triglycerides
NCT00782184 (15) [back to overview]Number of Participants Reaching LDL-C Target Goal <100 mg/dL
NCT00782184 (15) [back to overview]Percent Change From Baseline in High-Density Lipoprotein (HDL) Cholesterol
NCT00782184 (15) [back to overview]Number of Participants Reaching LDL-C Target Goal <77 mg/dL
NCT00782184 (15) [back to overview]Number of Participants Reaching LDL-C Target Goals of <70 mg/dL
NCT00782184 (15) [back to overview]Percent Change From Baseline in Apolipoprotein A-1
NCT00782184 (15) [back to overview]Percent Change From Baseline in Apolipoprotein B
NCT00782184 (15) [back to overview]Percent Change From Baseline in Apolipoprotein B/A-1 Ratio
NCT00782184 (15) [back to overview]Percent Change From Baseline in High-sensitivity C-Reactive Protein (Hs-CRP)
NCT00783263 (7) [back to overview]Number of Participants in Each Stratum Who Reached Their Target LDL-C Level
NCT00783263 (7) [back to overview]Number of Participants Who Reached the LDL-C Level of <70 mg/dl
NCT00783263 (7) [back to overview]Number of Participants Who Reached Their Target LDL-C Level
NCT00783263 (7) [back to overview]Number of Participants in Each Stratum Who Reached the LDL-C Level of <70 mg/dl
NCT00783263 (7) [back to overview]Percent Change From Baseline in Other Lipid, Lipoprotein, Apolipoprotein and High-sensitivity C-reactive Protein (Hs-CRP)Levels
NCT00783263 (7) [back to overview]Percent Change From Baseline in LDL-Cholesterol (mg/dL) After 6 Weeks of Treatment in Each Stratum
NCT00783263 (7) [back to overview]Percent Change From Baseline in LDL-Cholesterol (mg/dL) After 6 Weeks of Treatment
NCT00794677 (9) [back to overview]Percent Change of Fasting Non-high Density Lipoprotein Cholesterol From Baseline
NCT00794677 (9) [back to overview]Log (AUC of Plasma Total Cholesterol) After an Oral Bolus
NCT00794677 (9) [back to overview]Log (AUC of Plasma Triglyceride) After an Oral Bolus
NCT00794677 (9) [back to overview]Log(Fasting Plasma Levels of Diet-derived Oxysterols (7-ketocholesterol))
NCT00794677 (9) [back to overview]Log(Maximal Plasma Concentration (Cmax) of 7-ketocholesterol) After an Oral Bolus
NCT00794677 (9) [back to overview]Log[Area-under-the-plasma-concentration-curve(AUC) 0-8 Hours 7-ketocholesterol] After an Oral Bolus
NCT00794677 (9) [back to overview]Percent Change in Fasting High Density Lipoprotein Cholesterol
NCT00794677 (9) [back to overview]Percent Change of Fasting Apolipoprotein B From Baseline
NCT00794677 (9) [back to overview]Percent Change of Fasting Low Density Lipoprotein Cholesterol From Baseline
NCT00810303 (18) [back to overview]Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20
NCT00810303 (18) [back to overview]Cmax of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30
NCT00810303 (18) [back to overview]AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15
NCT00810303 (18) [back to overview]Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30
NCT00810303 (18) [back to overview]Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15
NCT00810303 (18) [back to overview]Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16
NCT00810303 (18) [back to overview]Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30
NCT00810303 (18) [back to overview]Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16
NCT00810303 (18) [back to overview]Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15
NCT00810303 (18) [back to overview]AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30
NCT00810303 (18) [back to overview]AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16
NCT00810303 (18) [back to overview]AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16
NCT00810303 (18) [back to overview]AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15
NCT00810303 (18) [back to overview]AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5
NCT00810303 (18) [back to overview]AUC0-24h of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30
NCT00810303 (18) [back to overview]AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30
NCT00810303 (18) [back to overview]Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5
NCT00810303 (18) [back to overview]AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20
NCT00817843 (1) [back to overview]Treatment Difference in (Postprandial-Fasting) FMD
NCT00819403 (2) [back to overview]Biomarkers of Inflammation
NCT00819403 (2) [back to overview]Ex Vivo Effects of Treatment With Vytorin Versus Zocor for 6 Weeks on Platelet Alpha Thrombin PAR-1 Receptor Expression
NCT00862251 (18) [back to overview]Percent Change From Baseline in Triglycerides
NCT00862251 (18) [back to overview]Percent Change From Baseline in Total Cholesterol (TC)
NCT00862251 (18) [back to overview]Percent Change From Baseline in TC/HDL-C Ratio
NCT00862251 (18) [back to overview]Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C)
NCT00862251 (18) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) After Switching to Treatment With Ezetimibe/Simvastatin vs Doubling the Dose of Statin (Simvastatin or Atorvastatin).
NCT00862251 (18) [back to overview]Percent Change From Baseline in LDL-C/HDL-C Ratio
NCT00862251 (18) [back to overview]In Participants Treated With Simvastatin at Baseline, Number of Participants Who Reached the Target LDL-Cholesterol Level of < 70 mg/dL (1.81 mmol/L)
NCT00862251 (18) [back to overview]In Participants Treated With Simvastatin at Baseline, Percent Change From Baseline in LDL-C After Switching to Treatment With Ezetimibe/Simvastatin vs Doubling the Dose of Simvastatin
NCT00862251 (18) [back to overview]In Participants Treated With Atorvastatin at Baseline, Percent Change From Baseline in LDL-C After Switching to Treatment With Ezetimibe/Simvastatin vs Doubling the Dose of Atorvastatin
NCT00862251 (18) [back to overview]Percent Change From Baseline in LDL-C After Switching to Treatment With Ezetimibe/Simvastatin vs Switching Treatment to Rosuvastatin
NCT00862251 (18) [back to overview]Percent Change From Baseline in Non-HDL-C/HDL-C Ratio
NCT00862251 (18) [back to overview]Number of Participants Who Reached the Target LDL-Cholesterol Level of < 70 mg/dL (1.81 mmol/L)
NCT00862251 (18) [back to overview]Percent Change From Baseline Apolipoprotein A-I (Apo A-I)
NCT00862251 (18) [back to overview]Percent Change From Baseline in Apo B/Apo A-I Ratio
NCT00862251 (18) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo B)
NCT00862251 (18) [back to overview]Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C)
NCT00862251 (18) [back to overview]Percent Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP)
NCT00862251 (18) [back to overview]In Participants Treated With Atorvastatin at Baseline, Number of Participants Who Reached the Target LDL-Cholesterol Level of < 70 mg/dL (1.81 mmol/L)
NCT00863265 (3) [back to overview]Percent Cholesterol Absorption
NCT00863265 (3) [back to overview]LDL Cholesterol
NCT00863265 (3) [back to overview]Cholesterol Excretion
NCT00867165 (49) [back to overview]Percentage Change From Baseline HDL-C at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline HDL-C at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline High-density Lipoprotein Cholesterol (HDL-C) at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Apolipoprotein A-I (Apo A-I) at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Apolipoprotein B (Apo B) at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Campesterol at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Campesterol at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Campesterol at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Campesterol at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Cholestanol at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Cholestanol at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Cholestanol at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Cholestanol at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP) at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP) at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Lathosterol at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Lathosterol at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in LDL-C:HDL-C Ratio at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in LDL-C:HDL-C Ratio at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline in LDL-C:HDL-C Ratio at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in LDL-C:HDL-C Ratio at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Non-HDL-C at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Non-HDL-C at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Non-HDL-C at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Non-HDL-C at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Sitosterol at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Sitosterol at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Sitosterol at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TC at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TC at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TC at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TC:HDL-C Ratio at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TC:HDL-C Ratio at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TC:HDL-C Ratio at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TC:HDL-C Ratio at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TG at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TG at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in TG at Week 8
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Total Cholesterol (TC) at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Lathosterol at Week 4
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Triglycerides (TG) at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Apo B:Apo A-I Ratio at Week 12
NCT00867165 (49) [back to overview]Percentage Change From Baseline in Lathosterol at Week 12
NCT00867165 (49) [back to overview]Percent Change From Baseline in LDL-C at Week 2
NCT00867165 (49) [back to overview]Percent Change From Baseline in LDL-C at Week 4
NCT00867165 (49) [back to overview]Percent Change From Baseline in LDL-C at Week 8
NCT00867165 (49) [back to overview]Percent Change From Baseline in Sitosterol at Week 2
NCT00867165 (49) [back to overview]Percentage Change From Baseline HDL-C at Week 2
NCT00871351 (5) [back to overview]Percent Change in Total Lipids and Hs-CRP
NCT00871351 (5) [back to overview]Percent Change in Total Lipids and High Sensitivity C-reactive Protein (Hs-CRP)
NCT00871351 (5) [back to overview]Percent Change in Low-Density Lipoprotein - Cholesterol (LDL-C) Values
NCT00871351 (5) [back to overview]Percent Change in LDL-C
NCT00871351 (5) [back to overview]Number of Participants Whose LDL-C Levels Reached the Lipid Management Target Values
NCT00879710 (1) [back to overview]Changes in LDL Cholesterol
NCT00908011 (1) [back to overview]The Primary Endpoint is the Difference in Final Value of Serum Apolipoprotein B Between Participants Treated With Rosuvastatin Versus Participants Treated With Both Rosuvastatin and Ezetimibe.
NCT00909389 (1) [back to overview]Number of Participants Who Had an Adverse Event (AE).
NCT00932620 (2) [back to overview]Changes in Low-density Lipoprotein Cholesterol (LDL-C)
NCT00932620 (2) [back to overview]Changes in Small Dense Low-density Lipoprotein Cholesterol (sdLDL-C) Levels
NCT00988364 (2) [back to overview]L5 Concentration in Metabolic Syndrome Patients
NCT00988364 (2) [back to overview]L5 Concentration After Treatment of Ezetimibe, Simvastatin, or Vytorin in Metabolic Syndrome Patients
NCT01154036 (28) [back to overview]Percentage of Participants That Reach Target LDL-C Level of < 70 mg/dL (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Apo B/Apo A-I Ratio (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Apo B/Apo A-I Ratio (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Apo B (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Apo A-I (Phase II)
NCT01154036 (28) [back to overview]Percentage of Participants That Reach Target LDL-C Level of < 70 mg/dL (Phase I)
NCT01154036 (28) [back to overview]Percentage of Participants That Reach Target LDL-C Level of < 100 mg/dL (Phase II)
NCT01154036 (28) [back to overview]Percentage of Participants That Reach Target LDL-C Level of < 100 mg/dL (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Triglycerides (TG) (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in TC/HDL-C Ratio (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Non-HDL-C/HDL-C Ratio (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Non-HDL-C/HDL-C Ratio (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Non-HDL-C (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Non-HDL-C (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C) (Phase II).
NCT01154036 (28) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C) (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in LDL-C/HDL-C Ratio (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in LDL-C/HDL-C Ratio (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Hs-CRP (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP) (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo B) (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in High-density Lipoprotein-Cholesterol (HDL-C) (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Apolipoprotein A-I (Apo A-I) (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in HDL-C (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) (Phase II)
NCT01154036 (28) [back to overview]Percent Change From Baseline in Triglycerides (TG) (Phase I)
NCT01154036 (28) [back to overview]Percent Change From Baseline in TC/HDL-C Ratio (Phase II)
NCT01218204 (45) [back to overview]Cmax of Atorvastatin- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Cmax of GSK1292263- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Maximum Observed Concentration (Cmax) of GSK1292263- Part A
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Clinical Chemistry Value of PCI- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Clinical Chemistry Value of PCI- Part B (run-in)
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Clinical Chemistry Value of PCI- Part B (Washout)
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Clinically Significant ECG Findings- Part B (Washout)
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Hematology Value of PCI- Part A
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Hematology Value of PCI- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Hematology Value of PCI- Part B (Washout)
NCT01218204 (45) [back to overview]Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs)- Part A
NCT01218204 (45) [back to overview]Number of Participants With Any AEs and SAEs- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]AUC (0-24) of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]AUC (0-24) of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part A
NCT01218204 (45) [back to overview]Area Under the Concentration-time Curve From Time Zero (Pre-dose) to 24 Hours [AUC(0-24)] of GSK1292263- Part A
NCT01218204 (45) [back to overview]Weighted Mean Area Under Concentration Curve From 0 to 24 Hours (AUC [0-24]) Change From Baseline for Triglycerides at Day 14
NCT01218204 (45) [back to overview]Tlag of GSK1292263- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Percent Change From Baseline in Lipid Metabolism: LDL/HDL Ratio at Day 14 (24 Hours)
NCT01218204 (45) [back to overview]Percent Change From Baseline in Lipid Metabolism: Apolipoprotein E at Day 14 (24 Hours)
NCT01218204 (45) [back to overview]Number of Participants With Abnormal- Clinically Significant Electrocardiogram (ECG) Findings- Part A
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Clinically Significant ECG Findings- Part B (Run-in)
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Clinically Significant ECG Findings- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Clinical Chemistry Value of PCI- Part A
NCT01218204 (45) [back to overview]Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) of GSK1292263- Part A
NCT01218204 (45) [back to overview]Number of Participants With Any AEs and SAEs- Part B (Washout)
NCT01218204 (45) [back to overview]Number of Participants With Any AEs and SAEs- Part B (Run-in)
NCT01218204 (45) [back to overview]Time of Occurrence of Cmax (Tmax) and Terminal Phase Half-life (t1/2) GSK1292263- Part A
NCT01218204 (45) [back to overview]Number of Participants With Vital Signs of PCI- Part B (Washout)
NCT01218204 (45) [back to overview]Number of Participants With Vital Signs of Potential Clinical Importance (PCI)- Part A
NCT01218204 (45) [back to overview]Number of Participants With Vital Signs of Potential Clinical Importance- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Number of Participants With Vital Signs of Potential Clinical Importance- Part B (Run-in)
NCT01218204 (45) [back to overview]Percent Change From Baseline for Lipid Metabolism: Apolipoprotein A1 and Apolipoprotein B100 at Day 14
NCT01218204 (45) [back to overview]Percent Change From Baseline in Lipid Metabolism: High Density Lipids Cholesterol (HDLc), Low Density Lipids Cholesterol (LDLc), Tryglycerides, Non-HDLc and Total Cholesterol at Day 14 (24 Hours)
NCT01218204 (45) [back to overview]Tmax and t1/2 of GSK1292263- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Tmax of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part A
NCT01218204 (45) [back to overview]Tmax of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Tmax of Atorvastatin- Part A
NCT01218204 (45) [back to overview]Tmax of Atorvastatin- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Cmax of Atorvastatin- Part A
NCT01218204 (45) [back to overview]Cmax of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]Cmax of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part A
NCT01218204 (45) [back to overview]AUC(0-24) of GSK1292263- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]AUC (0-24) of Atorvastatin- Part B (Pooled Treatment Arm)
NCT01218204 (45) [back to overview]AUC (0-24) of Atorvastatin- Part A
NCT01218204 (45) [back to overview]Number of Participants With Abnormal Hematology Value of PCI- Part B (Run-in)
NCT01370590 (6) [back to overview]Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) After 6 Weeks of Treatment
NCT01370590 (6) [back to overview]Percent Change From Baseline in Triglycerides (TG) After 6 Weeks of Treatment
NCT01370590 (6) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) After 6 Weeks of Treatment
NCT01370590 (6) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) After 6 Weeks of Treatment
NCT01370590 (6) [back to overview]Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) After 6 Weeks of Treatment
NCT01370590 (6) [back to overview]Percent Change From Baseline in Apolipoprotein (Apo) B After 6 Weeks of Treatment
NCT01370603 (6) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) After 6 Weeks of Treatment
NCT01370603 (6) [back to overview]Percent Change From Baseline in Triglycerides (TG) After 6 Weeks of Treatment
NCT01370603 (6) [back to overview]Percent Change From Baseline in Apolipoprotein (Apo) B After 6 Weeks of Treatment
NCT01370603 (6) [back to overview]Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) After 6 Weeks of Treatment
NCT01370603 (6) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) After 6 Weeks of Treatment
NCT01370603 (6) [back to overview]Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) After 6 Weeks of Treatment
NCT01375764 (12) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12
NCT01375764 (12) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe
NCT01375764 (12) [back to overview]Percent Change From Baseline in LDL-C at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe
NCT01375764 (12) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT01375764 (12) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12
NCT01375764 (12) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe
NCT01375764 (12) [back to overview]Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at Week 12
NCT01375764 (12) [back to overview]Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe
NCT01375764 (12) [back to overview]Change From Baseline in LDL-C at Week 12
NCT01375764 (12) [back to overview]Change From Baseline in LDL-C at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe
NCT01375764 (12) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 12
NCT01375764 (12) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe
NCT01375777 (6) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT01375777 (6) [back to overview]Percent Change From Baseline in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) at Week 12
NCT01375777 (6) [back to overview]Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at Week 12
NCT01375777 (6) [back to overview]Change From Baseline in LDL-C at Week 12
NCT01375777 (6) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 12
NCT01375777 (6) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A-1 Ratio at Week 12
NCT01381679 (9) [back to overview]Number of Participants Achieving Individual LDL Cholesterol (LDL-C) Target Level
NCT01381679 (9) [back to overview]Change From Baseline in Total Cholesterol (TC) at Month 3
NCT01381679 (9) [back to overview]Change From Baseline in TC at Month 12
NCT01381679 (9) [back to overview]Change From Baseline in LDL-C at Month 3
NCT01381679 (9) [back to overview]Change From Baseline in HDL-C at Month 12
NCT01381679 (9) [back to overview]Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at Month 3
NCT01381679 (9) [back to overview]Change From Baseline in LDL-C at Month 12
NCT01381679 (9) [back to overview]Change From Baseline in Triglycerides (TG) at Month 3
NCT01381679 (9) [back to overview]Change From Baseline in TG at Month 12
NCT01420549 (1) [back to overview]Reduction of LDL Cholesterol Levels
NCT01516879 (15) [back to overview]Percent Change From Baseline in Triglycerides at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in Very Low-density Lipoprotein Cholesterol (VLDL-C) at Week 52
NCT01516879 (15) [back to overview]Percent Change From Week 12 to Week 52 in LDL-C
NCT01516879 (15) [back to overview]Percentage of Participants With an LDL-C Response at Week 52
NCT01516879 (15) [back to overview]Change From Baseline in LDL-C at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in LDL-C at Week 12
NCT01516879 (15) [back to overview]Percent Change From Baseline in LDL-C at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in Total Cholesterol at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at Week 52
NCT01516879 (15) [back to overview]Percent Change From Baseline in Total Cholesterol at Week 12
NCT01611883 (10) [back to overview]Percent Change in Low-density Lipoprotein Cholesterol (LDL-C) From Baseline
NCT01611883 (10) [back to overview]Percent Change in High-density Lipoprotein Cholesterol (HDL-C) From Baseline
NCT01611883 (10) [back to overview]"Percentage of Participants With Adverse Event (AE) Exacerbation of Diabetes"
NCT01611883 (10) [back to overview]Change in Glycoalbumin From Baseline
NCT01611883 (10) [back to overview]Change in Glycated Hemoglobin (HbA1c) From Baseline
NCT01611883 (10) [back to overview]Change in Fasting Plasma Glucose (FPG) From Baseline
NCT01611883 (10) [back to overview]Percentage of Participants With Changes in Diabetes Medications Due to Worsening of Diabetes
NCT01611883 (10) [back to overview]Percent Change in Triglycerides From Baseline
NCT01611883 (10) [back to overview]Percent Change in Total Cholesterol (TC) From Baseline
NCT01611883 (10) [back to overview]Percent Change in Non-HDL-cholesterol From Baseline
NCT01644188 (26) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12 - On-Treatment Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent-to-treat (ITT) Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 52 - On-Treatment Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 12 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Apolipoprotein A-1 (Apo A-1) at Week 24 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in HDL-C at Week 12 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 12 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 24 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 104 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 24 - On-Treatment Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Calculated LDL--C at Week 24 - On--Treatment Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo-B) at Week 24 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 52 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Apo-B at Week 12 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Apo B at Week 24 - On-Treatment Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Apo A-1 at Week 12 - ITT Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 104 - On-Treatment Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Total-C at Week 12 - ITT Analysis
NCT01644188 (26) [back to overview]Percentage of Participants Achieving Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis
NCT01644188 (26) [back to overview]Percentage of Participants Achieving Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - On-Treatment Analysis
NCT01644188 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Lipoprotein (a) at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Total-C at Week 12 - ITT Analysis
NCT01644474 (18) [back to overview]Percentage of Participants Achieving Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 12 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent-to-Treat (ITT) Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Apolipoprotein A-1 (Apo A-1) at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Lipoprotein (a) at Week 12 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Apo B at Week 12 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percentage of Participants Achieving Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in HDL-C at Week 12 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis
NCT01644474 (18) [back to overview]Percent Change From Baseline in Apo A-1 at Week 12 - ITT Analysis
NCT01709513 (26) [back to overview]Percentage of Participants Who Experienced Skeletal Muscle-related Adverse Event (AE)
NCT01709513 (26) [back to overview]Percent Change From Baseline in Apo A--1 at Week 12 -- ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Apo A-1 at Week 24 - ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Apo B at Week 12 -- ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Apo B at Week 24 -- On--Treatment Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Apolipoprotein (Apo) B at Week 24 -- ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Calculated LDL--C at Week 12 -- ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12 - On--Treatment Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent--To-Treat (ITT) Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 - On--Treatment Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 Versus Atorvastatin - Raw Data Description - Intent-To-Treat (ITT) Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 12 -- ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 24 - ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Non--HDL-C at Week 24 -- On--Treatment Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Non--High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 -- ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Total Cholesterol (Total--C) at Week 24 - ITT Analysis
NCT01709513 (26) [back to overview]Percent Change From Baseline in Total-C at Week 12 - ITT Analysis
NCT01709513 (26) [back to overview]Percent Change in Fasting Triglycerides From Baseline to Week 12 -- ITT Analysis
NCT01709513 (26) [back to overview]Percent Change in HDL-C From Baseline to Week 12 -- ITT Analysis
NCT01709513 (26) [back to overview]Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis
NCT01709513 (26) [back to overview]Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - On-Treatment Analysis
NCT01709513 (26) [back to overview]Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or Moderate or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - ITT Analysis
NCT01709513 (26) [back to overview]Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or Moderate or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - On-Treatment Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 24 - On-Treatment Analysis
NCT01730040 (24) [back to overview]Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - ITT Analysis
NCT01730040 (24) [back to overview]Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - On-Treatment Analysis
NCT01730040 (24) [back to overview]Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Total-C at Week 12 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Non-High-density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 24 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 12 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in HDL-C at Week 12 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis
NCT01730040 (24) [back to overview]Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - On-Treatment Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Apolipoprotein (Apo) B at Week 24 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Apo B at Week 24 - On-Treatment Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Apo B at Week 12 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 12 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 - On-Treatment Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent-to-treat (ITT) Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12 - On-Treatment Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Apo A-1 at Week 12 - ITT Analysis
NCT01730040 (24) [back to overview]Percent Change From Baseline in Apo A-1 at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - On-Treatment Analysis
NCT01730053 (24) [back to overview]Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12 - On-Treatment Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent-to-Treat (ITT) Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Total-C at Week 12 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Non-High-density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 24 - On-Treatment Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 24 - On-Treatment Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Apolipoprotein (Apo) B at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 12 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in HDL-C at Week 12 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Lipoprotein (a) at Week 12 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Apo A-1 at Week 12 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Apo A-1 at Week 24 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Apo B at Week 12 - ITT Analysis
NCT01730053 (24) [back to overview]Percent Change From Baseline in Apo B at Week 24 - On-Treatment Analysis
NCT01730053 (24) [back to overview]Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - On-Treatment Analysis
NCT01763827 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in HDL-C at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Percentage of Participants Who Achieved a Mean LDL-C at Weeks 10 and 12 of Less Than 70 mg/dL
NCT01763827 (22) [back to overview]Percent Change From Baseline in Very Low Density Lipoprotein Cholesterol (VLDL-C) at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Lipoprotein (a) at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Total Cholesterol/High Density Lipoprotein-cholesterol Ratio at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Total Cholesterol/High Density Lipoprotein-cholesterol Ratio at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Triglycerides at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Triglycerides at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Percentage of Participants Who Achieved LDL-C < 70 mg/dL at Week 12
NCT01763827 (22) [back to overview]Change From Baseline in LDL-C at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Change From Baseline in LDL-C at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in VLDL-C at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in Lipoprotein (a) at the Mean of Weeks 10 and 12
NCT01763827 (22) [back to overview]Percent Change From Baseline in LDL-C at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in HDL-C at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Triglycerides at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Triglycerides at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Very Low-Density Cholesterol (VLDL-C) at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Very Low-Density Cholesterol (VLDL-C) at Week 12
NCT01763866 (22) [back to overview]Percentage of Participants Who Achieved LDL-C < 70 mg/dL at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in HDL-C at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Change From Baseline in LDL-C at Week 12
NCT01763866 (22) [back to overview]Change From Baseline in LDL-C at at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percentage of Participants Who Achieved a Mean LDL-C at Weeks 10 and 12 of Less Than 70 mg/dL
NCT01763866 (22) [back to overview]Percent Change From Baseline in LDL-C at the Mean of Weeks 10 and 12
NCT01763866 (22) [back to overview]Percent Change From Baseline in Lipoprotein(a) at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percentage of Participants With Mean LDL-C at Weeks 10 and 12 of Less Than 70 mg/dL (1.8 mmol/L)
NCT01763905 (22) [back to overview]Percent Change From Baseline in Lipoprotein (a) at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Non-HDL-C at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in the Total Cholesterol/High Density Lipoprotein Cholesterol Ratio at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in LDL-C at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in the Total Cholesterol/High Density Lipoprotein Cholesterol Ratio at Week 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Triglycerides at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in LDL-C at Week 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) at Week 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Lipoprotein (a) at Week 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Very Low-Density Lipoprotein Cholesterol at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Change From Baseline in LDL-C at Week 12
NCT01763905 (22) [back to overview]Change From Baseline in LDL-C at the Mean of Weeks 10 and 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Very Low-Density Lipoprotein Cholesterol at Week 12
NCT01763905 (22) [back to overview]Percentage of Participants With LDL-C < 70 mg/dL (1.8 mmol/L) at Week 12
NCT01763905 (22) [back to overview]Percent Change From Baseline in Triglycerides at Week 12
NCT01766713 (1) [back to overview]Change in Liver Fat as Measured by MRI-PDFF
NCT01849068 (2) [back to overview]Change in Intestinal mRNA Expression Levels of LDL Receptor Between the Two 12-week Interventions
NCT01849068 (2) [back to overview]Change in Intestinal mRNA Expression Levels of SREBP-2, NPC1L1, ABCG5/8, PCSK9 and HMG CoA Reductase Between the Two 12-week Interventions
NCT01890967 (10) [back to overview]Percentage Change From Baseline in Free Proprotein Convertase Subtilisin/Kexin Type 9 Antibody (PCSK9) Levels
NCT01890967 (10) [back to overview]Change From Baseline in High Sensitivity C-Reactive Protein (hsCRP)
NCT01890967 (10) [back to overview]Number of Participants Who Develop Treatment Emergent Anti-LY3015014 Antibodies
NCT01890967 (10) [back to overview]Number of Participants With an Injection Site Reaction
NCT01890967 (10) [back to overview]Percentage Change From Baseline in Lipoprotein(a) [Lp(a)]
NCT01890967 (10) [back to overview]Percentage Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C)
NCT01890967 (10) [back to overview]Percentage Change From Baseline in Total Proprotein Convertase Subtilisin/Kexin Type 9 Antibody (PCSK9) Levels
NCT01890967 (10) [back to overview]Percentage Change From Baseline in Apolipoprotein A1 (Apo A1), Apolipoprotein B (Apo B)
NCT01890967 (10) [back to overview]Percentage Change From Baseline in LDL-C, Total Cholesterol (TC), High-Density Lipoprotein Cholesterol (HDL-C), Triglycerides (TG), Non-HDL-C
NCT01890967 (10) [back to overview]Pharmacokinetics (PK): Area Under the Concentration-Time Curve at Steady-State (AUC,ss) for LY3015014
NCT01984424 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in HDL-C at Week 24
NCT01984424 (24) [back to overview]Change From Baseline in LDL-C at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Change From Baseline in LDL-C at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in LDL-C at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in LDL-C at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Lipoprotein(a) at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Total Cholesterol at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Total Cholesterol at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Triglycerides at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Triglycerides at Week 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in Very Low-density Lipoprotein Cholesterol (VLDL-C) at the Mean of Weeks 22 and 24
NCT01984424 (24) [back to overview]Percent Change From Baseline in VLDL-C at Week 24
NCT01984424 (24) [back to overview]Percentage of Participants Who Achieved a Mean LDL-C at Weeks 22 and 24 of Less Than 70 mg/dL
NCT01984424 (24) [back to overview]Percentage of Participants Who Achieved LDL-C at Week 24 of Less Than 70 mg/dL
NCT02055976 (48) [back to overview]Change From Baseline in Very Low Density Lipoprotein-Cholesterol (VLDL-C) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Triglyceride (TG) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Total Cholesterol (TC) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Total Cholesterol (TC) / High Density Lipoprotein- Cholesterol (HDL-C) Ratio at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Non-High Density Lipoprotein- Cholesterol (Non-HDL-C) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Low Density Lipoprotein-Cholesterol (LDL-C) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Lipoprotein (a) (Lp[a]) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in High Density Lipoprotein- Cholesterol (HDL-C) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Apolipoprotein B (ApoB) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Apolipoprotein B (ApoB) / Apolipoprotein A-I (ApoA-I) Ratio at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Apolipoprotein A-II (ApoA-II) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Change From Baseline in Apolipoprotein A-I (ApoA-I) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of PF-04950615
NCT02055976 (48) [back to overview]Apolipoprotein B (ApoB) / Apolipoprotein A-I (ApoA-I) Ratio
NCT02055976 (48) [back to overview]Apolipoprotein B (ApoB)
NCT02055976 (48) [back to overview]Apolipoprotein A-II (ApoA-II)
NCT02055976 (48) [back to overview]Apolipoprotein A-I (ApoA-I)
NCT02055976 (48) [back to overview]Percent Change From Baseline in Fasting Low Density Lipoprotein-Cholesterol (LDL-C) at Day 85
NCT02055976 (48) [back to overview]Percent Change From Baseline in Fasting Low Density Lipoprotein-Cholesterol (LDL-C) at Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Apolipoprotein A-I (ApoA-I) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Very Low Density Lipoprotein-Cholesterol (VLDL-C) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Triglyceride (TG) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Total Cholesterol (TC) / High Density Lipoprotein- Cholesterol (HDL-C) Ratio at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein- Cholesterol (Non-HDL-C) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Lipoprotein (a) (Lp[a]) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in High Density Lipoprotein- Cholesterol (HDL-C) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Apolipoprotein B (ApoB) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Percent Change From Baseline in Apolipoprotein B (ApoB) / Apolipoprotein A-I (ApoA-I) Ratio at Day 85 and Day 113
NCT02055976 (48) [back to overview]Terminal Elimination Half-Life (t1/2) of PF-04950615
NCT02055976 (48) [back to overview]Percent Change From Baseline in Apolipoprotein A-II (ApoA-II) at Day 85 and Day 113
NCT02055976 (48) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) or Serious Adverse Events (SAEs)
NCT02055976 (48) [back to overview]Non-High Density Lipoprotein- Cholesterol (Non-HDL-C)
NCT02055976 (48) [back to overview]Maximum Observed Plasma Concentration (Cmax) of PF-04950615
NCT02055976 (48) [back to overview]Low Density Lipoprotein-Cholesterol (LDL-C)
NCT02055976 (48) [back to overview]Lipoprotein (a) (Lp[a])
NCT02055976 (48) [back to overview]Number of Participants With Anti-Drug Antibody (ADA) Response
NCT02055976 (48) [back to overview]Minimum Observed Plasma Trough Concentration (Cmin) of PF-04950615
NCT02055976 (48) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-04950615
NCT02055976 (48) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of PF-04950615
NCT02055976 (48) [back to overview]High Density Lipoprotein- Cholesterol (HDL-C)
NCT02055976 (48) [back to overview]Very Low Density Lipoprotein-Cholesterol (VLDL-C)
NCT02055976 (48) [back to overview]Triglyceride (TG)
NCT02055976 (48) [back to overview]Total Cholesterol (TC) / High Density Lipoprotein- Cholesterol (HDL-C) Ratio
NCT02055976 (48) [back to overview]Total Cholesterol (TC)
NCT02055976 (48) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-04950615
NCT02055976 (48) [back to overview]Plasma Concentration of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9)
NCT02055976 (48) [back to overview]Percentage of Participants Achieving Low-density Lipoprotein Cholesterol (LDL-C) Less Than (<) 10, 25, 40, 70 and 100 Milligram Per Deciliter
NCT02227784 (7) [back to overview]Percent Change From Baseline to 3 Months in Apolipoprotein AI (apoAI)
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
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 Apolipoprotein A-I
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 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 Lipoprotein-a
NCT02260648 (7) [back to overview]Percent Change From Baseline to Week 12 in Low-Density Lipoprotein Cholesterol (LDL-C) Measured by Beta Quantification
NCT02304926 (20) [back to overview]Triglycerides Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Apolipoprotein B Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]High-density Lipoprotein Cholesterol (HDLc) Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Leukocyte Adhesion Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Leukocyte Rolling Flux Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Leukocyte Rolling Velocity Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Levels of E-selectin Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Levels of Glutathione (GSH) Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Levels of High-sensitive C-reactive Protein (hsCRP) Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Levels of Intercellular Adhesion Molecule 1 (ICAM-1) Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Levels of Interleukin-6 (IL-6) Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Levels of Tumor Necrosis Factor α (TNF-α) Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Levels of Vascular Cell Adhesion Molecule 1 (VCAM-1) Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Low Density Lipoprotein Size Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Low-density Lipoprotein Cholesterol (LDLc) Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Membrane Potential Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Mitochondrial Oxygen (O2) Consumption Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Non-HDL Cholesterol Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Reactive Oxygen Species (ROS) Production Before and After Simvastatin/Ezetimibe Administration
NCT02304926 (20) [back to overview]Total Cholesterol Before and After Simvastatin/Ezetimibe Administration
NCT02476006 (11) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Week 12
NCT02476006 (11) [back to overview]Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT02476006 (11) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol at Week 12
NCT02476006 (11) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 12
NCT02476006 (11) [back to overview]Percent Change From Baseline in Triglycerides at Week 12
NCT02476006 (11) [back to overview]Percentage of Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 12
NCT02476006 (11) [back to overview]Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) and/or >=50% Reduction From Baseline in LDL-C at Week 12
NCT02476006 (11) [back to overview]Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 12
NCT02476006 (11) [back to overview]Assessment of Participant's Acceptability of Self-Injection Using Self Injection Assessment Questionnaire (SIAQ): Feeling About Injections, Self Confidence, Satisfaction With Self-Injections
NCT02476006 (11) [back to overview]Assessment of Participant's Acceptability of Self-Injection Using Self Injection Assessment Questionnaire (SIAQ): Self Image, Injection-Site Reactions, Ease of Use
NCT02476006 (11) [back to overview]Percentage of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in Aspartate Aminotransferase (AST) ≥3 Times ULN
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in ALT and/or AST ≥3 Times ULN
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in ALT ≥5 Times ULN
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in ALT ≥10 Times ULN
NCT02550288 (18) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience 1 or More Allergic Reaction or Rash AEs
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) ≥3 Times Upper Limit of Normal (ULN)
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience 1 or More Hepatitis-related AEs
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience 1 or More Gastrointestinal-related Adverse Events (AEs)
NCT02550288 (18) [back to overview]Percentage of Participants With Potential Hy's Law Condition
NCT02550288 (18) [back to overview]Percentage of Participants Who Have Elevations in Creatine Kinase (CK) ≥10xULN
NCT02550288 (18) [back to overview]Percentage of Participants Who Have Elevations in CK ≥10xULN With Muscle Symptoms
NCT02550288 (18) [back to overview]Percentage of Participants Who Have Elevations in CK ≥10xULN and Drug-Related Muscle Symptoms
NCT02550288 (18) [back to overview]Percentage of Participants Who Have Consecutive Elevations in ALT and/or AST ≥5 Times ULN
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience 1 or More Gallbladder-related AEs
NCT02550288 (18) [back to overview]Percentage of Participants Who Have Consecutive Elevations in ALT and/or AST ≥10 Times ULN
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in AST ≥5 Times ULN
NCT02550288 (18) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in AST ≥10 Times ULN
NCT02634580 (24) [back to overview]Percent Change From Baseline in Triglycerides at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percentage of Participants Who Achieved a Mean LDL-C at Weeks 10 and 12 of Less Than 70 mg/dL
NCT02634580 (24) [back to overview]Percentage of Participants Who Achieved a LDL-C of Less Than 70 mg/dL at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in VLDL-C at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in VLDL-C at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Change From Baseline in LDL-C at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Total Cholesterol at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Triglycerides at Week 12
NCT02634580 (24) [back to overview]Change From Baseline in LDL-C at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A-1 Ratio at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A-1 Ratio at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in HDL-C at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in HDL-C at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Lipoprotein(a) at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Total Cholesterol at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Non-HDL-C at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at the Mean of Weeks 10 and 12
NCT02634580 (24) [back to overview]Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at Week 12
NCT02642159 (23) [back to overview]Percent Change From Baseline in Total-C at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in LDL-C Particle Number at Week 24: Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 24 : Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in Apo B at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in Measured LDL-C at Week 12: Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in Measured LDL-C at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in Measured Low-Density Lipoprotein Cholesterol (LDL-C) at Week 24: Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 12: Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in Non-HDL-C at Week 24: Overall Intent-to-treat (ITT) Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 : Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo-B) at Week 24: Overall ITT Analysis
NCT02642159 (23) [back to overview]Absolute Change From Baseline in Fasting Plasma Glucose (FPG) at Week 12 and 24 : Overall ITT Analysis
NCT02642159 (23) [back to overview]Absolute Change From Baseline in Hemoglobin A1c (HbA1c) at Week 12 and 24 : Overall ITT Analysis
NCT02642159 (23) [back to overview]Absolute Change From Baseline in Number of Glucose-Lowering Treatments at Week 12 and 24 : Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 24: Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in HDL-C at Week 24 : Overall ITT Analysis
NCT02642159 (23) [back to overview]Percent Change From Baseline in HDL-C at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in LDL-C Particle Number at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02642159 (23) [back to overview]Percent Change From Baseline in Measured LDL-C at Week 12: ITT- Intent to Prescribe Fenofibrate Stratum
NCT02715726 (22) [back to overview]Percent Change From Baseline in Fasting Triglycerides (TG) at Week 24: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 12: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol at Week 12: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol at Week 24: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Lipoprotein (a) (Lp[a]) at Week 24: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Lipoprotein (a) at Week 12: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol at Week 12: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol at Week 24: On-Treatment Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Total Cholesterol at Week 12: ITT Analysis
NCT02715726 (22) [back to overview]Percentage of Participants Reaching Calculated Low Density Lipoprotein Cholesterol <70 mg/dL (1.81 mmol/L) at Week 24: ITT Analysis
NCT02715726 (22) [back to overview]Percentage of Participants Reaching Calculated Low Density Lipoprotein Cholesterol <70 mg/dL (1.81 mmol/L) at Week 24: On-Treatment Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol at Week 24: On-Treatment Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Apolipoprotein A-1 (Apo A-1) at Week 24: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Apolipoprotein A-1 at Week 12 : ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 24: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 12: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 24: On-Treatment Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol at Week 12: ITT Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol at Week 12: On-Treatment Analysis
NCT02715726 (22) [back to overview]Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol at Week 24: Intent-to-treat (ITT) Analysis
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) and/or Aspartate Aminotransferase (AST) ≥10 Times Upper Normal Limit (ULN)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Elevation in Alanine Aminotransferase (ALT) ≥5 Times Upper Normal Limit (ULN)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Elevation in Alanine Aminotransferase (ALT) ≥10 Times Upper Normal Limit (ULN)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in Aspartate Aminotransferase (AST) ≥3 Times Upper Normal Limit (ULN)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) and/or Aspartate Aminotransferase (AST) ≥3 Times Upper Normal Limit (ULN)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience 1 or More Hepatitis-related AEs
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) ≥3 Times Upper Normal Limit (ULN)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience 1 or More Gastrointestinal-related AEs
NCT02741245 (19) [back to overview]Percentage Change From Baseline in Low-density Lipoprotein-cholesterol (LDL-C)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience 1 or More Allergic Reaction or Rash AEs
NCT02741245 (19) [back to overview]Percentage of Participants With Potential Hy's Law Condition
NCT02741245 (19) [back to overview]Percentage of Participants Who Had Study Drug Discontinued Due to Adverse Event
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Elevations in Creatine Kinase (CK) ≥10 Times ULN and Drug-Related Muscle Symptoms
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Elevations in Creatine Kinase (CK) ≥10 Times ULN
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience 1 or More Gallbladder-related AEs
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Elevation in Aspartate Aminotransferase (AST) ≥10 Times Upper Normal Limit (ULN)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Elevation in Aspartate Aminotransferase (AST) ≥5 Times Upper Normal Limit (ULN)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience at Least 1 Adverse Event (AE)
NCT02741245 (19) [back to overview]Percentage of Participants Who Experience Elevations in Creatine Kinase (CK) ≥10 Times ULN With Muscle Symptoms
NCT02748057 (3) [back to overview]Percentage of Participants Who Had Study Drug Discontinued Due to an AE
NCT02748057 (3) [back to overview]Percentage Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C)
NCT02748057 (3) [back to overview]Percentage of Participants Who Experience at Least 1 Adverse Event (AE)
NCT02890992 (20) [back to overview]Percent Change From Baseline in Fasting Triglyceride at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in Total Cholesterol (Total-C) at Week 8
NCT02890992 (20) [back to overview]Percent Change From Baseline in Apolipoprotein (Apo) B at Week 8
NCT02890992 (20) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Week 8
NCT02890992 (20) [back to overview]Percent Change From Baseline in Apolipoprotein A-1 at Week 8
NCT02890992 (20) [back to overview]Percentage of Participants Achieving Calculated Low Density Lipoprotein Cholesterol (LDL-C) <130 mg/dL (3.37 mmol/L) at Week 8
NCT02890992 (20) [back to overview]Percent Change From Baseline in Calculated LDL-C at Week 12: Cohort 4
NCT02890992 (20) [back to overview]Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol (LDL-C) at Week 8
NCT02890992 (20) [back to overview]Percentage of Participants Achieving Calculated LDL-C <110 mg/dL (2.84 mmol/L) at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in Apolipoprotein A-1 at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in Apolipoprotein B at Week 8
NCT02890992 (20) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in Fasting Triglyceride at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in HDL-C at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in Lipoprotein(a) at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in Calculated Low Density Lipoprotein Cholesterol (LDL-C) at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in Ratio Apolipoprotein B/Apolipoprotein A-1 at Week 8
NCT02890992 (20) [back to overview]Percent Change From Baseline in Lipoprotein(a) at Week 8
NCT02890992 (20) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein (HDL-C) at Week 8
NCT02890992 (20) [back to overview]Absolute Change From Baseline in Non-High-Density Lipoprotein (Non-HDL-C) at Week 8
NCT02971033 (3) [back to overview]Change in Alanine Aminotransferase (ALT)
NCT02971033 (3) [back to overview]Change in Viral Load
NCT02971033 (3) [back to overview]Second Phase Slope
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Non-High-density Lipoprotein Cholesterol (Non-HDL-C) at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Lumen Volume at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Lipoprotein (a) (Lp[a]) at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in High-density Lipoprotein Cholesterol at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Fasting Triglycerides (TGs) at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in External Elastic Membrane (EEM) Volume at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Apolipoprotein B (Apo B) at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Apolipoprotein A-1 (Apo A-1) at Week 36
NCT02984982 (24) [back to overview]Number of Participants With Cardiovascular (CV) Adverse Events
NCT02984982 (24) [back to overview]Percent Change From Baseline in Normalized Total Atheroma Volume (TAV) at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in Calculated Low-density Lipoprotein Cholesterol at Week 12 and Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Calculated Low-density Lipoprotein Cholesterol at Week 12 and Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in Total Cholesterol at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in Non-High-density Lipoprotein Cholesterol at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in Lumen Volume at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in Lipoprotein (a) at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in High-density Lipoprotein Cholesterol at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in Fasting Triglycerides at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in External Elastic Membrane Volume at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in Apolipoprotein B at Week 36
NCT02984982 (24) [back to overview]Percent Change From Baseline in Apolipoprotein A-1 at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Total Cholesterol (TC) at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Percent Atheroma Volume (PAV) at Week 36
NCT02984982 (24) [back to overview]Absolute Change From Baseline in Normalized Total Atheroma Volume at Week 36
NCT03001076 (14) [back to overview]Percent Change From Baseline to Weeks 4 and 8 in TGs
NCT03001076 (14) [back to overview]Percent Change From Baseline to Weeks 4 and 8 in Non-HDL-C
NCT03001076 (14) [back to overview]Percent Change From Baseline to Weeks 4 and 8 in TC
NCT03001076 (14) [back to overview]Percent Change From Baseline to Week 12 in Low-Density Lipoprotein Cholesterol (LDL-C)
NCT03001076 (14) [back to overview]Percent Change From Baseline to Week 12 in Non-high-density Lipoprotein Cholesterol (Non-HDL-C)
NCT03001076 (14) [back to overview]Percent Change From Baseline to Week 12 in Total Cholesterol (TC)
NCT03001076 (14) [back to overview]Percent Change From Baseline to Week 12 in Triglycerides (TGs)
NCT03001076 (14) [back to overview]Absolute Change From Baseline to Weeks 4, 8, and 12 in LDL-C
NCT03001076 (14) [back to overview]Number of Participants With Treatment-emergent Adverse Events (TEAEs)
NCT03001076 (14) [back to overview]Percent Change From Baseline to Weeks 4 and 8 in HDL-C
NCT03001076 (14) [back to overview]Percent Change From Baseline to Weeks 4 and 8 in LDL-C
NCT03001076 (14) [back to overview]Percent Change From Baseline to Week 12 in High-sensitivity C-reactive Protein (hsCRP)
NCT03001076 (14) [back to overview]Percent Change From Baseline to Week 12 in High-density Lipoprotein Cholesterol (HDL-C)
NCT03001076 (14) [back to overview]Percent Change From Baseline to Week 12 in Apolipoprotein B (apoB)
NCT03051100 (5) [back to overview]Percent Change From Baseline in Lipid Profile Parameters at Week 6
NCT03051100 (5) [back to overview]Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 6
NCT03051100 (5) [back to overview]Percent Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP) at Week 6
NCT03051100 (5) [back to overview]Number of Participants With LDL-C Reduction ≥50% From Baseline at Week 6
NCT03051100 (5) [back to overview]Number of Participants With LDL-C <70 mg/dL at Week 6
NCT03337308 (7) [back to overview]Percent Change From Baseline to Week 12 in High-density Lipoprotein Cholesterol (HDL-C)
NCT03337308 (7) [back to overview]Percent Change From Baseline to Week 12 in Apolipoprotein B (Apo B)
NCT03337308 (7) [back to overview]Percent Change From Baseline to Week 12 in High-sensitivity C-reactive Protein (hsCRP)
NCT03337308 (7) [back to overview]Percent Change From Baseline to Week 12 in Low-density Lipoprotein Cholesterol (LDL-C)
NCT03337308 (7) [back to overview]Percent Change From Baseline to Week 12 in Triglycerides (TGs)
NCT03337308 (7) [back to overview]Percent Change From Baseline to Week 12 in Total Cholesterol (TC)
NCT03337308 (7) [back to overview]Percent Change From Baseline to Week 12 in Non-high-density Lipoprotein Cholesterol (Non-HDL-C)
NCT03510715 (13) [back to overview]Percent Change From Baseline in Apolipoprotein (Apo) B at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Percent Change From Baseline in Fasting Triglycerides (TG) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein Cholesterol at Week 12: On-treatment Analysis
NCT03510715 (13) [back to overview]Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Percent Change From Baseline in Lipoprotein a (Lp) (a) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein Cholesterol at Weeks 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Absolute Change From Baseline in LDL-C Level at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Number of Participants With Tanner Staging at Baseline, Weeks 12, 24 and 48
NCT03510715 (13) [back to overview]Percent Change From Baseline in Apolipoprotein A1 (Apo A1) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12: Intent-to-Treat (ITT) Analysis
NCT03510715 (13) [back to overview]Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Weeks 12, 24 and 48 - ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Percent Change From Baseline in Total Cholesterol (Total-C) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510715 (13) [back to overview]Percentage of Participants Reporting >=15 Percent (%) Reduction in LDL-C Level at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Who Achieved Low Density Lipoprotein Cholesterol Level <130 mg/dL (3.37 mmol/L) at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Achieving Low Density Lipoprotein Cholesterol <110 mg/dL (2.84 mmol/L) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Achieving Low Density Lipoprotein Cholesterol <110 mg/dL (2.84 mmol/L) at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Total Cholesterol at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Low Density Lipoprotein Cholesterol at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 24: Intent-to-treat (ITT) Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Lipoprotein (a) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Lipoprotein (a) at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in High-Density Lipoprotein Cholesterol at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Fasting Triglycerides (TG) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Who Achieved Low Density Lipoprotein Cholesterol Level Lower Than (<) 130 mg/dL (3.37 mmol/L) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Fasting Triglycerides (TG) at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Apolipoprotein B at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Apolipoprotein A1 at Week 12: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Apolipoprotein A1 (Apo A1) at Week 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]Number of Participants With Tanner Staging at Baseline and Weeks 24, 68 and 104
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Who Achieved Low Density Lipoprotein Cholesterol < 130 mg/dL (3.37 mmol/L) at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Who Achieved Low Density Lipoprotein Cholesterol < 110 mg/dL (2.84 mmol/L) at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Who Achieved at Least 50% Reduction in Low Density Lipoprotein Cholesterol Level From Baseline at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Who Achieved at Least 50% Reduction in Low Density Lipoprotein Cholesterol Level From Baseline at Weeks 12 and 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Who Achieved at Least 30 Percent (%) Reduction in Low Density Lipoprotein Cholesterol Level From Baseline at Weeks 12 and 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percentage of Participants Achieved at Least 30% Reduction in Low Density Lipoprotein Cholesterol Level From Baseline at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change in Low Density Lipoprotein Cholesterol From Baseline to Weeks 8, 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change in Low Density Lipoprotein Cholesterol From Baseline to Weeks 8, 12 and 24: ITT Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Total Cholesterol at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Low Density Lipoprotein Cholesterol at Weeks 12, and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Lipoprotein (a) at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Fasting Triglycerides at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Apolipoprotein B at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Percent Change From Baseline in Apolipoprotein A1 at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Number of Participants With Treatment-Emergent (TE) Positive Anti-Alirocumab Antibodies (ADA) Response
NCT03510884 (44) [back to overview]DB Period: Number of Participants With Treatment-Emergent (TE) Positive Anti-Alirocumab Antibodies (ADA) Response
NCT03510884 (44) [back to overview]DB Period: Absolute Change From Baseline in Apo B/Apo A-1 Ratio at Weeks 12 and 24: On-treatment Estimand
NCT03510884 (44) [back to overview]DB Period: Absolute Change From Baseline in Apo B/Apo A-1 Ratio at Weeks 12 and 24: ITT Estimand
NCT03510884 (44) [back to overview]Change From Baseline in Cogstate Battery Test - Overall Composite Score at Weeks 24, 68 and 104
NCT03510884 (44) [back to overview]OL Period: Percent Change in Low Density Lipoprotein Cholesterol From Baseline to Week 104: On-treatment Estimand
NCT03510884 (44) [back to overview]OL Period: Percent Change in Low Density Lipoprotein Cholesterol From Baseline to Week 104: ITT Estimand
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in Homeostatic Model Assessment of Insulin Resistance (HOMA-IR) Index
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in High-sensitivity C-reactive Protein (hsCRP)
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in High-density Lipoprotein Cholesterol (HDL-C)
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in HbA1c
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in Fasting Plasma Glucose
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in Apolipoprotein B (Apo B)
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in 2-hour Post Prandial Plasma Glucose (PPG)
NCT03531905 (16) [back to overview]Number of Participants With LDL-C <70 Milligrams Per Deciliter (mg/dL) at Week 12
NCT03531905 (16) [back to overview]Number of Participants With Any Treatment-emergent Adverse Event (TEAE)
NCT03531905 (16) [back to overview]Change From Baseline to Week 12 in Hemoglobin A1C (HbA1c)
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12/EOS in LDL-C (Comparing Ezetimibe With Placebo)
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12/End of Study (EOS) in Low-density Lipoprotein Cholesterol (LDL-C)
NCT03531905 (16) [back to overview]Secondary Outcome Measure: Number of Participants With an LDL-C Reduction of ≥50% From Baseline at Week 12
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in Total Cholesterol (TC)
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in Non-high-density Lipoprotein Cholesterol (Non-HDL-C)
NCT03531905 (16) [back to overview]Percent Change From Baseline to Week 12 in Triglycerides (TGs)

Number of Participants That Experienced One or More Components of the Composite Clinical Endpoint of AVE (Aortic Valve Events)

Composite endpoint of AVE (aortic valve events) consists of AVR surgery, CHF (as a result of progression of AS), or cardiovascular death (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg308
Placebo326

[back to top]

Incident Cancer

Number of participants with incident cancer (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg105
Placebo70

[back to top]

Nonfatal Myocardial Infarction (MI)

Number of participants that experienced nonfatal myocardial infarction (MI) (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg17
Placebo26

[back to top]

Nonhemorrhagic Stroke

Number of participants that experienced nonhemorrhagic stroke (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg33
Placebo29

[back to top]

Percutaneous Coronary Intervention (PCI)

Number of participants that experienced percutaneous coronary intervention (PCI) (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg8
Placebo17

[back to top]

Percent Change in Time Weighted Average Triglycerides From Baseline to End of Follow-up

Mean percent change (time-weighted average over follow-up) from baseline: Time-weighted average calculated using values at week 8, week 24, year 1 and every 6 months with time interval (days) between 2 successive values used as the weighting factor. For the first follow-up value, the weight was the number of days from randomization. (NCT00092677)
Timeframe: Baseline to End of follow-up (median = 4.35 years)

InterventionPercent Change (Mean)
EZ/Simva 10/40 mg-14.9
Placebo5.1

[back to top]

Percent Change in Time Weighted Average Total Cholesterol From Baseline to End of Follow-up

Mean percent change (time-weighted average over follow-up) from baseline: Time-weighted average calculated using values at week 8, week 24, year 1 and every 6 months with time interval (days) between 2 successive values used as the weighting factor. For the first follow-up value, the weight was the number of days from randomization. (NCT00092677)
Timeframe: Baseline to End of follow-up (median = 4.35 years)

InterventionPercent Change (Mean)
EZ/Simva 10/40 mg-34.8
Placebo-2.7

[back to top]

Percent Change in Time Weighted Average Low-density Lipoprotein Cholesterol (LDL-C) From Baseline to End of Follow-up

Mean percent change (time-weighted average over follow-up) from baseline: Time-weighted average calculated using values at week 8, week 24, year 1 and every 6 months with time interval (days) between 2 successive values used as the weighting factor. For the first follow-up value, the weight was the number of days from randomization. (NCT00092677)
Timeframe: Baseline to End of follow-up (median = 4.35 years)

InterventionPercent Change (Mean)
EZ/Simva 10/40 mg-53.8
Placebo-3.8

[back to top]

Percent Change in Time Weighted Average High-density Lipoprotein Cholesterol (HDL-C) From Baseline to End of Follow-up

Mean percent change (time-weighted average over follow-up) from baseline: Time-weighted average calculated using values at week 8, week 24, year 1 and every 6 months with time interval (days) between 2 successive values used as the weighting factor. For the first follow-up value, the weight was the number of days from randomization. (NCT00092677)
Timeframe: Baseline to End of follow-up (median = 4.35 years)

InterventionPercent change (Mean)
EZ/Simva 10/40 mg6.5
Placebo2.5

[back to top]

Aortic Valve Replacement (AVR)

Number of participants that experienced aortic valve replacement (AVR) (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg267
Placebo278

[back to top]

Number of Participants That Experienced One or More Components of the Composite Clinical Endpoint of ICE (Ischemic Cardiovascular Events)

Composite endpoint of ICE (ischemic cardiovascular events) consists of cardiovascular death, nonfatal MI, CABG, PCI, hospitalized unstable angina, and nonhemorrhagic stroke (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg148
Placebo187

[back to top]

Number of Participants That Experienced One or More Components of the Composite Clinical Endpoint of MCE (Major Cardiovascular Events)

Composite endpoint of MCE consists of cardiovascular death, AVR (aortic valve replacement) surgery, CHF(congestive heart failure) as a result of progression of aortic stenosis, nonfatal MI (myocardial infarction), CABG (coronary artery bypass) surgery, PCI (percutaneous coronary intervention), hospitalized unstable angina, and nonhemorrhagic stroke (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg333
Placebo355

[back to top]

Cardiovascular Death

Number of participants that experienced cardiovascular death (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg47
Placebo56

[back to top]

Change From Baseline in Peak Transaortic Jet Velocity

Mean change from baseline in peak transaortic jet velocity (NCT00092677)
Timeframe: Baseline to End of follow-up (median = 4.35 years) or pre-aortic valve replacement

Interventionm/sec (Mean)
EZ/Simva 10/40 mg0.613
Placebo0.618

[back to top]

Congestive Heart Failure (CHF) Due to Progression of Aortic Stenosis (AS)

Number of participants that experienced Congestive Heart Failure (CHF) due to progression of aortic stenosis (AS) (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg25
Placebo23

[back to top]

Hospitalization for Unstable Angina

Number of participants that experienced hospitalization for unstable angina (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg5
Placebo8

[back to top]

Death Due to Cancer

Number of participants that died due to cancer (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg39
Placebo23

[back to top]

Death (Any Cause)

Number of participants that died (any cause) (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg105
Placebo100

[back to top]

Coronary Artery Bypass Grafting (CABG)

Number of participants that experienced coronary artery bypass grafting (CABG) (NCT00092677)
Timeframe: Entire follow-up (median = 4.35 years)

InterventionParticipants (Number)
EZ/Simva 10/40 mg69
Placebo100

[back to top]

Total Cholesterol Concentration of Chylomicron-remnant (Sf 60-400) Subfractions After a Cholesterol-Rich Test Meal

On each of 2 days prior to the last day of each treatment period, participants consumed 2 large eggs in the evening. On the morning of the final day of each treatment period, fasting participants were given a site-prepared, cholesterol-enriched milkshake that provided 1114 calories of total energy (~44% of calories from fat, ~40% of calories from carbohydrate and ~17% of calories from protein) and 504 mg of cholesterol. The milkshake was consumed over a 15-minute period. Plasma samples were collected immediately prior to consumption of the test meal (baseline) and at 2, 3, 4, and 6 hours afterwards for isolation and analysis of lipoprotein subfractions. The geometric mean concentration level was calculated using data obtained at all timepoints. (NCT00101439)
Timeframe: Immediately prior to consumption of the test meal (baseline) and at 2, 3, 4, and 6 hours after test meal on Day 28 of each treatment period.

Interventionmg/dL (Geometric Mean)
Ezetimibe4.87
Placebo4.78

[back to top]

Total Cholesterol Concentration of Chylomicron (Sf≥400) Fractions After a Cholesterol-Rich Test Meal

On each of 2 days prior to the last day of each treatment period, participants consumed 2 large eggs in the evening. On the morning of the final day of each treatment period, fasting participants were given a site-prepared, cholesterol-enriched milkshake that provided 1114 calories of total energy (~44% of calories from fat, ~40% of calories from carbohydrate and ~17% of calories from protein) and 504 mg of cholesterol. The milkshake was consumed over a 15-minute period. Plasma samples were collected immediately prior to consumption of the test meal (baseline) and at 2, 3, 4, and 6 hours afterwards for isolation and analysis of lipoprotein fractions. The geometric mean concentration level was calculated using data obtained at all timepoints. (NCT00101439)
Timeframe: Immediately prior to consumption of the test meal (baseline) and at 2, 3, 4, and 6 hours after test meal on Day 28 of each treatment period.

Interventionmg/dL (Geometric Mean)
Ezetimibe0.45
Placebo0.50

[back to top]

Major Vascular Events Analyzed Among All Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo

Major vascular events defined as non-fatal myocardial infarction or cardiac death, any stroke, or any arterial revascularization procedure (excluding dialysis access procedures). Numbers provided = number of patients with events. (NCT00125593)
Timeframe: Median follow-up 4.9 years

Interventionparticipants (Number)
Simvastatin Plus Ezetimibe701
Placebo814

[back to top]

Major Vascular Events Analyzed Amongst Patients Initially Randomized to Simvastatin Plus Ezetimibe Versus Placebo (Original Protocol-defined Primary Outcome)

Major vascular events defined as non-fatal myocardial infarction or cardiac death, any stroke, or any arterial revascularization procedure (excluding dialysis access procedures). Numbers provided = number of patients with events. (NCT00125593)
Timeframe: Median follow-up 4.9 years

Interventionparticipants (Number)
Simvastatin Plus Ezetimibe639
Placebo749

[back to top]

Non-hemorrhagic Stroke Among All of Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo

Stroke was defined as rapid onset of focal or global neurological deficit, with duration greater than 24 hours. Clinical notes and brain imaging were sought to determine the stroke etiology, and if the stroke was fatal and post-mortem examination findings were available, this information was also assessed. All potential stroke events (including transient ischemic attack and intracerebral hemorrhage) were adjudicated, using pre-specified objective criteria, by clinicians blinded to study treatment allocation and lipid levels. Numbers provided = number of patients with events. (NCT00125593)
Timeframe: Median follow-up 4.9 years

Interventionparticipants (Number)
Simvastatin Plus Ezetimibe131
Placebo174

[back to top]

Key Outcome as Per Statistical Analysis Plan = Major Atherosclerotic Events Among All Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo

Major atherosclerotic events defined as non-fatal myocardial infarction or coronary death, non-hemorrhagic stroke, or any arterial revascularization procedure (excluding dialysis access procedures). Numbers provided = number of patients with events. (NCT00125593)
Timeframe: Median follow-up 4.9 years

Interventionparticipants (Number)
Simvastatin Plus Ezetimibe526
Placebo619

[back to top]

Coronary or Non-coronary Revascularization Among All Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo

Revascularization included any arterial revascularization procedure, whether surgical or percutaneous, but excluded revascularization performed for hemodialysis vascular access (e.g. fistuloplasty) or to the donor kidney transplant artery. Revascularization included amputations for vascular disease (rather than for trauma or infection). All potential revascularization events (including angiography) were adjudicated, using pre-specified objective criteria, by clinicians blinded to study treatment allocation and lipid levels. Numbers provided = number of patients with events. (NCT00125593)
Timeframe: Median follow-up 4.9 years

Interventionparticipants (Number)
Simvastatin Plus Ezetimibe284
Placebo352

[back to top]

End-stage Renal Disease Among All Patients Not on Dialysis at the Time of Randomization to Simvastatin Plus Ezetimibe Versus Placebo

End-stage renal disease was defined as initiation of maintenance dialysis or renal transplantation. Temporary dialysis was excluded. All potential dialysis and transplant events were adjudicated, using pre-specified objective criteria, by clinicians blinded to study treatment allocation and lipid levels. Numbers provided = number of patients with events. (NCT00125593)
Timeframe: Median follow-up 4.9 years

Interventionparticipants (Number)
Simvastatin Plus Ezetimibe1057
Placebo1084

[back to top]

Major Coronary Events Among All Patients Ever Randomized to Simvastatin Plus Ezetimibe Versus All Patients Allocated to Placebo

Major coronary events defined as coronary death or non-fatal myocardial infarction. Myocardial infarction adjudicated based on the presence of serial changes in cardiac biomarkers (e.g. troponin, creatine kinase), typical ECG changes and typical cardiac symptoms. If myocardial infarction was fatal and post-mortem examination findings were available, this information was also assessed. All potential coronary events were adjudicated, using pre-specified objective criteria, by clinicians blinded to study treatment allocation and lipid levels. Numbers provided = number of patients with events. (NCT00125593)
Timeframe: Median follow-up 4.9 years

Interventionparticipants (Number)
Simvastatin Plus Ezetimibe213
Placebo230

[back to top]

Percent Change From Baseline in Total Cholesterol (TC)

(NCT00129402)
Timeframe: baseline to 6 weeks

Interventionpercent change (Least Squares Mean)
Pooled Subjects Who Received Ezetimibe With Simvastatin-38.23
Pooled Subjects Who Received Simvastatin Monotherapy-26.28

[back to top]

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

(NCT00129402)
Timeframe: baseline to 6 weeks

Interventionpercent change (Least Squares Mean)
Pooled Subjects Who Received Ezetimibe With Simvastatin-46.84
Pooled Subjects Who Received Simvastatin Monotherapy-32.68

[back to top]

Percent Change From Baseline in Triglycerides (TG)

(NCT00129402)
Timeframe: baseline to 6 weeks

Interventionpercent change (Median)
Pooled Subjects Who Received Ezetimibe With Simvastatin-16.56
Pooled Subjects Who Received Simvastatin Monotherapy-12.28

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)

Least squares mean percent change from Baseline in LDL-C at the end of Step 1 (Week 6) in the pooled groups who received ezetimibe plus simvastatin compared with pooled groups who received simvastatin monotherapy (NCT00129402)
Timeframe: baseline to 6 weeks

Interventionpercent change (Least Squares Mean)
Pooled Subjects Who Received Ezetimibe With Simvastatin-49.45
Pooled Subjects Who Received Simvastatin Monotherapy-34.43

[back to top]

Percent Change From Baseline in Apolipoprotein B (Apo B)

(NCT00129402)
Timeframe: baseline to 6 weeks

Interventionpercent change (Least Squares Mean)
Pooled Subjects Who Received Ezetimibe With Simvastatin-38.92
Pooled Subjects Who Received Simvastatin Monotherapy-26.69

[back to top]

Percent Change From Baseline in HDL-C

(NCT00129402)
Timeframe: baseline to 6 weeks

Interventionpercent change (Least Squares Mean)
Pooled Subjects Who Received Ezetimibe With Simvastatin6.58
Pooled Subjects Who Received Simvastatin Monotherapy6.47

[back to top]

LDL-C Lowering Efficacy

LDL-C = low density lipoprotein cholesterol, measured in mg/dl. (NCT00166504)
Timeframe: 6 weeks

InterventionPercent Change from Baseline (Least Squares Mean)
Vytorin-51
Atorvastatin-41

[back to top]

Time to First Occurrence of CV Death, Nonfatal MI, UA With Hospitalization, All Revascularization Occurring ≥30 Days After Randomization, and Non-fatal Stroke (Kaplan-Meier Estimate of Percentage of Participants Experiencing a Qualifying Event)

The time (in months) from study start to the first occurrence of any of the following clinical outcomes was recorded: CV death, non-fatal MI, documented UA that requires admission into a hospital, all revascularization (including non-coronary) occurring at least 30 days after randomization, and non-fatal stroke. A Clinical Endpoints Committee (CEC) reviewed and adjudicated each suspected efficacy endpoint event while blinded to treatment. Participants who did not have any endpoint event until last visit or who were lost to follow-up and had no event were censored at the time of last available information (last study visit). The Kaplan-Meier estimate reports the percentage of participants who experienced CV death, non-fatal MI, unstable angina with hospitalization, all revascularization occurring ≥ 30 days after randomization, and non-fatal stroke within 7 Years from randomization. (NCT00202878)
Timeframe: Up to approximately 9 years

InterventionPercentage of Participants (Number)
Ezetimibe/Simvastatin34.49
Simvastatin36.20

[back to top]

Time to First Occurrence of Death From Any Cause, Major Coronary Event, or Non-fatal Stroke (Kaplan-Meier Estimate of Percentage of Participants Experiencing a Qualifying Event)

The time (in months) from study start to the first occurrence of any of the following clinical outcomes was recorded: death from any cause, major coronary event (non-fatal myocardial infarction, documented unstable angina requiring hospitalization, or coronary revascularization with percutaneous coronary intervention or coronary artery bypass grafting ≥ 30 days after randomization), or non-fatal stroke. A Clinical Endpoints Committee (CEC) reviewed and adjudicated each suspected efficacy endpoint event while blinded to treatment. Participants who did not have any endpoint event until last visit or who were lost to follow-up and had no event were censored at the time of last available information (last study visit). The Kaplan-Meier estimate reports the percentage of participants who experienced death from any cause, major coronary event, or non-fatal stroke within 7 years from randomization. (NCT00202878)
Timeframe: Up to approximately 9 years

InterventionPercentage of Participants (Number)
Ezetimibe/Simvastatin38.65
Simvastatin40.25

[back to top]

Time to First Occurrence of Cardiovascular Death, Major Coronary Event, or Non-fatal Stroke (Kaplan-Meier Estimate of Percentage of Participants Experiencing a Qualifying Event)

The time (in months) from study start to the first occurrence of any of the following clinical outcomes was recorded: cardiovascular death, major coronary Event (non-fatal myocardial infarction [MI], documented unstable angina [UA] requiring hospitalization, or coronary revascularization with percutaneous coronary intervention (PCI) or coronary artery bypass grafting (CABG) ≥ 30 days after randomization), or non-fatal Stroke. A Clinical Endpoints Committee (CEC) reviewed and adjudicated each suspected efficacy endpoint event while blinded to treatment. Participants who did not have any endpoint event until last visit or who were lost to follow-up and had no event were censored at the time of last available information (last study visit). The Kaplan-Meier estimate reports the percentage of participants who experienced cardiovascular death, major coronary event, or non-fatal stroke within 7 years from randomization. (NCT00202878)
Timeframe: Up to approximately 9 years

InterventionPercentage of Participants (Number)
Ezetimibe/Simvastatin32.72
Simvastatin34.67

[back to top]

Time to First Occurrence of Coronary Heart Disease (CHD) Death, Non-fatal MI, or Urgent Coronary Revascularization With PCI or CABG ≥ 30 Days After Randomization (Kaplan-Meier Estimate of Percentage of Participants Experiencing a Qualifying Event)

The time (in months) from study start to the first occurrence of any of the following clinical outcomes was recorded: CHD death, non-fatal MI, or urgent coronary revascularization with PCI or CABG ≥ 30 days after randomization. A Clinical Endpoints Committee (CEC) reviewed and adjudicated each suspected efficacy endpoint event while blinded to treatment. Participants who did not have any endpoint event until last visit or who were lost to follow-up and had no event were censored at the time of last available information (last study visit). The Kaplan-Meier estimate reports the percentage of participants who experienced CHD death, non-fatal MI, or urgent coronary revascularization with PCI or CABG ≥ 30 days after randomization within 7 years from randomization. (NCT00202878)
Timeframe: Up to approximately 9 years

InterventionPercentage of Participants (Number)
Ezetimibe/Simvastatin17.52
Simvastatin18.88

[back to top]

LFT Elevation

(NCT00203476)
Timeframe: 12 weeks

Interventionparticipants (Number)
Niacin1
Colestipol1
Ezetimibe2

[back to top]

LDL Goal Attainment

Each participant had his LDL goal calculated based on the NCEP ATPIII guidelines. (NCT00203476)
Timeframe: 12 weeks

Interventionparticipants (Number)
Niacin6
Colestipol6
Ezetimibe9

[back to top]

Incidents of Rhabdomyolysis

(NCT00203476)
Timeframe: 12 weeks

Interventionparticipants (Number)
Niacin0
Colestipol0
Ezetimibe0

[back to top]

Change in HDL From Baseline to 12 Weeks.

(NCT00203476)
Timeframe: baseline and 12 weeks

,,
Interventionmg/dl (Mean)
baseline12 weeks
Colestipol39.2237.56
Ezetimibe32.9034.70
Niacin42.3343.00

[back to top]

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

Ezetimibe/simvastatin co-administered with niacin extended release compared to ezetimibe/simvastatin monotherapy on the percent change from baseline in non-HDL-C after 64 weeks - 64 week measure minus baseline (NCT00271817)
Timeframe: Baseline and 64 weeks

InterventionPercent change (Mean)
Ezetimibe/Simvastatin-45.1
Ezetimibe/Simvastatin + Niacin-52.4

[back to top]

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

Ezetimibe/simvastatin co-administered with niacin extended release compared to niacin extended release monotherapy on the percent change from baseline in non-HDL-C after 24 weeks - 24 week measure minus baseline (NCT00271817)
Timeframe: Baseline and 24 weeks

InterventionPercent change (Mean)
Niacin-22.0
Ezetimibe/Simvastatin + Niacin-55.6

[back to top]

Percent Change From Baseline in Triglycerides (TG)

Ezetimibe/simvastatin co-administered with niacin extended release compared to ezetimibe/simvastatin monotherapy on the percent change from baseline in Triglycerides after 24 weeks - 24 week measure minus baseline (NCT00271817)
Timeframe: baseline and 24 Weeks

InterventionPercent change (Median)
Ezetimibe/Simvastatin23.7
Ezetimibe/Simvastatin + Niacin-42.5

[back to top]

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

Ezetimibe/simvastatin co-administered with niacin extended release compared to ezetimibe/simvastatin monotherapy on the percent change from baseline in LDL-C after 24 weeks - 24 week measure minus baseline (NCT00271817)
Timeframe: Baseline and 24 weeks

InterventionPercent change (Mean)
Ezetimibe/Simvastatin-53.5
Ezetimibe/Simvastatin + Niacin-58.5

[back to top]

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

Ezetimibe/simvastatin co-administered with niacin extended release compared to ezetimibe/simvastatin monotherapy on the percent change from baseline in LDL-C after 64 weeks - 64 week measure minus baseline (NCT00271817)
Timeframe: Baseline and 64 weeks

InterventionPercent change (Mean)
Ezetimibe/Simvastatin-49.3
Ezetimibe/Simvastatin + Niacin-54.0

[back to top]

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

Ezetimibe/simvastatin co-administered with niacin extended release compared to niacin extended release monotherapy on the percent change, from baseline in LDL-C after 24 weeks - 24 Week Measure Minus Baseline (NCT00271817)
Timeframe: Baseline and 24 Weeks

InterventionPercent change (Mean)
Niacin-20.1
Ezetimibe/Simvastatin + Niacin-58.5

[back to top]

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

Ezetimibe/simvastatin co-administered with niacin extended release compared to ezetimibe/simvastatin monotherapy on the percent change from baseline in non-HDL-C after 24 weeks - 24 week measure minus baseline (NCT00271817)
Timeframe: Baseline and 24 weeks

InterventionPercent change (Mean)
Ezetimibe/Simvastatin-47.9
Ezetimibe/Simvastatin + Niacin-55.6

[back to top]

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

Ezetimibe/simvastatin co-administered with niacin extended release compared to ezetimibe/simvastatin monotherapy on the percent change from baseline in HDL-C after 24 weeks - 24 week measure minus baseline (NCT00271817)
Timeframe: Baseline and 24 weeks

InterventionPercent change (Mean)
Ezetimibe/Simvastatin8.1
Ezetimibe/Simvastatin + Niacin30.2

[back to top]

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

Ezetimibe/simvastatin co-administered with niacin extended release compared to ezetimibe/simvastatin monotherapy on the percent change from baseline in HDL-C after 64 weeks - 64 week measure minus baseline (NCT00271817)
Timeframe: Baseline and 64 weeks

InterventionPercent change (Mean)
Ezetimibe/Simvastatin9.0
Ezetimibe/Simvastatin + Niacin30.5

[back to top]

Percent Change From Baseline in Triglycerides (TG)

Ezetimibe/simvastatin co-administered with niacin extended release compared to ezetimibe/simvastatin monotherapy on the percent change from baseline in Triglycerides after 64 weeks - 64 week measure minus baseline (NCT00271817)
Timeframe: Baseline and 64 weeks

InterventionPercent change (Median)
Ezetimibe/Simvastatin-26.8
Ezetimibe/Simvastatin + Niacin-44.5

[back to top]

Percent Change in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-26.7
Atorvastatin-10.2

[back to top]

Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-31.9
Atorvastatin-11.0

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-21.4
Atorvastatin-7.7

[back to top]

Percent Change From Baseline in Apolipoprotein B: Apolipoprotein A-I Ratio at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-19.0
Atorvastatin-5.8

[back to top]

Percent Change From Baseline in C-Reactive Protein (CRP) at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

Interventionpercent (Least Squares Mean)
Atorvastatin + Ezetimibe-6.7
Atorvastatin-9.2

[back to top]

Number of Participants Who Attained Target LDL-C <100 mg/dL at Week 6

(NCT00276458)
Timeframe: 6 weeks

,
InterventionParticipants (Number)
<100 mg/dL≥100 mg/dL
Atorvastatin4547
Atorvastatin + Ezetimibe7715

[back to top]

Percent Change in High Density Lipoprotein -Cholesterol (HDL-C)at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe3.2
Atorvastatin0.8

[back to top]

Percent Change in C-Reactive Protein (CRP) at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-19.2
Atorvastatin-9.1

[back to top]

Percent Change From Baseline in Total-Cholesterol:High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-20.6
Atorvastatin-7.5

[back to top]

Percent Change in Apolipoprotein A-I at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-1.9
Atorvastatin-1.2

[back to top]

Percent Change From Baseline in Triglycerides (TG) at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-17.8
Atorvastatin-5.5

[back to top]

Percent Change From Baseline in Total-Cholesterol at Week 6

([6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

Interventionpercent (Least Squares Mean)
Atorvastatin + Ezetimibe-19.7
Atorvastatin-7.4

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (HDL-C):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 Weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-27.2
Atorvastatin-9.9

[back to top]

Percent Change From Baseline in Low Density Lipoprotein-Cholesterol (LDL-C) at Week 6

[(6 week value - baseline value)/baseline value]*100%. (NCT00276458)
Timeframe: 6 weeks

InterventionPercent (Least Squares Mean)
Atorvastatin + Ezetimibe-30.8
Atorvastatin-10.9

[back to top]

Percent Change From Baseline to Week 6 in Apolipoprotein B (Apo B)

Percent Change in Apo B = [(week 6 value - baseline value)/baseline value]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-17.8
Atorvastatin-7.7

[back to top]

Percent Change From Baseline to Week 6 in Apolipoprotein A-I (Apo A-I)

Percent Change in Apo A-I = [(week 6 value - baseline value)/baseline value]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-0.3
Atorvastatin-1.2

[back to top]

Percent Change From Baseline to Week 6 in Apolipoprotein B:Apolipoprotein A-I (Apo B:Apo A-I) Ratio

Percent Change in Apo B:Apo A-I Ratio = [(week 6 ratio - baseline ratio)/baseline ratio]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-16.9
Atorvastatin-5.9

[back to top]

Percent Change From Baseline to Week 6 in C Reactive Protein (CRP)

Percent Change in CRP = [(week 6 value - baseline value)/baseline value]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-18.3
Atorvastatin-11.5

[back to top]

Percent Change From Baseline to Week 6 in Non-High-Density Lipoprotein-Cholesterol:High-Density Lipoprotein-Cholesterol (Non-HDL-C:HDL-C) Ratio

Percent Change in non-HDL-C:HDL-C Ratio = [(week 6 ratio - baseline ratio)/baseline ratio]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-22.2
Atorvastatin-7.6

[back to top]

Percent Change From Baseline to Week 6 in Total-Cholesterol

Percent Change in Total-C = [(week 6 value - baseline value)/baseline value]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-16.9
Atorvastatin-6.9

[back to top]

Percent Change From Baseline to Week 6 in Triglycerides (TG)

Percent Change in TG = [(week 6 value - baseline value)/baseline value]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-12.3
Atorvastatin-5.9

[back to top]

Percent Change From Baseline to Week 6 in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C)

Percent Change in Non-HDL-C = [(week 6 value - baseline value)/baseline value]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-23.3
Atorvastatin-9.0

[back to top]

Percent Change From Baseline to Week 6 in Low-Density Lipoprotein-Cholesterol:High-Density Lipoprotein-Cholesterol (LDL-C:HDL-C) Ratio

Percent Change in LDL-C:HDL-C Ratio = [(week 6 ratio - baseline ratio)/baseline ratio]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent change (Least Squares Mean)
Atorvastatin + Ezetemibe-26.4
Atorvastatin-9.9

[back to top]

Percent Change From Baseline to Week 6 in Low-Density Lipoprotein (LDL)-C

Percent Change in LDL-C = [(week 6 value - baseline value)/baseline value]*100% (NCT00276484)
Timeframe: Baseline and 6 weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-27.4
Atorvastatin-11.0

[back to top]

Percent Change From Baseline to Week 6 in High-Density Lipoprotein Cholesterol (HDL-C)

Percent Change in HDL-C = [(week 6 value - baseline value)/baseline value]*100% (NCT00276484)
Timeframe: Baseline and 6 weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-0.5
Atorvastatin-1.0

[back to top]

Percent Change From Baseline to Week 6 in Total-Cholesterol (TC):High-Density Lipoprotein Cholesterol (HDL-C) Ratio

Percent Change in TC:HDL-C Ratio = [(week 6 ratio - baseline ratio)/baseline ratio]*100% (NCT00276484)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorvastatin + Ezetemibe-16.0
Atorvastatin-5.6

[back to top]

Number of Patients Who Attained Target Low-Density Lipoprotein Cholesterol (LDL-C) <70 mg/dL at Week 6

(NCT00276484)
Timeframe: 6 Weeks

,
InterventionParticipants (Number)
<70 mg/dL>=70 mg/dL
Atorvastatin88191
Atorvastatin + Ezetemibe20473

[back to top]

Number of Participants Who Achieve the Target LDL-C Concentration of < 3.3 mmol/L (130 mg/dL)

12-hour fasting blood samples were collected in participants to measure high density lipoprotein-cholesterol (HDL-C), triglycerides and total cholesterol. LDL-C was measured using Friedewald calculation (LDL-C = Total C - [HDL-C + TG/5] after treatment for 6 weeks. (NCT00319449)
Timeframe: 6 weeks post treatment

InterventionParticipants (Number)
Ezetimibe 10 mg7
Placebo 10 mg8

[back to top]

High Density Lipoprotein-cholesterol (HDL-C), Total Cholesterol and Triglycerides at Baseline and After 6 Weeks of Treatment With Ezetimibe 10 mg Added to Atorvastatin 10 mg Versus Placebo Added to Atorvastatin 10 mg

12-hour fasting blood samples were collected in participants and the high density lipoprotein-cholesterol (HDL-C), triglycerides and total cholesterol was measured with the basic lipid panel test. (NCT00319449)
Timeframe: 6 weeks post treatment

,
Interventionmg/dL (Mean)
HDL-C at baselineHDL-C at 6 weeksTotal Cholesterol at baselineTotal Cholesterol at 6 weeksTriglycerides at baselineTriglycerides at 6 weeks
Ezetimibe 10 mg53.25052.625219.125156.375139.500115.250
Placebo 10 mg57.66753.500226.000185.667131.667120.250

[back to top]

Low Density Lipoprotein-cholesterol (LDL-C) at Baseline and After 6 Weeks of Treatment With Ezetimibe 10 mg Added to Atorvastatin 10 mg Versus Placebo Added to Atorvastatin 10 mg

12-hour fasting blood samples were collected in participants to measure high density lipoprotein-cholesterol (HDL-C), triglycerides and total cholesterol. LDL-C was measured using Friedewald calculation (LDL-C = Total C - [HDL-C + TG/5]) before and after treatment. (NCT00319449)
Timeframe: Baseline and 6 weeks

,
Interventionmg/dL (Mean)
Baseline6 weeks post treatment
Ezetimibe 10 mg148.125106.000
Placebo 10 mg151.083108.273

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)

Percent change from Baseline in LDL-C (NCT00359281)
Timeframe: Baseline to Day 8

InterventionPercent Change (Mean)
Atorvastatin 20 mg + Lomitapide 10 mg-30.99
Simvastatin 20 mg + Lomitapide 10 mg-26.43
Ezetimibe 10 mg + Lomitapide 10 mg-28.36
Rosuvastatin 20 mg + Lomitapide 10 mg-41.74
Fenofibrate 145 mg + Lomitapide 10 mg-20.12
Atorvastatin 20 mg + Lomitapide 60 mg-66.02
Rosuvastatin 20 mg + Lomitapide 60 mg-63.20
Dextrometh-rophan 30 mg + Lomitapide 60 mg-46.07
ER Niacin 1000 mg + Lomitapide 10 mg-20.89

[back to top]

AUC0-t Rosuvastatin (Lomitapide 60 mg)

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for rosuvastatin (Lomitapide 60 mg) (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
Rosuvastatin 20 mg + Lomitapide 60 mg132.21

[back to top]

AUC0-t Atorvastatin Acid (Lomitapide 60 mg)

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for atorvastatin acid (Lomitapide 60 mg) (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
Atorvastatin 20 mg + Lomitapide 60 mg152.32

[back to top]

AUC0-t Fenofibric Acid

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for fenofibric acid (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
Fenofibrate 145 mg + Lomitapide 10 mg89.62

[back to top]

AUC0-t Nicotinic Acid

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for nicotinic acid (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
ER Niacin 1000 mg + Lomitapide 10 mg110.22

[back to top]

AUC0-t Nicotinuric Acid

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for nicotinuric acid (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
ER Niacin 1000 mg + Lomitapide 10 mg79.15

[back to top]

AUC0-t Rosuvastatin (Lomitapide 10 mg)

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for rosuvastatin (Lomitapide 10 mg) (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
Rosuvastatin 20 mg + Lomitapide 10 mg102.05

[back to top]

AUC0-t Simvastatin

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for simvastatin (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
Simvastatin 20 mg + Lomitapide 10 mg162.25

[back to top]

AUC0-t Simvastatin Acid

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for simvastatin acid (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
Simvastatin 20 mg + Lomitapide 10 mg138.76

[back to top]

AUC0-t Total Ezetimibe

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for total ezetimibe (NCT00359281)
Timeframe: 0 to 24 hours

InterventionRatio (Geometric Mean)
Ezetimibe 10 mg + Lomitapide 10 mg105.71

[back to top]

Area Under Concentration-time Curve From 0 to Last Measureable Concentration (AUC0-t) Atorvastatin Acid (Lomitapide 10 mg)

Geometric Mean Ratio ln(AUC0-t) Day 8/Day 1 for atorvastatin acid (Lomitapide 10 mg) (NCT00359281)
Timeframe: 0 to 24 hour

InterventionRatio (Geometric Mean)
Atorvastatin 20 mg + Lomitapide 10 mg110.97

[back to top]

Percent Change in Flow Mediated Dilation

(NCT00376246)
Timeframe: before food, 3 hours postprandially and 6 hours postprandially

,
Interventionpercent change (Median)
Before Food (0 hour)3 Hours Postprandially6 Hours Postprandially
Ezetimibe11.611.113.9
Placebo12.310.912.8

[back to top]

Lipid Profile- Change in LDL(Low Density Lipoprotein)

(NCT00376246)
Timeframe: before food, 3 hours post prandial, 6 hours postprandial

,
Interventionmg/dl (Mean)
before food (0 hour)3 hour postprandial6 hour postprandial
Ezetimibe928987
Placebo102104101

[back to top]

Percent Change in Apolipoprotein A1 (Apo A1) at 12 Weeks as Compared to Baseline

(NCT00405067)
Timeframe: baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-10.7
Lomitapide Monotherapy-8.0
Ezetimibe Monotherapy2.3

[back to top]

Percent Change in Apolipoprotein B (Apo B) at 12 Weeks as Compared to Baseline

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-36.6
Lomitapide Monotherapy-23.7
Ezetimibe Monotherapy-14.5

[back to top]

Percent Change in Body Weight at 12 Weeks as Compared to Baseline

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-1.4
Lomitapide Monotherapy-1.0
Ezetimibe Monotherapy-0.1

[back to top]

Percent Change in HDL-C at 12 Weeks Compared to Baseline

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-9.2
Lomitapide Monotherapy-6.2
Ezetimibe Monotherapy5.9

[back to top]

Percent Change in High-sensitivity C-reactive Protein (Hs-CRP) at 12 Weeks as Compared to Baseline

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy40.4
Lomitapide Monotherapy81.3
Ezetimibe Monotherapy233.3

[back to top]

Percent Change in LDL-C at 12 Weeks Therapy Compared to Baseline Between Treatments

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-46.2
Lomitapide Monotherapy-29.9
Ezetimibe Monotherapy-19.6

[back to top]

Percent Change in Lipoprotein(a)[Lp(a)]at 12 Weeks as Compared to Baseline

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-12.0
Lomitapide Monotherapy-11.4
Ezetimibe Monotherapy7.5

[back to top]

Percent Change in Tryglycerides (TGs) at 12 Weeks Compared to Baseline

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-7.0
Lomitapide Monotherapy-5.8
Ezetimibe Monotherapy2.7

[back to top]

Percent of Change at 12 Weeks Therapy Compared to Baseline Between Treatments for the Following Parameters: Total Cholesterol (TC)

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-34.4
Lomitapide Monotherapy-22.8
Ezetimibe Monotherapy-12.0

[back to top]

Percent Change in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at 12 Weeks as Compared to Baseline.

(NCT00405067)
Timeframe: Baseline and 12 weeks of treatment

InterventionPercent Change (Mean)
Combination Therapy-41.3
Lomitapide Monotherapy-26.9
Ezetimibe Monotherapy-17.0

[back to top]

Percent Change From Baseline in Low Density Lipoprotein Cholesterol: High Density Lipoprotein Cholesterol (LDL-C: HDL-C) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-37.8
EZ/Simva 10 mg/20 mg-51.8
Atorva 20mg-42.1
EZ/Simva 10 mg/40 mg-56.6
Atorva 40 mg-48.2

[back to top]

Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 6 in Patients With Atherosclerotic Vascular Disease (AVD)

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-37.1
EZ/Simva 10 mg/20 mg-48.7
Atorva 20mg-36.9
EZ/Simva 10 mg/40 mg-56.1
Atorva 40 mg-45.8

[back to top]

Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg3.4
EZ/Simva 10 mg/20 mg6.8
Atorva 20mg5.6
EZ/Simva 10 mg/40 mg8.8
Atorva 40 mg4.9

[back to top]

Percent Change From Baseline in Low Density Lipoprotein (LDL-C) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-36.5
EZ/Simva 10 mg/20 mg-49.6
Atorva 20mg-39.4
EZ/Simva 10 mg/40 mg-53.9
Atorva 40 mg-46.0

[back to top]

Percent Change From Baseline in Very Low Density Lipoprotein Cholesterol (VLDL-C) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-17.7
EZ/Simva 10 mg/20 mg-18.3
Atorva 20mg-21.6
EZ/Simva 10 mg/40 mg-23.4
Atorva 40 mg-22.7

[back to top]

Percent Change From Baseline in Triglyceride (TG) (mg/dL) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Median)
Atorva 10 mg-21.7
EZ/Simva 10 mg/20 mg-23.3
Atorva 20mg-27.5
EZ/Simva 10 mg/40 mg-29.5
Atorva 40 mg-30.0

[back to top]

Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 6 in Patients Without Atherosclerotic Vascular Disease (AVD)

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-36.3
EZ/Simva 10 mg/20 mg-50.1
Atorva 20mg-40.3
EZ/Simva 10 mg/40 mg-53.2
Atorva 40 mg-46.1

[back to top]

Percent Change From Baseline in Total-Cholesterol: High Density Lipoprotein-Cholesterol (Total-C:HDL- C) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-28.1
EZ/Simva 10 mg/20 mg-36.9
Atorva 20mg-31.5
EZ/Simva 10 mg/40 mg-41.2
Atorva 40 mg-35.3

[back to top]

Percent Change From Baseline in Total Cholesterol(mg/dL) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-26.5
EZ/Simva 10 mg/20 mg-33.7
Atorva 20mg-28.3
EZ/Simva 10 mg/40 mg-37.3
Atorva 40 mg-32.8

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol: High Density Lipoprotein Cholesterol (Non-HDL-C:HDL-C) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-34.7
EZ/Simva 10 mg/20 mg-46.2
Atorva 20mg-39.2
EZ/Simva 10 mg/40 mg-51.2
Atorva 40 mg-43.5

[back to top]

Percent Change From Baseline in High-Sensitivity C-reactive (Hs-CRP) (mg/dL) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Median)
Atorva 10 mg-16.8
EZ/Simva 10 mg/20 mg-17.2
Atorva 20mg-22.4
EZ/Simva 10 mg/40 mg-27.6
Atorva 40 mg-30.0

[back to top]

Percent Change From Baseline in Apolipoprotein-B: Apolipoprotein-A1 (Apo-B:Apo-A1) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-27.4
EZ/Simva 10 mg/20 mg-38.4
Atorva 20mg-32.0
EZ/Simva 10 mg/40 mg-41.9
Atorva 40 mg-36.2

[back to top]

Percent Change From Baseline in Apolipoprotein-A1 (Apo-A1) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg0.8
EZ/Simva 10 mg/20 mg3.2
Atorva 20mg1.0
EZ/Simva 10 mg/40 mg3.0
Atorva 40 mg1.4

[back to top]

Percent Change From Baseline in Apolipoprotein- B (Apo-B) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-27.9
EZ/Simva 10 mg/20 mg-37.2
Atorva 20mg-31.9
EZ/Simva 10 mg/40 mg-41.1
Atorva 40 mg-35.8

[back to top]

Percent Change From Baseline in Non- High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 6

(NCT00409773)
Timeframe: Baseline and 6 Weeks

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg-33.5
EZ/Simva 10 mg/20 mg-43.8
Atorva 20mg-36.5
EZ/Simva 10 mg/40 mg-48.3
Atorva 40 mg-41.4

[back to top]

Percent Change in Low-density Lipoprotein Cholesterol (LDL-C) From Baseline to Endpoint After 8 Weeks of Treatment

(NCT00413972)
Timeframe: Baseline, 8 weeks

Interventionpercent change of LDL-C (Mean)
Vytorin 10/10-41.69
Vytorin 10/20-46.83
Vytorin 10/40-49.10
Placebo-7.53

[back to top]

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

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ2.4
Atorva 20 mg / Atorva 40 mg-0.8

[back to top]

Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ2.5
Atorva 20 mg / Atorva 40 mg0.7

[back to top]

Percent Change From Baseline in LDL-C at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-26.7
Atorva 20 mg / Atorva 40 mg-12.8

[back to top]

Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-22.5
Atorva 20 mg / Atorva 40 mg-17.9

[back to top]

Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-22.9
Atorva 20 mg / Atorva 40 mg-16.0

[back to top]

Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-27.2
Atorva 20 mg / Atorva 40 mg-12.6

[back to top]

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

(NCT00418834)
Timeframe: Baseine and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-20.0
Atorva 20 mg / Atorva 40 mg-15.8

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-23.5
Atorva 20 mg / Atorva 40 mg-11.2

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-20.4
Atorva 20 mg / Atorva 40 mg-13.8

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-24.0
Atorva 20 mg / Atorva 40 mg-11.1

[back to top]

Percent Change From Baseline in Ratio of Highly Selective C-Reactive Protein (Hs-CRP) at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-21.7
Atorva 20 mg / Atorva 40 mg-14.6

[back to top]

Percent Change From Baseline in Ratio of Highly Selective C-Reactive Protein (Hs-CRP) at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-13.5
Atorva 20 mg / Atorva 40 mg-10.7

[back to top]

Percent Change From Baseline in Total Cholesterol (TC) at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-13.6
Atorva 20 mg / Atorva 40 mg-11.6

[back to top]

Percent Change From Baseline in Total Cholesterol (TC) at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-15.9
Atorva 20 mg / Atorva 40 mg-8.0

[back to top]

Percent Change From Baseline in Total Cholesterol (TC): High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-16.9
Atorva 20 mg / Atorva 40 mg-7.9

[back to top]

Percent Change From Baseline in Total Cholesterol (TC):High Density Lipoprotein Cholesterol (HDL-C) Ratio at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-14.4
Atorva 20 mg / Atorva 40 mg-9.8

[back to top]

Percent Change From Baseline in Triglycerides (TG) at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-11.8
Atorva 20 mg / Atorva 40 mg-8.5

[back to top]

Percent Change From Baseline in Triglycerides (TG) at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-12.9
Atorva 20 mg / Atorva 40 mg-5.7

[back to top]

Number of Patients Who Achieved LDL-C <100 mg/dL for Patients Without Atherosclerotic Vascular Disease (AVD) and LDL-C <70 mg/dL for Patients With Atherosclerotic Vascular Disease (AVD) at Week 6

(NCT00418834)
Timeframe: Week 6

,
InterventionParticipants (Number)
<100 mg/dL (w/o AVD) and <70 mg/dL (w/ AVD)>100 mg/dL (w/o AVD) and ≥70 mg/dL (w/AVD)
Atorva 10 mg + EZ274241
Atorva 20 mg / Atorva 40 mg127388

[back to top]

Number of Patients Who Achieved LDL-C<100 mg/dL for Patients Without AVD and LDL-C<70 mg/dL for Patients With AVD at Week 12

(NCT00418834)
Timeframe: Week 12

,
InterventionParticipants (Number)
<100 mg/dL (w/o AVD) and <70 mg/dL (w/ AVD)≥100 mg/dL (w/o AVD) and ≥70 mg/dL (w/ AVD)
Atorva 10 mg + EZ255261
Atorva 20 mg / Atorva 40 mg200309

[back to top]

Number of Patients Who Achieved Low Density Lipoprotein Cholesterol (LDL-C) <70 mg/dL at Week 12

(NCT00418834)
Timeframe: Week 12

,
InterventionParticipants (Number)
<70 mg/dL≥70 mg/dL
Atorva 10 mg + EZ225291
Atorva 20 mg / Atorva 40 mg164345

[back to top]

Number of Patients Who Achieved Low Density Lipoprotein Cholesterol (LDL-C) <70 mg/dL at Week 6

(NCT00418834)
Timeframe: Week 6

,
InterventionParticipants (Number)
<70 mg/dL≥70 mg/dL
Atorva 10 mg + EZ244271
Atorva 20 mg / Atorva 40 mg92423

[back to top]

Percent Change From Baseline in Apo Lipoprotein B (Apo B):Apo Lipoprotein A-I (Apo A-I) Ratio at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-13.5
Atorva 20 mg / Atorva 40 mg-8.2

[back to top]

Percent Change From Baseline in Apo Lipoprotein A-I (Apo A-I) at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ0.7
Atorva 20 mg / Atorva 40 mg-2.0

[back to top]

Percent Change From Baseline in Apo Lipoprotein A-I (Apo A-I) at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-1.1
Atorva 20 mg / Atorva 40 mg-1.7

[back to top]

Percent Change From Baseline in Apo Lipoprotein B (Apo B) at Week 12

(NCT00418834)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-14.0
Atorva 20 mg / Atorva 40 mg-10.8

[back to top]

Percent Change From Baseline in Apo Lipoprotein B (Apo B) at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-16.8
Atorva 20 mg / Atorva 40 mg-7.7

[back to top]

Percent Change From Baseline in Apo Lipoprotein B (Apo B):Apo Lipoprotein A-I (Apo A-I) Ratio at Week 6

(NCT00418834)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Atorva 10 mg + EZ-14.8
Atorva 20 mg / Atorva 40 mg-5.2

[back to top]

Percent Change in Low-Density Lipoprotein Cholesterol (LDL-C) From Baseline to Endpoint, After 6 Weeks of Treatment

(NCT00423488)
Timeframe: 6 weeks of treatment (from Baseline to Endpoint)

Interventionpercentage change (Mean)
Ezetimibe 10 mg + Simvastatin Placebo + Simvastatin 20 mg-32.2
Ezetimibe Placebo + Simvastatin 40 mg-20.8

[back to top]

Change in Low-density-lipoprotein Cholesterol (LDL-C) at 6 Weeks

Percentage change in LDL C from baseline to endpoint after 6 weeks of treatment. (NCT00423579)
Timeframe: Baseline and 6 weeks

Interventionpercentage change (Mean)
Ezetimibe/Simvastatin 10/20 mg + Simvastatin Placebo-26.5
Ezetimibe/Simvastatin Placebo + Simvastatin 40 mg-11.9

[back to top]

Number of Participants Reaching the LDL-C (Low Density Lipoprotein-Cholesterol) Goal (< 100 mg/dl) After 6 Weeks of Treatment

Primary objective is to evaluate the proportion of patients achieving LDL-C target <100 mg/dl recommend in National Cholesterol Education Program Adult Treatment Panel III (NCEP ATP III) after 6 weeks of treatment(vytorin 10/20 vs. atorvastatin 10 mg) (NCT00442897)
Timeframe: After 6 weeks of treatment

InterventionParticipants (Number)
Vytorin89
Atorvastatin63

[back to top]

Number of Participants Reaching the LDL-C Goal (< 100 mg/dl) After 12 Weeks of Treatment

If patients didn't achieve LDL-C <100 mg/dl after 6 weeks of treatment, they received the double dosage of study drug for the next 6 weeks (vytorin 10/40 or atorvastatin 20 mg) and If achieved LDL-C < 100 mg/dl, they received the same dosage of study drug for the next 6 weeks. (NCT00442897)
Timeframe: After 12 weeks of the treatment

InterventionParticipants (Number)
Vytorin85
Atorvastatin63

[back to top]

Stroke

Fatal or non-fatal (NCT00461630)
Timeframe: During scheduled treatment period (median duration 3.9 years)

Interventionparticipants (Number)
ER Niacin/Laropiprant498
Placebo499

[back to top]

Coronary or Non-coronary Revascularisation

(NCT00461630)
Timeframe: During scheduled treatment period (median duration 3.9 years)

Interventionparticipants (Number)
ER Niacin/Laropiprant807
Placebo897

[back to top]

Major Coronary Events

Non-fatal myocardial infarction (MI) or coronary death (NCT00461630)
Timeframe: During scheduled treatment period (median duration 3.9 years)

Interventionparticipants (Number)
ER Niacin/Laropiprant668
Placebo694

[back to top]

Major Vascular Event

Non-fatal myocardial infarction or coronary death, non-fatal or fatal stroke, or revascularisation (NCT00461630)
Timeframe: During scheduled treatment period (median duration 3.9 years)

Interventionparticipants (Number)
ER Niacin/Laropiprant1696
Placebo1758

[back to top]

Mortality

All-cause mortality (NCT00461630)
Timeframe: During scheduled treatment period (median duration 3.9 years)

Interventionparticipants (Number)
ER Niacin/Laropiprant798
Placebo732

[back to top]

Percentage of Patients Achieving a Target of Fasting LDL-C of <2mmol/l at Study End

Fasting LDL-C was the primary efficacy variable. The primary efficacy analysis was based on the proportion of patients achieving a target of <2mmol/l in fasting LDL-C at study end. (NCT00462748)
Timeframe: 6 Weeks

InterventionPercent (Number)
Ezetimibe/Simvastatin67.4
Atorvostatin36.3
Rosuvastatin17.4

[back to top]

Interleukin-6

A commercial ELISA assay detecting IL-6 (Siemens, USA) was applied. (NCT00474123)
Timeframe: Fasting venous blood samples were drawn immediately after randomization and after at the conclusions of the six weeks study period.

Interventionpercentage (Median)
Simvastatin 80 mg0
Simvastatin 20mg/Ezetimibe 10 mg0

[back to top]

Monocyte Chemoattractant Protein (MCP)-1

Serum samples were stored at -70°C and were determined simultaneously by ELISA in order to avoid variation of assay conditions. Commercial ELISA assays detecting MCP-1/ICAM-1 (R&D Systems, Europe, Abingdon, UK). (NCT00474123)
Timeframe: Change from baseline at 6 weeks

Interventionpercentage (Mean)
Simvastatin 80 mg11
Simvastatin 20mg/Ezetimibe 10 mg10

[back to top]

Oxidized Low-Density Lipoprotein Cholesterol

Serum samples were stored at -70°C and were determined simultaneously by ELISA in order to avoid variation of assay conditions. Commercial ELISA assays detecting oxLDL (Mercodia, USA) were applied. (NCT00474123)
Timeframe: Change from baseline at 6 weeks

InterventionPercentage (Mean)
Simvastatin 80 mg-18
Simvastatin 20mg/Ezetimibe 10 mg-15

[back to top]

Platelet Function Analyzer [PFA]-100

Samples were collected in 3.8% sodium citrate (buffered, pH 5.5, Vacutainer, Becton Dickinson, Plymouth, UK) for platelet function tests. Platelet function assays were processed within 2 hours of blood collection. The PFA-100 records the closure time (CT), witch means the time in seconds (s) from the start of the test until the platelet plug occludes the aperture. (NCT00474123)
Timeframe: Change from baseline at 6 weeks

InterventionPercentage (Mean)
Simvastatin 80 mg27
Simvastatin 20mg/Ezetimibe 10 mg8

[back to top]

Soluble CD40 Ligand

A commercial ELISA assay detecting sCD40L (R&D Systems, USA) was applied. Detection limits and intra-assay variability was respectively, as follows: sCD-40L 15.6 pg/mL (intra-assay variability not available). (NCT00474123)
Timeframe: Fasting venous blood samples were drawn immediately after randomization and after at the conclusions of the six weeks study period.

Interventionpercentage (Mean)
Simvastatin 80 mg6
Simvastatin 20mg/Ezetimibe 10 mg6

[back to top]

Soluble Intercellular Adhesion Molecule (sICAM)-1

serum samples were stored at -70°C and were determined simultaneously by ELISA in order to avoid variation of assay conditions. Commercial ELISA assays detecting MCP-1/ICAM-1 (R&D Systems, Europe, Abingdon, UK) (NCT00474123)
Timeframe: Change from baseline at 6 weeks

Interventionpercentage (Mean)
Simvastatin 80 mg10
Simvastatin 20mg/Ezetimibe 10 mg10

[back to top]

C-reactive Protein

Serum was separated by centrifugation from the blood samples. For high-sensitivity C-Reactive Protein measurement, whole venous blood was collected in tubes without anticoagulant and centrifuged at room temperature. Serum C-Reactive Protein was assessed with a high-sensitivity, latex microparticle-enhanced immunoturbidimetric assay (Behring Nephelometer Analyzer System; Behring Diagnostics, Somerville, NJ). (NCT00474123)
Timeframe: Change from baseline at 6 weeks

InterventionPercentage (Median)
Simvastatin 80 mg-16
Simvastatin 20mg/Ezetimibe 10 mg-11

[back to top]

Endothelial Progenitor Cells

Endothelial progenitor cells were evaluated by flow cytometry. Selected cells were positive for CD31, CD34 and VEGFR receptors. (NCT00474123)
Timeframe: Fasting venous blood samples were drawn immediately after randomization and at the conclusions of the six week study period.

Interventionpercentage (Mean)
Simvastatin 80 mg0.4
Simvastatin 20mg/Ezetimibe 10 mg0.1

[back to top]

Triglyceride

(NCT00474123)
Timeframe: Fasting venous blood samples were drawn immediately after randomization and at the conclusions of the six week study period.

Interventionpercentage (Mean)
Simvastatin 80 mg-4
Simvastatin 20mg/Ezetimibe 10 mg-14

[back to top]

LDL Cholesterol

(NCT00474123)
Timeframe: Fasting venous blood samples were drawn immediately after randomization and at the conclusions of the six week study period.

Interventionpercentage (Mean)
Simvastatin 80 mg-28
Simvastatin 20mg/Ezetimibe 10 mg-29

[back to top]

Change in LDL-c From Baseline to 6 Months in Subjects With Type 1 Diabetes Taking Vytorin or Zocor.

Change in LDL-c between Zocor and Vytorin treatment in subjects with Type 1 Diabetes measured at baseline to the 6-month study visit. (NCT00477204)
Timeframe: Baseline to 6 months

Interventionmg/dl (Mean)
Vytorin (Ezetimibe/Simvastatin)-67
Zocor (Simvastatin)-6

[back to top]

Percent Change in Low Density Lipoprotein-Cholesterol (LDL-C) at Study Endpoint After Six Weeks of Treatment

Percent Change in LDL-C at study endpoint after six weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Least Squares Mean)
Ezetemibe + Simvastatin-27.66
Rosuvastatin-16.94

[back to top]

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

Percent change from baseline in non HDL-C at study endpoint after 6 weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Least Squares Mean)
Ezetemibe + Simvastatin-23.42
Rosuvastatin-14.01

[back to top]

Percent Change From Baseline in High-sensitivity C (Hs-C) Reactive Protein

Percent change from baseline in hs-C reactive protein at study endpoint after 6 weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Median)
Ezetemibe + Simvastatin-8.33
Rosuvastatin0.00

[back to top]

Percent Change From Baseline in Triglycerides.

Percent change from baseline in triglycerides at study endpoint after 6 weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Median)
Ezetemibe + Simvastatin-11.00
Rosuvastatin-5.26

[back to top]

The Percentage of Participants Achieving Designated Low Density Lipoprotein-Cholesterol (LDL-C) Levels After 6 Weeks of Treatment

"The percentage of participants who achieved a target LDL-C goal of < 100 mg/dL, of <70 mg/dL, and of <77 mg/dL at study endpoint after six weeks of treatment.~The numerator is the number of participants in a treatment group who achieved a target LDL-C goal and the denominator is the total number of participants within that treatment group." (NCT00479713)
Timeframe: after 6 weeks of treatment

,
InterventionPercent of participant population (Number)
LDL-C <100LDL-C <70
Ezetemibe + Simvastatin72.4625.25
Rosuvastatin56.2311.11

[back to top]

Percent Change From Baseline in Apolipoprotein B

Percent change from baseline in apolipoprotein (Apo) B at study endpoint after 6 weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Least Squares Mean)
Ezetemibe + Simvastatin-17.87
Rosuvastatin-9.77

[back to top]

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

Percent change from baseline in total cholesterol/HDL-C ratio at study endpoint after 6 weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Least Squares Mean)
Ezetemibe + Simvastatin-17.76
Rosuvastatin-11.51

[back to top]

Percent Change From Baseline in Low Density Lipoprotein-Cholesterol (LDL-C)/High Density Lipoprotein-Cholesterol (HDL-C) Ratio

Percent change from baseline in LDL-C/HDL-C ratio at study endpoint after 6 weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Least Squares Mean)
Ezetemibe + Simvastatin-27.41
Rosuvastatin-17.82

[back to top]

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

Percent change from baseline in HDL-C at study endpoint after 6 weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Least Squares Mean)
Ezetemibe + Simvastatin2.12
Rosuvastatin3.03

[back to top]

Percent Change From Baseline in Total Cholesterol

Percent change from baseline in total cholesterol at study endpoint after 6 weeks of treatment is calculated as the difference between week 6 measure and baseline measure divided by baseline measure *100. (NCT00479713)
Timeframe: Baseline and 6 weeks

Interventionpercent change from baseline (Least Squares Mean)
Ezetemibe + Simvastatin-17.53
Rosuvastatin-10.33

[back to top]

CPK

(NCT00481351)
Timeframe: 12 week

Interventionmg/dl (Mean)
group1 Ezetimibe169
Group 2 Simvastatin131

[back to top]

High Density Lipoprotein

(NCT00481351)
Timeframe: 12 week

Interventionmg/dl (Mean)
group1 Ezetimibe51.31
Group 2 Simvastatin44.33

[back to top]

Low Density Lipoprotein

(NCT00481351)
Timeframe: 12week

Interventionmg/dl (Mean)
group1 Ezetimibe74.85
Group 2 Simvastatin71.92

[back to top]

Total Cholesterol

(NCT00481351)
Timeframe: 12 week

Interventionmg/dl (Mean)
group1 Ezetimibe152.61
Group 2 Simvastatin148.29

[back to top]

Alanine Aminotransferase

(NCT00481351)
Timeframe: 12 weeks

Interventionmg/dl (Mean)
group1 Ezetimibe30.46
Group 2 Simvastatin18.33

[back to top]

Change in Lower Density Lipoprotein Cholesterol From Baseline After 8 Weeks.

(NCT00496730)
Timeframe: Baseline and Week 8

Interventionmg/dL (Mean)
Vytorin83.52
Atorvastatin98.27

[back to top]

Mean Percent Change of Low Density Lipoprotein-Cholesterol (LDL-C) From Baseline After 8 Weeks.

(NCT00496730)
Timeframe: Baseline and 8 Weeks

InterventionPercent of Baseline Value (Mean)
Vytorin-49.29
Atorvastatin-38.05

[back to top]

Number of Patients Attaining LDL-C Goal After 8 Weeks Treatment.

"Number of Patients Attaining LDL-C Goal After 8 Weeks Treatment.~LDL-C goal is based on National Cholesterol Education Program (NCEP) III guideline (LDL-C goals and cutpoints for therapeutic life changes and drug Therapy in different risk)." (NCT00496730)
Timeframe: Baseline and 8 weeks

InterventionParticipants attaining LDL-C goal (Number)
Vytorin105
Atorvastatin93

[back to top]

Percent Change in Apolipoprotein A1 (ApoA-1) After 6 Weeks Combination Treatment

Percent change in ApoA-1 = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E103.8100
R20 to R20 + E102.6800
S40 to S40 + E101.4900
S80 to S80 + E102.1300

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) After 6 Weeks Combination Treatment

Percent change in LDL-C = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-59.7200
R20 to R20 + E10-63.4800
S40 to S40 + E10-55.2200
S80 to S80 + E10-57.4200

[back to top]

Percent Change in Apolipoprotein B (ApoB) After 6 Weeks Combination Treatment

Percent change in ApoB = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-46.1100
R20 to R20 + E10-49.5000
S40 to S40 + E10-41.9500
S80 to S80 + E10-44.1700

[back to top]

Percent Change in ApoB/ApoA-1 After 6 Weeks Combination Treatment

Percent change in ApoB/ApoA-1 = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-47.3900
R20 to R20 + E10-50.2400
S40 to S40 + E10-42.5400
S80 to S80 + E10-44.7600

[back to top]

Percent Change in Triglycerides (TG) After 6 Weeks Combination Treatment

Percent change in TG = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-28.8500
R20 to R20 + E10-35.0000
S40 to S40 + E10-22.9500
S80 to S80 + E10-25.8200

[back to top]

Percent Change in Total Cholesterol (TC) After 6 Weeks Combination Treatment

Percent change in TC = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-43.0000
R20 to R20 + E10-46.6300
S40 to S40 + E10-39.5600
S80 to S80 + E10-41.7100

[back to top]

Percent Change in TC/HDL-C After 6 Weeks Combination Treatment

Percent change in TC/HDL-C = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-45.5200
R20 to R20 + E10-49.4600
S40 to S40 + E10-41.2700
S80 to S80 + E10-43.4500

[back to top]

Percent Change in Non-high-density Lipoprotein Cholesterol (nonHDL-C) After 6 Weeks Combination Treatment

Percent change in nonHDL-C = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-54.6500
R20 to R20 + E10-58.9100
S40 to S40 + E10-49.9300
S80 to S80 + E10-52.3700

[back to top]

Percent Change in Non-HDL-C/HDL-C After 6 Weeks Combination Treatment

Percent change in non-HDL-C/HDL-C = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-56.4200
R20 to R20 + E10-60.8900
S40 to S40 + E10-51.1100
S80 to S80 + E10-53.5100

[back to top]

Percent Change in LDL-C/HDL-C After 6 Weeks Combination Treatment

Percent change in LDL-C/HDL-C = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-61.4700
R20 to R20 + E10-65.2500
S40 to S40 + E10-57.1300
S80 to S80 + E10-58.6600

[back to top]

Percent Change in LDL-C After 6 Weeks Monotherapy

Percent change in LDL-C = (Monotherapy treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on monotherapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10-46.4900
R20 to R20 + E10-53.5900
S40 to S40 + E10-40.8600
S80 to S80 + E10-46.3500

[back to top]

Percent Change in High-sensitivity C-reactive Protein (Hs-CRP) After 6 Weeks Combination Treatment

Percent change in hs-CRP = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E10107.1200
R20 to R20 + E10-9.5300
S40 to S40 + E1015.0300
S80 to S80 + E100.4200

[back to top]

Percent Change in High-density Lipoprotein Cholesterol (HDL-C) After 6 Weeks Combination Treatment

Percent change in HDL-C = (Combination treatment value - Baseline value)/Baseline value*100 (NCT00525824)
Timeframe: Mean of Weeks 4 and 6 on combination therapy (Last observation carried forward)

InterventionPercentage (Mean)
R10 to R10 + E106.4100
R20 to R20 + E107.4600
S40 to S40 + E103.9200
S80 to S80 + E104.3400

[back to top]

Percentage of Patients Who Achieved LDL-C <100 mg/dL at Week 12

(NCT00535405)
Timeframe: 12 Weeks

InterventionPercent of Patients (Mean)
Atorvastatin 10 mg58.7
Ezetimibe 10 mg/Simvastatin 20 mg83.6
Atorvastatin 20 mg76.9
Ezetimibe 10 mg/Simvastatin 40 mg90.3
Atorva 40 mg79.5

[back to top]

Percent Change From Baseline in Low Density Lipoprotein (LDL-C) at Week 12

(NCT00535405)
Timeframe: Baseline and 12 weeks

InterventionPercent change in LDL-C (Least Squares Mean)
Atorvastatin 10 mg-39.5
Ezetimibe 10 mg/Simvastatin 20 mg-54.2
Atorvastatin 20 mg-46.6
Ezetimibe 10 mg/Simvastatin 40 mg-59.1
Atorva 40 mg-50.8

[back to top]

Percentage of Patients Who Achieved LDL-C <70 mg/dL at Week 12

(NCT00535405)
Timeframe: 12 weeks

InterventionPercent of Patients (Mean)
Atorvastatin 10 mg9.9
Ezetimibe 10 mg/Simvastatin 20 mg51.3
Atorvastatin 20 mg26.1
Ezetimibe 10 mg/Simvastatin 40 mg68.2
Atorva 40 mg38.1

[back to top]

Percentage of Patients Without Atherosclerosis Vascular Disease (AVD) Who Achieved LDL-C <100 mg/dL or Patients With AVD Who Achieved LDL-C <70 mg/dL at Week 12

Patients with AVD Who Achieved LDL-C <70 mg/dL. AVD was defined as a history of myocardial infarction, stable angina, coronary artery procedures or evidence of clinically significant myocardial ischemia. (NCT00535405)
Timeframe: 12 Weeks

InterventionPercent of Patients (Mean)
Atorvastatin 10 mg45.0
Ezetimibe 10 mg/Simvastatin 20 mg69.0
Atorvastatin 20 mg61.3
Ezetimibe 10 mg/Simvastatin 40 mg82.1
Atorva 40 mg69.9

[back to top]

Percentage of Patients With High Risk for CHD Who Achieved LDL-C <70 mg/dL at Week 12

Risk was assessed utilizing a history of established CHD or CHD risk equivalent and Framingham Risk scoring. (NCT00535405)
Timeframe: 12 Weeks

InterventionPercent of Patients (Mean)
Atorvastatin 10 mg10.9
Ezetimibe 10 mg/Simvastatin 20 mg54.3
Atorvastatin 20 mg28.9
Ezetimibe 10 mg/Simvastatin 40 mg69.2
Atorva 40 mg38.2

[back to top]

Percentage of Patients With AVD Who Achieved LDL-C <70 mg/dL at Week 12

Patients with AVD Who Achieved LDL-C <70 mg/dL. AVD was defined as a history of myocardial infarction, stable angina, coronary artery procedures or evidence of clinically significant myocardial ischemia. (NCT00535405)
Timeframe: 12 Weeks

InterventionPercent of Patients (Mean)
Atorvastatin 10 mg10.0
Ezetimibe 10 mg/Simvastatin 20 mg44.4
Atorvastatin 20 mg31.6
Ezetimibe 10 mg/Simvastatin 40 mg65.8
Atorva 40 mg44.4

[back to top]

Alzheimer's Disease Assessment Scale-cognitive Component-Japanese Version(ADAS-Jcog)

Alzheimer's Disease Assessment Scale-cognitive component-Japanese version is a cognitive test for Alzheimer's disease. This test includes some aspects that assess memory ,orientation, language, praxis, and so on. The possible range of this test is 0-70 points.Higher total points indicate more impairment. (NCT00548145)
Timeframe: baseline and 12 months

,
Interventionscores on a scale (Mean)
baseline12month
Cholesterol-lowering Medicine Other Than Statin19.5020.59
Pitavastatin18.5920.20

[back to top]

Absolute Change From Baseline in Percent Hepatic Fat

Absolute change from Baseline in percent hepatic fat (NCT00559962)
Timeframe: Baseline and 12 weeks on study drug

,
InterventionPercent of Hepatic Fat (Mean)
Placebo0.03
AEGR-733 5 mg4.72
Placebo0.03
AEGR-733 2.5 mg4.95
AEGR-733 5 mg4.72
AEGR-733 7.5 mg3.94
AEGR-733 10 mg7.86
AEGR-733 5 mg + Atorvastatin 20 mg3.68
AEGR-733 5 mg + Fenofibrate 145 mg7.70
AEGR-733 5 mg + Ezetimibe 10 mg7.55

[back to top]

Plaque Volume

SFA plaque volume (NCT00587678)
Timeframe: 2 years

Interventioncm^3 (Mean)
Simvastatin 40mg10.5
Simvastatin 40mg/Ezetimibe 10 mg10.5
Ezetimibe 10mg10.8

[back to top]

Triglycerides

(NCT00587678)
Timeframe: 2 years

Interventionmg/dl (Mean)
Simvastatin 40mg171
Simvastatin 40mg/Ezetimibe 10 mg119
Ezetimibe 10mg152

[back to top]

V02 - Maximal Oxygen Consumption

(NCT00587678)
Timeframe: 2 years

Interventionml/min/kg (Mean)
Simvastatin 40mg14.8
Simvastatin 40mg/Ezetimibe 10 mg12.1
Ezetimibe 10mg12.3

[back to top]

Total Cholesterol

(NCT00587678)
Timeframe: 2 years

Interventionmg/dl (Mean)
Simvastatin 40mg152
Simvastatin 40mg/Ezetimibe 10 mg136
Ezetimibe 10mg144

[back to top]

6-minute Walk Distance

(NCT00587678)
Timeframe: 2 years

Interventionft. (Mean)
Simvastatin 40mg1078
Simvastatin 40mg/Ezetimibe 10 mg1038
Ezetimibe 10mg1099

[back to top]

High Density Lipoprotein Cholesterol

(NCT00587678)
Timeframe: 2 years

Interventionmg/dl (Mean)
Simvastatin 40mg44
Simvastatin 40mg/Ezetimibe 10 mg46
Ezetimibe 10mg43

[back to top]

Log Treadmill Exercise Time

(NCT00587678)
Timeframe: 2 years

Interventionlog time in seconds (Mean)
Simvastatin 40mg5.92
Simvastatin 40mg/Ezetimibe 10 mg5.79
Ezetimibe 10mg5.78

[back to top]

Low Density Lipoprotein Cholesterol

(NCT00587678)
Timeframe: 2 years

Interventionmg/dl (Mean)
Simvastatin 40mg83
Simvastatin 40mg/Ezetimibe 10 mg68
Ezetimibe 10mg77

[back to top]

Magnetic Resonance Angiographic Index

MRA index is a measure of angiographic severity of disease. 0 = no disease and 4 is severe disease. (NCT00587678)
Timeframe: 2 years

Interventionunits on scale (0 = normal, 4 = worst) (Mean)
Simvastatin 40mg0.71
Simvastatin 40mg/Ezetimibe 10 mg1.32
Ezetimibe 10mg0.63

[back to top]

Perfusion Index

Perfusion index is a MRI measure of calf muscle perfusion indexed to the arterial input. The value is between 0 and 1 with 0 being worst and 1 being best. (NCT00587678)
Timeframe: 2 years

InterventionUnits on a scale (0 = worst, 1 = best) (Mean)
Simvastatin 40mg0.34
Simvastatin 40mg/Ezetimibe 10 mg0.37
Ezetimibe 10mg0.54

[back to top]

Phosphocreatine Recovery Time Constant - the Time it Takes for Phosphocreatine Levels to Recover to Plateau.

Phosphocreatine recovery time constant is the time it takes for phosphocreatine levels to recover to plateau after the completion of exercise. This ranges from 20 to 1000 seconds. 20-40 seconds is normal and any value over 40 seconds is abnormal. (NCT00587678)
Timeframe: 2 years

Interventionseconds (Mean)
Simvastatin 40mg84
Simvastatin 40mg/Ezetimibe 10 mg73
Ezetimibe 10mg74

[back to top]

Mean Percent Change in Apolipoprotein AI (apoAI) From Baseline to Final Visit

[(Week 12 apoAI minus baseline apoAI)/baseline apoAI] x 100 (NCT00639158)
Timeframe: Baseline to 12 weeks (Final Visit)

InterventionPercent change (Mean)
ABT-335 + 40 mg Atorvastatin + 10 mg Ezetimibe1.8
Placebo + 40 mg Atorvastatin + 10 mg Ezetimibe-1.3

[back to top]

Mean Percent Change in Apolipoprotein B (apoB) From Baseline to Final Visit

[(Week 12 apoB minus baseline apoB)/baseline apoB] x 100 (NCT00639158)
Timeframe: Baseline to 12 weeks (Final Visit)

InterventionPercent change (Mean)
ABT-335 + 40 mg Atorvastatin + 10 mg Ezetimibe-49.1
Placebo + 40 mg Atorvastatin + 10 mg Ezetimibe-44.7

[back to top]

Mean Percent Change in Apolipoprotein CIII (apoCIII) From Baseline to Final Visit

[(Week 12 apoCIII minus baseline apoCIII)/baseline apoCIII] x 100 (NCT00639158)
Timeframe: Baseline to 12 weeks (Final Visit)

InterventionPercent change (Mean)
ABT-335 + 40 mg Atorvastatin + 10 mg Ezetimibe-42.5
Placebo + 40 mg Atorvastatin + 10 mg Ezetimibe-25.3

[back to top]

Mean Percent Change in High-Density Lipoprotein Cholesterol (HDL-C) From Baseline to Final Visit

[(Week 12 HDL-C minus baseline HDL-C)/baseline HDL-C] x 100 (NCT00639158)
Timeframe: Baseline to 12 weeks (Final Visit)

InterventionPercent change (Mean)
ABT-335 + 40 mg Atorvastatin + 10 mg Ezetimibe13.0
Placebo + 40 mg Atorvastatin + 10 mg Ezetimibe4.2

[back to top]

Mean Percent Change in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) From Baseline to Final Visit

[(Week 12 non-HDL-C minus baseline non-HDL-C)/baseline non-HDL-C] x 100 (NCT00639158)
Timeframe: Baseline to 12 weeks (Final Visit)

InterventionPercent change (Mean)
ABT-335 + 40 mg Atorvastatin + 10 mg Ezetimibe-55.6
Placebo + 40 mg Atorvastatin + 10 mg Ezetimibe-51.0

[back to top]

Median Percent Change in High-Sensitivity C-Reactive Protein (hsCRP) From Baseline to Final Visit

[(Week 12 hsCRP minus baseline hsCRP)/baseline hSCRP] x 100 (NCT00639158)
Timeframe: Baseline to 12 weeks (Final Visit)

InterventionPercent change (Median)
ABT-335 + 40 mg Atorvastatin + 10 mg Ezetimibe-52.1
Placebo + 40 mg Atorvastatin + 10 mg Ezetimibe-40.3

[back to top]

Median Percent Change in Triglycerides From Baseline to Final Visit

[(Week 12 triglycerides minus baseline triglycerides)/baseline triglycerides] x 100 (NCT00639158)
Timeframe: Baseline to 12 Weeks (Final Visit)

InterventionPercent change (Median)
ABT-335 + 40 mg Atorvastatin + 10 mg Ezetimibe-57.3
Placebo + 40 mg Atorvastatin + 10 mg Ezetimibe-39.7

[back to top]

Mean Percent Change in Very Low-Density Lipoprotein Cholesterol (VLDL-C) From Baseline to Final Visit

[(Week 12 VLDL-C minus baseline VLDL-C)/baseline VLDL-C] x 100 (NCT00639158)
Timeframe: Baseline to 12 weeks (final visit)

InterventionPercent change (Mean)
ABT-335 + 40 mg Atorvastatin + 10 mg Ezetimibe-57.8
Placebo + 40 mg Atorvastatin + 10 mg Ezetimibe-41.1

[back to top]

Percentage Change in Low Density Lipoprotein-Cholesterol (LDL-C) From Baseline at Study Endpoint, After 8 Weeks of Treatment

(NCT00652327)
Timeframe: Assessed at the end of 8 weeks of treatment (from baseline to endpoint)

InterventionPercentage change (Mean)
Ezetimibe + Statin-26.56
Double Statin-9.7

[back to top]

Number of Participants With Adverse Events and Adverse Reactions

"An adverse event is any unfavorable medical event occurring in a subject to whom an investigational product is administered, and a causal relationship between the administered investigational product and an adverse event is not always clarified.~That is, an adverse event is any unfavorable or unintended sign (including an abnormal change in laboratory test values), symptom, or disease, and a causal relationship to the relevant investigational product is not considered.~Any adverse event that was treatment-related was considered an adverse reaction." (NCT00653523)
Timeframe: Throughout 1 year of study

InterventionParticipants (Number)
Adverse EventsAdverse Reactions
Ezetimibe + Simvastatin14336

[back to top]

Number of Participants With Adverse Events and Adverse Reactions

"An adverse event is any unfavorable medical event occurring in a subject to whom an investigational product is administered, and a causal relationship between the administered investigational product and an adverse event is not always clarified.~That is, an adverse event is any unfavorable or unintended sign (including an abnormal change in laboratory test values), symptom, or disease, and a causal relationship to the relevant investigational product is not considered.~Any adverse event that was considered treatment-related was considered an adverse reaction." (NCT00654095)
Timeframe: Throughout 1 year of study

InterventionParticipants (Number)
Adverse EventsAdverse Reactions
Ezetimibe + Atorvastatin14161

[back to top]

Mean Change From Baseline of Low Density Lipoprotein-Cholesterol (LDL-C) at Week 6

(NCT00654628)
Timeframe: Baseline and week 6

Interventionmg/dL (Mean)
Ezetimibe/Simvastatin 10/20 mg-82.0

[back to top]

Mean Percent Change From Baseline of High Density Lipoprotein-C (HDL-C) at Week 12

(NCT00654628)
Timeframe: Baseline and week 12

InterventionPercent Change (Mean)
Ezetimibe/Simvastatin 10/20 mg9.4

[back to top]

Mean Percent Change From Baseline of High Density Lipoprotein-C (HDL-C) at Week 6

(NCT00654628)
Timeframe: Baseline and week 6

InterventionPercent Change (Mean)
Ezetimibe/Simvastatin 10/20 mg4.5

[back to top]

Mean Percent Change From Baseline of Low Density Lipoprotein-Cholesterol (LDL-C) at Week 12

(NCT00654628)
Timeframe: Baseline and week 12

InterventionPercent Change (Mean)
Ezetimibe/Simvastatin 10/20 mg-53.8

[back to top]

Mean Percent Change From Baseline of Low Density Lipoprotein-Cholesterol (LDL-C) at Week 6

(NCT00654628)
Timeframe: Baseline and week 6

InterventionPercent Change (Mean)
Ezetimibe/Simvastatin 10/20 mg-51.4

[back to top]

Mean Percent Change From Baseline of Total-Cholesterol (TC) at Week 12

(NCT00654628)
Timeframe: Baseline and week 12

InterventionPercent Change (Mean)
Ezetimibe/Simvastatin 10/20 mg-39.5

[back to top]

Mean Percent Change From Baseline of Total-Cholesterol (TC) at Week 6

(NCT00654628)
Timeframe: Baseline and week 6

InterventionPercent Change (Mean)
Ezetimibe/Simvastatin 10/20 mg-38.1

[back to top]

Mean Percent Change of Triglycerides From Baseline at Week 12

(NCT00654628)
Timeframe: Baseline and week 12

InterventionPercent Change (Median)
Ezetimibe/Simvastatin 10/20 mg-24.7

[back to top]

Mean Percent Change of Triglycerides From Baseline at Week 6

(NCT00654628)
Timeframe: Baseline and week 6

InterventionPercent Change (Median)
Ezetimibe/Simvastatin 10/20 mg-22.2

[back to top]

The Percentage of Participants Achieving Low Density Lipoprotein-C (LDL-C) Treatment Goal After 12-week Treatment.

Goal attainment percentage of LDL-C after 12-week treatment. LDL-C goal attainment was based on National Cholesterol Education program (NCEP) Adult Treatment Panel (ATP) III guidelines (2004). Newly Diagnosed Dyslipidemia Patients Including: 1)Intermediate Risk (>2 Risk Factors) with Total Cholesterol above 200 mg/dL or Low Density Lipoprotein C (LDL-C) level >130 who failed a 3-month diet control period, or 2) high risk patients with a history of coronary artery disease or diabetes having a total cholesterol >200 mg/dl or LDL-C level >130 mg/dl. (NCT00654628)
Timeframe: Baseline and week 12

InterventionPercentage of participants (Number)
Ezetimibe/Simvastatin 10/20 mg87.8

[back to top]

The Percentage of Participants Achieving Low Density Lipoprotein-C (LDL-C) Treatment Goal After 6-week Treatment.

Goal attainment percentage of LDL-C after 6-week treatment. LDL-C goal attainment was based on National Cholesterol Education program (NCEP) Adult Treatment Panel (ATP) III guidelines (2004). Newly Diagnosed Dyslipidemia Patients Including: 1)Intermediate Risk (>2 Risk Factors) with Total Cholesterol above 200 mg/dL or Low Density Lipoprotein C (LDL-C) level >130 who failed a 3-month diet control period, or 2) high risk patients with a history of coronary artery disease or diabetes having a total cholesterol >200 mg/dl or LDL-C level >130 mg/dl. (NCT00654628)
Timeframe: Baseline and week 6

InterventionPercentage of participants (Number)
Ezetimibe/Simvastatin 10/20 mg90.4

[back to top]

Mean Change From Baseline of Low Density Lipoprotein-Cholesterol (LDL-C) at Week 12

(NCT00654628)
Timeframe: Baseline and week 12

Interventionmg/dL (Mean)
Ezetimibe/Simvastatin 10/20 mg-85.6

[back to top]

Effect of Intensive Lipid Modification Medication Therapy on Progression of Atherosclerosis and Restenosis of Femoral Arteries Measured Using High Resolution Magnetic Resonance Imaging (MRI) to Examine the Femoral Artery for Progression of Atherosclerosis

"The primary outcome variable was the change in superficial femoral artery (SFA) wall volume over 24-months, as determined by MRI. The 24-month changes in SFA lumen and SFA total vessel volumes were also analyzed.~Analysis details: A total of 102 patients were randomized. 87 patients completed baseline MRI. Between randomization and the baseline visit, 1 patient withdrew from the study, 8 patients opted out from baseline imaging, and 6 additional patients declined blood collection at baseline. The multilevel models (primary endpoint) used all available imaging data (n=91), including patients who only completed baseline imaging (n=20) or completed at least 2 imaging visits other than baseline (n=4)." (NCT00687076)
Timeframe: Measured at baseline and 24 Months

Interventionmm^3, at 24-months (Mean)
Triple Therapy58.1
Mono Therapy60.5

[back to top]

Change in Total Cholesterol (mg/dl) From Baseline to Month 12

Lipids: Total cholesterol (mg/dl); Lipid Data at 12-Months (change from baseline) [mg/dl]. (NCT00687076)
Timeframe: Measured at baseline and 12 months

Interventionmg/dl (Median)
Triple Therapy-30.0
Mono Therapy-7.5

[back to top]

Change From Baseline in Total Cholesterol, From Fasting Plasma Samples

plasma levels of total cholesterol (NCT00701727)
Timeframe: 7 weeks

Interventionmg/dL total cholesterol (Mean)
Placebo219
Ezetimibe187

[back to top]

Low-density Lipoprotein (LDL);

Change from baseline in plasma low-density lipoprotein(LDL), measured in fasting blood samples (NCT00701727)
Timeframe: 7 weeks

Interventionmg/dL LDL (Mean)
Placebo148
Ezetimibe116

[back to top]

Cholesterol Efflux Rate (Ra Cholesterol)

The efflux, or mobilization, rate of cholesterol from peripheral tissues into the plasma will be measured as mg/kg/hr. An IV infusion of [13C2] cholesterol mixed in 10% Intralipid® and 10 % ethanol is given piggy-backed into normal saline over 20 hours (4pm - 12 noon). This is used to determine rate of appearance (Ra) cholesterol, which will be measured by dilution of infused [13C2] cholesterol during the plateau phase of plasma enrichment (approximately the last 4 hours of the infusion), as well as to provide the plasma cholesterol that will be traced into biliary sterols. (NCT00701727)
Timeframe: 7 weeks

Interventionmg/kg/hr cholesterol (Mean)
Placebo4.6
Ezetimibe4.4

[back to top]

de Novo Cholesterol Synthesis (DNC)

Plasma DNC will be measured following the isotope infusion of deuterated water, expressed as %. (NCT00701727)
Timeframe: 7 weeks

Intervention%/day plasma DNC (Mean)
Placebo3.4
Ezetimibe4.7

[back to top]

Fecal Excretion of Plasma-derived Cholesterol

"(Fecal excretion of plasma-derived cholesterol):The following measurements will be made following isotope infusion:~The composition of fecal neutral and acidic sterols will be measured as % of total.~The excretion rate of fecal neutral and acidic sterols will be measured as mg/day.~The isotopic enrichment of both fecal neutral and acidic sterols will be measured as atomic percent excess (% APE).~Fecal isotope excretion, or recovery, of plasma-derived cholesterol will be calculated as %/day." (NCT00701727)
Timeframe: 7 weeks

Interventionmg/day cholesterol excreted (Mean)
Placebo1593
Ezetimibe1950

[back to top]

High-density Lipoprotein (HDL)

Change from baseline in plasma HDL, measured in fasting blood samples (NCT00701727)
Timeframe: 7 weeks

Interventionmg/dL HDL (Mean)
Placebo46
Ezetimibe45

[back to top]

Triglycerides (TG)

Change from baseline in plasma triglycerides, measured in fasting blood samples (NCT00701727)
Timeframe: 7 weeks

Interventionmg/dL TG (Mean)
Placebo128
Ezetimibe121

[back to top]

Safety as Measured by Number of Subjects With at Least One Adverse Event

Evaluation of the overall safety of ezetimibe as measured by number of subjects who experienced at least one adverse event (NCT00704535)
Timeframe: 28 days after Visit 1

Interventionsubjects (Number)
Ezetimibe as Prescribed by the Physician in Normal Practice45

[back to top]

To Evaluate the Efficacy of Ezetimibe in Lowering Serum Cholesterol Levels 28 Days After Visit 1 (Baseline)

Change in mean total cholesterol values (NCT00704535)
Timeframe: 28 days after Visit 1

Interventionmg/dL (Mean)
Ezetimibe as Prescribed by the Physician in Normal Practice-62.70

[back to top]

Safety as Measured by Adverse Event Relatedness to Study Drug as Reported by the Investigator.

To evaluate the overall safety of ezetimibe as measured by adverse event relatedness to study drug as reported by the investigator. (NCT00704535)
Timeframe: 28 days after Visit 1

Interventionadverse events (Number)
Related to treatmentNot related to treatmentRelatedness not reported
Ezetimibe as Prescribed by the Physician in Normal Practice20826

[back to top]

Safety as Measured by Severity of Adverse Events as Determined by the Investigator

To evaulate the safety of ezetimibe as measured by severity of adverse events, as determined by the investigator (NCT00704535)
Timeframe: 28 days after Visit 1

Interventionadverse events (Number)
Mild adverse eventsModerate adverse eventsSevere adverse events
Ezetimibe as Prescribed by the Physician in Normal Practice4941

[back to top]

Safety as Measured by Dose Adjustment Upon Incidence of an Adverse Event

To evaluate the overall safety of ezetimibe as measured by action taken by the investigator upon incidence of an adverse event (NCT00704535)
Timeframe: 28 days after Visit 1

Interventionadverse event (Number)
Treatment dosage unchangedTreatment dosage reducedTreatment temporarily discontinued
Ezetimibe as Prescribed by the Physician in Normal Practice4563

[back to top]

Safety as Measured by Outcome of Adverse Events

To evaluate overall safety of ezetimibe as measured by outcome of adverse events (NCT00704535)
Timeframe: 28 days after Visit 1

Interventionadverse events (Number)
Adverse event clearedAdverse event still presentAdverse event outcome not reported
Ezetimibe as Prescribed by the Physician in Normal Practice4923

[back to top]

Tolerability as Measured by Subject Self-assessment

Evaluation of the overall tolerability of ezetimibe as measured by subject self-assessment (NCT00704535)
Timeframe: 28 days after Visit 1

Interventionsubjects (Number)
ExcellentVery goodGoodFairPoorNot reported
Ezetimibe as Prescribed by the Physician in Normal Practice1325195671354354

[back to top]

Safety as Measured by Number and Type of Adverse Events.

Evaluation of the overall safety of ezetimibe as measured by the number and type of adverse events. (NCT00704535)
Timeframe: 28 days after Visit 1

Interventionadverse events (Number)
gastrointestinal upsetabdominal painbody weaknessconstipationcrampy abdominal paindiarrheadizzinessepigastric discomfortflatulenceheadacheleg cramps/muscle painmild myalgiamyalgianauseaoily flatusurticariavague abdominal discomfort
Ezetimibe as Prescribed by the Physician in Normal Practice241316412131247111

[back to top]

Number of Participants Reporting Adverse Events

Safety and tolerability of LDL lowering with co-administration therapy as measured by the number of participants reporting adverse events (AE). (AE defined as any untoward medical occurrence or unfavorable and unintended sign in a subject administered the pharmaceutical product whether or not considered related to the use of that product.) (NCT00705081)
Timeframe: 4-6 weeks after the first visit

InterventionParticipants (Number)
Not Previously Treated1
Previously Treated With Statin1

[back to top]

Intensity of Adverse Events Reported

Intensity of adverse events reported after co-administration therapy (NCT00705081)
Timeframe: 4-6 weeks after the first visit

,
InterventionParticipants (Number)
MildModerateSevere
Not Previously Treated100
Previously Treated With Statin100

[back to top]

Participants Achieving Low-density Lipoprotein-cholesterol (LDL-C) Target Levels With Co-administration Therapy

Achievement of LDL-C target levels as determined by physician (NCT00705081)
Timeframe: 4-6 weeks after the first visit

InterventionParticipants (Number)
Not Previously Treated101
Previously Treated With Statin106

[back to top]

Percentage of Patients Per Group Who Reach Goal for Total Cholesterol (TC) (< 4.5 mmol/L) According to All-Russian Scientific Cardiologists Society (ARSCS) Recommendations by End of Observation

Statins included in this outcome measure included: 1. statin dose (atorvastatin, fluvastatin, rosuvastatin, simvastatin) titration. 2. shift to a different (atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastin, simvastatin) statin . 3. Ezetimibe added to existing statin (atorvastatin, lovastatin, rosuvastatin, simvastatin). (NCT00730132)
Timeframe: Visit 2 (Month 2, end of observation)

InterventionPercentage of patients (Number)
Ezetimibe Added to Existing Statin50.4
Statin Dose Titration33.5
New Statin37.4

[back to top]

Percentage of Patients Per Group Who Reached Goal for Low Density Lipoprotein (LDL-C) (< 2.6 mmol/L) According to ARSCS Recommendations by End of Observation

(NCT00730132)
Timeframe: Visit 2 (Month 2, end of observation)

InterventionPercentage of patients (Number)
Ezetimibe Added to Existing Statin42.3
Statin Dose Titration26.3
New Statin33.9

[back to top]

Percentage of Relative Change of LDL-C Level Measured on Visit 2 Compared With the Baseline (Visit 1) in Each of the Three Therapy Groups

(NCT00730132)
Timeframe: Visit 2 (Month 2, end of observation) and Visit 1 (Day 0, baseline)

Interventionmmol/L (Mean)
Ezetimibe Added to Existing Statin32.06
Statin Dose Titration26.81
New Statin28.24

[back to top]

Percentage of Relative Change of Total Cholesterol (TC) Level Measured on Visit 2 Compared With the Baseline (Visit 1) in Each of the Three Therapy Groups

(NCT00730132)
Timeframe: Visit 2 (Month 2, end of observation) and Visit 1 (Day 0, baseline)

Interventionmmol/L (Mean)
Ezetimibe Added to Existing Statin25.76
Statin Dose Titration20.01
New Statin22.82

[back to top]

Percentage of Patients Receiving Each Variant of Modified Lipid-lowering Therapy: Statin Dose Titration, Administration of a New Statin, Administration of a Ezetimibe in Addition to a Current Statin.

Statins included: 1. statin dose (atorvastatin, fluvastatin, rosuvastatin, simvastatin) titration . 2. shift to a (atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastin, simvastatin) different statin . 3. Ezetimibe added to existing statin (atorvastatin, lovastatin, rosuvastatin, simvastatin). (NCT00730132)
Timeframe: During the study

InterventionPercentage of patients (Number)
Statin dose titrationNew statin administeredEzetimibe added on to existing statin
All Participants Analyzed32.142.425.5

[back to top]

Total Cholesterol

Total cholesterol fasting (NCT00762229)
Timeframe: 4 weeks

Interventionmg/dL (Mean)
Ezetimibe 10 mg180
Ezetimibe 5 mg167

[back to top]

LDL Cholesterol

LDL cholesterol (NCT00762229)
Timeframe: 4 weeks

Interventionmg/dL (Mean)
Ezetimibe 10 mg103
Ezetimibe 5 mg97

[back to top]

Percent Change From Baseline in LDL-Cholesterol/HDL-Cholesterol Ratio

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-28.77
Atorvastatin 40 mg-12.66

[back to top]

Percent Change From Baseline in Low Density Lipoprotein (LDL)-C

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-26.81
Atorvastatin 40 mg-11.81

[back to top]

Percent Change From Baseline in Non-HDL Cholesterol

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-22.50
Atorvastatin 40 mg-10.88

[back to top]

Percent Change From Baseline in Non-HDL Cholesterol/HDL-Cholesterol Ratio

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-24.41
Atorvastatin 40 mg-11.20

[back to top]

Percent Change From Baseline in Total Cholesterol

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-15.97
Atorvastatin 40 mg-7.73

[back to top]

Percent Change From Baseline in Total Cholesterol/HDL-Cholesterol Ratio

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-18.63
Atorvastatin 40 mg-8.60

[back to top]

Percent Change From Baseline in Triglycerides

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-5.41
Atorvastatin 40 mg-7.54

[back to top]

Number of Participants Reaching LDL-C Target Goal <100 mg/dL

Target LDL-C level of < 100 mg/dL (2.59 mmol/L) at study endpoint after 6 weeks of treatment for the Full Analysis Set (FAS) population. (NCT00782184)
Timeframe: Treatment Week 6

Interventionparticipants (Number)
Ezetimibe/Simvastatin 10/4081
Atorvastatin 40 mg52

[back to top]

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

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/405.37
Atorvastatin 40 mg2.89

[back to top]

Number of Participants Reaching LDL-C Target Goal <77 mg/dL

Target LDL-C level of < 77 mg/dL (2.00 mmol/L) at study endpoint after 6 weeks of treatment for the Full Analysis Set (FAS) population. (NCT00782184)
Timeframe: Treatment Week 6

Interventionparticipants (Number)
Ezetimibe/Simvastatin 10/4045
Atorvastatin 40 mg11

[back to top]

Number of Participants Reaching LDL-C Target Goals of <70 mg/dL

Target LDL-C level of < 70 mg/dL (1.81 mmol/L) at study endpoint after 6 weeks of treatment for the Full Analysis Set (FAS) population. (NCT00782184)
Timeframe: Treatment Week 6

Interventionparticipants (Number)
Ezetimibe/Simvastatin 10/4034
Atorvastatin 40 mg6

[back to top]

Percent Change From Baseline in Apolipoprotein A-1

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/402.56
Atorvastatin 40 mg-2.69

[back to top]

Percent Change From Baseline in Apolipoprotein B

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-17.23
Atorvastatin 40 mg-9.53

[back to top]

Percent Change From Baseline in Apolipoprotein B/A-1 Ratio

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-18.59
Atorvastatin 40 mg-5.67

[back to top]

Percent Change From Baseline in High-sensitivity C-Reactive Protein (Hs-CRP)

(NCT00782184)
Timeframe: Baseline (Treatment Day 1), Treatment Week 6

Interventionpercent change from baseline (Least Squares Mean)
Ezetimibe/Simvastatin 10/40-6.18
Atorvastatin 40 mg-8.86

[back to top]

Number of Participants in Each Stratum Who Reached Their Target LDL-C Level

Participants in stratum I were analyzed to evaluate the LDL-C lowering efficacy with the additional of ezetimibe 10 mg to rosuvastatin 5 mg daily for 6 weeks compared with doubling the baseline dose to rosuvastatin 10 mg daily for 6 weeks. Participants in stratum II were analyzed to evaluate the LDL-C lowering efficacy with the additional of ezetimibe 10 mg to rosuvastatin 10 mg daily for 6 weeks compared with doubling the baseline dose to rosuvastatin 20 mg daily for 6 weeks. (NCT00783263)
Timeframe: 6 weeks of treatment

Interventionparticipants (Number)
Rosuvastatin 5 mg + Ezetimibe 10 mg (Stratum I)54
Rosuvastatin 10 mg (Stratum I)30
Rosuvastatin 10 mg + Ezetimibe 10 mg (Stratum II)76
Rosuvastatin 20 mg (Stratum II)37

[back to top]

Number of Participants Who Reached the LDL-C Level of <70 mg/dl

Participants across all strata who reached the LDL-C Level of <70 mg/dl after the addition of ezetimibe 10 mg to rosuvastatin (5 or 10 mg) daily for 6 weeks compared with doubling the baseline dose of rosuvastatin (10 or 20 mg) daily for 6 weeks. (NCT00783263)
Timeframe: 6 weeks of treatment

Interventionparticipants (Number)
Rosuvastatin (5 or 10 mg) + Ezetimibe 10 mg96
Rosuvastatin 10 or 20 mg38

[back to top]

Number of Participants Who Reached Their Target LDL-C Level

Participants were analyzed to evaluate the LDL-C (<100 mg/dL for moderately high risk patients and high risk patients without AVD and <70 mg/dL for high risk patients with AVD) lowering efficacy with the addition of ezetimibe 10 mg to (5 or 10 mg) compared with doubling the baseline rosuvastatin (10 or 20 mg), daily for 6 weeks of treatment. (NCT00783263)
Timeframe: 6 weeks of treatment

Interventionparticipants (Number)
Rosuvastatin (5 or 10 mg) + Ezetimibe 10 mg130
Rosuvastatin (10 or 20 mg)67

[back to top]

Number of Participants in Each Stratum Who Reached the LDL-C Level of <70 mg/dl

Participants in stratum I and in stratum II who reached the LDL-C Level of <70 mg/dl after the addition of ezetimibe to rosuvastatin (5 or 10 mg)daily for 6 weeks compared with doubling the baseline dose of rosuvastatin (10 or 20 mg). (NCT00783263)
Timeframe: 6 weeks of treatment

Interventionparticipants (Number)
Rosuvastatin 5 mg + Ezetimibe 10 mg31
Rosuvastatin 10 mg12
Rosuvastatin 10 mg + Ezetimibe 10 mg65
Rosuvastatin 20 mg26

[back to top]

Percent Change From Baseline in Other Lipid, Lipoprotein, Apolipoprotein and High-sensitivity C-reactive Protein (Hs-CRP)Levels

Participants who were analyzed to assess the Total Cholesterol (TC), Triglycerides, High-Density Lipoprotein Cholesterol, Non High-Density Lipoprotein Cholesterol, LDL Cholesterol/HDL Cholesterol, Total Cholesterol/HDL Cholesterol, Non-HDL Cholesterol/HDL Cholesterol, Apolipoprotein B (Apo B), Apolipoprotein A-I (Apo A-I), Apolipoprotein B/Apo A-I, high-sensitivity C-reactive protein (hs-CRP)levels after 6 weeks of treatment. (NCT00783263)
Timeframe: Baseline to 6 weeks

,
Interventionpercentage change (Mean)
Total Cholesterol (TC)TriglyceridesHigh-Density Lipoprotein CholesterolNon High-Density Liproprotein CholesterolLDL Cholesterol/HDL CholesterolTotal Cholesterol/HDL CholesterolNon-HDL Cholestrol/HDL CholesterolApolipoprotein B (Apo B)Apolipoprotein A-I (Apo A-I)Apolipoprotein B/Apo A-Ihs-C-Reactive Protein
Rosuvastatin (5 or 10 mg) + Ezetimibe 10 mg-13.00-5.96-0.67-17.59-19.48-10.57-14.51-14.31-1.44-11.98-13.98
Rosuvastatin 10 or 20 mg-3.76-3.602.18-5.29-6.18-4.40-5.31-4.251.06-4.11-12.82

[back to top]

Percent Change From Baseline in LDL-Cholesterol (mg/dL) After 6 Weeks of Treatment in Each Stratum

The percent change from baseline in LDL-C (mg/dL) after 6 weeks of treatment by stratum I and stratum II in participants who were administered with ezetimibe 10 mg to rosuvastatin (5 or 10 mg) in comparison with the doubling of the baseline dose of rosuvastatin (10 or 20 mg) daily for 6 weeks. (NCT00783263)
Timeframe: Baseline to 6 weeks

Interventionpercentage change (Mean)
Rosuvastatin 5 mg + Ezetimibe 10 mg (Stratum I)-18.57
Rosuvastatin 10 mg (Stratum I)-4.96
Rosuvastatin 10 mg + Ezetimibe 10 mg (Stratum II)-24.00
Rosuvastatin 20 mg (Stratum II)-6.07

[back to top]

Percent Change From Baseline in LDL-Cholesterol (mg/dL) After 6 Weeks of Treatment

The percent change from baseline in LDL-C (mg/dL) after 6 weeks of treatment in participants who were administered ezetimibe 10 mg to rosuvastatin (5 or 10 mg) in comparison with doubling the baseline dose of rosuvastatin (10 or 20 mg) daily for 6 weeks. (NCT00783263)
Timeframe: Baseline to 6 weeks

Interventionpercent change (Mean)
Rosuvastatin (5 or 10 mg) + Ezetimibe 10 mg-21.57
Rosuvastatin (10 or 20 mg)-5.58

[back to top]

Percent Change of Fasting Non-high Density Lipoprotein Cholesterol From Baseline

Change = [(Week 6 - baseline)/baseline value *100] (NCT00794677)
Timeframe: Baseline (placebo run-in) and 6 weeks

Interventionpercent change from baseline (Mean)
Ezetimibe-22.675
Placebo-1.322

[back to top]

Log (AUC of Plasma Total Cholesterol) After an Oral Bolus

Area under the curve (AUC) calculated over 8 hours (NCT00794677)
Timeframe: 6 weeks

InterventionLog(mg*hr/dl) (Mean)
Ezetimibe2.928
Placebo2.719

[back to top]

Log (AUC of Plasma Triglyceride) After an Oral Bolus

Area under the curve (AUC) calculated over 8 hours (NCT00794677)
Timeframe: 6 weeks

InterventionLog(mg*hr/dl) (Mean)
Ezetimibe4.894
Placebo5.044

[back to top]

Log(Fasting Plasma Levels of Diet-derived Oxysterols (7-ketocholesterol))

(NCT00794677)
Timeframe: 6 weeks

InterventionLog(mg/dl) (Mean)
Ezetimibe-1.119
Placebo-1.070

[back to top]

Log(Maximal Plasma Concentration (Cmax) of 7-ketocholesterol) After an Oral Bolus

Log Cmax of 7 ketocholesterol after an oral bolus in patients with primary hypercholesterolemia. (NCT00794677)
Timeframe: 6 weeks

InterventionLog(mg/dl) (Mean)
Ezetimibe0.973
Placebo1.246

[back to top]

Log[Area-under-the-plasma-concentration-curve(AUC) 0-8 Hours 7-ketocholesterol] After an Oral Bolus

Log of Area-under-the-plasma-concentration curve (AUC 0-8hrs) of 7-ketocholesterol after an oral bolus in patients with primary hypercholesterolemia after treatment with ezetimibe versus placebo (NCT00794677)
Timeframe: 6 weeks

InterventionLog(mg*hr/dl) (Mean)
Ezetimibe1.925
Placebo2.177

[back to top]

Percent Change in Fasting High Density Lipoprotein Cholesterol

Change = [(Week 6 - baseline)/baseline value *100] (NCT00794677)
Timeframe: Baseline (placebo run-in) and 6 weeks

Interventionpercent change from baseline (Mean)
Ezetimibe-1.936
Placebo-7.333

[back to top]

Percent Change of Fasting Apolipoprotein B From Baseline

Change = [(Week 6 - baseline)/baseline value *100] (NCT00794677)
Timeframe: Baseline (placebo run-in) and 6 weeks

Interventionpercent change from baseline (Mean)
Ezetimibe-17.990
Placebo-2.577

[back to top]

Percent Change of Fasting Low Density Lipoprotein Cholesterol From Baseline

Change = [(Week 6 - baseline)/baseline value *100] (NCT00794677)
Timeframe: Baseline (placebo run-in) and 6 weeks

Interventionpercent change from baseline (Mean)
Ezetimibe-22.891
Placebo-1.045

[back to top]

Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study days 16-20

Interventionng/ml (Mean)
Study Group0.659

[back to top]

Cmax of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng/ml (Mean)
Study Group0.918

[back to top]

AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 15

Interventionng*h/ml (Mean)
Study Group51.9

[back to top]

Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng/ml (Mean)
Study Group45.3

[back to top]

Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 15

Interventionng/ml (Mean)
Study Group4.82

[back to top]

Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 16

Interventionng/ml (Mean)
Study Group5.54

[back to top]

Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng/ml (Mean)
Study Group4.46

[back to top]

Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 16

Interventionng/ml (Mean)
Study Group60.9

[back to top]

Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 15

Interventionng/ml (Mean)
Study Group79.0

[back to top]

AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng*h/ml (Mean)
Study Group51.2

[back to top]

AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of free ezetimibe in the blood samplings. (NCT00810303)
Timeframe: study day 16

Interventionng*h/ml (Mean)
Study Group58.6

[back to top]

AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 16

Interventionng*h/ml (Mean)
Study Group411

[back to top]

AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 15

Interventionng*h/ml (Mean)
Study Group466

[back to top]

AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5

The area under the concentrations-time curve (AUC) was calculated with the measured data points from the time of administration until the last quantificable concentration by the trapezoidal formula and the extrapolation to infinity. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study days 1-5

Interventionng*h/ml (Mean)
Study Group29.7

[back to top]

AUC0-24h of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng*h/ml (Mean)
Study Group11.4

[back to top]

AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30

The area under the concentrations-time curve (AUC0-24) was calculated with the measured data points from the time of administration up to 24 h after administration by the trapezoidal formula. The concentration-time curve is the result of time points of blood sampling and its measured concentration of ezetimibe glucuronide in the blood samplings. (NCT00810303)
Timeframe: study day 30

Interventionng*h/ml (Mean)
Study Group325

[back to top]

Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5

The maximum concentration (Cmax) were obtained directly from the measured concentration-time curves. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study days 1-5

Interventionng/ml (Mean)
Study Group0.622

[back to top]

AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20

The area under the concentrations-time curve (AUC) was calculated with the measured data points from the time of administration until the last quantificable concentration by the trapezoidal formula and the extrapolation to infinity. The concentration-time curve is the result of time points of blood sampling and its measured concentration of efavirenz in the blood samplings. (NCT00810303)
Timeframe: study days 16-20

Interventionng*h/ml (Mean)
Study Group27.0

[back to top]

Treatment Difference in (Postprandial-Fasting) FMD

A comparison of the postprandial minus fasting change in FMD under treatment with simvastatin 80 mg versus simvastatin 10/10 mg (NCT00817843)
Timeframe: After 6 weeks of treatment

Intervention% (change FMD) (Mean)
Simvastatin 80 mg-0.34
Simvastatin 10 mg / Ezetimibe 10 mg-0.43

[back to top]

Biomarkers of Inflammation

(NCT00819403)
Timeframe: 6 weeks

,
Interventionmg/dl (Mean)
CRPIL-6
Simvastatin3.511.24
Simvastatin/Ezetimibe3.571.33

[back to top]

Ex Vivo Effects of Treatment With Vytorin Versus Zocor for 6 Weeks on Platelet Alpha Thrombin PAR-1 Receptor Expression

Measured using whole blood flow cytometry (NCT00819403)
Timeframe: 6 weeks

,
Interventionng/dl (Mean)
PAR 1/4 antigenPAR 1/4 activity
Simvastatin35.423.6
Simvastatin/Ezetimibe34.522.5

[back to top]

Percent Change From Baseline in Triglycerides

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-5.51
Doubling Statin Dose-2.63
Rosuvastatin-3.35

[back to top]

Percent Change From Baseline in Total Cholesterol (TC)

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent Change (Least Squares Mean)
Ezetimibe/Simvastatin-13.21
Doubling Statin Dose-4.88
Rosuvastatin-10.58

[back to top]

Percent Change From Baseline in TC/HDL-C Ratio

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-12.52
Doubling Statin Dose-4.36
Rosuvastatin-10.70

[back to top]

Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C)

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-18.39
Doubling Statin Dose-6.77
Rosuvastatin-15.14

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) After Switching to Treatment With Ezetimibe/Simvastatin vs Doubling the Dose of Statin (Simvastatin or Atorvastatin).

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-23.13
Doubling Statin Dose-8.37

[back to top]

Percent Change From Baseline in LDL-C/HDL-C Ratio

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-21.55
Doubling Statin Dose-7.39
Rosuvastatin-18.99

[back to top]

In Participants Treated With Simvastatin at Baseline, Number of Participants Who Reached the Target LDL-Cholesterol Level of < 70 mg/dL (1.81 mmol/L)

(NCT00862251)
Timeframe: Week 6

Interventionparticipants (Number)
Ezetimibe/Simvastatin84
Doubling Simvastatin Dose19

[back to top]

In Participants Treated With Simvastatin at Baseline, Percent Change From Baseline in LDL-C After Switching to Treatment With Ezetimibe/Simvastatin vs Doubling the Dose of Simvastatin

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-21.59
Doubling Simvastatin Dose-7.98

[back to top]

In Participants Treated With Atorvastatin at Baseline, Percent Change From Baseline in LDL-C After Switching to Treatment With Ezetimibe/Simvastatin vs Doubling the Dose of Atorvastatin

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-24.58
Doubling Atorvastatin Dose-8.85

[back to top]

Percent Change From Baseline in LDL-C After Switching to Treatment With Ezetimibe/Simvastatin vs Switching Treatment to Rosuvastatin

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-23.13
Rosuvastatin-19.32

[back to top]

Percent Change From Baseline in Non-HDL-C/HDL-C Ratio

(NCT00862251)
Timeframe: Baseline and Week 6

Interventionpercent change (Least Squares Mean)
Ezetimibe/Simvastatin-16.77
Doubling Statin Dose-5.32
Rosuvastatin-14.64

[back to top]

Number of Participants Who Reached the Target LDL-Cholesterol Level of < 70 mg/dL (1.81 mmol/L)

(NCT00862251)
Timeframe: Week 6

Interventionparticipants (Number)
Ezetimibe/Simvastatin171
Doubling Statin Dose43
Rosuvastatin134

[back to top]

Percent Change From Baseline Apolipoprotein A-I (Apo A-I)

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin0.64
Doubling Statin Dose-0.93
Rosuvastatin0.86

[back to top]

Percent Change From Baseline in Apo B/Apo A-I Ratio

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-13.67
Doubling Statin Dose-4.75
Rosuvastatin-11.14

[back to top]

Percent Change From Baseline in Apolipoprotein B (Apo B)

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-14.98
Doubling Statin Dose-6.97
Rosuvastatin-12.03

[back to top]

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

(NCT00862251)
Timeframe: Baseline and Week 6

Interventionpercent change (Least Squares Mean)
Ezetimibe/Simvastatin1.47
Doubling Statin Dose1.00
Rosuvastatin1.99

[back to top]

Percent Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP)

(NCT00862251)
Timeframe: Baseline and Week 6

InterventionPercent change (Least Squares Mean)
Ezetimibe/Simvastatin-4.42
Doubling Statin Dose-1.64
Rosuvastatin-9.11

[back to top]

In Participants Treated With Atorvastatin at Baseline, Number of Participants Who Reached the Target LDL-Cholesterol Level of < 70 mg/dL (1.81 mmol/L)

(NCT00862251)
Timeframe: Week 6

Interventionparticipants (Number)
Ezetimibe/Simvastatin87
Doubling Atorvastatin Dose24

[back to top]

Percent Cholesterol Absorption

Percent of intestinal cholesterol absorbed. Intestinal cholesterol is comprised of dietary cholesterol intake and endogenous cholesterol secreted into the intestinal lumen. Cholesterol absorption is the percent of intestinal cholesterol that is taken back up into the body and excluded from fecal excretion. It is also referred to as the efficiency of intestinal cholesterol absorption. (NCT00863265)
Timeframe: Determined on the final 5 days of each dietary period

InterventionPercent (Mean)
Phytosterol-Deficient Diet69.0
Diet Plus Ezetimibe46.2
Diet Plus Ezetimibe Plus Phytosterols32.6

[back to top]

LDL Cholesterol

(NCT00863265)
Timeframe: At the end of week 3 on each diet

Interventionmg/deciliter (Mean)
Phytosterol-Deficient Diet129
Phytosterol-Deficient Diet Plus Ezetimibe108
Phytosterol-Deficient Diet Plus Ezetimibe Plus Phytosterols101

[back to top]

Cholesterol Excretion

Milligrams of fecal cholesterol and cholesterol metabolites excreted per day (NCT00863265)
Timeframe: At the end of week 3 on each diet

Interventionmg per day (Mean)
Phytosterol-Deficient Diet505
Diet Plus Ezetimibe794
Diet Plus Ezetimibe Plus Phytosterols962

[back to top]

Percentage Change From Baseline HDL-C at Week 4

Serum HDL-C levels measured by photometry after precipitation at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe0.86
Placebo0.33

[back to top]

Percentage Change From Baseline HDL-C at Week 8

Serum HDL-C levels measured by photometry after precipitation at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe1.41
Placebo-0.52

[back to top]

Percentage Change From Baseline High-density Lipoprotein Cholesterol (HDL-C) at Week 12

Serum HDL-C levels measured by photometry after precipitation at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe2.11
Placebo1.41

[back to top]

Percentage Change From Baseline in Apolipoprotein A-I (Apo A-I) at Week 12

Serum Apo A-I levels measured at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe1.80
Placebo3.71

[back to top]

Percentage Change From Baseline in Apolipoprotein B (Apo B) at Week 12

Serum Apo B measured at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Ezetimibe-21.66
Placebo-1.42

[back to top]

Percentage Change From Baseline in Campesterol at Week 12

Plasma campesterol measured at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-67.59
Placebo-2.92

[back to top]

Percentage Change From Baseline in Campesterol at Week 2

Plasma campesterol measured at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-53.87
Placebo-4.38

[back to top]

Percentage Change From Baseline in Campesterol at Week 4

Plasma campesterol measured at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-62.27
Placebo-4.28

[back to top]

Percentage Change From Baseline in Campesterol at Week 8

Plasma campesterol measured at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-66.79
Placebo-4.19

[back to top]

Percentage Change From Baseline in Cholestanol at Week 12

Plasma cholestanol measured at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-28.71
Placebo3.42

[back to top]

Percentage Change From Baseline in Cholestanol at Week 2

Plasma cholestanol measured at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-25.44
Placebo-7.09

[back to top]

Percentage Change From Baseline in Cholestanol at Week 4

Plasma cholestanol measured at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-27.40
Placebo-1.79

[back to top]

Percentage Change From Baseline in Cholestanol at Week 8

Plasma cholestanol measured at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-29.19
Placebo-0.44

[back to top]

Percentage Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP) at Week 12

Plasma hs-CRP measured at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe9.35
Placebo-7.92

[back to top]

Percentage Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP) at Week 4

Plasma hs-CRP measured at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe10.00
Placebo56.11

[back to top]

Percentage Change From Baseline in Lathosterol at Week 2

Plasma lathosterol measured at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe34.07
Placebo14.06

[back to top]

Percentage Change From Baseline in Lathosterol at Week 8

Plasma lathosterol measured at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe35.87
Placebo-0.82

[back to top]

Percentage Change From Baseline in LDL-C:HDL-C Ratio at Week 12

Serum LDL-C:HDL-C Ratio calculated at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-28.01
Placebo0.34

[back to top]

Percentage Change From Baseline in LDL-C:HDL-C Ratio at Week 2

Serum LDL-C:HDL-C Ratio calculated at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-23.35
Placebo1.15

[back to top]

Percentage Change From Baseline in LDL-C:HDL-C Ratio at Week 4

Serum LDL-C:HDL-C Ratio calculated at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-25.72
Placebo-0.57

[back to top]

Percentage Change From Baseline in LDL-C:HDL-C Ratio at Week 8

Serum LDL-C:HDL-C Ratio calculated at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-26.43
Placebo2.87

[back to top]

Percentage Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 12

Serum LDL-C levels calculated at baseline and after 12 weeks of study drug administration. LDL-C were calculated by the method of Friedewald equation, LDL-C = Total Cholesterol (TC) - (High-density lipoprotein cholesterol [HDL-C] + triglyceride [TG]/5). (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercent Change (Least Squares Mean)
Ezetimibe-27.70
Placebo-0.95

[back to top]

Percentage Change From Baseline in Non-HDL-C at Week 12

Serum Non-HDL-C calculated at baseline and after 12 weeks of study drug administration. Non-HDL-C values were calculated as follows: Non-HDL-C (mg/dL) = TC - HDL-C. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-25.47
Placebo0.28

[back to top]

Percentage Change From Baseline in Non-HDL-C at Week 2

Serum Non-HDL-C calculated at baseline and after 2 weeks of study drug administration. Non-HDL-C values were calculated as follows: Non-HDL-C (mg/dL) = TC - HDL-C. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-22.54
Placebo1.64

[back to top]

Percentage Change From Baseline in Non-HDL-C at Week 4

Serum Non-HDL-C calculated at baseline and after 4 weeks of study drug administration. Non-HDL-C values were calculated as follows: Non-HDL-C (mg/dL) = TC - HDL-C. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-24.94
Placebo-0.33

[back to top]

Percentage Change From Baseline in Non-HDL-C at Week 8

Serum Non-HDL-C calculated at baseline and after 8 weeks of study drug administration. Non-HDL-C values were calculated as follows: Non-HDL-C (mg/dL) = TC - HDL-C. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-25.41
Placebo1.14

[back to top]

Percentage Change From Baseline in Sitosterol at Week 12

Plasma sitosterol measured at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-60.65
Placebo2.09

[back to top]

Percentage Change From Baseline in Sitosterol at Week 4

Plasma sitosterol measured at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-58.82
Placebo-0.30

[back to top]

Percentage Change From Baseline in Sitosterol at Week 8

Plasma sitosterol measured at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-61.59
Placebo-0.57

[back to top]

Percentage Change From Baseline in TC at Week 2

Serum TC levels measured using enzymatic methods at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-18.69
Placebo1.40

[back to top]

Percentage Change From Baseline in TC at Week 4

Serum TC levels measured using enzymatic methods at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-20.57
Placebo-0.29

[back to top]

Percentage Change From Baseline in TC at Week 8

Serum TC levels measured using enzymatic methods at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-20.84
Placebo0.54

[back to top]

Percentage Change From Baseline in TC:HDL-C Ratio at Week 12

Serum TC:HDL-C Ratio calculated at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-21.09
Placebo1.20

[back to top]

Percentage Change From Baseline in TC:HDL-C Ratio at Week 2

Serum TC:HDL-C Ratio calculated at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-17.21
Placebo2.56

[back to top]

Percentage Change From Baseline in TC:HDL-C Ratio at Week 4

Serum TC:HDL-C Ratio calculated at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-19.36
Placebo1.48

[back to top]

Percentage Change From Baseline in TC:HDL-C Ratio at Week 8

Serum TC:HDL-C Ratio calculated at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-20.07
Placebo3.41

[back to top]

Percentage Change From Baseline in TG at Week 2

Serum TG levels measured using enzymatic methods at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-3.90
Placebo5.83

[back to top]

Percentage Change From Baseline in TG at Week 4

Serum TG levels measured using enzymatic methods at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-5.54
Placebo9.65

[back to top]

Percentage Change From Baseline in TG at Week 8

Serum TG levels measured using enzymatic methods at baseline and after 8 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-9.99
Placebo-1.38

[back to top]

Percentage Change From Baseline in Total Cholesterol (TC) at Week 12

Serum TC levels measured using enzymatic methods at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-20.74
Placebo0.19

[back to top]

Percentage Change From Baseline in Lathosterol at Week 4

Plasma lathosterol measured at baseline and after 4 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe33.02
Placebo6.73

[back to top]

Percentage Change From Baseline in Triglycerides (TG) at Week 12

Serum TG levels measured using enzymatic methods at baseline and after 12 weeks of study drug. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage change (Least Squares Mean)
Ezetimibe-6.23
Placebo8.44

[back to top]

Percentage Change From Baseline in Apo B:Apo A-I Ratio at Week 12

Serum Apo B:Apo A-I Ratio calculated at baseline and after 12 weeks of study drug administration (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-22.16
Placebo-2.87

[back to top]

Percentage Change From Baseline in Lathosterol at Week 12

Plasma lathosterol measured at baseline and after 12 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe36.62
Placebo12.57

[back to top]

Percent Change From Baseline in LDL-C at Week 2

Serum LDL-C levels calculated at baseline and after 2 weeks of study drug administration. LDL-C were calculated by the method of Friedewald equation, LDL-C = Total Cholesterol (TC) - (High-density lipoprotein cholesterol [HDL-C] + triglyceride [TG]/5). (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-24.75
Placebo0.23

[back to top]

Percent Change From Baseline in LDL-C at Week 4

Serum LDL-C levels calculated at baseline and after 4 weeks of study drug administration. LDL-C were calculated by the method of Friedewald equation, LDL-C = Total Cholesterol (TC) - (High-density lipoprotein cholesterol [HDL-C] + triglyceride [TG]/5). (NCT00867165)
Timeframe: Baseline and Week 4

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-26.93
Placebo-2.99

[back to top]

Percent Change From Baseline in LDL-C at Week 8

Serum LDL-C levels calculated at baseline and after 8 weeks of study drug administration. LDL-C were calculated by the method of Friedewald equation, LDL-C = Total Cholesterol (TC) - (High-density lipoprotein cholesterol [HDL-C] + triglyceride [TG]/5). (NCT00867165)
Timeframe: Baseline and Week 8

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-27.22
Placebo0.49

[back to top]

Percent Change From Baseline in Sitosterol at Week 2

Plasma sitosterol measured at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe-50.20
Placebo-0.59

[back to top]

Percentage Change From Baseline HDL-C at Week 2

Serum HDL-C levels measured by photometry after precipitation at baseline and after 2 weeks of study drug administration. (NCT00867165)
Timeframe: Baseline and Week 2

InterventionPercentage Change (Least Squares Mean)
Ezetimibe0.01
Placebo0.96

[back to top]

Percent Change in Total Lipids and Hs-CRP

Total cholesterol, triglycerides, high-density lipoprotein cholesterol (HDL-C), non-HDL-C, and hs-CRP were measured at the start of the treatment period (at start of administration of atorvastatin 10 mg alone) and at the end of study drug (Week 16 or discontinuation). (NCT00871351)
Timeframe: End of washout to Week 16 or discontinuation

,,
InterventionPercent change (Mean)
Total CholesterolTriglyceridesHigh-Density Lipoprotein Cholesterol (HDL-C)Non-HDL-CHigh Sensitivity C-reactive Protein (Hs-CRP)
Atorvastatin-32.8-18.87.4-41.4-2.9
Ezetimibe + Atorvastatin-39.9-25.310.3-50.173.0
Rosuvastatin-24.4-12.09.9-31.3-13.6

[back to top]

Percent Change in Total Lipids and High Sensitivity C-reactive Protein (Hs-CRP)

Total cholesterol, triglycerides, high-density lipoprotein cholesterol (HDL-C), non-HDL-C, and hs-CRP were measured at 4 weeks after the start of the treatment period (after completion of administration of atorvastatin 10 mg alone) and at Week 16 or at discontinuation. (NCT00871351)
Timeframe: End of Week 4 to Week 16 or discontinuation

,,
InterventionPercent change (Mean)
Total CholesterolTriglyceridesHigh-Density Lipoprotein Cholesterol (HDL-C)Non-HDL-CHigh Sensitivity C-Reactive Protein (Hs-CRP)
Atorvastatin-10.30.20.5-13.79.9
Ezetimibe + Atorvastatin-18.0-0.84.5-25.049.0
Rosuvastatin1.914.72.52.025.7

[back to top]

Percent Change in Low-Density Lipoprotein - Cholesterol (LDL-C) Values

LDL-C was measured before group study drug administration (Week 4, end of atorvastatin single therapy) and at the end of study drug administration (after 12 weeks of study drug treatment, or at discontinuation). (NCT00871351)
Timeframe: End of Week 4 to Week 16 or discontinuation

InterventionPercent change (Mean)
Ezetimibe + Atorvastatin-25.8
Atorvastatin-15.1
Rosuvastatin0.8

[back to top]

Percent Change in LDL-C

LDL-C was measured at the start of the atorvastatin 10 mg treatment period (end of the washout period) and at the end of administration of the study drug (Week 16 or discontinuation). (NCT00871351)
Timeframe: End of washout period to Week 16 or discontinuation

InterventionPercent change (Mean)
Ezetimibe + Atorvastatin-49.6
Atorvastatin-41.1
Rosuvastatin-30.5

[back to top]

Number of Participants Whose LDL-C Levels Reached the Lipid Management Target Values

"LDL-C was measured at the end of administration of the study drug (Week 16 or discontinuation).~Target values:~For participants with history of coronary artery disease: <100 mg/dL;~for participants with at least 3 cardiovascular (CV) risk factors: <120 mg/dL;~for participants with 1-2 CV risk factors: <140 mg/dL;~for participants with no CV risk factors: <160 mg/dL." (NCT00871351)
Timeframe: Week 16 or discontinuation

InterventionParticipants (Number)
Ezetimibe + Atorvastatin37
Atorvastatin19
Rosuvastatin1

[back to top]

Changes in LDL Cholesterol

"Subjects with T1DM or T2DM were assigned to alternating therapy with simvastatin (40 mg) or ezetimibe (10 mg) for 6 weeks in a crossover design.~The data are reported as follows.~Subjects with type 1 diabetes mellitus:~Simvastatin: Changes in LDL after 6-week therapy with simvastatin (irrespective of the treatment order) Ezetimibe: Changes in LDL after 6-week therapy with ezetimibe (irrespective of the treatment order)~Subjects with type 2 diabetes mellitus:~Simvastatin: Changes in LDL after 6-week therapy with simvastatin (irrespective of the treatment order) Ezetimibe: Changes in LDL after 6-week therapy with ezetimibe (irrespective of the treatment order)" (NCT00879710)
Timeframe: 6 weeks after starting drug therapy

,
Interventionmmol/L (Mean)
simvastatinezetimibe
Subjects With Type 1 Diabetes Mellitus,-0.83-0.93
Subjects With Type 2 Diabetes Mellitus-1.47-0.32

[back to top]

The Primary Endpoint is the Difference in Final Value of Serum Apolipoprotein B Between Participants Treated With Rosuvastatin Versus Participants Treated With Both Rosuvastatin and Ezetimibe.

(NCT00908011)
Timeframe: 3 months from baseline

Interventionmmol/L (Mean)
Ezetimibe0.88
Standard Care0.89

[back to top]

Number of Participants Who Had an Adverse Event (AE).

"The objective of this study was to evaluate the overall safety and tolerability of Vytorin (R) Tablet (Ezetimibe+Simvastatin) when used in patients with hypercholesterolemia.~All AEs observed by or volunteered to the investigator during this observational study, regardless of suspected causal relationship, were to have been considered an AE." (NCT00909389)
Timeframe: Throughout study up to Day 29 (Final Visit)

Interventionparticipants (Number)
Filipino Patients With Hypercholesterolemia62

[back to top]

Changes in Low-density Lipoprotein Cholesterol (LDL-C)

(NCT00932620)
Timeframe: 3 months

InterventionLDL-C, mg/dL (Mean)
Simvastatin 40-43
Simvastatin/Ezetimibe 10/10-49

[back to top]

Changes in Small Dense Low-density Lipoprotein Cholesterol (sdLDL-C) Levels

(NCT00932620)
Timeframe: Baseline and 3 months

InterventionsdLDL-C, mg/dL (Mean)
Simvastatin 40 mg-42
Simvastatin 10 mg Plus Ezetimibe 10 mg-46

[back to top]

L5 Concentration in Metabolic Syndrome Patients

Patient's blood samples were collected before treatment. L5 were purified by ultracentrifugation then FPLC. Quantification analysis will indicate the L5 concentration (mg/dL) per group. (NCT00988364)
Timeframe: 0 months, at the start

Interventionmg/dL (Mean)
Ezetimibe35.97
Simvastatin17.8233
Vytorin29.736
Placebo23.1

[back to top]

L5 Concentration After Treatment of Ezetimibe, Simvastatin, or Vytorin in Metabolic Syndrome Patients

Patient's blood samples were collected at the corresponding time point for L5 purification. L5 quantification and characterization were investigated with chemical analysis, proteomics and in-vitro cell signaling analysis. Final data analysis will determine total L5 concentration (mg/dL). (NCT00988364)
Timeframe: 3 months

Interventionmg/dL (Mean)
Ezetimibe30.17
Simvastatin19.19
Vytorin14.17
Placebo15.15

[back to top]

Percentage of Participants That Reach Target LDL-C Level of < 70 mg/dL (Phase II)

(NCT01154036)
Timeframe: Week 12 (end of Phase II)

InterventionPercentage of Participants (Number)
Phase II: EZ 10mg + Atorva 20mg [A]18.3
Phase II: Atorva 40mg0.8
Phase II: EZ 10mg + Atorva 20mg [R]15.4
Phase II: Rosuvastatin 20mg3.0
Phase II: EZ 10mg+Atorva 10mgNA

[back to top]

Percent Change From Baseline in Apo B/Apo A-I Ratio (Phase II)

Apo B/Apo A-I Ratio calculated at Baseline (Week 6; end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase 1) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]-11.2
Phase II: Atorva 40mg-6.4
Phase II: EZ 10mg + Atorva 20mg [R]-11.2
Phase II: Rosuvastatin 20mg-5.4
Phase II: EZ 10mg+Atorva 10mg-6.7

[back to top]

Percent Change From Baseline in Apo B/Apo A-I Ratio (Phase I)

Apo B/Apo A-I ratio calculated at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-13.0
Phase I: Atorvastatin 20 mg-4.8
Phase 1: Rosuvastatin 10 mg-8.8

[back to top]

Percent Change From Baseline in Apo B (Phase II)

Apo-B levels measured at Baseline (Week 6; end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase 1) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]-12.0
Phase II: Atorva 40mg-6.3
Phase II: EZ 10mg + Atorva 20mg [R]-14.0
Phase II: Rosuvastatin 20mg-4.9
Phase II: EZ 10mg+Atorva 10mg-4.0

[back to top]

Percent Change From Baseline in Apo A-I (Phase II)

Apo-A-I levels measured at Baseline (end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase I) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]1.6
Phase II: Atorva 40mg1.4
Phase II: EZ 10mg + Atorva 20mg [R]-0.6
Phase II: Rosuvastatin 20mg0.0
Phase II: EZ 10mg+Atorva 10mg-0.7

[back to top]

Percentage of Participants That Reach Target LDL-C Level of < 70 mg/dL (Phase I)

(NCT01154036)
Timeframe: Week 6 (End of Phase I)

InterventionPercentage of Participants (Number)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg19.3
Phase I: Atorvastatin 20 mg3.0
Rosuvastatin 10 mg6.6

[back to top]

Percentage of Participants That Reach Target LDL-C Level of < 100 mg/dL (Phase II)

(NCT01154036)
Timeframe: Week 12 (End of Phase II)

InterventionPercentage of Participants (Number)
Phase II: EZ 10mg + Atorva 20mg [A]55.8
Phase II: Atorva 40mg34.1
Phase II: EZ 10mg + Atorva 20mg [R]53.5
Phase II: Rosuvastatin 20mg35.8
Phase II: EZ 10mg+Atorva 10mgNA

[back to top]

Percentage of Participants That Reach Target LDL-C Level of < 100 mg/dL (Phase I)

(NCT01154036)
Timeframe: Week 6 (End of Phase I)

InterventionPercentage of Participants (Number)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg56.3
Phase I: Atorvastatin 20 mg37.4
Rosuvastatin 10 mg43.6

[back to top]

Percent Change From Baseline in Triglycerides (TG) (Phase II)

TG levels measured at Baseline (Week 6: end of Phase I) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. Baseline and post-baseline measurements were log-transformed in the response vector, with fixed effects for treatment, time and the interaction of time by treatment. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase I) and Week 12 (end of Phase II)

InterventionPercentage Change (Least Squares Mean)
Phase II: EZ 10mg + Atorva 20mg [A]-5.9
Phase II: Atorva 40mg-3.1
Phase II: EZ 10mg + Atorva 20mg [R]-10.2
Phase II: Rosuvastatin 20mg-3.2
Phase II: EZ 10mg+Atorva 10mgNA

[back to top]

Percent Change From Baseline in TC/HDL-C Ratio (Phase I)

TC/HDL-C ratio calculated at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-14.3
Phase I: Atorvastatin 20 mg-4.5
Rosuvastatin 10 mg-9.0

[back to top]

Percent Change From Baseline in Non-HDL-C/HDL-C Ratio (Phase II)

Non HDL-C/HDL-C Ratio calculated at baseline (Week 6; end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase 1) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]-18.2
Phase II: Atorva 40mg-8.8
Phase II: EZ 10mg + Atorva 20mg [R]-16.3
Phase II: Rosuvastatin 20mg-5.9
Phase II: EZ 10mg+Atorva 10mg-1.9

[back to top]

Percent Change From Baseline in Non-HDL-C/HDL-C Ratio (Phase I)

Non HDL-C/HDL-C ratio calculated at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-18.9
Phase I: Atorvastatin 20 mg-6.3
Phase 1: Rosuvastatin 10 mg-12.2

[back to top]

Percent Change From Baseline in Non-HDL-C (Phase II)

Non-HDL-C levels calculated at Baseline (end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase I) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]-17.5
Phase II: Atorva 40mg-5.5
Phase II: EZ 10mg + Atorva 20mg [R]-18.1
Phase II: Rosuvastatin 20mg-6.3
Phase II: EZ 10mg+Atorva 10mg-0.5

[back to top]

Percent Change From Baseline in Non-HDL-C (Phase I)

Non-HDL-C measured at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-18.0
Phase I: Atorvastatin 20 mg-7.9
Rosuvastatin 10 mg-11.1

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C) (Phase II).

LDL-C levels measured at Baseline (Week 6; end of Phase 1) and after 6 weeks of study drug administration (Week 12). Baseline was defined as the average of the values at Visits 5 and 6. LDL-C was calculated using the Friedewald method when triglyceride (TG)<350 mg/dL (3.95 mmol/L) and beta quantification ultracentrifugation when TG ≥350 mg/dL (3.95 mmol/L). (NCT01154036)
Timeframe: Baseline (Week 6) and Week 12

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]-16.4
Phase II: Atorva 40mg-8.1
Phase II: EZ 10mg + Atorva 20mg [R]-19.3
Phase II: Rosuvastatin 20mg-8.4
Phase II: EZ 10mg+Atorva 10mg2.4

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C) (Phase I)

LDL-C levels measured at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4. LDL-C was calculated using the Friedewald method when triglyceride (TG)<350 mg/dL (3.95 mmol/L) and beta quantification ultracentrifugation when TG≥350 mg/dL (3.95 mmol/L). (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I )

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-24.8
Phase I: Atorvastatin 20 mg-10.1
Phase I: Rosuvastatin 10 mg-13.8

[back to top]

Percent Change From Baseline in LDL-C/HDL-C Ratio (Phase II)

LDL-C/HDL-C Ratio calculated at Baseline (end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase 1) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]-20.6
Phase II: Atorva 40mg-8.2
Phase II: EZ 10mg + Atorva 20mg [R]-18.2
Phase II: Rosuvastatin 20mg-7.5
Phase II: EZ 10mg+Atorva 10mg-4.5

[back to top]

Percent Change From Baseline in LDL-C/HDL-C Ratio (Phase I)

LDL-C/HDL-C ratio calculated at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-23.9
Phase I: Atorvastatin 20 mg-7.1
Phase 1: Rosuvastatin 10 mg-14.7

[back to top]

Percent Change From Baseline in Hs-CRP (Phase II)

hs-CRP measured at Baseline (Week 6; end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. Baseline and post-baseline measurements were log-transformed in the response vector, with fixed effects for treatment, time and the interaction of time by treatment. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase 1) and Week 12 (end of Phase II)

InterventionPercentage Change (Least Squares Mean)
Phase II: EZ 10mg + Atorva 20mg [A]-19.5
Phase II: Atorva 40mg-6.4
Phase II: EZ 10mg + Atorva 20mg [R]-10.9
Phase II: Rosuvastatin 20mg0.7
Phase II: EZ 10mg+Atorva 10mgNA

[back to top]

Percent Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP) (Phase I)

hs-CRP measured at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4. Baseline and post-baseline measurements were log-transformed in the response vector, with fixed effects for treatment, time and the interaction of time by treatment. (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Least Squares Mean)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-10.5
Phase I: Atorvastatin 20 mg-6.6
Phase I: Rosuvastatin 10 mg-9.0

[back to top]

Percent Change From Baseline in Apolipoprotein B (Apo B) (Phase I)

Apo-B measured at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-12.1
Phase I: Atorvastatin 20 mg-6.1
Rosuvastatin 10 mg-7.6

[back to top]

Percent Change From Baseline in High-density Lipoprotein-Cholesterol (HDL-C) (Phase I)

HDL-C measured at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg0.9
Phase I: Atorvastatin 20 mg-1.3
Rosuvastatin 10 mg1.0

[back to top]

Percent Change From Baseline in Apolipoprotein A-I (Apo A-I) (Phase I)

Apo-A-I measured at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-0.6
Phase I: Atorvastatin 20 mg-1.9
Rosuvastatin 10 mg1.4

[back to top]

Percent Change From Baseline in HDL-C (Phase II)

HDL-C levels measured at Baseline (end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase I) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]0.9
Phase II: Atorva 40mg1.0
Phase II: EZ 10mg + Atorva 20mg [R]-0.8
Phase II: Rosuvastatin 20mg0.0
Phase II: EZ 10mg+Atorva 10mg0.0

[back to top]

Percent Change From Baseline in Total Cholesterol (TC) (Phase I)

TC measured at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4 (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Median)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-13.6
Phase I: Atorvastatin 20 mg-6.3
Rosuvastatin 10 mg-8.2

[back to top]

Percent Change From Baseline in Total Cholesterol (TC) (Phase II)

TC levels measured at Baseline (end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase I) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]-10.2
Phase II: Atorva 40mg-2.9
Phase II: EZ 10mg + Atorva 20mg [R]-13.1
Phase II: Rosuvastatin 20mg-5.0
Phase II: EZ 10mg+Atorva 10mg2.2

[back to top]

Percent Change From Baseline in Triglycerides (TG) (Phase I)

TG measured at Baseline and after 6 weeks of treatment (Week 6; end of Phase I). Baseline was defined as the average value of the measurements taken at Visits 3 and 4. Baseline and post-baseline measurements were log-transformed in the response vector, with fixed effects for treatment, time and the interaction of time by treatment. (NCT01154036)
Timeframe: Baseline and Week 6 (end of Phase I)

InterventionPercentage Change (Least Squares Mean)
Phase I: Ezetimibe (EZ) 10 mg + Atorvastatin (Atorva) 10 mg-6.0
Phase I: Atorvastatin 20 mg-3.9
Rosuvastatin 10 mg-1.1

[back to top]

Percent Change From Baseline in TC/HDL-C Ratio (Phase II)

TC/HDL-C Ratio calculated at Baseline (end of Phase 1) and after 6 weeks of study drug administration (Week 12; end of Phase II). Baseline was defined as the average of the values at Visits 5 and 6. (NCT01154036)
Timeframe: Baseline (Week 6; end of Phase 1) and Week 12 (end of Phase II)

InterventionPercentage Change (Median)
Phase II: EZ 10mg + Atorva 20mg [A]-13.5
Phase II: Atorva 40mg-6.5
Phase II: EZ 10mg + Atorva 20mg [R]-11.7
Phase II: Rosuvastatin 20mg-4.0
Phase II: EZ 10mg+Atorva 10mg-1.0

[back to top]

Cmax of Atorvastatin- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of atorvastatin were collected on Day -1 and for atorvastatin on Days 1 and 14. Blood samples for PK were collected on Days -1 (co-dosing arms only) and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hour PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Days -1 and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionnanograms per milliliter (Geometric Mean)
Day -1Day 1Day 14
Atorvastatin 10 mg + Ezetimibe 10 mg2.0031.8721.949
Atorvastatin 10 mg + GSK1292263 100 mg2.0451.2921.453
Atorvastatin 10 mg + GSK1292263 300 mg2.4542.1952.154
Atorvastatin 10 mg + GSK1292263 800 mg1.6831.9262.139
Atorvastatin 10 mg + Placebo1.8161.8521.640
Atorvastatin 80 mg + GSK1292263 800 mg42.37631.01838.419
Atorvastatin 80 mg + Placebo37.05845.78141.092

[back to top]

Cmax of GSK1292263- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of GSK1292263 were taken on Days 1 and 14. For monotherapy arms, serial blood samples for the determination of the PK of GSK1292263 were collected on Days 1 and 14. Blood samples for PK were collected on Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hours PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. On Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionnanograms per milliliter (Geometric Mean)
Day 1Day 14
Atorvastatin 10 mg + GSK1292263 100 mg281.321361.595
Atorvastatin 10 mg + GSK1292263 300 mg475.297639.687
Atorvastatin 10 mg + GSK1292263 800 mg808.278886.418
Atorvastatin 80 mg + GSK1292263 800 mg790.315848.082
GSK1292263 100 mg263.279364.936
GSK1292263 300 mg478.676590.949
GSK1292263 800 mg787.922782.914

[back to top]

Maximum Observed Concentration (Cmax) of GSK1292263- Part A

Serial blood samples for the determination of the PK for GSK1292263 on Days 1 and 14 were collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (no 48 hour sample on Day 1). (NCT01218204)
Timeframe: On Days 1 and 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,
Interventionnanograms per milliliter (Geometric Mean)
Day 1Day 14
Atorvastatin 80 mg + GSK1292263 800 mg976.3351118.344
GSK1292263 800 mg986.811948.764

[back to top]

Number of Participants With Abnormal Clinical Chemistry Value of PCI- Part B (Pooled Treatment Arm)

Samples were collected fasting on Day -2, and prior to breakfast (early in the morning, fasting) on Days 2 (pre-dose), 4, 7, 10, 13 and on Day 15 prior to checkout (24 hours post-dose), and at Follow-up. When this resulted in multiple samples at the same time point, only one sample was collected (example, when 24 hours post dose = pre-dose (time 0) for the next dose). Data for only those parameters (Glucose, Total bilirubin, Albumin, Magnesium, CO2/HCO3, Calcium, ALT, AST, Inorganic phosphorus, Potassium and Sodium) are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to Day 26

,,,,,,,,,,
InterventionParticipants (Count of Participants)
Glucose, highGlucose, lowTotal bilirubin, highAlbumin, lowMagnesium, highCO2/HCO3, highCO2/HCO3, lowCalcium, highCalcium, lowALT, highAST, highInorganic phosphorus, highPotassium, lowSodium, high
Atorvastatin 10 mg + Ezetimibe 10 mg10101000100200
Atorvastatin 10 mg + GSK1292263 100 mg20200000000000
Atorvastatin 10 mg + GSK1292263 300 mg00011010100000
Atorvastatin 10 mg + GSK1292263 800 mg00002000011000
Atorvastatin 10 mg + Placebo00111000000000
Atorvastatin 80 mg + GSK1292263 800 mg00102000000000
Atorvastatin 80 mg + Placebo00003001000000
GSK1292263 100 mg10002000000000
GSK1292263 300 mg01003000000010
GSK1292263 800 mg00012000100001
Placebo00102100000000

[back to top]

Number of Participants With Abnormal Clinical Chemistry Value of PCI- Part B (run-in)

Samples were collected on Day 14 and 28 prior to breakfast (early in the morning, fasting). Data for only those parameters (Glucose, Magnesium, ALT, AST, Calcium, Inorganic phosphorus and Total bilirubin) are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Days 14 and 28

,
InterventionParticipants (Count of Participants)
Glucose, highMagnesium, highALT, highAST, highCalcium, highInorganic phosphorus, lowTotal bilirubin, high
Atorvastatin 10 mg1511000
Atorvastatin 80 mg0500111

[back to top]

Number of Participants With Abnormal Clinical Chemistry Value of PCI- Part B (Washout)

Samples were collected at screening, and on Days1 (first day of washout), 14 and 28 prior to breakfast (early in the morning, fasting). Data for only those parameters (Inorganic phosphorus, Sodium, Alanine aminotransferase [ALT], Potassium, Creatinine, Calcium, magnesium, Glucose, Total Bilirubin, Carbon dioxide/bicarbonate [CO2/HCO3] and Aspartate aminotransferase [AST]) are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to Day 28

InterventionParticipants (Count of Participants)
Inorganic phosphorus, highInorganic phosphorus, lowSodium, highSodium, lowALT, highPotassium, highPotassium, lowCreatinine, highCalcium, highMagnesium, highGlucose, highGlucose, lowTotal bilirubin, highCO2/bicarbonate, lowAST, high
Washout3211331123241611

[back to top]

Number of Participants With Abnormal Clinically Significant ECG Findings- Part B (Washout)

ECGs were taken at Screening, and on Day1 and Day 28. Single assessments were made. ECGs were taken in supine position. Additional ECGs were taken at the discretion of the investigator as needed based on symptoms or ECG findings. (NCT01218204)
Timeframe: Up to Day 28

InterventionParticipants (Count of Participants)
Day 1Day 28
Washout11

[back to top]

Number of Participants With Abnormal Hematology Value of PCI- Part A

Blood samples were collected fasting on Day -1, and prior to breakfast (early in the morning, fasting) on Days 2, 4, 7, 11 and on Day 15 prior to checkout (24 hours post last-dose), and at Follow-up. When this resulted in multiple samples at the same time point, only one sample was collected (example, when 24 hours post-dose = pre-dose (time 0) for the next dose). Data for only those parameters (Hematocrit, Hemoglobin and Total neutrophils) are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to Day 26

,
InterventionParticipants (Count of Participants)
Hematocrit, highHemoglobin, highTotal neutrophil, low
Atorvastatin 80 mg + GSK1292263 800 mg221
GSK1292263 800 mg100

[back to top]

Number of Participants With Abnormal Hematology Value of PCI- Part B (Pooled Treatment Arm)

Blood samples were collected fasting on Day -2, and prior to breakfast (early in the morning, fasting) on Days 2 (pre-dose), 4, 7, 10, 13 and on Day 15 prior to checkout (24hrs post-dose), and at Follow-up. When this resulted in multiple samples at the same time point, only one sample was collected (example, when 24hrs post dose = pre-dose (time 0) for the next dose). Data for only those parameters (Platelet count, Total neutrophils and Lymphocytes) are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to Day 26

,,,,,,,,,,
InterventionParticipants (Count of Participants)
Platelet count, lowTotal neutrophils, lowLymphocytes, low
Atorvastatin 10 mg + Ezetimibe 10 mg000
Atorvastatin 10 mg + GSK1292263 100 mg000
Atorvastatin 10 mg + GSK1292263 300 mg110
Atorvastatin 10 mg + GSK1292263 800 mg010
Atorvastatin 10 mg + Placebo000
Atorvastatin 80 mg + GSK1292263 800 mg000
Atorvastatin 80 mg + Placebo001
GSK1292263 100 mg001
GSK1292263 300 mg000
GSK1292263 800 mg000
Placebo010

[back to top]

Number of Participants With Abnormal Hematology Value of PCI- Part B (Washout)

Blood samples were collected at screening, and on Days 1 (first day of washout), 14 and 28 prior to breakfast (early in the morning, fasting). Data for only those parameters (White blood cells [WBC], Total neutrophils, Hematocrit and Lymphocytes) are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to Day 28

InterventionParticipants (Count of Participants)
WBC, highWBC, lowTotal neutrophil, lowHematocrit, highLymphocytes, low
Washout11122

[back to top]

Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs)- Part A

An AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect, or is an important medical events that jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, or a drug-induced liver injury. (NCT01218204)
Timeframe: Up to Day 26

,
InterventionParticipants (Count of Participants)
Any AEAny SAE
80 mg Atorvastatin + 800 mg GSK129226300
800 mg GSK129226320

[back to top]

Number of Participants With Any AEs and SAEs- Part B (Pooled Treatment Arm)

An AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect, or is an important medical events that jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, or a drug-induced liver injury. (NCT01218204)
Timeframe: Up to Day 26

,,,,,,,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Atorvastatin 10 mg + Ezetimibe 10 mg40
Atorvastatin 10 mg + GSK1292263 100 mg60
Atorvastatin 10 mg + GSK1292263 300 mg20
Atorvastatin 10 mg + GSK1292263 800 mg30
Atorvastatin 10 mg + Placebo30
Atorvastatin 80 mg + GSK1292263 800 mg60
Atorvastatin 80 mg + Placebo40
GSK1292263 100 mg50
GSK1292263 300 mg70
GSK1292263 800 mg80
Placebo40

[back to top]

AUC (0-24) of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of atorvastatin metabolites were collected on Day -1 and for atorvastatin metabolites on Days 1 and 14. Blood samples for PK were collected on Days -1 (co-dosing arms only) and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hour PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Days -1 and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionnanograms hour per milliliter (Geometric Mean)
Day -1Day 1Day 14
Atorvastatin 10 mg + Ezetimibe 10 mg12.4115.1018.18
Atorvastatin 10 mg + GSK1292263 100 mg16.7216.0210.07
Atorvastatin 10 mg + GSK1292263 300 mg20.2518.2816.54
Atorvastatin 10 mg + GSK1292263 800 mg14.3714.8913.82
Atorvastatin 10 mg + Placebo12.3813.6012.03
Atorvastatin 80 mg + GSK1292263 800 mg163.16146.23144.23
Atorvastatin 80 mg + Placebo133.96150.41156.41

[back to top]

AUC (0-24) of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part A

Serial blood samples for the determination of the PK for atorvastatin metabolites on Day -1 was collected at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose (24 hour sample Day -1 = 0 hour sample Day 1). Serial blood samples for the determination of the PK for atorvastatin metabolites on Days 1 and 14 will be collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose (no 48h sample on Day 1). (NCT01218204)
Timeframe: On Day -1 at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose. on Days 1 and 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose.

Interventionnanograms hour per milliliter (Geometric Mean)
Day -1Day 1Day 14
Atorvastatin 80 mg + GSK1292263 800 mg119.66127.70139.78

[back to top]

Area Under the Concentration-time Curve From Time Zero (Pre-dose) to 24 Hours [AUC(0-24)] of GSK1292263- Part A

Serial blood samples for the determination of the PK for GSK1292263, on Days 1 and 14 were collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (no 48 hour sample on Day 1). (NCT01218204)
Timeframe: On Days 1 and 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,
Interventionnanograms hour per milliliter (Geometric Mean)
Day 1Day 14
Atorvastatin 80 mg + GSK1292263 800 mg12953.8913206.52
GSK1292263 800 mg12032.2111890.40

[back to top]

Weighted Mean Area Under Concentration Curve From 0 to 24 Hours (AUC [0-24]) Change From Baseline for Triglycerides at Day 14

Blood samples were collected fasting on Days 1 (pre-dose), 7 and 15 prior to checkout (24 hours post-dose), and at Follow-up. When this results in multiple samples at the same time point, only one sample will be collected (example, when 24 hours post-dose = pre-dose (time 0) for the next dose). Baseline was Day -1 value. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value is missing, the change from Baseline was set to missing as well. Percent change from Baseline was calculated as the change from Baseline divided by the Baseline value then multiplied by 100. (NCT01218204)
Timeframe: Baseline and Day 14

Interventionmillimoles per liter (Geometric Mean)
Atorvastatin 10 mg + GSK1292263 100 mg0.13341
Atorvastatin 10 mg + GSK1292263 300 mg0.30812
Atorvastatin 10 mg + GSK1292263 800 mg0.12845
Atorvastatin 10 mg + Placebo0.25228
Atorvastatin 10 mg + Ezetimibe 10 mg0.09060
Atorvastatin 80 mg + GSK1292263 800 mg0.04974
Atorvastatin 80 mg + Placebo0.20164
GSK1292263 100 mg0.30543
GSK1292263 300 mg0.37442
GSK1292263 800 mg0.13079
Placebo0.28863

[back to top]

Tlag of GSK1292263- Part B (Pooled Treatment Arm)

Blood samples for PK were collected on Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. (NCT01218204)
Timeframe: On Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose.

Interventionhours (Median)
Atorvastatin 10 mg + GSK1292263 100 mg0.000
Atorvastatin 10 mg + GSK1292263 300 mg0.000
Atorvastatin 10 mg + GSK1292263 800 mg0.000
Atorvastatin 80 mg + GSK1292263 800 mg0.000
GSK1292263 100 mg0.000
GSK1292263 300 mg0.000
GSK1292263 800 mg0.000

[back to top]

Percent Change From Baseline in Lipid Metabolism: LDL/HDL Ratio at Day 14 (24 Hours)

Blood samples were collected fasting on Days 1 (pre-dose), 7 and 15 prior to checkout (24 hours post-dose), and at Follow-up. When this results in multiple samples at the same time point, only one sample will be collected (example, when 24 hours post-dose = pre-dose (time 0) for the next dose). Baseline was the closest scheduled value prior to dosing. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value is missing, the change from Baseline was set to missing as well. Percent change from Baseline was calculated as the change from Baseline divided by the Baseline value then multiplied by 100. (NCT01218204)
Timeframe: Baseline and Day 14

InterventionPercent change (Mean)
Atorvastatin 10 mg + GSK1292263 100 mg-12.25
Atorvastatin 10 mg + GSK1292263 300 mg-21.12
Atorvastatin 10 mg + GSK1292263 800 mg-41.61
Atorvastatin 10 mg + Placebo0.94
Atorvastatin 10 mg + Ezetimibe 10 mg-28.69
Atorvastatin 80 mg + GSK1292263 800 mg-34.35
Atorvastatin 80 mg + Placebo10.84
GSK1292263 100 mg-16.78
GSK1292263 300 mg-17.63
GSK1292263 800 mg-32.01
Placebo2.55

[back to top]

Percent Change From Baseline in Lipid Metabolism: Apolipoprotein E at Day 14 (24 Hours)

Blood samples were collected fasting on Days 1 (pre-dose), 7 and 15 prior to checkout (24 hours post-dose), and at Follow-up. When this results in multiple samples at the same time point, only one sample will be collected (example, when 24 hours post-dose = pre-dose (time 0) for the next dose). Baseline was the closest scheduled value prior to dosing. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value is missing, the change from Baseline was set to missing as well. Percent change from Baseline was calculated as the change from Baseline divided by the Baseline value then multiplied by 100. (NCT01218204)
Timeframe: Baseline and Day 14

InterventionPerecent change (Mean)
Atorvastatin 10 mg + GSK1292263 100 mg-21.97
Atorvastatin 10 mg + GSK1292263 300 mg-3.92
Atorvastatin 10 mg + GSK1292263 800 mg-31.41
Atorvastatin 10 mg + Placebo34.28
Atorvastatin 10 mg + Ezetimibe 10 mg-12.27
Atorvastatin 80 mg + GSK1292263 800 mg-13.19
Atorvastatin 80 mg + Placebo-13.41
GSK1292263 100 mg1.35
GSK1292263 300 mg-21.98
GSK1292263 800 mg-33.75
Placebo-1.58

[back to top]

Number of Participants With Abnormal- Clinically Significant Electrocardiogram (ECG) Findings- Part A

Single ECGs were taken after admission on Day -1 and at Follow-up (up to Day 26). On Days 1, 7, and 14 single ECGS were taken pre-breakfast (fasting) and at 1, 3, 6, 8, 14 and 24 hours post-dose. ECGs were taken in supine position. Additional ECGs were taken at the discretion of the investigator as needed based on symptoms or ECG findings. No value found to be abnormal clinically significant in Part A of the study. (NCT01218204)
Timeframe: Up to Day 26

InterventionParticipants (Count of Participants)
Atorvastatin 80 mg + GSK1292263 800 mg0
GSK1292263 800 mg0

[back to top]

Number of Participants With Abnormal Clinically Significant ECG Findings- Part B (Run-in)

ECGs were taken on Day 28. Single assessments were made. ECGs were taken in supine position. Additional ECGs were taken at the discretion of the investigator as needed based on symptoms or ECG findings. No data found to be abnormal clinically significant in run-in phase. (NCT01218204)
Timeframe: Day 28

InterventionParticipants (Count of Participants)
Atorvastatin 10 mg0
Atorvastatin 80 mg0

[back to top]

Number of Participants With Abnormal Clinically Significant ECG Findings- Part B (Pooled Treatment Arm)

Single ECGs were taken after admission on Day -2, and pre-breakfast on Days -1, 4, 10, and at Follow-up. On Days 1, 7, and 14 single ECGS were taken pre-breakfast (fasting) and at 1, 3, 6, 8, 14 and 24 hours post-dose. ECGs were taken in supine position. Additional ECGs were taken at the discretion of the investigator as needed based on symptoms or ECG findings. The data was found to be abnormal clinically significant in treatment phase. (NCT01218204)
Timeframe: Up to Day 26

InterventionParticipants (Count of Participants)
Atorvastatin 10 mg + GSK1292263 100 mg0
Atorvastatin 10 mg + GSK1292263 300 mg0
Atorvastatin 10 mg + GSK1292263 800 mg0
Atorvastatin 10 mg + Placebo0
Atorvastatin 10 mg + Ezetimibe 10 mg0
Atorvastatin 80 mg + GSK1292263 800 mg0
Atorvastatin 80 mg + Placebo0
GSK1292263 100 mg0
GSK1292263 300 mg0
GSK1292263 800 mg0
Placebo0

[back to top]

Number of Participants With Abnormal Clinical Chemistry Value of PCI- Part A

Samples were collected fasting on Day -1, and prior to breakfast (early in the morning, fasting) on Days 2, 4, 7, 11 and on Day 15 prior to checkout (24 hours post last-dose), and at Follow-up. When this resulted in multiple samples at the same time point, only one sample was collected (example, when 24 hours post-dose = pre-dose (time 0) for the next dose). No parameter was found to have any value of PCI. (NCT01218204)
Timeframe: Up to Day 26

InterventionParticipants (Count of Participants)
Atorvastatin 80 mg + GSK1292263 800 mg0
GSK1292263 800 mg0

[back to top]

Lag Time Before Observation of Drug Concentrations in Sampled Matrix (Tlag) of GSK1292263- Part A

Serial blood samples for the determination of the PK for GSK1292263 on Days 1 were collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (no 48h sample on Day 1). (NCT01218204)
Timeframe: On Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

Interventionhours (Median)
Atorvastatin 80 mg + GSK1292263 800 mg0.250
GSK1292263 800 mg0.000

[back to top]

Number of Participants With Any AEs and SAEs- Part B (Washout)

An AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect, or is an important medical events that jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, or a drug-induced liver injury. (NCT01218204)
Timeframe: Up to Day 28

,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Pre-treatment140
Washout370

[back to top]

Number of Participants With Any AEs and SAEs- Part B (Run-in)

An AE is defined as any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect, or is an important medical events that jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, or a drug-induced liver injury. (NCT01218204)
Timeframe: Up to Day 28

,
InterventionParticipants (Count of Participants)
Any AEAny SAE
Atorvastatin 10 mg190
Atorvastatin 80 mg80

[back to top]

Time of Occurrence of Cmax (Tmax) and Terminal Phase Half-life (t1/2) GSK1292263- Part A

Serial blood samples for the determination of the PK for GSK1292263, on Days 1 and 14 were collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (no 48 hour sample on Day 1). (NCT01218204)
Timeframe: On Days 1 and 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,
Interventionhours (Median)
tmax, Day 1tmax, Day 14t1/2, Day 1t1/2, Day 14
Atorvastatin 80 mg + GSK1292263 800 mg6.0003.00011.18520.629
GSK1292263 800 mg5.0005.06716.16419.395

[back to top]

Number of Participants With Vital Signs of PCI- Part B (Washout)

Assessment of vital signs including SBP, DBP heart rate was performed at Screening, on Days 1, 14 and 28 in the morning. At each time point, assessment was performed after resting in a supine or semi-supine position for at least 10 minutes. Data for only those parameters are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to day 28

InterventionParticipants (Count of Participants)
SBP, highHeart rate, high
Washout41

[back to top]

Number of Participants With Vital Signs of Potential Clinical Importance (PCI)- Part A

Assessment of vital signs including systolic blood pressure (SBP), diastolic blood pressure (DBP) and heart rate was performed after admission on Day -1 and at Follow-up. On Days 1, 7 and 14, they were taken at pre-dose, 1, 3, 6, 8, 14 and 24 hours after the morning dose. At each time point, assessment was performed after resting in a supine or semi-supine position for at least 10 minutes. Data for only those parameters are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to Day 26

,
InterventionParticipants (Count of Participants)
DBP, highDBP, low
Atorvastatin 80 mg + GSK1292263 800 mg00
GSK1292263 800 mg10

[back to top]

Number of Participants With Vital Signs of Potential Clinical Importance- Part B (Pooled Treatment Arm)

Assessment of vital signs including SBP, DBP and heart rate was performed after admission on Day-2, and pre-breakfast on Days -1, 4, and 10 in a fasting state early in the morning (prior to dosing), and at Follow-up. On Days 1, 7 and 14, they were also be taken at 1, 3, 6, 9, 12 and 24 hours after the morning dose. At each time point, assessment was performed after resting in a supine or semi-supine position for at least 10 minutes. Data for only those parameters are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to Day 26

,,,,,,,,,,
InterventionParticipants (Count of Participants)
SBP, highDBP, highDBP, lowHeart rate, high
Atorvastatin 10 mg + Ezetimibe 10 mg2010
Atorvastatin 10 mg + GSK1292263 100 mg0000
Atorvastatin 10 mg + GSK1292263 300 mg0000
Atorvastatin 10 mg + GSK1292263 800 mg1000
Atorvastatin 10 mg + Placebo3101
Atorvastatin 80 mg + GSK1292263 800 mg1110
Atorvastatin 80 mg + Placebo2000
GSK1292263 100 mg1110
GSK1292263 300 mg2000
GSK1292263 800 mg0000
Placebo0000

[back to top]

Number of Participants With Vital Signs of Potential Clinical Importance- Part B (Run-in)

Assessment of vital signs including SBP, DBP and heart rate was performed on Days 1, 14 and 28 in the morning. At each time point, assessment was performed after resting in a supine or semi-supine position for at least 10 minutes. Data for only those parameters are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Up to day 28

,
InterventionParticipants (Count of Participants)
SBP, highSBP, low
Atorvastatin 10 mg10
Atorvastatin 80 mg00

[back to top]

Percent Change From Baseline for Lipid Metabolism: Apolipoprotein A1 and Apolipoprotein B100 at Day 14

Blood samples were collected fasting on Days 1 (pre-dose), 7 and 15 prior to checkout (24 hours post-dose), and at Follow-up. When this results in multiple samples at the same time point, only one sample will be collected (example, when 24 hours post-dose = pre-dose (time 0) for the next dose). Baseline was the closest scheduled value prior to dosing. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value is missing, the change from Baseline was set to missing as well. Percent change from Baseline was calculated as the change from Baseline divided by the Baseline value then multiplied by 100. (NCT01218204)
Timeframe: Baseline and Day 14

,,,,,,,,,,
InterventionPercent change (Mean)
Apolipoprotein A1, 24 hoursApolipoprotein B100, 24 hours
Atorvastatin 10 mg + Ezetimibe 10 mg-3.88-15.49
Atorvastatin 10 mg + GSK1292263 100 mg-1.932.85
Atorvastatin 10 mg + GSK1292263 300 mg-8.72-17.93
Atorvastatin 10 mg + GSK1292263 800 mg4.17-22.22
Atorvastatin 10 mg + Placebo-7.19-5.03
Atorvastatin 80 mg + GSK1292263 800 mg-1.00-27.08
Atorvastatin 80 mg + Placebo-5.814.25
GSK1292263 100 mg3.76-10.21
GSK1292263 300 mg29.90-7.62
GSK1292263 800 mg-0.15-10.95
Placebo-0.18-2.39

[back to top]

Percent Change From Baseline in Lipid Metabolism: High Density Lipids Cholesterol (HDLc), Low Density Lipids Cholesterol (LDLc), Tryglycerides, Non-HDLc and Total Cholesterol at Day 14 (24 Hours)

Blood samples were collected fasting on Days 1 (pre-dose), 7 and 15 prior to checkout (24 hours post-dose), and at Follow-up. When this results in multiple samples at the same time point, only one sample will be collected (example, when 24 hours post-dose = pre-dose (time 0) for the next dose). Baseline was the closest scheduled value prior to dosing. The change from Baseline was calculated by subtracting the Baseline values from the individual post-randomization values. If either the Baseline or post-randomization value is missing, the change from Baseline was set to missing as well. Percent change from Baseline was calculated as the change from Baseline divided by the Baseline value then multiplied by 100. (NCT01218204)
Timeframe: Baseline and Day 14

,,,,,,,,,,
InterventionPercent change (Mean)
HDLcLDLcTriglyceidesNon-HDLcTotal cholesterol
Atorvastatin 10 mg + Ezetimibe 10 mg6.03-24.81-10.44-21.19-14.23
Atorvastatin 10 mg + GSK1292263 100 mg7.50-6.80-18.67-9.53-5.17
Atorvastatin 10 mg + GSK1292263 300 mg14.97-10.01-15.98-11.67-3.61
Atorvastatin 10 mg + GSK1292263 800 mg31.09-24.09-32.81-26.59-10.31
Atorvastatin 10 mg + Placebo-0.03-0.3710.702.080.89
Atorvastatin 80 mg + GSK1292263 800 mg26.22-18.63-21.39-21.88-5.52
Atorvastatin 80 mg + Placebo4.5015.012.27-0.941.09
GSK1292263 100 mg9.17-10.24-3.95-9.32-5.81
GSK1292263 300 mg9.76-11.86-30.84-17.02-12.06
GSK1292263 800 mg18.95-19.94-34.66-22.62-14.05
Placebo-1.370.7718.903.172.18

[back to top]

Tmax and t1/2 of GSK1292263- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of GSK1292263 were taken on Days 1 and 14. For monotherapy arms, serial blood samples for the determination of the PK of GSK1292263 were collected on Days 1 and 14. Blood samples for PK were collected on Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hours PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. On Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionhours (Median)
tmax, Day 1tmax, Day 14t1/2, Day 1t1/2, Day 14
Atorvastatin 10 mg + GSK1292263 100 mg3.9835.00012.63026.453
Atorvastatin 10 mg + GSK1292263 300 mg5.0084.00010.27021.569
Atorvastatin 10 mg + GSK1292263 800 mg4.0004.00010.41621.846
Atorvastatin 80 mg + GSK1292263 800 mg4.0004.00012.37224.225
GSK1292263 100 mg4.0004.00015.30523.893
GSK1292263 300 mg4.0003.98314.34225.203
GSK1292263 800 mg3.4754.00014.46419.478

[back to top]

Tmax of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part A

Serial blood samples for the determination of the PK for atorvastatin metabolites on Day -1 was collected at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose (24 hour sample Day -1 = 0 hour sample Day 1). Serial blood samples for the determination of the PK for atorvastatin metabolites on Days 1 and 14 will be collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose (no 48h sample on Day 1). (NCT01218204)
Timeframe: On Day -1 at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose. on Days 1 and 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose.

Interventionhours (Median)
Day -1Day 1Day 14
Atorvastatin 80 mg + GSK1292263 800 mg3.0004.0002.500

[back to top]

Tmax of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of atorvastatin metabolites were collected on Day -1 and for atorvastatin metabolites on Days 1 and 14. Blood samples for PK were collected on Days -1 (co-dosing arms only) and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hour PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Days -1 and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose and on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionhours (Median)
Day -1Day 1Day 14
Atorvastatin 10 mg + Ezetimibe 10 mg4.0004.0006.000
Atorvastatin 10 mg + GSK1292263 100 mg4.5006.0006.000
Atorvastatin 10 mg + GSK1292263 300 mg4.0006.0004.000
Atorvastatin 10 mg + GSK1292263 800 mg5.0004.0004.025
Atorvastatin 10 mg + Placebo4.0004.0005.000
Atorvastatin 80 mg + GSK1292263 800 mg3.9924.0004.000
Atorvastatin 80 mg + Placebo3.0003.0003.983

[back to top]

Tmax of Atorvastatin- Part A

Serial blood samples for the determination of the PK for atorvastatin on Day -1 was collected at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose (24 hour sample Day -1 = 0 hour sample Day 1). Serial blood samples for the determination of the PK for atorvastatin on Days 1 and 14 will be collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose (no 48h sample on Day 1). (NCT01218204)
Timeframe: On Day -1 at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose. on Days 1 and 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose.

Interventionhours (Median)
Day -1Day 1Day 14
Atorvastatin 80 mg + GSK1292263 800 mg3.0004.0002.250

[back to top]

Tmax of Atorvastatin- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of atorvastatin were collected on Day -1 and for atorvastatin on Days 1 and 14. Blood samples for PK were collected on Days -1 (co-dosing arms only) and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hour PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Days -1 and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionhours (Median)
Day -1Day 1Day 14
Atorvastatin 10 mg + Ezetimibe 10 mg4.0004.0002.000
Atorvastatin 10 mg + GSK1292263 100 mg2.5004.9924.000
Atorvastatin 10 mg + GSK1292263 300 mg3.0006.0004.000
Atorvastatin 10 mg + GSK1292263 800 mg3.9833.0003.500
Atorvastatin 10 mg + Placebo3.0173.9923.525
Atorvastatin 80 mg + GSK1292263 800 mg2.5083.4922.067
Atorvastatin 80 mg + Placebo1.5172.0003.000

[back to top]

Cmax of Atorvastatin- Part A

Serial blood samples for the determination of the PK for atorvastatin on Day -1 was collected at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose (24 hour sample Day -1 = 0 hour sample Day 1). Serial blood samples for the determination of the PK for atorvastatin on Days 1 and 14 will be collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose (no 48h sample on Day 1). (NCT01218204)
Timeframe: On Day -1 at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose. on Days 1 and 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose.

Interventionnanograms per milliliter (Geometric Mean)
Day -1Day 1Day 14
Atorvastatin 80 mg + GSK1292263 800 mg45.58725.86738.443

[back to top]

Cmax of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of atorvastatin metabolites were collected on Day -1 and for atorvastatin metabolites on Days 1 and 14. Blood samples for PK were collected on Days -1 (co-dosing arms only) and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hour PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Days -1 and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionnanograms per milliliter (Geometric Mean)
Day -1Day 1Day 14
Atorvastatin 10 mg + Ezetimibe 10 mg1.1851.2341.349
Atorvastatin 10 mg + GSK1292263 100 mg1.2981.0730.634
Atorvastatin 10 mg + GSK1292263 300 mg1.3881.2171.152
Atorvastatin 10 mg + GSK1292263 800 mg0.9471.0481.084
Atorvastatin 10 mg + Placebo0.9521.0280.869
Atorvastatin 80 mg + GSK1292263 800 mg26.10619.99122.645
Atorvastatin 80 mg + Placebo21.14926.40027.236

[back to top]

Cmax of Atorvastatin Metabolite (2-Hydroxyatorvastatin)- Part A

Serial blood samples for the determination of the PK for atorvastatin metabolites on Day -1 was collected at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose (24 hour sample Day -1 = 0 hour sample Day 1). Serial blood samples for the determination of the PK for atorvastatin metabolites on Days 1 and 14 will be collected at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose (no 48h sample on Day 1). (NCT01218204)
Timeframe: On Day -1 at immediately pre-morning dose=pre-breakfast (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14 and 24 hours post-morning dose. on Days 1 and 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hour post-morning dose.

Interventionnanograms per milliliter (Geometric Mean)
Day -1Day 1Day 14
Atorvastatin 80 mg + GSK1292263 800 mg17.52115.53521.271

[back to top]

AUC(0-24) of GSK1292263- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of GSK1292263 were taken on Days 1 and 14. For monotherapy arms, serial blood samples for the determination of the PK of GSK1292263 were collected on Days 1 and 14. Blood samples for PK were collected on Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hours PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Day 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. On Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionnanograms hour per milliliter (Geometric Mean)
Day 1Day 14
Atorvastatin 10 mg + GSK1292263 100 mg4218.024968.29
Atorvastatin 10 mg + GSK1292263 300 mg5373.787484.67
Atorvastatin 10 mg + GSK1292263 800 mg10384.2411224.58
Atorvastatin 80 mg + GSK1292263 800 mg9812.2110760.74
GSK1292263 100 mg2753.614061.78
GSK1292263 300 mg5342.776737.82
GSK1292263 800 mg8937.998837.31

[back to top]

AUC (0-24) of Atorvastatin- Part B (Pooled Treatment Arm)

For co-dosing arms, serial blood samples for the determination of the PK of atorvastatin were collected on Day -1 and for atorvastatin on Days 1 and 14. Blood samples for PK were collected on Days -1 (co-dosing arms only) and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hour PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Days -1 and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

,,,,,,
Interventionnanograms hour per milliliter (Geometric Mean)
Day -1Day 1Day 14
Atorvastatin 10 mg + Ezetimibe 10 mg19.5919.0520.24
Atorvastatin 10 mg + GSK1292263 100 mg23.1617.8415.58
Atorvastatin 10 mg + GSK1292263 300 mg28.7826.1923.77
Atorvastatin 10 mg + GSK1292263 800 mg19.2620.8320.41
Atorvastatin 10 mg + Placebo18.7719.3318.60
Atorvastatin 80 mg + GSK1292263 800 mg188.88174.13174.93
Atorvastatin 80 mg + Placebo173.62186.73188.31

[back to top]

AUC (0-24) of Atorvastatin- Part A

For co-dosing arms, serial blood samples for the determination of the PK of atorvastatin were collected on Day -1 and for atorvastatin on Days 1 and 14. Blood samples for PK were collected on Days -1 (co-dosing arms only) and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. Blood samples for PK were collected on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose (48 hour PK sample was collected on Day 16). (NCT01218204)
Timeframe: On Days -1 and 1 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, and 24 hours post-morning dose. on Day 14 at immediately pre-morning dose (time 0), 0.5, 1, 1.5, 2, 3, 4, 6, 8, 14, 24 and 48 hours post-morning dose

Interventionnanograms hour per milliliter (Geometric Mean)
Day -1Day 1Day 14
Atorvastatin 80 mg + GSK1292263 800 mg219.27199.15187.25

[back to top]

Number of Participants With Abnormal Hematology Value of PCI- Part B (Run-in)

Blood samples were collected on Day 14 and 28 prior to breakfast (early in the morning, fasting). Data for only those parameters (Lymphocytes) are presented for which findings are of PCI either high or low. (NCT01218204)
Timeframe: Days 14 and 28

,
InterventionParticipants (Count of Participants)
Lymphocytes, lowLymphocytes, high
Atorvastatin 10 mg00
Atorvastatin 80 mg10

[back to top]

Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) After 6 Weeks of Treatment

Non-HDL-C measured at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370590)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorva Fixed Dose Combination-50.1
Co-Administration Ezetimibe and Atorvastin-50.2

[back to top]

Percent Change From Baseline in Triglycerides (TG) After 6 Weeks of Treatment

Serum TG measured at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370590)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorva Fixed Dose Combination-28.3
Co-Administration Ezetimibe and Atorvastin-29.9

[back to top]

Percent Change From Baseline in Total Cholesterol (TC) After 6 Weeks of Treatment

Serum TC measured at baseline and after 6 week of treatment in each of the 2 treatment periods. (NCT01370590)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorva Fixed Dose Combination-38.1
Co-Administration Ezetimibe and Atorvastin-38.5

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) After 6 Weeks of Treatment

Serum LDL-C calculated using Friedewald formula at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370590)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorva Fixed Dose Combination-54.0
Co-Administration Ezetimibe and Atorvastin-53.8

[back to top]

Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) After 6 Weeks of Treatment

Serum HDL-C calculated at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370590)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorva Fixed Dose Combination5.4
Co-Administration Ezetimibe and Atorvastin4.6

[back to top]

Percent Change From Baseline in Apolipoprotein (Apo) B After 6 Weeks of Treatment

Serum Apo B measured at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370590)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorva Fixed Dose Combination-42.6
Co-Administration Ezetimibe and Atorvastin-43.3

[back to top]

Percent Change From Baseline in Total Cholesterol (TC) After 6 Weeks of Treatment

Serum TC measured at baseline and after 6 week of treatment in each of the 2 treatment periods. (NCT01370603)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorvastatin Fixed Dose Combination-43.0
Co-Administration Ezetimibe and Atorvastatin-42.9

[back to top]

Percent Change From Baseline in Triglycerides (TG) After 6 Weeks of Treatment

Serum TG measured at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370603)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorvastatin Fixed Dose Combination-36.2
Co-Administration Ezetimibe and Atorvastatin-36.2

[back to top]

Percent Change From Baseline in Apolipoprotein (Apo) B After 6 Weeks of Treatment

Serum Apo B measured at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370603)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorvastatin Fixed Dose Combination-48.7
Co-Administration Ezetimibe and Atorvastatin-48.3

[back to top]

Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) After 6 Weeks of Treatment

Serum HDL-C measured at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370603)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorvastatin Fixed Dose Combination2.3
Co-Administration Ezetimibe and Atorvastatin2.6

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) After 6 Weeks of Treatment

Serum LDL-C calculated using Friedewald formula at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370603)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorvastatin Fixed Dose Combination-58.9
Co-Administration Ezetimibe and Atorvastatin-58.7

[back to top]

Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) After 6 Weeks of Treatment

Non-HDL-C calculated at baseline and after 6 weeks of treatment in each of the 2 treatment periods. (NCT01370603)
Timeframe: Baseline and Week 6

InterventionPercentage Change (Least Squares Mean)
Ezetimibe/Atorvastatin Fixed Dose Combination-55.4
Co-Administration Ezetimibe and Atorvastatin-55.2

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12

LS means are based off an ANCOVA model which includes treatment group (3 evolocumab alone dose groups and the ezetimibe group) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.36
Evolocumab 280 mg-36.46
Evolocumab 350 mg-38.17
Evolocumab 420 mg-45.41

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe

LS means are based off an ANCOVA model which includes treatment group (evoloumab + ezetimibe and ezetimibe alone) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-10.74
Evolocumab + Ezetimibe-51.99

[back to top]

Percent Change From Baseline in LDL-C at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe

LDL-C was measured using ultracentrifugation. LS means are based off an ANCOVA model which includes treatment group (evolocumab + ezetimibe and ezetimibe alone) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-15.70
Evolocumab + Ezetimibe-62.98

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12

LDL-C was measured using ultracentrifugation. Least squares (LS) means are based off an analysis of covariance (ANCOVA) model which includes treatment group (3 evolocumab alone dose groups and the ezetimibe group) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-14.76
Evolocumab 280 mg-40.77
Evolocumab 350 mg-42.58
Evolocumab 420 mg-50.70

[back to top]

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

LS means are based off an ANCOVA model which includes treatment group (3 evolocumab alone dose groups and the ezetimibe group) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-14.97
Evolocumab 280 mg-39.83
Evolocumab 350 mg-41.63
Evolocumab 420 mg-48.58

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe

LS means are based off an ANCOVA model which includes treatment group (evolocumab + ezetimibe and ezetimibe alone) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-14.83
Evolocumab + Ezetimibe-59.82

[back to top]

Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at Week 12

LS means are based off an ANCOVA model which includes treatment group (3 evolocumab alone dose groups and the ezetimibe group) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-9.61
Evolocumab 280 mg-31.97
Evolocumab 350 mg-33.52
Evolocumab 420 mg-40.56

[back to top]

Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe

LS means are based off an ANCOVA model which includes treatment group (evoloumab + ezetimibe and ezetimibe alone) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.52
Evolocumab + Ezetimibe-49.44

[back to top]

Change From Baseline in LDL-C at Week 12

LDL-C was measured using ultracentrifugation. LS means are based off an ANCOVA model which includes treatment group (3 evolocumab alone dose groups and the ezetimibe group) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Ezetimibe-14.2
Evolocumab 280 mg-66.8
Evolocumab 350 mg-69.7
Evolocumab 420 mg-90.8

[back to top]

Change From Baseline in LDL-C at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe

LDL-C was measured using ultracentrifugation. LS means are based off an ANCOVA model which includes treatment group (evoloumab + ezetimibe and ezetimibe alone) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Ezetimibe-17.9
Evolocumab + Ezetimibe-109.8

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 12

LS means are based off an ANCOVA model which includes treatment group (3 evolocumab alone dose groups and the ezetimibe group) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-12.20
Evolocumab 280 mg-33.58
Evolocumab 350 mg-34.33
Evolocumab 420 mg-42.07

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 12: Ezetimibe Alone Versus Evolocumab + Ezetimibe

LS means are based off an ANCOVA model which includes treatment group (evoloumab + ezetimibe and ezetimibe) and stratification factors as covariates. (NCT01375764)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-10.84
Evolocumab + Ezetimibe-49.06

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12

LDL-C was measured using ultracentrifugation. (NCT01375777)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W-3.71
Placebo Q4W4.54
Ezetimibe-14.26
Evolocumab 70 mg Q2W-40.98
Evolocumab 105 mg Q2W-43.87
Evolocumab 140 mg Q2W-50.93
Evolocumab 280 mg Q4W-39.02
Evolocumab 350 mg Q4W-43.20
Evolocumab 420 mg Q4W-47.98

[back to top]

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

(NCT01375777)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W-2.89
Placebo Q4W-0.25
Ezetimibe-15.53
Evolocumab 70 mg Q2W-37.95
Evolocumab 105 mg Q2W-39.68
Evolocumab 140 mg Q2W-48.04
Evolocumab 280 mg Q4W-37.94
Evolocumab 350 mg Q4W-42.14
Evolocumab 420 mg Q4W-47.36

[back to top]

Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at Week 12

(NCT01375777)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W-1.21
Placebo Q4W-3.39
Ezetimibe-16.65
Evolocumab 70 mg Q2W-30.07
Evolocumab 105 mg Q2W-33.13
Evolocumab 140 mg Q2W-38.70
Evolocumab 280 mg Q4W-32.07
Evolocumab 350 mg Q4W-34.60
Evolocumab 420 mg Q4W-39.97

[back to top]

Change From Baseline in LDL-C at Week 12

LDL-C was measured using ultracentrifugation. (NCT01375777)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Placebo Q2W-3.4
Placebo Q4W7.3
Ezetimibe-19.2
Evolocumab 70 mg Q2W-55.7
Evolocumab 105 mg Q2W-66.0
Evolocumab 140 mg Q2W-69.3
Evolocumab 280 mg Q4W-53.5
Evolocumab 350 mg Q4W-56.7
Evolocumab 420 mg Q4W-65.0

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 12

(NCT01375777)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W-0.33
Placebo Q4W0.19
Ezetimibe-11.17
Evolocumab 70 mg Q2W-32.66
Evolocumab 105 mg Q2W-36.20
Evolocumab 140 mg Q2W-44.52
Evolocumab 280 mg Q4W-33.04
Evolocumab 350 mg Q4W-37.73
Evolocumab 420 mg Q4W-42.29

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A-1 Ratio at Week 12

(NCT01375777)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W2.03
Placebo Q4W0.14
Ezetimibe-12.35
Evolocumab 70 mg Q2W-32.80
Evolocumab 105 mg Q2W-38.30
Evolocumab 140 mg Q2W-48.13
Evolocumab 280 mg Q4W-36.10
Evolocumab 350 mg Q4W-40.43
Evolocumab 420 mg Q4W-45.33

[back to top]

Number of Participants Achieving Individual LDL Cholesterol (LDL-C) Target Level

Individual LDL-C target values were set according to the Austrian Cholesterol Consensus (ACC) 2007 for patients for patients suffering from coronary heart disease (CHD) or CHD equivalent in an office-based, routine medical care setting. Participants were categorized as either high-risk or very high-risk based on ACC criteria. The LDL-C target levels for each category were 100 mg/dL and 70 mg/dL, respectively (NCT01381679)
Timeframe: Up to 12 months

InterventionParticipants (Number)
All Participants678

[back to top]

Change From Baseline in Total Cholesterol (TC) at Month 3

(NCT01381679)
Timeframe: Baseline and Month 3

Interventionmg/dL (Mean)
All Participants-46.6

[back to top]

Change From Baseline in TC at Month 12

(NCT01381679)
Timeframe: Baseline and Month 12

Interventionmg/dL (Mean)
All Participants-54.5

[back to top]

Change From Baseline in LDL-C at Month 3

(NCT01381679)
Timeframe: Baseline and Month 3

Interventionmg/dL (Mean)
All Participants-41.7

[back to top]

Change From Baseline in HDL-C at Month 12

(NCT01381679)
Timeframe: Baseline and Month 12

Interventionmg/dL (Mean)
All Participants4.0

[back to top]

Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at Month 3

(NCT01381679)
Timeframe: Baseline and Month 3

Interventionmg/dL (Mean)
All Participants2.8

[back to top]

Change From Baseline in LDL-C at Month 12

(NCT01381679)
Timeframe: Baseline and Month 12

Interventionmg/dL (Mean)
All Participants-49.3

[back to top]

Change From Baseline in Triglycerides (TG) at Month 3

(NCT01381679)
Timeframe: Baseline and Month 3

Interventionmg/dL (Mean)
All Participants-33.8

[back to top]

Change From Baseline in TG at Month 12

(NCT01381679)
Timeframe: Baseline and Month 12

Interventionmg/dL (Mean)
All Participants-43.9

[back to top]

Reduction of LDL Cholesterol Levels

The primary efficacy variable was the percentage of LDL-C variation at the end of nine weeks of treatment, compared to baseline (pre-randomization), in participants who achieved LDL <100 mg/dL were considered to have been successfully treated. (NCT01420549)
Timeframe: Baseline compared to the end of 9 weeks of treatment

Interventionpercent change of LDL (Least Squares Mean)
Rosuvastatin + Ezetimibe-39.45
Simvastatin + Ezetimibe-29.13

[back to top]

Percent Change From Baseline in Triglycerides at Week 52

(NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo8.99
Evolocumab-2.55

[back to top]

Percent Change From Baseline in Very Low-density Lipoprotein Cholesterol (VLDL-C) at Week 52

Cholesterol was measured by means of ultracentrifugation. (NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo31.89
Evolocumab2.74

[back to top]

Percent Change From Week 12 to Week 52 in LDL-C

Cholesterol was measured by means of ultracentrifugation. (NCT01516879)
Timeframe: Week 12 and Week 52

Interventionpercent change (Least Squares Mean)
Placebo2.57
Evolocumab2.44

[back to top]

Percentage of Participants With an LDL-C Response at Week 52

An LDL-C response is defined as LDL-C level < 70 mg/dL (1.8 mmol/L) at Week 52. (NCT01516879)
Timeframe: Week 52

Interventionpercentage of participants (Number)
Placebo6.4
Evolocumab82.3

[back to top]

Change From Baseline in LDL-C at Week 52

Cholesterol was measured by means of ultracentrifugation. (NCT01516879)
Timeframe: Baseline and Week 52

Interventionmg/dL (Least Squares Mean)
Placebo5.1
Evolocumab-52.7

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 52

(NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo2.94
Evolocumab-41.26

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 52

(NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo4.46
Evolocumab-41.75

[back to top]

Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at Week 52

(NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo0.35
Evolocumab5.77

[back to top]

Percent Change From Baseline in LDL-C at Week 12

Cholesterol was measured by means of ultracentrifugation. (NCT01516879)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo3.17
Evolocumab-54.35

[back to top]

Percent Change From Baseline in LDL-C at Week 52

Cholesterol was measured by means of ultracentrifugation. (NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo6.83
Evolocumab-50.14

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 52

(NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo-5.37
Evolocumab-27.72

[back to top]

Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at Week 52

(NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo8.44
Evolocumab-41.82

[back to top]

Percent Change From Baseline in Total Cholesterol at Week 52

(NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo5.26
Evolocumab-28.18

[back to top]

Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at Week 52

(NCT01516879)
Timeframe: Baseline and Week 52

Interventionpercent change (Least Squares Mean)
Placebo6.47
Evolocumab-30.67

[back to top]

Percent Change From Baseline in Total Cholesterol at Week 12

(NCT01516879)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo2.85
Evolocumab-32.30

[back to top]

Percent Change in Low-density Lipoprotein Cholesterol (LDL-C) From Baseline

LDL-C levels measured at baseline and after 24 weeks of treatment (NCT01611883)
Timeframe: Baseline and Week 24

InterventionPercent Change (Least Squares Mean)
Ezetimibe-22.79
Placebo-1.75

[back to top]

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

HDL-C levels measured at baseline and after 24 weeks of treatment. (NCT01611883)
Timeframe: Baseline and Week 24

InterventionPercent Change (Least Squares Mean)
Ezetimibe3.86
Placebo1.41

[back to top]

"Percentage of Participants With Adverse Event (AE) Exacerbation of Diabetes"

"The Investigator took into account a participant's index of blood glucose control, diabetes medications, and compliance to diet and exercise therapy to assess overall control of the participant's diabetes and to determine if the participant's diabetes worsened. Participants who experienced the AE Exacerbation of Diabetes (verbatim term) were recorded." (NCT01611883)
Timeframe: up to 24 weeks

InterventionPercentage of Participants (Number)
Ezetimibe9.3
Placebo7.8

[back to top]

Change in Glycoalbumin From Baseline

Glycoalbumin is a blood marker used to assess blood glucose control over time and is reported as a percentage (%). Serum glycoalbumin levels were assessed at baseline and after 24 weeks of study drug administration. (NCT01611883)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Ezetimibe-0.02
Placebo-0.02

[back to top]

Change in Glycated Hemoglobin (HbA1c) From Baseline

HbA1c is blood marker used to report average blood glucose levels over a prolonged period of time and is reported as a percentage (%). HbA1C was measured at baseline and after 24 weeks of study drug administration. (NCT01611883)
Timeframe: Baseline and Week 24

InterventionPercent (Least Squares Mean)
Ezetimibe0.22
Placebo0.14

[back to top]

Change in Fasting Plasma Glucose (FPG) From Baseline

Plasma glucose levels were assessed after an overnight fast at baseline and after 24 weeks of study drug administration. (NCT01611883)
Timeframe: Baseline and Week 24

Interventionmg/dL (Least Squares Mean)
Ezetimibe6.6
Placebo11.4

[back to top]

Percentage of Participants With Changes in Diabetes Medications Due to Worsening of Diabetes

The percentage of participants who had changes to their medications used to treat their diabetes, other than small changes in insulin dosing (± 5 Units), were reported and summarized. (NCT01611883)
Timeframe: Up to 24 weeks

InterventionPercentage of Participants (Number)
Ezetimibe9.3
Placebo5.2

[back to top]

Percent Change in Triglycerides From Baseline

Triglycerides levels measured at baseline and after 24 weeks of treatment. (NCT01611883)
Timeframe: Baseline and Week 24

InterventionPercent Change (Least Squares Mean)
Ezetimibe-7.52
Placebo3.83

[back to top]

Percent Change in Total Cholesterol (TC) From Baseline

TC levels measured at Baseline and after 24 weeks of treatment. (NCT01611883)
Timeframe: Baseline and Week 24

InterventionPercent Change (Least Squares Mean)
Ezetimibe-15.01
Placebo-1.47

[back to top]

Percent Change in Non-HDL-cholesterol From Baseline

Non-HDL-C levels measured at baseline and after 24 weeks of treatment. (NCT01611883)
Timeframe: Baseline and Week 24

InterventionPercent Change (Least Squares Mean)
Ezetimibe-21.32
Placebo-2.25

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-42.6
Ezetimibe 10 mg-20.6

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including available post-baseline on-treatment data from Week 4 to Week 52 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-52.4
Ezetimibe 10 mg-22.7

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent-to-treat (ITT) Analysis

Adjusted Least-squares (LS) means and standard errors at Week 24 were obtained from a mixed-effect model with repeated measures (MMRM) to account for missing data. All available post-baseline data from week 4 to week 52 regardless of status on- or off-treatment were used in the model (ITT analysis). (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-50.6
Ezetimibe 10 mg-20.7

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 52 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 52 from MMRM model including available post-baseline on-treatment data from Week 4 to Week 52 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01644188)
Timeframe: From Baseline to Week 52

InterventionPercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-51.8
Ezetimibe 10 mg-19.7

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 12 - ITT Analysis

Adjusted means and standard errors at Week 12 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Mean)
Alirocumab 75 /up to 150 mg Q2W-13
Ezetimibe 10 mg-12.8

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis

Adjusted means and standard errors at Week 24 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Mean)
Alirocumab 75 /up to 150 mg Q2W-13
Ezetimibe 10 mg-12.8

[back to top]

Percent Change From Baseline in Apolipoprotein A-1 (Apo A-1) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W5
Ezetimibe 10 mg-1.3

[back to top]

Percent Change From Baseline in HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W8.7
Ezetimibe 10 mg2.8

[back to top]

Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W8.6
Ezetimibe 10 mg0.5

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 12 - ITT Analysis

Adjusted means and standard errors at Week 12 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Mean)
Alirocumab 75 /up to 150 mg Q2W-22.1
Ezetimibe 10 mg1.1

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 24 - ITT Analysis

Adjusted means and standard errors at Week 24 were obtained from multiple imputation approach followed by robust regression model for handling of missing data. All available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment were included in the imputation model. (NCT01644188)
Timeframe: From baseline to Week 52

Interventionpercent change (Mean)
Alirocumab 75 /up to 150 mg Q2W-27.8
Ezetimibe 10 mg-6.1

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 104 - ITT Analysis

Adjusted LS means and standard errors at Week 104 from MMRM including all available post-baseline data from Week 4 to Week 104 regardless of status on-or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 104

InterventionPercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-44.2
Ezetimibe 10 mg-15.2

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 24 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including available post-baseline on-treatment data from Week 4 to Week 52 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01644188)
Timeframe: From Baseline up to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-43.7
Ezetimibe 10 mg-20.2

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-42.1
Ezetimibe 10 mg-19.2

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-29.3
Ezetimibe 10 mg-14.6

[back to top]

Percent Change From Baseline in Calculated LDL--C at Week 24 - On--Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 52 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-52.4
Ezetimibe 10 mg-21.8

[back to top]

Percent Change From Baseline in Apolipoprotein B (Apo-B) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-40.7
Ezetimibe 10 mg-18.3

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 52 - ITT Analysis

Adjusted LS means and standard errors at Week 52 from a MMRM model including all available post-baseline data from week 4 to week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-49.5
Ezetimibe 10 mg-18.3

[back to top]

Percent Change From Baseline in Apo-B at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-39.7
Ezetimibe 10 mg-17.2

[back to top]

Percent Change From Baseline in Apo B at Week 24 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including available post-baseline on-treatment data from Week 4 to Week 52 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-42.1
Ezetimibe 10 mg-19.1

[back to top]

Percent Change From Baseline in Apo A-1 at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W1.5
Ezetimibe 10 mg-2.9

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 104 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 104 from MMRM model including available post-baseline on-treatment data from Week 4 to Week 104 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01644188)
Timeframe: From Baseline to Week 104

InterventionPercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-48.9
Ezetimibe 10 mg-17.0

[back to top]

Percent Change From Baseline in Total-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-29.4
Ezetimibe 10 mg-15.1

[back to top]

Percentage of Participants Achieving Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis

Adjusted percentages at Week 24 were obtained from multiple imputation approach for handling of missing data. All available post-baseline data from week 4 to week 52 regardless of status on- or off-treatment were included in the imputation model. (NCT01644188)
Timeframe: Up to Week 52

Interventionpercentage of participants (Number)
Alirocumab 75 /up to 150 mg Q2W77
Ezetimibe 10 mg45.6

[back to top]

Percentage of Participants Achieving Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - On-Treatment Analysis

Adjusted percentages at Week 24 from multiple imputation approach including available post-baseline on-treatment data from week 4 to week 52 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01644188)
Timeframe: Up to Week 52

Interventionpercentage of participants (Number)
Alirocumab 75 /up to 150 mg Q2W78.9
Ezetimibe 10 mg47.4

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from a MMRM including all available post-baseline data from week 4 to week 52 regardless of status on- or off-treatment. (NCT01644188)
Timeframe: From Baseline to Week 52

Interventionpercent change (Least Squares Mean)
Alirocumab 75 /up to 150 mg Q2W-51.2
Ezetimibe 10 mg-21.8

[back to top]

Percent Change From Baseline in Lipoprotein (a) at Week 24 - ITT Analysis

Adjusted means and standard errors at Week 24 from a multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Ezetimibe 10 mg-12.3
Alirocumab 75/Up to 150 mg Q2W-16.7

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-16.7
Alirocumab 75/Up to 150 mg Q2W-42.5

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-15.1
Alirocumab 75/Up to 150 mg Q2W-40.6

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-10.9
Alirocumab 75/Up to 150 mg Q2W-29.6

[back to top]

Percent Change From Baseline in Total-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-12.0
Alirocumab 75/Up to 150 mg Q2W-30.3

[back to top]

Percentage of Participants Achieving Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis

Adjusted percentages at Week 24 from multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Ezetimibe 10 mg2.4
Alirocumab 75/Up to 150 mg Q2W59.4

[back to top]

Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg1.6
Alirocumab 75/Up to 150 mg Q2W6.0

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 12 - ITT Analysis

Adjusted means and standard errors at Week 12 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Ezetimibe 10 mg-2.3
Alirocumab 75/Up to 150 mg Q2W-12.2

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent-to-Treat (ITT) Analysis

Adjusted Least-squares (LS) means and standard errors at Week 24 were obtained from a mixed-effect model with repeated measures (MMRM) to account for missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were used in the model (ITT analysis). (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-15.6
Alirocumab 75/Up to 150 mg Q2W-47.2

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-19.6
Alirocumab 75/Up to 150 mg Q2W-48.1

[back to top]

Percent Change From Baseline in Apolipoprotein A-1 (Apo A-1) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-0.6
Alirocumab 75/Up to 150 mg Q2W4.7

[back to top]

Percent Change From Baseline in Lipoprotein (a) at Week 12 - ITT Analysis

Adjusted means and standard errors at Week 12 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Ezetimibe 10 mg-14.2
Alirocumab 75/Up to 150 mg Q2W-17.2

[back to top]

Percent Change From Baseline in Apo B at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-11.7
Alirocumab 75/Up to 150 mg Q2W-37.3

[back to top]

Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-11.0
Alirocumab 75/Up to 150 mg Q2W-36.7

[back to top]

Percentage of Participants Achieving Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - ITT Analysis

Adjusted percentages at Week 24 were obtained from multiple imputation approach model for handling of missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were included in the imputation model. (NCT01644474)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Ezetimibe 10 mg32.2
Alirocumab 75/Up to 150 mg Q2W88.1

[back to top]

Percent Change From Baseline in HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg1.6
Alirocumab 75/Up to 150 mg Q2W9.0

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis

Adjusted means and standard errors at Week 24 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Ezetimibe 10 mg-10.8
Alirocumab 75/Up to 150 mg Q2W-11.9

[back to top]

Percent Change From Baseline in Apo A-1 at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01644474)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Ezetimibe 10 mg-2.2
Alirocumab 75/Up to 150 mg Q2W2.3

[back to top] [back to top]

Percent Change From Baseline in Apo A--1 at Week 12 -- ITT Analysis

Least squares (LS) means and standard errors (SE) taken from MMRM (mixed effect model with repeated measures) analysis. (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe3.9
Alirocumab 75 mg/ up to 150 mg5.5

[back to top]

Percent Change From Baseline in Apo A-1 at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe2.9
Alirocumab 75 mg/ up to 150 mg4.8

[back to top]

Percent Change From Baseline in Apo B at Week 12 -- ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.6
Alirocumab 75 mg/ up to 150 mg-36.1

[back to top]

Percent Change From Baseline in Apo B at Week 24 -- On--Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-14.4
Alirocumab 75 mg/ up to 150 mg-42.6

[back to top]

Percent Change From Baseline in Apolipoprotein (Apo) B at Week 24 -- ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post--baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.2
Alirocumab 75 mg/ up to 150 mg-36.3

[back to top]

Percent Change From Baseline in Calculated LDL--C at Week 12 -- ITT Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-15.6
Alirocumab 75 mg/ up to 150 mg-47.0

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12 - On--Treatment Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first) (on-treatment analysis). (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-18.0
Alirocumab 75 mg/ up to 150 mg-51.2

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent--To-Treat (ITT) Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted Least-squares (LS) means and standard errors at Week 24 were obtained from a mixed-effect model with repeated measures (MMRM) to account for missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were used in the model (ITT analysis). (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-14.6
Alirocumab 75 mg/ up to 150 mg-45.0

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 - On--Treatment Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first) (on-treatment analysis). (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-17.1
Alirocumab 75 mg/ up to 150 mg-52.2

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 Versus Atorvastatin - Raw Data Description - Intent-To-Treat (ITT) Analysis

(NCT01709513)
Timeframe: From Baseline up to Week 24

Interventionpercent change (Mean)
Atorvastatin (Statin Rechallenge Arm)-31.9
Ezetimibe (Active Comparator)-15.2
Alirocumab 75 mg/ up to 150 mg-47.3

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis

Combined Estimate for Adjusted Mean (Standard Error) at Week 24 from multiple imputation followed by robust regression including all available post-baseline data from Week 4 to Week 24 regardless of status on or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Ezetimibe-3.6
Alirocumab 75 mg/ up to 150 mg-9.3

[back to top]

Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe6.8
Alirocumab 75 mg/ up to 150 mg7.7

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 12 -- ITT Analysis

Combined Estimate for Adjusted Mean (Standard Error) at Week 24 from multiple imputation followed by robust regression including all available post-baseline data from Week 4 to Week 24 regardless of status on or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Mean)
Ezetimibe-4.5
Alirocumab 75 mg/ up to 150 mg-21.7

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 24 - ITT Analysis

Combined Estimate for Adjusted Mean (Standard Error) at Week 24 from multiple imputation followed by robust regression including all available post-baseline data from Week 4 to Week 24 regardless of status on or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Ezetimibe-7.3
Alirocumab 75 mg/ up to 150 mg-25.9

[back to top]

Percent Change From Baseline in Non--HDL-C at Week 24 -- On--Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first). (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-17.1
Alirocumab 75 mg/ up to 150 mg-46.9

[back to top]

Percent Change From Baseline in Non--High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 -- ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-14.6
Alirocumab 75 mg/ up to 150 mg-40.2

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-15.8
Alirocumab 75 mg/ up to 150 mg-41.5

[back to top]

Percent Change From Baseline in Total Cholesterol (Total--C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-10.9
Alirocumab 75 mg/ up to 150 mg-31.8

[back to top]

Percent Change From Baseline in Total-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.6
Alirocumab 75/ up to 150-32.7

[back to top]

Percent Change in Fasting Triglycerides From Baseline to Week 12 -- ITT Analysis

Combined Estimate for Adjusted Mean (Standard Error) at Week 24 from multiple imputation followed by robust regression including all available post-baseline data from Week 4 to Week 24 regardless of status on or off-treatment. (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Mean)
Ezetimibe-9.4
Alirocumab 75 mg/ up to 150 mg-8.0

[back to top]

Percent Change in HDL-C From Baseline to Week 12 -- ITT Analysis

Least-squares (LS) means and standard errors (SE) taken from MMRM (mixed-effect model with repeated measures) analysis (NCT01709513)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe7.6
Alirocumab 75 mg/ up to 150 mg9.0

[back to top]

Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis

Adjusted percentages at Week 24 were obtained from a multiple imputation approach model for handling of missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were included in the imputation model (ITT analysis). (NCT01709513)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Ezetimibe0.8
Alirocumab 75 mg/ up to 150 mg32.5

[back to top]

Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - On-Treatment Analysis

Adjusted percentages at Week 24 were obtained from a multiple imputation approach model including available post-baseline on-treatment data from Week 4 to Week 24 i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first (on-treatment analysis). (NCT01709513)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Ezetimibe0.8
Alirocumab 75 mg/ up to 150 mg39.0

[back to top]

Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or Moderate or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - ITT Analysis

Adjusted percentages at Week 24 were obtained from a multiple imputation approach model for handling of missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were included in the imputation model (ITT analysis). (NCT01709513)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Ezetimibe4.4
Alirocumab 75 mg/ up to 150 mg41.9

[back to top]

Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or Moderate or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - On-Treatment Analysis

Adjusted percentages at Week 24 were obtained from a multiple imputation approach model including available post-baseline on-treatment data from Week 4 to Week 24 i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first (on-treatment analysis). (NCT01709513)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Ezetimibe5.6
Alirocumab 75 mg/ up to 150 mg51.2

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 24 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule [whatever atorvastatin, rosuvastatin or ezetimibe], whichever came first). (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-7.5
Ezetimibe 10 mg + Atorvastatin 20 mg-18.1
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-40.5
Atorvastatin 80 mg-7.0
Rosuvastatin 40 mg-18.4
Ezetimibe 10 mg + Atorvastatin 40 mg-23.3
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-50.5

[back to top]

Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - ITT Analysis

Adjusted percentages at Week 24 were obtained from a multiple imputation approach model for handling of missing data. All available post-baseline data from Week 4 to week 24 regardless of status on- or off-treatment were included in the imputation model (ITT analysis). (NCT01730040)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Atorvastatin 40 mg34.5
Ezetimibe 10 mg + Atorvastatin 20 mg68.4
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg87.2
Atorvastatin 80 mg18.5
Rosuvastatin 40 mg62.2
Ezetimibe 10 mg + Atorvastatin 40 mg65.1
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg84.6

[back to top]

Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - On-Treatment Analysis

Adjusted percentages at Week 24 were obtained from a multiple imputation approach model including available post-baseline on-treatment data from Week 4 to Week 24 i.e. up to 21 days after last injection or 3 days after the last capsule [whatever atorvastatin, rosuvastatin or ezetimibe], whichever came first (on-treatment analysis). (NCT01730040)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Atorvastatin 40 mg20.0
Ezetimibe 10 mg + Atorvastatin 20 mg55.1
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg82.3
Atorvastatin 80 mg10.5
Rosuvastatin 40 mg42.4
Ezetimibe 10 mg + Atorvastatin 40 mg55.3
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg83.7

[back to top]

Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis

Adjusted percentages at Week 24 were obtained from a multiple imputation approach model for handling of missing data. All available post-baseline data from Week 4 to week 24 regardless of status on- or off-treatment were included in the imputation model (ITT analysis). (NCT01730040)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Atorvastatin 40 mg16.0
Ezetimibe 10 mg + Atorvastatin 20 mg50.3
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg79.2
Atorvastatin 80 mg10.2
Rosuvastatin 40 mg42.2
Ezetimibe 10 mg + Atorvastatin 40 mg54.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg77.2

[back to top]

Percent Change From Baseline in Total-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-6.5
Ezetimibe 10 mg + Atorvastatin 20 mg-13.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-29.0
Atorvastatin 80 mg-9.9
Rosuvastatin 40 mg-13.5
Ezetimibe 10 mg + Atorvastatin 40 mg-19.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-29.0

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-4.0
Ezetimibe 10 mg + Atorvastatin 20 mg-11.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-27.1
Atorvastatin 80 mg-4.8
Rosuvastatin 40 mg-11.7
Ezetimibe 10 mg + Atorvastatin 40 mg-15.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-33.6

[back to top]

Percent Change From Baseline in Non-High-density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-6.3
Ezetimibe 10 mg + Atorvastatin 20 mg-15.1
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-36.7
Atorvastatin 80 mg-6.5
Rosuvastatin 40 mg-17.4
Ezetimibe 10 mg + Atorvastatin 40 mg-21.0
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-47.6

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-7.1
Ezetimibe 10 mg + Atorvastatin 20 mg-17.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-40.6
Atorvastatin 80 mg-13.0
Rosuvastatin 40 mg-19.8
Ezetimibe 10 mg + Atorvastatin 40 mg-27.5
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-42.3

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 24 - ITT Analysis

Adjusted means and standard errors at Week 24 from from a multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Atorvastatin 40 mg-20.2
Ezetimibe 10 mg + Atorvastatin 20 mg-10.6
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-23.6
Atorvastatin 80 mg-9.7
Rosuvastatin 40 mg-4.9
Ezetimibe 10 mg + Atorvastatin 40 mg0.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-30.8

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 12 - ITT Analysis

Adjusted means and standard errors at Week 12 from from a multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Atorvastatin 40 mg-11.7
Ezetimibe 10 mg + Atorvastatin 20 mg-5.4
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-24.0
Atorvastatin 80 mg-1.6
Rosuvastatin 40 mg11.5
Ezetimibe 10 mg + Atorvastatin 40 mg7.9
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-27.9

[back to top]

Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg1.9
Ezetimibe 10 mg + Atorvastatin 20 mg-0.1
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg4.8
Atorvastatin 80 mg4.7
Rosuvastatin 40 mg5.7
Ezetimibe 10 mg + Atorvastatin 40 mg2.0
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg7.7

[back to top]

Percent Change From Baseline in HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-3.2
Ezetimibe 10 mg + Atorvastatin 20 mg-1.7
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg4.1
Atorvastatin 80 mg3.0
Rosuvastatin 40 mg4.6
Ezetimibe 10 mg + Atorvastatin 40 mg4.6
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg8.5

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis

Adjusted means and standard errors at Week 24 from from a multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Atorvastatin 40 mg-6.7
Ezetimibe 10 mg + Atorvastatin 20 mg-3.3
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-12.0
Atorvastatin 80 mg-7.3
Rosuvastatin 40 mg-0.5
Ezetimibe 10 mg + Atorvastatin 40 mg-13.9
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-19.1

[back to top]

Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - On-Treatment Analysis

Adjusted percentages at Week 24 were obtained from a multiple imputation approach model including available post-baseline on-treatment data from Week 4 to Week 24 i.e. up to 21 days after last injection or 3 days after the last capsule [whatever atorvastatin, rosuvastatin or ezetimibe], whichever came first (on-treatment analysis). (NCT01730040)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Atorvastatin 40 mg37.8
Ezetimibe 10 mg + Atorvastatin 20 mg72.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg91.2
Atorvastatin 80 mg18.5
Rosuvastatin 40 mg64.0
Ezetimibe 10 mg + Atorvastatin 40 mg66.2
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg90.0

[back to top]

Percent Change From Baseline in Apolipoprotein (Apo) B at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-4.4
Ezetimibe 10 mg + Atorvastatin 20 mg-10.1
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-33.7
Atorvastatin 80 mg-3.5
Rosuvastatin 40 mg-10.9
Ezetimibe 10 mg + Atorvastatin 40 mg-14.3
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-41.9

[back to top]

Percent Change From Baseline in Apo B at Week 24 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (ie. up to 21 days after last injection or 3 days after the last capsule [whatever atorvastatin, rosuvastatin or ezetimibe], whichever came first). (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-5.1
Ezetimibe 10 mg + Atorvastatin 20 mg-12.6
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-37.7
Atorvastatin 80 mg-4.4
Rosuvastatin 40 mg-12.8
Ezetimibe 10 mg + Atorvastatin 40 mg-16.3
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-42.7

[back to top]

Percent Change From Baseline in Apo B at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-6.9
Ezetimibe 10 mg + Atorvastatin 20 mg-13.1
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-38.4
Atorvastatin 80 mg-9.5
Rosuvastatin 40 mg-14.1
Ezetimibe 10 mg + Atorvastatin 40 mg-20.3
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-36.2

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 12 - ITT Analysis

Adjusted means and standard errors at Week 12 from from a multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Atorvastatin 40 mg-4.7
Ezetimibe 10 mg + Atorvastatin 20 mg0.5
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-12.4
Atorvastatin 80 mg-4.6
Rosuvastatin 40 mg-3.7
Ezetimibe 10 mg + Atorvastatin 40 mg-16.8
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-12.1

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 - On-Treatment Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule [whatever atorvastatin, rosuvastatin or ezetimibe], whichever came first) (on-treatment analysis). (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-6.1
Ezetimibe 10 mg + Atorvastatin 20 mg-23.7
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-48.6
Atorvastatin 80 mg-5.0
Rosuvastatin 40 mg-22.9
Ezetimibe 10 mg + Atorvastatin 40 mg-24.5
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-57.8

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent-to-treat (ITT) Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted Least-squares (LS) means and standard errors at Week 24 were obtained from a mixed-effect model with repeated measures (MMRM) to account for missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were used in the model (ITT analysis). (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-5
Ezetimibe 10 mg + Atorvastatin 20 mg-20.5
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-44.1
Atorvastatin 80 mg-4.8
Rosuvastatin 40 mg-21.4
Ezetimibe 10 mg + Atorvastatin 40 mg-22.6
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-54

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12 - On-Treatment Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule [whatever atorvastatin, rosuvastatin or ezetimibe], whichever came first) (on-treatment analysis). (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-9.2
Ezetimibe 10 mg + Atorvastatin 20 mg-27.1
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-53.7
Atorvastatin 80 mg-14.6
Rosuvastatin 40 mg-23.3
Ezetimibe 10 mg + Atorvastatin 40 mg-30.7
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-50.9

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12 - ITT Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment (ITT analysis). (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-8.5
Ezetimibe 10 mg + Atorvastatin 20 mg-22.6
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg-48.4
Atorvastatin 80 mg-14.5
Rosuvastatin 40 mg-23.3
Ezetimibe 10 mg + Atorvastatin 40 mg-29.7
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg-50.5

[back to top]

Percent Change From Baseline in Apo A-1 at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg-0.8
Ezetimibe 10 mg + Atorvastatin 20 mg1.7
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg5.4
Atorvastatin 80 mg1.6
Rosuvastatin 40 mg5.6
Ezetimibe 10 mg + Atorvastatin 40 mg1.6
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg9.4

[back to top]

Percent Change From Baseline in Apo A-1 at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730040)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Atorvastatin 40 mg1.2
Ezetimibe 10 mg + Atorvastatin 20 mg1.0
Alirocumab 75 mg/up to 150 mg + Atorvastatin 20 mg7.6
Atorvastatin 80 mg2.2
Rosuvastatin 40 mg4.7
Ezetimibe 10 mg + Atorvastatin 40 mg-1.8
Alirocumab 75 mg/up to 150 mg + Atorvastatin 40 mg5.8

[back to top]

Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - ITT Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted percentages at Week 24 were obtained from a multiple imputation approach model for handling of missing data. All available post-baseline data from Week 4 to week 24 regardless of status on- or off-treatment were included in the imputation model (ITT analysis). (NCT01730053)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Rosuvastatin 20 mg45.0
Ezetimibe 10 mg + Rosuvastatin 10 mg57.2
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg84.9
Rosuvastatin 40 mg40.1
Ezetimibe 10 mg + Rosuvastatin 20 mg52.2
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg66.7

[back to top]

Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - On-Treatment Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted percentages at Week 24 were obtained from a multiple imputation approach model including available post-baseline on-treatment data from Week 4 to Week 24 i.e. up to 21 days after last injection or 3 days after the last capsule [whatever rosuvastatin or ezetimibe], whichever came first (on-treatment analysis). (NCT01730053)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Rosuvastatin 20 mg34.8
Ezetimibe 10 mg + Rosuvastatin 10 mg46.7
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg76.5
Rosuvastatin 40 mg30.6
Ezetimibe 10 mg + Rosuvastatin 20 mg45.1
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg66.1

[back to top]

Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 24 - ITT Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted percentages at Week 24 were obtained from a multiple imputation approach model for handling of missing data. All available post-baseline data from Week 4 to week 24 regardless of status on- or off-treatment were included in the imputation model (ITT analysis). (NCT01730053)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Rosuvastatin 20 mg31.3
Ezetimibe 10 mg + Rosuvastatin 10 mg43.1
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg77.8
Rosuvastatin 40 mg29.9
Ezetimibe 10 mg + Rosuvastatin 20 mg43.6
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg60.1

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12 - ITT Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment (ITT analysis). (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-17.1
Ezetimibe 10 mg + Rosuvastatin 10 mg-17.4
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-49.6
Rosuvastatin 40 mg-22.1
Ezetimibe 10 mg + Rosuvastatin 20 mg-19.3
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-32.3

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12 - On-Treatment Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule [whatever rosuvastatin or ezetimibe], whichever came first) (on-treatment analysis). (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-17.2
Ezetimibe 10 mg + Rosuvastatin 10 mg-20.3
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-52.6
Rosuvastatin 40 mg-22.9
Ezetimibe 10 mg + Rosuvastatin 20 mg-21.8
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-35.1

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 - Intent-to-Treat (ITT) Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted Least-squares (LS) means and standard errors at Week 24 were obtained from a mixed-effect model with repeated measures (MMRM) to account for missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were used in the model (ITT analysis). (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-16.3
Ezetimibe 10 mg + Rosuvastatin 10 mg-14.4
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-50.6
Rosuvastatin 40 mg-15.9
Ezetimibe 10 mg + Rosuvastatin 20 mg-11.0
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-36.3

[back to top]

Percent Change From Baseline in Total-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-8.9
Ezetimibe 10 mg + Rosuvastatin 10 mg-11.8
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-29.0
Rosuvastatin 40 mg-13.8
Ezetimibe 10 mg + Rosuvastatin 20 mg-13.9
Alirocumab 75 mg/ up to 150 mg + Rosuvastatin 20 mg-19.4

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-8.3
Ezetimibe 10 mg + Rosuvastatin 10 mg-8.7
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-28.9
Rosuvastatin 40 mg-8.5
Ezetimibe 10 mg + Rosuvastatin 20 mg-12.4
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-20.6

[back to top]

Percent Change From Baseline in Non-High-density Lipoprotein Cholesterol (Non-HDL-C) at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-11.3
Ezetimibe 10 mg + Rosuvastatin 10 mg-13.4
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-42.7
Rosuvastatin 40 mg-11.2
Ezetimibe 10 mg + Rosuvastatin 20 mg-12.9
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-31.4

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 24 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule [whatever rosuvastatin or ezetimibe], whichever came first). (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-12.9
Ezetimibe 10 mg + Rosuvastatin 10 mg-17.5
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-45.7
Rosuvastatin 40 mg-14.9
Ezetimibe 10 mg + Rosuvastatin 20 mg-18.2
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-35.6

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-11.7
Ezetimibe 10 mg + Rosuvastatin 10 mg-16.3
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-41.2
Rosuvastatin 40 mg-18.0
Ezetimibe 10 mg + Rosuvastatin 20 mg-18.7
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-29.8

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 24 - ITT Analysis

Adjusted means and standard errors at Week 24 from a multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Rosuvastatin 20 mg-4.0
Ezetimibe 10 mg + Rosuvastatin 10 mg-4.3
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-27.9
Rosuvastatin 40 mg-5.2
Ezetimibe 10 mg + Rosuvastatin 20 mg-5.8
Alirocumab 75 mg/ up to 150 mg + Rosuvastatin 20 mg-22.7

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 24 - On-Treatment Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (ie. up to 21 days after last injection or 3 days after the last capsule [whatever rosuvastatin or ezetimibe], whichever came first) (on-treatment analysis). (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-18.3
Ezetimibe 10 mg + Rosuvastatin 10 mg-20.3
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-53.5
Rosuvastatin 40 mg-17.0
Ezetimibe 10 mg + Rosuvastatin 20 mg-16.5
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-41.5

[back to top]

Percent Change From Baseline in Apolipoprotein (Apo) B at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-7.3
Ezetimibe 10 mg + Rosuvastatin 10 mg-9.7
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-36.5
Rosuvastatin 40 mg-9.8
Ezetimibe 10 mg + Rosuvastatin 20 mg-11.2
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-28.3

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 12 - ITT Analysis

Adjusted means and standard errors at Week 12 from a multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Mean)
Rosuvastatin 20 mg8.1
Ezetimibe 10 mg + Rosuvastatin 10 mg-8.2
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-14
Rosuvastatin 40 mg-2.7
Ezetimibe 10 mg + Rosuvastatin 20 mg-12.4
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-10.1

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 24 - ITT Analysis

Adjusted means and standard errors at Week 24 from a multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Rosuvastatin 20 mg-1.8
Ezetimibe 10 mg + Rosuvastatin 10 mg-8.3
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-11.2
Rosuvastatin 40 mg-9.9
Ezetimibe 10 mg + Rosuvastatin 20 mg-11.1
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-8.7

[back to top]

Percent Change From Baseline in HDL-C at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg0.7
Ezetimibe 10 mg + Rosuvastatin 10 mg0.2
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg5.9
Rosuvastatin 40 mg0.6
Ezetimibe 10 mg + Rosuvastatin 20 mg3.1
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg8.0

[back to top]

Percent Change From Baseline in HDL-C at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg1.7
Ezetimibe 10 mg + Rosuvastatin 10 mg4.0
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg9.1
Rosuvastatin 40 mg1.5
Ezetimibe 10 mg + Rosuvastatin 20 mg-1.8
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg7.2

[back to top]

Percent Change From Baseline in Lipoprotein (a) at Week 12 - ITT Analysis

Adjusted means and standard errors at Week 12 from a multiple imputation approach model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Mean)
Rosuvastatin 20 mg-0.7
Ezetimibe 10 mg + Rosuvastatin 10 mg-3.9
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-20.7
Rosuvastatin 40 mg3.5
Ezetimibe 10 mg + Rosuvastatin 20 mg7.9
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-16.0

[back to top]

Percent Change From Baseline in Apo A-1 at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg4.0
Ezetimibe 10 mg + Rosuvastatin 10 mg2.6
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg4.3
Rosuvastatin 40 mg0.9
Ezetimibe 10 mg + Rosuvastatin 20 mg1.8
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg9.1

[back to top]

Percent Change From Baseline in Apo A-1 at Week 24 - ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg5.4
Ezetimibe 10 mg + Rosuvastatin 10 mg5.0
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg6.7
Rosuvastatin 40 mg2.9
Ezetimibe 10 mg + Rosuvastatin 20 mg-0.9
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg6.7

[back to top]

Percent Change From Baseline in Apo B at Week 12 - ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT01730053)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-8.1
Ezetimibe 10 mg + Rosuvastatin 10 mg-12.1
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-36.1
Rosuvastatin 40 mg-13.7
Ezetimibe 10 mg + Rosuvastatin 20 mg-14.3
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-29.0

[back to top]

Percent Change From Baseline in Apo B at Week 24 - On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including available post-baseline on-treatment data from Week 4 to Week 24 (ie. up to 21 days after last injection or 3 days after the last capsule [whatever rosuvastatin or ezetimibe], whichever came first). (NCT01730053)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Rosuvastatin 20 mg-8.8
Ezetimibe 10 mg + Rosuvastatin 10 mg-11.2
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg-39.5
Rosuvastatin 40 mg-12.7
Ezetimibe 10 mg + Rosuvastatin 20 mg-12.6
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg-30.4

[back to top]

Percentage of Very High CV Risk Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) or High CV Risk Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 24 - On-Treatment Analysis

Calculated LDL-C values were obtained from Friedewald formula. Adjusted percentages at Week 24 were obtained from a multiple imputation approach model including available post-baseline on-treatment data from Week 4 to Week 24 i.e. up to 21 days after last injection or 3 days after the last capsule [whatever rosuvastatin or ezetimibe], whichever came first (on-treatment analysis). (NCT01730053)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Rosuvastatin 20 mg47.0
Ezetimibe 10 mg + Rosuvastatin 10 mg60.5
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 10 mg86.4
Rosuvastatin 40 mg41.3
Ezetimibe 10 mg + Rosuvastatin 20 mg54.8
Alirocumab 75 mg/up to 150 mg + Rosuvastatin 20 mg70.4

[back to top]

Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W0.05
Placebo QM1.54
Ezetimibe (Q2W)-13.47
Ezetimibe (QM)-14.75
Evolocumab Q2W-47.04
Evolocumab QM-49.39

[back to top]

Percent Change From Baseline in HDL-C at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Median)
Placebo Q2W-1.15
Placebo QM-5.27
Ezetimibe (Q2W)-2.79
Ezetimibe (QM)-1.47
Evolocumab Q2W4.76
Evolocumab QM4.06

[back to top]

Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Median)
Placebo Q2W-1.64
Placebo QM-4.67
Ezetimibe (Q2W)-0.92
Ezetimibe (QM)0.00
Evolocumab Q2W3.89
Evolocumab QM3.81

[back to top]

Percentage of Participants Who Achieved a Mean LDL-C at Weeks 10 and 12 of Less Than 70 mg/dL

(NCT01763827)
Timeframe: Weeks 10 and 12

Interventionpercentage of participants (Number)
Placebo Q2W0.0
Placebo QM0.0
Ezetimibe (Q2W)1.3
Ezetimibe (QM)2.8
Evolocumab Q2W73.6
Evolocumab QM71.3

[back to top]

Percent Change From Baseline in Very Low Density Lipoprotein Cholesterol (VLDL-C) at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Median)
Placebo Q2W-3.81
Placebo QM4.22
Ezetimibe (Q2W)-2.69
Ezetimibe (QM)-3.33
Evolocumab Q2W-8.40
Evolocumab QM-16.17

[back to top]

Percent Change From Baseline in Lipoprotein (a) at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Median)
Placebo Q2W0.00
Placebo QM0.00
Ezetimibe (Q2W)0.00
Ezetimibe (QM)-2.05
Evolocumab Q2W-20.41
Evolocumab QM-17.82

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W0.10
Placebo QM-1.34
Ezetimibe (Q2W)-17.75
Ezetimibe (QM)-18.57
Evolocumab Q2W-57.04
Evolocumab QM-56.12

[back to top]

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

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W-0.31
Placebo QM1.51
Ezetimibe (Q2W)-14.89
Ezetimibe (QM)-16.48
Evolocumab Q2W-50.12
Evolocumab QM-49.68

[back to top]

Percent Change From Baseline in Total Cholesterol/High Density Lipoprotein-cholesterol Ratio at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W0.44
Placebo QM6.42
Ezetimibe (Q2W)-9.14
Ezetimibe (QM)-11.90
Evolocumab Q2W-38.49
Evolocumab QM-39.41

[back to top]

Percent Change From Baseline in Total Cholesterol/High Density Lipoprotein-cholesterol Ratio at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W1.18
Placebo QM7.02
Ezetimibe (Q2W)-10.03
Ezetimibe (QM)-12.34
Evolocumab Q2W-38.45
Evolocumab QM-37.65

[back to top]

Percent Change From Baseline in Triglycerides at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Median)
Placebo Q2W-3.89
Placebo QM4.89
Ezetimibe (Q2W)-1.46
Ezetimibe (QM)-3.97
Evolocumab Q2W-9.16
Evolocumab QM-15.71

[back to top]

Percent Change From Baseline in Triglycerides at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Median)
Placebo Q2W-1.91
Placebo QM2.01
Ezetimibe (Q2W)0.00
Ezetimibe (QM)-2.41
Evolocumab Q2W-8.14
Evolocumab QM-15.64

[back to top]

Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W-1.41
Placebo QM1.32
Ezetimibe (Q2W)-14.64
Ezetimibe (QM)-16.48
Evolocumab Q2W-50.22
Evolocumab QM-51.96

[back to top]

Percentage of Participants Who Achieved LDL-C < 70 mg/dL at Week 12

(NCT01763827)
Timeframe: Week 12

Interventionpercentage of participants (Number)
Placebo Q2W1.4
Placebo QM0.0
Ezetimibe (Q2W)1.4
Ezetimibe (QM)1.4
Evolocumab Q2W72.9
Evolocumab QM65.4

[back to top]

Change From Baseline in LDL-C at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionmg/dL (Least Squares Mean)
Placebo Q2W1.2
Placebo QM0.0
Ezetimibe (Q2W)-23.1
Ezetimibe (QM)-25.9
Evolocumab Q2W-78.4
Evolocumab QM-81.9

[back to top]

Change From Baseline in LDL-C at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Placebo Q2W1.9
Placebo QM-0.1
Ezetimibe (Q2W)-23.4
Ezetimibe (QM)-25.0
Evolocumab Q2W-78.4
Evolocumab QM-77.9

[back to top]

Percent Change From Baseline in VLDL-C at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Median)
Placebo Q2W-1.58
Placebo QM0.00
Ezetimibe (Q2W)-0.94
Ezetimibe (QM)-3.61
Evolocumab Q2W-9.52
Evolocumab QM-16.33

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W0.59
Placebo QM1.84
Ezetimibe (Q2W)-13.17
Ezetimibe (QM)-14.02
Evolocumab Q2W-47.21
Evolocumab QM-46.59

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W1.01
Placebo QM3.85
Ezetimibe (Q2W)-13.39
Ezetimibe (QM)-14.49
Evolocumab Q2W-48.12
Evolocumab QM-51.10

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12

(NCT01763827)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W1.12
Placebo QM4.51
Ezetimibe (Q2W)-12.69
Ezetimibe (QM)-14.29
Evolocumab Q2W-48.45
Evolocumab QM-48.26

[back to top]

Percent Change From Baseline in Lipoprotein (a) at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Median)
Placebo Q2W0.12
Placebo QM0.00
Ezetimibe (Q2W)0.00
Ezetimibe (QM)-2.08
Evolocumab Q2W-18.37
Evolocumab QM-19.24

[back to top]

Percent Change From Baseline in LDL-C at the Mean of Weeks 10 and 12

(NCT01763827)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Placebo Q2W-0.43
Placebo QM-1.41
Ezetimibe (Q2W)-17.52
Ezetimibe (QM)-19.12
Evolocumab Q2W-56.93
Evolocumab QM-58.81

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W7.34
A10 PBO QM-0.43
A10 EZE (Q2W)3.29
A10 EZE (QM)7.18
A10 EvoMab Q2W-25.87
A10 EvoMab QM-20.25
A80 PBO Q2W-2.23
A80 PBO QM3.41
A80 EZE (Q2W)8.01
A80 EZE (QM)10.20
A80 EvoMab Q2W-24.61
A80 EvoMab QM-24.68
R5 PBO Q2W11.40
R5 PBO QM4.49
R5 EvoMab Q2W-25.09
R5 EvoMab QM-20.85
R40 PBO Q2W10.38
R40 PBO QM10.21
R40 EvoMab Q2W-26.11
R40 EvoMab QM-21.97
S40 PBO Q2W-6.81
S40 PBO QM-1.06
S40 EvoMab Q2W-38.06
S40 EvoMab QM-29.23

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W9.86
A10 PBO QM0.97
A10 EZE (Q2W)-21.96
A10 EZE (QM)-17.08
A10 EvoMab Q2W-61.56
A10 EvoMab QM-58.19
A80 PBO Q2W14.49
A80 PBO QM11.83
A80 EZE (Q2W)-14.60
A80 EZE (QM)-19.80
A80 EvoMab Q2W-61.80
A80 EvoMab QM-58.68
R5 PBO Q2W8.12
R5 PBO QM5.10
R5 EvoMab Q2W-60.09
R5 EvoMab QM-59.40
R40 PBO Q2W9.42
R40 PBO QM2.59
R40 EvoMab Q2W-58.89
R40 EvoMab QM-52.40
S40 PBO Q2W4.70
S40 PBO QM3.40
S40 EvoMab Q2W-65.86
S40 EvoMab QM-57.02

[back to top]

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

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W8.25
A10 PBO QM2.43
A10 EZE (Q2W)-18.27
A10 EZE (QM)-14.78
A10 EvoMab Q2W-53.39
A10 EvoMab QM-52.20
A80 PBO Q2W11.79
A80 PBO QM9.95
A80 EZE (Q2W)-14.34
A80 EZE (QM)-17.26
A80 EvoMab Q2W-54.84
A80 EvoMab QM-50.05
R5 PBO Q2W7.92
R5 PBO QM5.85
R5 EvoMab Q2W-52.04
R5 EvoMab QM-51.57
R40 PBO Q2W8.61
R40 PBO QM3.35
R40 EvoMab Q2W-50.97
R40 EvoMab QM-46.42
S40 PBO Q2W1.89
S40 PBO QM5.66
S40 EvoMab Q2W-59.02
S40 EvoMab QM-50.96

[back to top]

Percent Change From Baseline in Non-High-Density Lipoprotein Cholesterol (Non-HDL-C) at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W6.80
A10 PBO QM1.28
A10 EZE (Q2W)-20.71
A10 EZE (QM)-16.56
A10 EvoMab Q2W-53.48
A10 EvoMab QM-56.09
A80 PBO Q2W10.74
A80 PBO QM8.45
A80 EZE (Q2W)-16.19
A80 EZE (QM)-18.79
A80 EvoMab Q2W-54.44
A80 EvoMab QM-56.31
R5 PBO Q2W7.02
R5 PBO QM3.73
R5 EvoMab Q2W-52.59
R5 EvoMab QM-55.47
R40 PBO Q2W6.19
R40 PBO QM1.58
R40 EvoMab Q2W-52.08
R40 EvoMab QM-55.72
S40 PBO Q2W0.74
S40 PBO QM6.81
S40 EvoMab Q2W-59.33
S40 EvoMab QM-56.01

[back to top]

Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W5.96
A10 PBO QM2.24
A10 EZE (Q2W)-14.39
A10 EZE (QM)-10.86
A10 EvoMab Q2W-40.44
A10 EvoMab QM-42.45
A80 PBO Q2W4.26
A80 PBO QM6.42
A80 EZE (Q2W)-11.92
A80 EZE (QM)-12.25
A80 EvoMab Q2W-40.22
A80 EvoMab QM-40.43
R5 PBO Q2W5.41
R5 PBO QM5.02
R5 EvoMab Q2W-39.33
R5 EvoMab QM-42.00
R40 PBO Q2W4.55
R40 PBO QM1.71
R40 EvoMab Q2W-36.04
R40 EvoMab QM-38.62
S40 PBO Q2W-0.14
S40 PBO QM5.45
S40 EvoMab Q2W-47.20
S40 EvoMab QM-43.17

[back to top]

Percent Change From Baseline in HDL-C at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W0.22
A10 PBO QM0.01
A10 EZE (Q2W)-1.76
A10 EZE (QM)-0.40
A10 EvoMab Q2W7.04
A10 EvoMab QM7.88
A80 PBO Q2W5.02
A80 PBO QM0.30
A80 EZE (Q2W)0.62
A80 EZE (QM)0.21
A80 EvoMab Q2W9.09
A80 EvoMab QM7.36
R5 PBO Q2W2.87
R5 PBO QM-0.16
R5 EvoMab Q2W6.07
R5 EvoMab QM7.18
R40 PBO Q2W-0.39
R40 PBO QM0.73
R40 EvoMab Q2W4.65
R40 EvoMab QM5.57
S40 PBO Q2W1.14
S40 PBO QM-2.65
S40 EvoMab Q2W10.92
S40 EvoMab QM6.41

[back to top]

Percent Change From Baseline in Triglycerides at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W6.49
A10 PBO QM9.17
A10 EZE (Q2W)-3.16
A10 EZE (QM)1.57
A10 EvoMab Q2W-5.61
A10 EvoMab QM-13.38
A80 PBO Q2W6.16
A80 PBO QM8.05
A80 EZE (Q2W)-8.10
A80 EZE (QM)-4.86
A80 EvoMab Q2W-9.27
A80 EvoMab QM-6.36
R5 PBO Q2W12.43
R5 PBO QM12.26
R5 EvoMab Q2W-10.28
R5 EvoMab QM-7.26
R40 PBO Q2W8.44
R40 PBO QM10.75
R40 EvoMab Q2W-9.15
R40 EvoMab QM-15.43
S40 PBO Q2W9.29
S40 PBO QM13.78
S40 EvoMab Q2W-11.67
S40 EvoMab QM-15.93

[back to top]

Percent Change From Baseline in Triglycerides at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W8.27
A10 PBO QM14.35
A10 EZE (Q2W)-0.43
A10 EZE (QM)4.88
A10 EvoMab Q2W-3.79
A10 EvoMab QM-13.26
A80 PBO Q2W6.65
A80 PBO QM8.22
A80 EZE (Q2W)-7.40
A80 EZE (QM)-3.11
A80 EvoMab Q2W-10.07
A80 EvoMab QM-1.10
R5 PBO Q2W13.57
R5 PBO QM12.96
R5 EvoMab Q2W-4.46
R5 EvoMab QM-6.88
R40 PBO Q2W10.97
R40 PBO QM10.00
R40 EvoMab Q2W-5.58
R40 EvoMab QM-10.51
S40 PBO Q2W8.07
S40 PBO QM16.72
S40 EvoMab Q2W-13.71
S40 EvoMab QM-14.65

[back to top]

Percent Change From Baseline in Very Low-Density Cholesterol (VLDL-C) at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W6.51
A10 PBO QM9.53
A10 EZE (Q2W)-5.35
A10 EZE (QM)1.77
A10 EvoMab Q2W-6.85
A10 EvoMab QM-11.77
A80 PBO Q2W6.24
A80 PBO QM8.31
A80 EZE (Q2W)-8.52
A80 EZE (QM)-6.13
A80 EvoMab Q2W-8.96
A80 EvoMab QM-6.38
R5 PBO Q2W12.86
R5 PBO QM12.54
R5 EvoMab Q2W-12.22
R5 EvoMab QM-7.25
R40 PBO Q2W7.06
R40 PBO QM8.13
R40 EvoMab Q2W-9.09
R40 EvoMab QM-15.05
S40 PBO Q2W8.64
S40 PBO QM16.37
S40 EvoMab Q2W-14.57
S40 EvoMab QM-16.50

[back to top]

Percent Change From Baseline in Very Low-Density Cholesterol (VLDL-C) at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W8.32
A10 PBO QM14.74
A10 EZE (Q2W)-4.61
A10 EZE (QM)3.45
A10 EvoMab Q2W-6.16
A10 EvoMab QM-11.73
A80 PBO Q2W6.73
A80 PBO QM8.54
A80 EZE (Q2W)-7.92
A80 EZE (QM)-6.00
A80 EvoMab Q2W-9.69
A80 EvoMab QM-1.06
R5 PBO Q2W13.79
R5 PBO QM12.47
R5 EvoMab Q2W-8.20
R5 EvoMab QM-6.28
R40 PBO Q2W10.09
R40 PBO QM8.59
R40 EvoMab Q2W-6.10
R40 EvoMab QM-9.95
S40 PBO Q2W7.63
S40 PBO QM20.97
S40 EvoMab Q2W-14.83
S40 EvoMab QM-15.86

[back to top]

Percentage of Participants Who Achieved LDL-C < 70 mg/dL at Week 12

(NCT01763866)
Timeframe: Week 12

Interventionpercentage of participants (Number)
A10 PBO Q2W2.0
A10 PBO QM5.9
A10 EZE (Q2W)22.4
A10 EZE (QM)19.2
A10 EvoMab Q2W85.4
A10 EvoMab QM84.2
A80 PBO Q2W13.0
A80 PBO QM9.8
A80 EZE (Q2W)52.0
A80 EZE (QM)55.8
A80 EvoMab Q2W93.1
A80 EvoMab QM91.0
R5 PBO Q2W7.7
R5 PBO QM5.5
R5 EvoMab Q2W85.0
R5 EvoMab QM86.5
R40 PBO Q2W39.6
R40 PBO QM28.0
R40 EvoMab Q2W92.3
R40 EvoMab QM92.3
S40 PBO Q2W1.9
S40 PBO QM6.4
S40 EvoMab Q2W94.4
S40 EvoMab QM84.8

[back to top]

Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W6.09
A10 PBO QM2.80
A10 EZE (Q2W)-12.14
A10 EZE (QM)-9.85
A10 EvoMab Q2W-40.74
A10 EvoMab QM-40.07
A80 PBO Q2W4.31
A80 PBO QM6.18
A80 EZE (Q2W)-10.53
A80 EZE (QM)-11.06
A80 EvoMab Q2W-40.79
A80 EvoMab QM-36.25
R5 PBO Q2W4.68
R5 PBO QM6.07
R5 EvoMab Q2W-38.57
R5 EvoMab QM-39.26
R40 PBO Q2W5.96
R40 PBO QM2.69
R40 EvoMab Q2W-35.17
R40 EvoMab QM-32.30
S40 PBO Q2W-0.20
S40 PBO QM5.13
S40 EvoMab Q2W-47.24
S40 EvoMab QM-39.47

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W7.89
A10 PBO QM0.21
A10 EZE (Q2W)-15.98
A10 EZE (QM)-10.95
A10 EvoMab Q2W-50.90
A10 EvoMab QM-47.15
A80 PBO Q2W11.64
A80 PBO QM6.54
A80 EZE (Q2W)-12.31
A80 EZE (QM)-12.16
A80 EvoMab Q2W-49.77
A80 EvoMab QM-46.47
R5 PBO Q2W6.35
R5 PBO QM4.63
R5 EvoMab Q2W-50.15
R5 EvoMab QM-48.58
R40 PBO Q2W4.91
R40 PBO QM3.24
R40 EvoMab Q2W-45.61
R40 EvoMab QM-43.71
S40 PBO Q2W0.35
S40 PBO QM3.57
S40 EvoMab Q2W-55.95
S40 EvoMab QM-49.16

[back to top]

Percent Change From Baseline in HDL-C at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W-0.99
A10 PBO QM-0.45
A10 EZE (Q2W)-1.13
A10 EZE (QM)-0.92
A10 EvoMab Q2W5.54
A10 EvoMab QM7.66
A80 PBO Q2W4.48
A80 PBO QM-1.37
A80 EZE (Q2W)0.86
A80 EZE (QM)-0.59
A80 EvoMab Q2W8.44
A80 EvoMab QM7.76
R5 PBO Q2W0.87
R5 PBO QM-0.94
R5 EvoMab Q2W6.23
R5 EvoMab QM7.72
R40 PBO Q2W-0.60
R40 PBO QM-0.40
R40 EvoMab Q2W4.86
R40 EvoMab QM6.35
S40 PBO Q2W0.13
S40 PBO QM-2.14
S40 EvoMab Q2W10.35
S40 EvoMab QM6.71

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W6.13
A10 PBO QM-1.21
A10 EZE (Q2W)-14.51
A10 EZE (QM)-12.33
A10 EvoMab Q2W-54.17
A10 EvoMab QM-49.65
A80 PBO Q2W4.19
A80 PBO QM6.50
A80 EZE (Q2W)-13.69
A80 EZE (QM)-12.19
A80 EvoMab Q2W-53.59
A80 EvoMab QM-50.76
R5 PBO Q2W1.44
R5 PBO QM4.00
R5 EvoMab Q2W-52.97
R5 EvoMab QM-52.13
R40 PBO Q2W1.64
R40 PBO QM3.16
R40 EvoMab Q2W-47.53
R40 EvoMab QM-45.65
S40 PBO Q2W-1.80
S40 PBO QM-0.52
S40 EvoMab Q2W-59.53
S40 EvoMab QM-52.56

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W6.41
A10 PBO QM0.78
A10 EZE (Q2W)-15.77
A10 EZE (QM)-11.47
A10 EvoMab Q2W-53.56
A10 EvoMab QM-53.33
A80 PBO Q2W4.48
A80 PBO QM5.79
A80 EZE (Q2W)-15.17
A80 EZE (QM)-12.91
A80 EvoMab Q2W-52.43
A80 EvoMab QM-56.20
R5 PBO Q2W2.82
R5 PBO QM2.58
R5 EvoMab Q2W-52.46
R5 EvoMab QM-56.66
R40 PBO Q2W2.17
R40 PBO QM2.60
R40 EvoMab Q2W-48.47
R40 EvoMab QM-54.17
S40 PBO Q2W-1.00
S40 PBO QM-1.42
S40 EvoMab Q2W-58.76
S40 EvoMab QM-57.47

[back to top]

Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W7.55
A10 PBO QM0.81
A10 EZE (Q2W)-17.29
A10 EZE (QM)-11.43
A10 EvoMab Q2W-50.95
A10 EvoMab QM-51.44
A80 PBO Q2W10.20
A80 PBO QM5.48
A80 EZE (Q2W)-14.22
A80 EZE (QM)-13.62
A80 EvoMab Q2W-49.14
A80 EvoMab QM-53.26
R5 PBO Q2W5.07
R5 PBO QM2.54
R5 EvoMab Q2W-49.79
R5 EvoMab QM-53.59
R40 PBO Q2W3.71
R40 PBO QM1.98
R40 EvoMab Q2W-47.07
R40 EvoMab QM-52.95
S40 PBO Q2W-0.31
S40 PBO QM2.49
S40 EvoMab Q2W-55.65
S40 EvoMab QM-54.37

[back to top]

Change From Baseline in LDL-C at Week 12

(NCT01763866)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
A10 PBO Q2W8.6
A10 PBO QM0.8
A10 EZE (Q2W)-30.1
A10 EZE (QM)-23.3
A10 EvoMab Q2W-77.0
A10 EvoMab QM-75.1
A80 PBO Q2W12.7
A80 PBO QM7.0
A80 EZE (Q2W)-9.9
A80 EZE (QM)-19.5
A80 EvoMab Q2W-59.0
A80 EvoMab QM-54.8
R5 PBO Q2W7.8
R5 PBO QM2.4
R5 EvoMab Q2W-69.2
R5 EvoMab QM-73.3
R40 PBO Q2W5.1
R40 PBO QM-2.0
R40 EvoMab Q2W-52.1
R40 EvoMab QM-46.7
S40 PBO Q2W-4.5
S40 PBO QM-0.6
S40 EvoMab Q2W-83.5
S40 EvoMab QM-72.5

[back to top]

Change From Baseline in LDL-C at at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionmg/dL (Least Squares Mean)
A10 PBO Q2W6.8
A10 PBO QM-0.4
A10 EZE (Q2W)-32.4
A10 EZE (QM)-25.1
A10 EvoMab Q2W-76.8
A10 EvoMab QM-80.1
A80 PBO Q2W11.0
A80 PBO QM5.5
A80 EZE (Q2W)-13.0
A80 EZE (QM)-21.3
A80 EvoMab Q2W-58.8
A80 EvoMab QM-60.1
R5 PBO Q2W6.5
R5 PBO QM0.1
R5 EvoMab Q2W-68.9
R5 EvoMab QM-77.8
R40 PBO Q2W3.4
R40 PBO QM-4.8
R40 EvoMab Q2W-52.3
R40 EvoMab QM-55.3
S40 PBO Q2W-5.7
S40 PBO QM1.7
S40 EvoMab Q2W-83.8
S40 EvoMab QM-78.4

[back to top]

Percentage of Participants Who Achieved a Mean LDL-C at Weeks 10 and 12 of Less Than 70 mg/dL

(NCT01763866)
Timeframe: Weeks 10 and 12

Interventionpercentage of participants (Number)
A10 PBO Q2W5.7
A10 PBO QM5.6
A10 EZE (Q2W)20.0
A10 EZE (QM)16.7
A10 EvoMab Q2W88.1
A10 EvoMab QM85.8
A80 PBO Q2W13.7
A80 PBO QM9.3
A80 EZE (Q2W)50.9
A80 EZE (QM)62.3
A80 EvoMab Q2W94.4
A80 EvoMab QM92.5
R5 PBO Q2W7.0
R5 PBO QM5.3
R5 EvoMab Q2W88.7
R5 EvoMab QM89.9
R40 PBO Q2W38.9
R40 PBO QM28.8
R40 EvoMab Q2W93.5
R40 EvoMab QM94.5
S40 PBO Q2W1.9
S40 PBO QM3.9
S40 EvoMab Q2W93.6
S40 EvoMab QM88.5

[back to top]

Percent Change From Baseline in LDL-C at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W8.54
A10 PBO QM0.35
A10 EZE (Q2W)-23.88
A10 EZE (QM)-18.98
A10 EvoMab Q2W-61.41
A10 EvoMab QM-62.47
A80 PBO Q2W13.12
A80 PBO QM9.76
A80 EZE (Q2W)-16.85
A80 EZE (QM)-21.25
A80 EvoMab Q2W-61.80
A80 EvoMab QM-65.05
R5 PBO Q2W7.55
R5 PBO QM2.79
R5 EvoMab Q2W-59.33
R5 EvoMab QM-63.79
R40 PBO Q2W6.57
R40 PBO QM-0.02
R40 EvoMab Q2W-59.08
R40 EvoMab QM-62.94
S40 PBO Q2W3.26
S40 PBO QM6.00
S40 EvoMab Q2W-66.17
S40 EvoMab QM-62.45

[back to top]

Percent Change From Baseline in Lipoprotein(a) at the Mean of Weeks 10 and 12

(NCT01763866)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
A10 PBO Q2W6.07
A10 PBO QM-0.77
A10 EZE (Q2W)1.44
A10 EZE (QM)6.85
A10 EvoMab Q2W-26.01
A10 EvoMab QM-22.64
A80 PBO Q2W-3.45
A80 PBO QM1.51
A80 EZE (Q2W)8.05
A80 EZE (QM)9.96
A80 EvoMab Q2W-23.97
A80 EvoMab QM-27.46
R5 PBO Q2W11.41
R5 PBO QM3.65
R5 EvoMab Q2W-24.26
R5 EvoMab QM-23.16
R40 PBO Q2W8.59
R40 PBO QM6.26
R40 EvoMab Q2W-24.96
R40 EvoMab QM-25.93
S40 PBO Q2W-10.57
S40 PBO QM-4.99
S40 EvoMab Q2W-38.64
S40 EvoMab QM-32.16

[back to top]

Percentage of Participants With Mean LDL-C at Weeks 10 and 12 of Less Than 70 mg/dL (1.8 mmol/L)

(NCT01763905)
Timeframe: Weeks 10 and 12

Interventionpercentage of participants (Number)
Ezetimibe (Q2W)2.0
Ezetimibe (QM)0.0
Evolocumab Q2W45.5
Evolocumab QM42.0

[back to top]

Percent Change From Baseline in Lipoprotein (a) at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-2.30
Ezetimibe (QM)1.55
Evolocumab Q2W-26.20
Evolocumab QM-23.72

[back to top]

Percent Change From Baseline in Non-HDL-C at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-17.18
Ezetimibe (QM)-14.54
Evolocumab Q2W-48.72
Evolocumab QM-49.13

[back to top]

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

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-16.53
Ezetimibe (QM)-13.16
Evolocumab Q2W-48.62
Evolocumab QM-46.15

[back to top]

Percent Change From Baseline in the Total Cholesterol/High Density Lipoprotein Cholesterol Ratio at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-13.44
Ezetimibe (QM)-11.20
Evolocumab Q2W-40.83
Evolocumab QM-41.14

[back to top]

Percent Change From Baseline in LDL-C at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-19.21
Ezetimibe (QM)-16.62
Evolocumab Q2W-56.11
Evolocumab QM-55.31

[back to top]

Percent Change From Baseline in the Total Cholesterol/High Density Lipoprotein Cholesterol Ratio at Week 12

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-14.13
Ezetimibe (QM)-9.92
Evolocumab Q2W-40.42
Evolocumab QM-38.57

[back to top]

Percent Change From Baseline in Triglycerides at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-3.74
Ezetimibe (QM)-0.32
Evolocumab Q2W-6.32
Evolocumab QM-6.73

[back to top]

Percent Change From Baseline in LDL-C at Week 12

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-18.08
Ezetimibe (QM)-15.05
Evolocumab Q2W-56.14
Evolocumab QM-52.60

[back to top]

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

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)1.77
Ezetimibe (QM)1.64
Evolocumab Q2W5.34
Evolocumab QM6.47

[back to top]

Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)0.33
Ezetimibe (QM)1.44
Evolocumab Q2W5.48
Evolocumab QM7.18

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 12

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-13.14
Ezetimibe (QM)-11.37
Evolocumab Q2W-47.66
Evolocumab QM-45.51

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-13.00
Ezetimibe (QM)-11.94
Evolocumab Q2W-47.86
Evolocumab QM-48.31

[back to top]

Percent Change From Baseline in Lipoprotein (a) at Week 12

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-1.74
Ezetimibe (QM)5.81
Evolocumab Q2W-27.03
Evolocumab QM-22.07

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 12

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-12.95
Ezetimibe (QM)-9.97
Evolocumab Q2W-45.81
Evolocumab QM-43.07

[back to top]

Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-13.67
Ezetimibe (QM)-11.02
Evolocumab Q2W-45.88
Evolocumab QM-46.01

[back to top]

Percent Change From Baseline in Very Low-Density Lipoprotein Cholesterol at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-5.76
Ezetimibe (QM)-2.93
Evolocumab Q2W-7.60
Evolocumab QM-6.46

[back to top]

Change From Baseline in LDL-C at Week 12

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionmg/dL (Least Squares Mean)
Ezetimibe (Q2W)-36.2
Ezetimibe (QM)-30.2
Evolocumab Q2W-106.0
Evolocumab QM-99.0

[back to top]

Change From Baseline in LDL-C at the Mean of Weeks 10 and 12

(NCT01763905)
Timeframe: Baseline and Weeks 10 and 12

Interventionmg/dL (Least Squares Mean)
Ezetimibe (Q2W)-39.1
Ezetimibe (QM)-33.0
Evolocumab Q2W-105.4
Evolocumab QM-103.6

[back to top]

Percent Change From Baseline in Very Low-Density Lipoprotein Cholesterol at Week 12

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-5.49
Ezetimibe (QM)-2.25
Evolocumab Q2W-6.16
Evolocumab QM-2.18

[back to top]

Percentage of Participants With LDL-C < 70 mg/dL (1.8 mmol/L) at Week 12

(NCT01763905)
Timeframe: Week 12

Interventionpercentage of participants (Number)
Ezetimibe (Q2W)2.0
Ezetimibe (QM)0.0
Evolocumab Q2W50.0
Evolocumab QM37.5

[back to top]

Percent Change From Baseline in Triglycerides at Week 12

(NCT01763905)
Timeframe: Baseline and Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe (Q2W)-5.47
Ezetimibe (QM)2.16
Evolocumab Q2W-3.88
Evolocumab QM-2.53

[back to top]

Change in Liver Fat as Measured by MRI-PDFF

(NCT01766713)
Timeframe: Baseline, 24 weeks

,
Interventionpercentage of total fat (Mean)
Baselineweek 24
Ezetimibe15.011.6
Placebo18.516.4

[back to top]

Change in Intestinal mRNA Expression Levels of LDL Receptor Between the Two 12-week Interventions

"We combined the results at the end of each ezetimibe phase from both sequence (average and standard deviation).~We combined the results at the end of each placebo phase from both sequence (average and standard deviation)." (NCT01849068)
Timeframe: At the end of the two 12-week interventions (Week 12 and 24)

Intervention#copies/100000 copies housekeeping gene (Mean)
Ezetimibe110531
Placebo95140

[back to top]

Change in Intestinal mRNA Expression Levels of SREBP-2, NPC1L1, ABCG5/8, PCSK9 and HMG CoA Reductase Between the Two 12-week Interventions

"We combined the results at the end of each ezetimibe phase from both sequence (average and standard deviation).~We combined the results at the end of each placebo phase from both sequence (average and standard deviation)." (NCT01849068)
Timeframe: At the end of the two 12-week interventions (Week 12 and 24)

,
Intervention#copies/100000 copies housekeeping gene (Mean)
HMGCoA reductasePCSK9SREBP-2NPC1L1ABCG5ABCG8
Ezetimibe3549119079193012454298271811125315
Placebo3112688091182349448686283863129551

[back to top]

Percentage Change From Baseline in Free Proprotein Convertase Subtilisin/Kexin Type 9 Antibody (PCSK9) Levels

LS Mean was calculated using MMRM analysis with baseline measurement, disease classification, statin dose, treatment, visit, and treatment by visit interaction included in the model. Percent change from baseline response is the dependent variable. (NCT01890967)
Timeframe: Baseline, Week 16

InterventionPercentage change (Least Squares Mean)
Placebo Q4W9.9
20 mg LY3015014 Q4W-16.3
120 mg LY3015014 Q4W-36.6
300 mg LY3015014 Q4W-68.0
100 mg LY3015014 Q8W-4.4
300 mg LY3015014 Q8W-35.2

[back to top]

Change From Baseline in High Sensitivity C-Reactive Protein (hsCRP)

LS Mean was calculated using MMRM analysis with baseline measurement, disease classification, statin dose, treatment, visit, and treatment by visit interaction included in the model. Percent change from baseline response is the dependent variable. (NCT01890967)
Timeframe: Baseline, Week 16

InterventionPercentage change (Least Squares Mean)
Placebo Q4W0.5
20 mg LY3015014 Q4W-0.2
120 mg LY3015014 Q4W1.6
300 mg LY3015014 Q4W-0.3
100 mg LY3015014 Q8W-0.3
300 mg LY3015014 Q8W-0.7

[back to top]

Number of Participants Who Develop Treatment Emergent Anti-LY3015014 Antibodies

(NCT01890967)
Timeframe: Baseline through Week 24

InterventionParticipants (Number)
Placebo Q4W4
20 mg LY3015014 Q4W6
120 mg LY3015014 Q4W10
300 mg LY3015014 Q4W5
100 mg LY3015014 Q8W4
300 mg LY3015014 Q8W3

[back to top]

Number of Participants With an Injection Site Reaction

(NCT01890967)
Timeframe: Baseline through Week 24

InterventionParticipants (Number)
Placebo Q4W26
20 mg LY3015014 Q4W42
120 mg LY3015014 Q4W57
300 mg LY3015014 Q4W51
100 mg LY3015014 Q8W36
300 mg LY3015014 Q8W41

[back to top]

Percentage Change From Baseline in Lipoprotein(a) [Lp(a)]

Data was log-transformed for MMRM analysis, with change from baseline as the dependent variable, and baseline measurement, disease classification, statin dose, treatment, visit, and treatment by visit interaction included as independent variables. Percentage change from baseline in the original scale was then back-calculated from the log-transformed MMRM analysis. (NCT01890967)
Timeframe: Baseline, Week 16

InterventionPercentage Change (Least Squares Mean)
Placebo Q4W-0.31
20 mg LY3015014 Q4W-16.63
120 mg LY3015014 Q4W-19.02
300 mg LY3015014 Q4W-37.29
100 mg LY3015014 Q8W-7.54
300 mg LY3015014 Q8W-21.01

[back to top]

Percentage Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C)

Least square (LS) Means was calculated using analysis of covariance (ANCOVA) adjusted for disease classification, statin dose, baseline LDL-C measurement. Percent change from baseline response is the dependent variable. (NCT01890967)
Timeframe: Baseline, Week 16

InterventionPercentage change (Least Squares Mean)
Placebo Q4W7.6
20 mg LY3015014 Q4W-14.9
120 mg LY3015014 Q4W-40.5
300 mg LY3015014 Q4W-50.5
100 mg LY3015014 Q8W-14.9
300 mg LY3015014 Q8W-37.1

[back to top]

Percentage Change From Baseline in Total Proprotein Convertase Subtilisin/Kexin Type 9 Antibody (PCSK9) Levels

LS Mean was calculated using MMRM analysis with baseline measurement, disease classification, statin dose, treatment, visit, and treatment by visit interaction included in the model. Percent change from baseline response is the dependent variable. (NCT01890967)
Timeframe: Baseline, Week 16

InterventionPercentage change (Least Squares Mean)
Placebo Q4W14.6
20 mg LY3015014 Q4W9.1
120 mg LY3015014 Q4W86.4
300 mg LY3015014 Q4W130.6
100 mg LY3015014 Q8W21.8
300 mg LY3015014 Q8W41.0

[back to top]

Percentage Change From Baseline in Apolipoprotein A1 (Apo A1), Apolipoprotein B (Apo B)

LS Mean was calculated using MMRM analysis with baseline measurement, disease classification, statin dose, treatment, visit, and treatment by visit interaction included in the model. Percent change from baseline response is the dependent variable. (NCT01890967)
Timeframe: Baseline, Week 16

,,,,,
InterventionPercentage change (Least Squares Mean)
Apo A1Apo B
100 mg LY3015014 Q8W3.8-16.0
120 mg LY3015014 Q4W6.5-34.9
20 mg LY3015014 Q4W2.4-16.6
300 mg LY3015014 Q4W6.2-46.8
300 mg LY3015014 Q8W5.8-31.9
Placebo Q4W0.34.2

[back to top]

Percentage Change From Baseline in LDL-C, Total Cholesterol (TC), High-Density Lipoprotein Cholesterol (HDL-C), Triglycerides (TG), Non-HDL-C

LS Mean was calculated using mixed model repeated measures (MMRM) analysis with baseline measurement, disease classification, statin dose, treatment, visit, and treatment by visit interaction included in the model. Percent change from baseline response is the dependent variable. (NCT01890967)
Timeframe: Baseline, Week 16

,,,,,
InterventionPercentage change (Least Squares Mean)
LDL-CTGTCHDL-CNon-HDL-C
100 mg LY3015014 Q8W-18.4-7.2-11.04.5-16.1
120 mg LY3015014 Q4W-46.4-7.2-27.87.3-39.3
20 mg LY3015014 Q4W-18.0-6.1-10.54.5-16.1
300 mg LY3015014 Q4W-56.5-15.1-34.18.8-48.9
300 mg LY3015014 Q8W-42.2-10.6-24.68.4-35.8
Placebo Q4W5.93.53.51.64.9

[back to top]

Pharmacokinetics (PK): Area Under the Concentration-Time Curve at Steady-State (AUC,ss) for LY3015014

(NCT01890967)
Timeframe: Week 12-16 (Q4W) - Predose, Week 8-16 (Q8W) - Predose

Interventionμg∙hr/mL (Geometric Mean)
20 mg LY3015014 Q4W1590
120 mg LY3015014 Q4W9670
300 mg LY3015014 Q4W27300
100 mg LY3015014 Q8W7800
300 mg LY3015014 Q8W26600

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-12.62
Evolocumab-44.60

[back to top]

Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-12.84
Evolocumab-40.04

[back to top]

Percent Change From Baseline in HDL-C at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe2.90
Evolocumab7.40

[back to top]

Change From Baseline in LDL-C at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baselie and weeks 22 and 24

Interventionmg/dL (Least Squares Mean)
Ezetimibe-31.0
Evolocumab-106.8

[back to top]

Change From Baseline in LDL-C at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionmg/dL (Least Squares Mean)
Ezetimibe-31.2
Evolocumab-102.9

[back to top]

Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.42
Evolocumab-45.28

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.74
Evolocumab-43.50

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A1 Ratio at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and Weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.86
Evolocumab-45.99

[back to top]

Percent Change From Baseline in High-density Lipoprotein Cholesterol (HDL-C) at Week 24

(NCT01984424)
Timeframe: Baseline and weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe1.66
Evolocumab7.85

[back to top]

Percent Change From Baseline in LDL-C at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-16.70
Evolocumab-54.50

[back to top]

Percent Change From Baseline in LDL-C at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-16.69
Evolocumab-52.76

[back to top]

Percent Change From Baseline in Lipoprotein(a) at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and Weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-1.63
Evolocumab-22.71

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe0.17
Evolocumab-21.06

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-14.62
Evolocumab-45.72

[back to top]

Percent Change From Baseline in Non-high-density Lipoprotein Cholesterol (Non-HDL-C) at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-14.38
Evolocumab-47.44

[back to top]

Percent Change From Baseline in Total Cholesterol at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.43
Evolocumab-38.04

[back to top]

Percent Change From Baseline in Total Cholesterol at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.57
Evolocumab-36.64

[back to top]

Percent Change From Baseline in Total Cholesterol/HDL-C Ratio at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.48
Evolocumab-41.39

[back to top]

Percent Change From Baseline in Triglycerides at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-0.95
Evolocumab-5.39

[back to top]

Percent Change From Baseline in Triglycerides at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-1.07
Evolocumab-2.88

[back to top]

Percent Change From Baseline in Very Low-density Lipoprotein Cholesterol (VLDL-C) at the Mean of Weeks 22 and 24

(NCT01984424)
Timeframe: Baseline and weeks 22 and 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-2.15
Evolocumab-6.81

[back to top]

Percent Change From Baseline in VLDL-C at Week 24

(NCT01984424)
Timeframe: Baseline and week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe-2.66
Evolocumab-3.90

[back to top]

Percentage of Participants Who Achieved a Mean LDL-C at Weeks 22 and 24 of Less Than 70 mg/dL

(NCT01984424)
Timeframe: Weeks 22 and 24

Interventionpercentage of participants (Number)
Ezetimibe1.4
Evolocumab29.9

[back to top]

Percentage of Participants Who Achieved LDL-C at Week 24 of Less Than 70 mg/dL

(NCT01984424)
Timeframe: Week 24

Interventionpercentage of participants (Number)
Ezetimibe0.0
Evolocumab27.4

[back to top]

Change From Baseline in Very Low Density Lipoprotein-Cholesterol (VLDL-C) at Day 85 and Day 113

VLDL is a type of lipoprotein made by the liver and one of the five major groups of lipoproteins, that enable fats and cholesterol to move within the water-based solution of the bloodstream. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-2.70-3.98
Atorvastatin + PF-04950615 100 mg-6.17-7.25
Atorvastatin + PF-04950615 150 mg-6.57-5.35
Atorvastatin + PF-04950615 50 mg-5.68-4.29
Atorvastatin + PF-04950615 Placebo1.150.34
PF-04950615 100 mg-2.63-0.76
PF-04950615 150 mg-2.58-2.98
PF-04950615 50 mg-0.76-1.52
PF-04950615 Placebo-1.071.89

[back to top]

Change From Baseline in Triglyceride (TG) at Day 85 and Day 113

Triglycerides are a type of fat circulating in the blood and account for the majority of the fats circulating in the blood. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-10.14-23.45
Atorvastatin + PF-04950615 100 mg-27.96-45.33
Atorvastatin + PF-04950615 150 mg-29.52-30.13
Atorvastatin + PF-04950615 50 mg-28.68-20.02
Atorvastatin + PF-04950615 Placebo2.58-0.58
PF-04950615 100 mg-15.870.35
PF-04950615 150 mg-11.67-12.46
PF-04950615 50 mg-3.76-10.68
PF-04950615 Placebo-11.226.22

[back to top]

Change From Baseline in Total Cholesterol (TC) at Day 85 and Day 113

Total cholesterol is the sum of all the cholesterol within the blood. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-24.02-31.11
Atorvastatin + PF-04950615 100 mg-90.71-85.71
Atorvastatin + PF-04950615 150 mg-101.43-95.83
Atorvastatin + PF-04950615 50 mg-78.64-73.44
Atorvastatin + PF-04950615 Placebo-13.56-21.68
PF-04950615 100 mg-102.80-97.89
PF-04950615 150 mg-110.02-111.96
PF-04950615 50 mg-80.50-76.22
PF-04950615 Placebo-10.52-5.22

[back to top]

Change From Baseline in Total Cholesterol (TC) / High Density Lipoprotein- Cholesterol (HDL-C) Ratio at Day 85 and Day 113

Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionratio (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-0.6236-0.7864
Atorvastatin + PF-04950615 100 mg-1.9433-1.9113
Atorvastatin + PF-04950615 150 mg-1.9835-1.8704
Atorvastatin + PF-04950615 50 mg-1.6394-1.5671
Atorvastatin + PF-04950615 Placebo0.0879-0.1560
PF-04950615 100 mg-1.8407-1.7563
PF-04950615 150 mg-2.0469-2.0461
PF-04950615 50 mg-1.4204-1.4648
PF-04950615 Placebo0.15370.2493

[back to top]

Change From Baseline in Non-High Density Lipoprotein- Cholesterol (Non-HDL-C) at Day 85 and Day 113

Non-HDL-C calculated as total cholesterol minus HDL cholesterol. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-26.82-34.45
Atorvastatin + PF-04950615 100 mg-95.50-92.00
Atorvastatin + PF-04950615 150 mg-104.07-98.15
Atorvastatin + PF-04950615 50 mg-82.30-77.33
Atorvastatin + PF-04950615 Placebo-8.98-18.40
PF-04950615 100 mg-104.26-99.26
PF-04950615 150 mg-110.00-111.33
PF-04950615 50 mg-78.32-76.92
PF-04950615 Placebo-6.00-0.52

[back to top]

Change From Baseline in Low Density Lipoprotein-Cholesterol (LDL-C) at Day 85 and Day 113

LDL-C is cholesterol in the bloodstream that is carried by low density lipoprotein. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-24.73-28.05
Atorvastatin + PF-04950615 100 mg-85.85-80.98
Atorvastatin + PF-04950615 150 mg-95.11-90.54
Atorvastatin + PF-04950615 50 mg-76.40-73.33
Atorvastatin + PF-04950615 Placebo-9.52-17.48
PF-04950615 100 mg-99.28-97.63
PF-04950615 150 mg-105.19-107.57
PF-04950615 50 mg-77.58-74.78
PF-04950615 Placebo-3.91-1.91

[back to top]

Change From Baseline in Lipoprotein (a) (Lp[a]) at Day 85 and Day 113

Lp(a) is a lipoprotein subclass which consists of an LDL-like particle and the specific apolipoprotein(a). Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-1.859-2.655
Atorvastatin + PF-04950615 100 mg-10.119-9.815
Atorvastatin + PF-04950615 150 mg-10.239-9.913
Atorvastatin + PF-04950615 50 mg-7.492-6.815
Atorvastatin + PF-04950615 Placebo-2.746-3.574
PF-04950615 100 mg-7.100-8.074
PF-04950615 150 mg-6.763-7.098
PF-04950615 50 mg-5.272-6.060
PF-04950615 Placebo-3.513-3.326

[back to top]

Change From Baseline in High Density Lipoprotein- Cholesterol (HDL-C) at Day 85 and Day 113

HDL-C is cholesterol in the bloodstream that is carried by high density lipoprotein. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg2.803.34
Atorvastatin + PF-04950615 100 mg4.796.29
Atorvastatin + PF-04950615 150 mg2.632.33
Atorvastatin + PF-04950615 50 mg3.663.90
Atorvastatin + PF-04950615 Placebo-4.58-3.28
PF-04950615 100 mg1.461.37
PF-04950615 150 mg-0.02-0.63
PF-04950615 50 mg-2.180.70
PF-04950615 Placebo-4.52-4.70

[back to top]

Change From Baseline in Apolipoprotein B (ApoB) at Day 85 and Day 113

ApoB is a major protein that makes up LDL cholesterol and is involved in transporting cholesterol and triglycerides to cells and tissues in the body. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-9.93-13.93
Atorvastatin + PF-04950615 100 mg-53.33-49.71
Atorvastatin + PF-04950615 150 mg-56.43-53.61
Atorvastatin + PF-04950615 50 mg-41.44-39.56
Atorvastatin + PF-04950615 Placebo-2.19-7.70
PF-04950615 100 mg-54.33-51.15
PF-04950615 150 mg-56.75-56.83
PF-04950615 50 mg-37.86-37.46
PF-04950615 Placebo-1.042.48

[back to top]

Change From Baseline in Apolipoprotein B (ApoB) / Apolipoprotein A-I (ApoA-I) Ratio at Day 85 and Day 113

Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionratio (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-0.0643-0.0998
Atorvastatin + PF-04950615 100 mg-0.3910-0.3698
Atorvastatin + PF-04950615 150 mg-0.4211-0.3998
Atorvastatin + PF-04950615 50 mg-0.3078-0.2998
Atorvastatin + PF-04950615 Placebo0.0337-0.0170
PF-04950615 100 mg-0.3748-0.3626
PF-04950615 150 mg-0.4042-0.3965
PF-04950615 50 mg-0.2626-0.2750
PF-04950615 Placebo0.06850.0702

[back to top]

Change From Baseline in Apolipoprotein A-II (ApoA-II) at Day 85 and Day 113

ApoA-II is the second most abundant component of the HDL cholesterol. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg0.9070.370
Atorvastatin + PF-04950615 100 mg0.0730.090
Atorvastatin + PF-04950615 150 mg-0.450-0.637
Atorvastatin + PF-04950615 50 mg-0.216-0.073
Atorvastatin + PF-04950615 Placebo-0.938-1.104
PF-04950615 100 mg0.3540.759
PF-04950615 150 mg0.2400.002
PF-04950615 50 mg-0.904-0.640
PF-04950615 Placebo-1.698-1.228

[back to top]

Change From Baseline in Apolipoprotein A-I (ApoA-I) at Day 85 and Day 113

ApoA1 is a major protein that is a component of HDL cholesterol and helps in clearing cholesterol from the blood by removing cholesterol from organs and tissues to be destroyed by the liver. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Change from baseline = observed value minus baseline value. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionmg/dL (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-1.11-0.34
Atorvastatin + PF-04950615 100 mg5.566.56
Atorvastatin + PF-04950615 150 mg3.633.72
Atorvastatin + PF-04950615 50 mg1.022.52
Atorvastatin + PF-04950615 Placebo-9.65-7.86
PF-04950615 100 mg-2.091.87
PF-04950615 150 mg-0.17-3.54
PF-04950615 50 mg-6.02-0.50
PF-04950615 Placebo-13.83-10.09

[back to top]

Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of PF-04950615

Area under the plasma concentration time-curve from time zero to end of dosing interval (tau). This outcome measure was to be analyzed in participants who received at least 1 dose of the PF-04950615. (NCT02055976)
Timeframe: Single dose (Day 1: pre-dose, 24, 48, 72, 96, 120, 144, 168 hour (hr) post-dose), Multiple dose (Day 99: pre-dose, 24, 72, 120, 168, 336, 504, 672, 1008 hr post-dose)

,,,,,
Interventionmicrogram*day per milliliter(mcg*day/mL) (Geometric Mean)
Single doseMultiple dose
Atorvastatin + PF-04950615 100 mg52.3392.46
Atorvastatin + PF-04950615 150 mg77.11242.5
Atorvastatin + PF-04950615 50 mg32.9863.54
PF-04950615 100 mg51.49136.6
PF-04950615 150 mg82.05273.5
PF-04950615 50 mg32.9763.74

[back to top]

Apolipoprotein B (ApoB) / Apolipoprotein A-I (ApoA-I) Ratio

Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionratio (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg0.67750.59680.56570.54450.55640.56090.56000.58050.59590.56820.59860.61320.58820.58770.57770.69500.70820.69910.6845
Atorvastatin + PF-04950615 100 mg0.66060.41350.33630.33000.24630.30580.24210.28000.23130.26420.25920.26960.29040.22670.29080.50290.59380.61250.6321
Atorvastatin + PF-04950615 150 mg0.65670.42220.32710.24500.20780.21960.19830.21420.20480.20260.21570.23350.24910.24050.25480.37780.50040.55740.6161
Atorvastatin + PF-04950615 50 mg0.68460.48960.40440.43080.31360.36560.29000.35920.26680.35840.36920.37680.39280.29080.38880.57720.62330.63680.6640
Atorvastatin + PF-04950615 Placebo0.66870.66120.66600.67120.67730.67760.68730.67880.68040.69380.69580.70230.65840.67160.65560.66920.65800.66640.6424
PF-04950615 100 mg0.73240.57920.50170.42160.36290.37200.32500.36320.32830.38040.33580.34350.36500.33220.35570.47300.63520.68390.7178
PF-04950615 150 mg0.71670.53000.47180.37630.32830.32540.30500.31880.31330.31960.31460.31250.30750.31420.32350.43250.53750.60750.6639
PF-04950615 50 mg0.78900.64280.58440.57760.48680.48200.44280.46960.44720.46160.49760.52640.51640.47960.51400.70240.79160.81480.8088
PF-04950615 Placebo0.69800.71000.72300.72260.72480.70230.70480.75480.74650.76300.75000.76650.78830.77300.76830.78300.75700.74520.7359

[back to top]

Apolipoprotein B (ApoB)

ApoB is a major protein that makes up LDL cholesterol and is involved in transporting cholesterol and triglycerides to cells and tissues in the body. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg96.7084.6880.3879.3679.7780.7380.1882.6882.8679.6885.1886.7784.0583.3282.7798.50100.45101.23103.09
Atorvastatin + PF-04950615 100 mg92.5459.8349.0449.3836.8346.4235.5042.5034.0838.2938.7139.2144.2934.7142.8373.0487.7189.0093.63
Atorvastatin + PF-04950615 150 mg90.4060.2647.4236.5031.0932.8329.4331.9630.5229.4832.0033.6537.5535.5536.4854.6174.8781.8791.57
Atorvastatin + PF-04950615 50 mg92.7667.7256.1260.2044.2852.0841.0451.3638.4849.4452.8351.3257.3642.1253.5082.0089.5090.1693.36
Atorvastatin + PF-04950615 Placebo95.6594.6295.7296.6596.3596.0096.2794.3195.6993.8197.2393.4695.0894.3688.4095.1695.0896.0096.88
PF-04950615 100 mg104.0282.8871.7162.2853.4654.2049.2553.6049.4353.2550.6349.3553.6348.8752.5269.9192.7098.26105.91
PF-04950615 150 mg101.8878.0070.2758.0850.5450.2546.9248.5047.5845.7947.7945.1345.8847.0045.8762.7577.6786.0495.74
PF-04950615 50 mg106.5488.4082.5282.2468.7669.3262.4067.2462.2862.0069.9668.6872.5666.7269.0897.20108.96111.39112.46
PF-04950615 Placebo103.13104.86107.61107.39108.35107.23103.74110.39107.22104.13107.78102.09110.91107.48105.61111.35110.09108.43111.41

[back to top]

Apolipoprotein A-II (ApoA-II)

ApoA-II is the second most abundant component of the HDL cholesterol. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg32.18932.70932.49533.13632.27332.39532.09132.63632.28232.40533.12733.09533.15532.43232.55932.90532.81832.87733.623
Atorvastatin + PF-04950615 100 mg30.22330.16130.67531.12930.66732.27930.83831.90831.11730.27131.55430.29632.05431.85030.31331.35832.32531.62932.033
Atorvastatin + PF-04950615 150 mg30.47130.44330.73831.30431.18331.03530.62231.00430.99129.98731.14829.97431.43631.07329.78731.37032.83531.87832.352
Atorvastatin + PF-04950615 50 mg30.70030.88430.22430.52831.23231.60831.20831.60031.77230.70832.60030.48432.86831.90830.44232.06832.70432.16431.848
Atorvastatin + PF-04950615 Placebo31.51531.60832.03632.06231.84632.09631.15031.68531.90030.77332.09230.57732.50031.72430.38831.82432.04431.95633.120
PF-04950615 100 mg31.23230.97230.60831.51631.12531.10031.40432.40832.70431.45432.65831.95732.92532.55232.36132.37433.28732.89133.578
PF-04950615 150 mg30.29430.55830.66431.27530.89631.07130.97531.13831.08330.03331.80430.53331.22931.43830.23931.24232.02931.86732.070
PF-04950615 50 mg29.94030.08830.76030.56830.62030.74029.76830.72029.76028.54830.26029.03631.35230.52029.30030.90431.41231.06131.433
PF-04950615 Placebo31.35431.47331.63531.53032.20031.88231.47831.92230.83029.86131.31729.65731.57030.86530.12631.83932.17831.43932.345

[back to top]

Apolipoprotein A-I (ApoA-I)

ApoA1 is a major protein that is a component of HDL cholesterol and helps in clearing cholesterol from the blood by removing cholesterol from organs and tissues to be destroyed by the liver. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg145.34144.68145.57148.50146.41146.23145.91144.64141.95142.18144.18144.23145.91144.64145.00144.27144.45147.09153.64
Atorvastatin + PF-04950615 100 mg142.60146.65147.46153.00152.88155.79149.88153.88151.25149.46152.92148.17154.54154.96149.17148.75151.21148.83151.54
Atorvastatin + PF-04950615 150 mg140.31144.48146.88150.46151.78151.78150.13150.33149.13145.83150.43144.04150.86150.23144.13150.04154.17149.52150.96
Atorvastatin + PF-04950615 50 mg137.02140.72140.44141.56143.20144.32143.48144.52145.80138.40145.50138.04147.40145.92139.21144.08145.46143.52142.96
Atorvastatin + PF-04950615 Placebo145.65146.08147.00147.04145.31144.28143.46142.42143.46137.62142.62136.00147.48143.12137.72145.60148.52147.60154.88
PF-04950615 100 mg145.38145.12145.79150.08150.08150.04153.33152.32152.52145.96151.88145.13151.29149.26149.09148.48148.74148.09151.70
PF-04950615 150 mg146.75149.79152.45157.04155.17155.96155.08155.75153.92144.96154.25146.58149.83150.46143.96149.17151.29149.13151.13
PF-04950615 50 mg138.90142.12146.76145.76145.96146.36145.08146.00142.84136.32143.88132.88143.88142.56138.40141.68141.36140.96144.13
PF-04950615 Placebo150.13150.09150.48151.00151.65154.32149.30149.04145.70138.87146.17136.30144.65141.17140.04144.48149.13148.83154.36

[back to top]

Percent Change From Baseline in Fasting Low Density Lipoprotein-Cholesterol (LDL-C) at Day 85

LDL-C is cholesterol in the bloodstream that is carried by low density lipoprotein. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85

Interventionpercent change (Mean)
Atorvastatin + PF-04950615 50 mg-55.65
Atorvastatin + PF-04950615 100 mg-68.25
Atorvastatin + PF-04950615 150 mg-74.00
Atorvastatin + PF-04950615 Placebo-5.91
Atorvastatin + Ezetimibe 10 mg-18.56
PF-04950615 50 mg-47.25
PF-04950615 100 mg-62.24
PF-04950615 150 mg-65.89
PF-04950615 Placebo-1.21

[back to top]

Percent Change From Baseline in Fasting Low Density Lipoprotein-Cholesterol (LDL-C) at Day 113

LDL-C is cholesterol in the bloodstream that is carried by low density lipoprotein. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 113

Interventionpercent change (Mean)
Atorvastatin + PF-04950615 50 mg-54.41
Atorvastatin + PF-04950615 100 mg-64.46
Atorvastatin + PF-04950615 150 mg-69.98
Atorvastatin + PF-04950615 Placebo-12.10
Atorvastatin + Ezetimibe 10 mg-20.55
PF-04950615 50 mg-44.94
PF-04950615 100 mg-61.79
PF-04950615 150 mg-66.98
PF-04950615 Placebo0.39

[back to top]

Percent Change From Baseline in Apolipoprotein A-I (ApoA-I) at Day 85 and Day 113

ApoA1 is a major protein that is a component of HDL cholesterol and helps in clearing cholesterol from the blood by removing cholesterol from organs and tissues to be destroyed by the liver. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-0.340.15
Atorvastatin + PF-04950615 100 mg4.204.82
Atorvastatin + PF-04950615 150 mg3.263.13
Atorvastatin + PF-04950615 50 mg0.871.93
Atorvastatin + PF-04950615 Placebo-6.44-5.16
PF-04950615 100 mg-1.001.53
PF-04950615 150 mg0.44-1.84
PF-04950615 50 mg-3.820.13
PF-04950615 Placebo-9.10-6.55

[back to top]

Percent Change From Baseline in Very Low Density Lipoprotein-Cholesterol (VLDL-C) at Day 85 and Day 113

VLDL is a type of lipoprotein made by the liver and one of the five major groups of lipoproteins, that enable fats and cholesterol to move within the water-based solution of the bloodstream. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-6.48-10.80
Atorvastatin + PF-04950615 100 mg-22.99-26.62
Atorvastatin + PF-04950615 150 mg-28.96-19.28
Atorvastatin + PF-04950615 50 mg-23.42-17.23
Atorvastatin + PF-04950615 Placebo7.08-1.89
PF-04950615 100 mg5.6610.72
PF-04950615 150 mg-3.54-10.36
PF-04950615 50 mg-7.61-9.72
PF-04950615 Placebo-3.6318.73

[back to top]

Percent Change From Baseline in Triglyceride (TG) at Day 85 and Day 113

Triglycerides are a type of fat circulating in the blood and account for the majority of the fats circulating in the blood. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-5.20-15.23
Atorvastatin + PF-04950615 100 mg-16.85-27.65
Atorvastatin + PF-04950615 150 mg-23.38-17.70
Atorvastatin + PF-04950615 50 mg-21.00-14.44
Atorvastatin + PF-04950615 Placebo3.74-3.82
PF-04950615 100 mg-9.401.32
PF-04950615 150 mg-5.21-8.47
PF-04950615 50 mg2.62-8.31
PF-04950615 Placebo-9.334.57

[back to top]

Percent Change From Baseline in Total Cholesterol (TC) at Day 85 and Day 113

Total cholesterol is the sum of all the cholesterol within the blood. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-10.85-14.02
Atorvastatin + PF-04950615 100 mg-42.64-40.55
Atorvastatin + PF-04950615 150 mg-48.22-45.58
Atorvastatin + PF-04950615 50 mg-36.26-34.28
Atorvastatin + PF-04950615 Placebo-5.47-9.18
PF-04950615 100 mg-41.98-40.27
PF-04950615 150 mg-45.28-45.71
PF-04950615 50 mg-32.56-30.50
PF-04950615 Placebo-3.82-1.62

[back to top]

Percent Change From Baseline in Total Cholesterol (TC) / High Density Lipoprotein- Cholesterol (HDL-C) Ratio at Day 85 and Day 113

Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-14.65-18.57
Atorvastatin + PF-04950615 100 mg-47.06-46.04
Atorvastatin + PF-04950615 150 mg-50.43-47.68
Atorvastatin + PF-04950615 50 mg-39.99-38.20
Atorvastatin + PF-04950615 Placebo2.19-3.81
PF-04950615 100 mg-43.25-41.49
PF-04950615 150 mg-45.74-45.65
PF-04950615 50 mg-29.51-31.07
PF-04950615 Placebo3.816.98

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein- Cholesterol (Non-HDL-C) at Day 85 and Day 113

Non-HDL-C calculated as total cholesterol minus HDL cholesterol. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-16.20-20.67
Atorvastatin + PF-04950615 100 mg-60.62-58.57
Atorvastatin + PF-04950615 150 mg-67.69-63.92
Atorvastatin + PF-04950615 50 mg-50.98-48.56
Atorvastatin + PF-04950615 Placebo-4.77-10.59
PF-04950615 100 mg-56.87-54.54
PF-04950615 150 mg-60.17-60.43
PF-04950615 50 mg-41.11-40.19
PF-04950615 Placebo-2.490.88

[back to top]

Percent Change From Baseline in Lipoprotein (a) (Lp[a]) at Day 85 and Day 113

Lp(a) is a lipoprotein subclass which consists of an LDL-like particle and the specific apolipoprotein(a). Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-15.22-18.64
Atorvastatin + PF-04950615 100 mg-58.53-57.94
Atorvastatin + PF-04950615 150 mg-46.51-59.42
Atorvastatin + PF-04950615 50 mg-47.11-42.30
Atorvastatin + PF-04950615 Placebo-19.37-24.35
PF-04950615 100 mg-37.29-47.60
PF-04950615 150 mg-43.37-49.77
PF-04950615 50 mg-37.85-45.26
PF-04950615 Placebo-18.40-15.89

[back to top]

Percent Change From Baseline in High Density Lipoprotein- Cholesterol (HDL-C) at Day 85 and Day 113

HDL-C is cholesterol in the bloodstream that is carried by high density lipoprotein. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg5.426.31
Atorvastatin + PF-04950615 100 mg9.4611.97
Atorvastatin + PF-04950615 150 mg5.865.27
Atorvastatin + PF-04950615 50 mg7.267.39
Atorvastatin + PF-04950615 Placebo-7.31-4.83
PF-04950615 100 mg2.932.35
PF-04950615 150 mg2.351.05
PF-04950615 50 mg-3.101.86
PF-04950615 Placebo-7.16-7.53

[back to top]

Percent Change From Baseline in Apolipoprotein B (ApoB) at Day 85 and Day 113

ApoB is a major protein that makes up LDL cholesterol and is involved in transporting cholesterol and triglycerides to cells and tissues in the body. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-9.97-14.17
Atorvastatin + PF-04950615 100 mg-57.02-53.45
Atorvastatin + PF-04950615 150 mg-62.31-59.48
Atorvastatin + PF-04950615 50 mg-44.30-42.64
Atorvastatin + PF-04950615 Placebo-1.77-7.54
PF-04950615 100 mg-51.62-49.10
PF-04950615 150 mg-55.31-54.88
PF-04950615 50 mg-35.16-34.66
PF-04950615 Placebo-0.133.43

[back to top]

Percent Change From Baseline in Apolipoprotein B (ApoB) / Apolipoprotein A-I (ApoA-I) Ratio at Day 85 and Day 113

Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg-9.13-14.00
Atorvastatin + PF-04950615 100 mg-58.47-55.05
Atorvastatin + PF-04950615 150 mg-63.09-60.32
Atorvastatin + PF-04950615 50 mg-44.37-43.21
Atorvastatin + PF-04950615 Placebo5.51-2.03
PF-04950615 100 mg-50.97-49.84
PF-04950615 150 mg-55.16-53.65
PF-04950615 50 mg-32.09-34.11
PF-04950615 Placebo10.4111.47

[back to top]

Terminal Elimination Half-Life (t1/2) of PF-04950615

Terminal elimination half-life is the time measured for the plasma concentration to decrease by one half. This outcome measure was to be analyzed in participants who received at least 1 dose of the PF-04950615. (NCT02055976)
Timeframe: Multiple dose (Day 99: pre-dose, 24, 72, 120, 168, 336, 504, 672, 1008 hr post-dose)

Interventionday (Mean)
Atorvastatin + PF-04950615 50 mg7.716
Atorvastatin + PF-04950615 100 mg9.471
Atorvastatin + PF-04950615 150 mg10.56
PF-04950615 50 mg9.404
PF-04950615 100 mg9.570
PF-04950615 150 mg9.333

[back to top]

Percent Change From Baseline in Apolipoprotein A-II (ApoA-II) at Day 85 and Day 113

ApoA-II is the second most abundant component of the HDL cholesterol. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. Percent change from baseline = ([observed value divided by baseline value] minus 1) multiplied by 100. (NCT02055976)
Timeframe: Baseline, Day 85, 113

,,,,,,,,
Interventionpercent change (Mean)
Change at Day 85Change at Day 113
Atorvastatin + Ezetimibe 10 mg3.131.48
Atorvastatin + PF-04950615 100 mg0.170.13
Atorvastatin + PF-04950615 150 mg-1.34-1.99
Atorvastatin + PF-04950615 50 mg-0.85-0.21
Atorvastatin + PF-04950615 Placebo-2.93-2.77
PF-04950615 100 mg1.342.64
PF-04950615 150 mg0.980.39
PF-04950615 50 mg-2.87-1.94
PF-04950615 Placebo-4.97-3.29

[back to top]

Number of Participants With Treatment-Emergent Adverse Events (TEAEs) or Serious Adverse Events (SAEs)

An adverse event (AE) was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. Serious adverse event (SAE) was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. TEAEs are events between first dose of study drug and up to Day 169 that were absent before treatment or that worsened relative to pretreatment state. Adverse events included treatment emergent injection site adverse events and any clinically significant abnormal laboratory value. (NCT02055976)
Timeframe: Baseline up to Day 169

,,,,,,,,
Interventionparticipants (Number)
AEsSAEs
Atorvastatin + Ezetimibe 10 mg50
Atorvastatin + PF-04950615 100 mg160
Atorvastatin + PF-04950615 150 mg130
Atorvastatin + PF-04950615 50 mg171
Atorvastatin + PF-04950615 Placebo131
PF-04950615 100 mg161
PF-04950615 150 mg150
PF-04950615 50 mg160
PF-04950615 Placebo110

[back to top]

Non-High Density Lipoprotein- Cholesterol (Non-HDL-C)

Non-HDL-C calculated as total cholesterol minus HDL cholesterol. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg165.86140.77131.52130.27130.59133.41129.32132.05130.64126.68134.91139.05133.68130.82131.41163.36170.41169.41174.45
Atorvastatin + PF-04950615 100 mg155.5497.7879.3377.8858.9271.7953.3866.6352.5858.1358.0860.0466.0451.5063.54117.42142.08144.83153.75
Atorvastatin + PF-04950615 150 mg154.7198.4876.1757.9648.2651.0944.9651.4645.6544.2648.6549.8760.0554.1455.7885.09119.83133.30148.52
Atorvastatin + PF-04950615 50 mg159.58113.5293.2495.6869.9281.0866.2079.6459.9275.7681.8377.2888.5664.0482.50134.80149.17149.60155.48
Atorvastatin + PF-04950615 Placebo163.90161.23162.16162.35160.04159.16159.46157.31157.62153.15161.54154.92156.36154.08146.36158.60155.52161.80159.12
PF-04950615 100 mg182.86143.24123.25103.1688.7190.6881.8388.1680.3086.0882.2578.0085.2977.8783.00113.13154.17164.83183.52
PF-04950615 150 mg182.17137.50122.7399.1388.2982.4679.4282.0878.9673.2176.1372.1774.5074.7572.35102.75128.96144.58162.65
PF-04950615 50 mg188.72154.36142.84138.40115.36115.52103.72112.60101.60101.80115.48110.40118.36107.76111.80164.60187.96190.96193.88
PF-04950615 Placebo181.17189.36193.70191.61192.09192.59184.74194.30186.70180.17185.96175.17190.52183.35180.65191.78191.09184.48193.59

[back to top]

Maximum Observed Plasma Concentration (Cmax) of PF-04950615

This outcome measure was to be analyzed in participants who received at least 1 dose of the PF-04950615. (NCT02055976)
Timeframe: Single dose (Day 1: pre-dose, 24, 48, 72, 96, 120, 144, 168 hr post-dose), Multiple dose (Day 99: pre-dose, 24, 72, 120, 168, 336, 504, 672, 1008 hr post-dose)

,,,,,
Interventionmicrogram per milliliter (mcg/mL) (Geometric Mean)
Single doseMultiple dose
Atorvastatin + PF-04950615 100 mg5.0748.343
Atorvastatin + PF-04950615 150 mg7.38221.91
Atorvastatin + PF-04950615 50 mg3.1736.197
PF-04950615 100 mg4.74412.22
PF-04950615 150 mg7.72623.64
PF-04950615 50 mg2.9945.874

[back to top]

Low Density Lipoprotein-Cholesterol (LDL-C)

LDL-C is cholesterol in the bloodstream that is carried by low density lipoprotein. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg135.36111.50105.86102.64101.68107.50103.05104.95106.2399.27109.18110.64106.14104.14107.32132.73139.14139.45140.91
Atorvastatin + PF-04950615 100 mg123.8571.8355.3851.9637.5848.2935.1339.6332.3337.2136.2938.0041.9632.1342.8886.71111.38113.75123.42
Atorvastatin + PF-04950615 150 mg129.1976.0457.7139.0031.0034.2629.5231.8329.9629.6133.1333.9138.0937.3638.4861.8795.30110.57124.04
Atorvastatin + PF-04950615 50 mg135.3686.7270.3673.7649.0861.5644.4058.2439.7656.8861.5058.9666.4845.1662.17108.16126.13126.52131.28
Atorvastatin + PF-04950615 Placebo135.90130.35132.08132.50133.27129.60128.50126.23127.92125.27130.31126.38125.80127.76118.88131.92129.32133.92129.28
PF-04950615 100 mg158.00120.20102.6380.4467.2965.2060.6764.8457.9163.5460.6359.8361.6757.0061.4887.22130.22140.78154.52
PF-04950615 150 mg159.90114.6396.5077.0867.7163.5860.7561.8359.2955.7557.3354.7154.2557.4253.3978.96103.08119.54137.13
PF-04950615 50 mg164.22128.68118.20113.2890.3293.3680.6487.7676.9681.3290.9686.6493.8084.5289.44137.00160.80165.17168.50
PF-04950615 Placebo155.22165.09167.22165.39166.04168.14154.00167.30158.83152.91156.70151.30163.70155.57153.30161.17163.52158.17168.55

[back to top]

Lipoprotein (a) (Lp[a])

Lp(a) is a lipoprotein subclass which consists of an LDL-like particle and the specific apolipoprotein(a). Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg19.46820.45017.24318.98217.80017.87318.05017.21417.31417.57316.99117.60916.86816.68216.81416.61817.23617.38217.059
Atorvastatin + PF-04950615 100 mg20.99818.34815.33314.12912.44613.37912.83312.52511.67510.87111.35410.87911.83711.07911.18315.11217.32917.48317.404
Atorvastatin + PF-04950615 150 mg18.84016.20414.16711.39210.76510.55210.4099.6339.0398.5789.0099.2398.8559.1239.56511.96114.42216.05216.635
Atorvastatin + PF-04950615 50 mg18.45216.22414.89214.20812.62812.83211.15211.64810.34410.70811.35810.96012.23210.75612.10815.47616.84217.26417.824
Atorvastatin + PF-04950615 Placebo19.26518.52319.18419.25818.78518.30417.04616.91216.83515.89216.54216.51915.76415.39614.49215.50015.82816.00415.384
PF-04950615 100 mg15.45814.58012.61712.54811.58310.88810.3299.94410.1919.4879.5299.2618.5378.2968.28710.54311.99613.46513.613
PF-04950615 150 mg13.40011.78312.7689.9968.8009.3128.0678.8217.6216.8586.9796.6376.7926.8586.7877.6428.4429.60010.626
PF-04950615 50 mg14.08012.46412.00010.14010.93610.4249.4849.38010.0409.3929.2488.8087.9408.6088.0209.86410.10010.20411.271
PF-04950615 Placebo16.23915.85916.44316.44316.02617.42315.84315.96115.07814.31313.50012.72613.69112.80012.91313.59613.13913.18314.741

[back to top]

Number of Participants With Anti-Drug Antibody (ADA) Response

Participants tested positive for ADA response on at least one post-baseline visit were reported. Participants with ADA titer level >=6.23 for PF-04950615 were considered ADA positive. (NCT02055976)
Timeframe: Baseline up to Day 169

Interventionparticipants (Number)
Atorvastatin + PF-04950615 50 mg14
Atorvastatin + PF-04950615 100 mg6
Atorvastatin + PF-04950615 150 mg14
PF-04950615 50 mg13
PF-04950615 100 mg16
PF-04950615 150 mg11

[back to top]

Minimum Observed Plasma Trough Concentration (Cmin) of PF-04950615

This outcome measure was to be analyzed in participants who received at least 1 dose of the PF-04950615. (NCT02055976)
Timeframe: Multiple dose (Day 99: pre-dose, 24, 72, 120, 168, 336, 504, 672, 1008 hr post-dose)

Interventionmcg/mL (Geometric Mean)
Atorvastatin + PF-04950615 50 mg2.176
Atorvastatin + PF-04950615 100 mg4.041
Atorvastatin + PF-04950615 150 mg12.95
PF-04950615 50 mg2.858
PF-04950615 100 mg6.571
PF-04950615 150 mg13.47

[back to top]

Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-04950615

Area under the plasma concentration-time profile from time zero to the time of the last quantifiable concentration. This outcome measure was to be analyzed in participants who received at least 1 dose of the PF-04950615. (NCT02055976)
Timeframe: Multiple dose (Day 99: pre-dose, 24, 72, 120, 168, 336, 504, 672, 1008 hr post-dose)

Interventionmcg*day/mL (Geometric Mean)
Atorvastatin + PF-04950615 50 mg87.86
Atorvastatin + PF-04950615 100 mg140.3
Atorvastatin + PF-04950615 150 mg434.2
PF-04950615 50 mg96.32
PF-04950615 100 mg220.9
PF-04950615 150 mg486.7

[back to top]

Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of PF-04950615

Area under the plasma concentration-time profile from time zero extrapolated to infinite time. This outcome measure was to be analyzed in participants who received at least 1 dose of the PF-04950615. (NCT02055976)
Timeframe: Multiple dose (Day 99: pre-dose, 24, 72, 120, 168, 336, 504, 672, 1008 hr post-dose)

Interventionmcg*day/mL (Geometric Mean)
Atorvastatin + PF-04950615 50 mg94.83
Atorvastatin + PF-04950615 100 mg176.9
Atorvastatin + PF-04950615 150 mg469.5
PF-04950615 50 mg111.7
PF-04950615 100 mg237.4
PF-04950615 150 mg248.4

[back to top]

High Density Lipoprotein- Cholesterol (HDL-C)

HDL-C is cholesterol in the bloodstream that is carried by high density lipoprotein. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg56.9857.0058.6760.2360.0559.0058.2358.8258.5557.4558.0059.7760.3659.4560.3257.8259.0959.4560.50
Atorvastatin + PF-04950615 100 mg54.7557.0458.3859.9660.0861.7560.5062.2160.0458.8362.9659.5462.5463.2561.0459.4660.6359.0059.04
Atorvastatin + PF-04950615 150 mg57.0058.4360.3362.7964.5263.8362.3962.2962.0960.3564.8359.7062.3264.4159.3962.7864.2661.9662.48
Atorvastatin + PF-04950615 50 mg54.5855.6856.4858.5259.3659.9657.9259.7660.1258.4060.2958.2462.6862.3658.1359.1660.5858.7257.48
Atorvastatin + PF-04950615 Placebo58.5458.1960.5259.3558.0857.9657.6257.3157.8154.8856.8553.9659.9258.2855.2860.7260.9659.4861.88
PF-04950615 100 mg60.4060.3261.3362.3263.9262.5265.2563.6464.9161.9263.9263.0964.5464.3963.0063.6163.2663.0062.04
PF-04950615 150 mg62.0262.0864.0066.5865.3867.9665.2165.1765.2162.6366.2962.0064.6365.1761.8363.8864.0063.6765.00
PF-04950615 50 mg57.2257.2059.6060.2460.9260.8459.7659.3659.4057.1659.1655.0460.0060.0857.9258.5659.4059.0460.29
PF-04950615 Placebo60.8759.7360.5760.3061.4864.1459.9159.7459.3956.6157.7856.3559.3058.3056.1758.0062.3961.8765.05

[back to top]

Very Low Density Lipoprotein-Cholesterol (VLDL-C)

VLDL is a type of lipoprotein made by the liver and one of the five major groups of lipoproteins, that enable fats and cholesterol to move within the water-based solution of the bloodstream. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg22.4821.9520.2922.6821.5922.7321.5920.9519.2321.5520.8219.7720.1418.6418.5021.5923.6821.4124.55
Atorvastatin + PF-04950615 100 mg23.7919.7018.0020.4219.0419.8815.3321.3317.6717.4617.5017.6318.0415.9616.5423.2122.2522.2121.42
Atorvastatin + PF-04950615 150 mg20.9217.2215.5816.5014.6515.3914.0418.0414.3913.8713.8314.0418.6814.5915.2616.6117.3916.5217.30
Atorvastatin + PF-04950615 50 mg19.9221.3619.6417.2017.0415.7618.9616.5616.3614.3615.9214.2416.2014.4415.8320.4818.1317.0018.88
Atorvastatin + PF-04950615 Placebo21.4223.8521.7223.0421.6521.8821.9223.6521.6920.8821.7722.5821.7219.3221.8819.3219.1620.5619.60
PF-04950615 100 mg17.6616.0816.2516.2816.4219.6816.4618.1217.0416.8316.7914.0916.4616.0915.9617.9117.6116.1723.00
PF-04950615 150 mg16.6318.0018.9516.2517.1713.0415.5016.9615.5413.5414.6314.0416.2113.1313.8717.3818.5418.9218.00
PF-04950615 50 mg17.4419.8018.6418.5217.2017.0017.2820.0017.4815.4419.0416.6817.8417.7615.9219.7219.5219.3019.13
PF-04950615 Placebo17.5020.6822.4820.4318.1319.0024.2222.7822.2620.1322.6116.4321.1320.0019.3921.6120.0918.5719.68

[back to top]

Triglyceride (TG)

Triglycerides are a type of fat circulating in the blood and account for the majority of the fats circulating in the blood. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg152.59146.41128.43145.91144.64130.00139.95135.23121.64137.55139.27142.45137.82133.41129.14153.14156.27149.23167.91
Atorvastatin + PF-04950615 100 mg158.21130.30124.58143.96119.17133.38111.25161.75126.58124.25125.50130.25128.25116.29112.88159.25164.79164.13151.63
Atorvastatin + PF-04950615 150 mg127.65112.1795.71123.96101.96100.0496.52130.71100.5792.5293.9195.00131.32102.5994.39115.96123.39113.83122.43
Atorvastatin + PF-04950615 50 mg121.04134.20126.44109.52105.5697.84113.68108.16108.1294.40103.1392.36110.5697.80101.58133.40115.13115.44120.76
Atorvastatin + PF-04950615 Placebo140.23154.27150.40149.31133.65147.92154.65159.19148.50139.50156.27142.81156.84131.68141.64133.40131.08139.44149.40
PF-04950615 100 mg124.40115.40103.50113.52109.04142.84109.17119.44114.22117.21112.13100.04118.17109.91116.26139.83119.91119.91166.22
PF-04950615 150 mg111.58114.25130.91114.25113.7994.29105.67109.29113.2990.67103.1399.92115.0893.54101.43124.50129.13133.33128.26
PF-04950615 50 mg122.40128.20122.72125.64125.00111.24115.12123.80123.48102.28122.68118.64122.96116.16111.72138.08135.80129.00126.67
PF-04950615 Placebo130.39121.09136.91130.65130.26122.09158.30140.61142.30136.78146.43119.17133.91139.00136.61159.43137.35131.74125.41

[back to top]

Total Cholesterol (TC) / High Density Lipoprotein- Cholesterol (HDL-C) Ratio

Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionratio (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg4.02233.56683.35103.27003.25503.33183.28823.32593.32773.26323.38553.39863.30733.28323.23593.91323.98413.92054.0036
Atorvastatin + PF-04950615 100 mg4.01542.78612.41002.37542.02582.25331.93002.13961.92542.07581.99882.07212.14171.86502.10423.15333.52423.63923.7471
Atorvastatin + PF-04950615 150 mg3.85002.75002.30831.96581.77301.82961.74041.87541.74431.74481.77091.85612.03051.88141.96912.48223.00783.27483.4830
Atorvastatin + PF-04950615 50 mg4.01183.13722.72522.68842.24282.40202.19242.36882.02802.31482.39252.37242.45642.04762.46883.37763.54333.62403.8140
Atorvastatin + PF-04950615 Placebo3.96293.94653.85883.93083.89153.88523.94963.93383.94193.95964.00854.05083.76483.79123.82483.79843.75083.91003.7436
PF-04950615 100 mg4.25583.50363.13672.77722.43382.57802.30002.51242.28832.57082.32582.27962.40752.25172.36392.90873.60703.81264.2000
PF-04950615 150 mg4.26103.40293.09412.60502.36172.28002.25292.30042.26582.22252.19882.21422.21212.18962.23352.82083.35003.64503.8970
PF-04950615 50 mg4.54083.92643.60243.49403.06763.02602.84523.00442.83002.84363.05283.12043.08682.91763.07603.98964.42564.50574.4975
PF-04950615 Placebo4.10764.32594.33744.30174.28224.10234.22224.40744.29094.33614.37914.26134.42004.31574.35704.47174.28434.18044.1182

[back to top]

Total Cholesterol (TC)

Total cholesterol is the sum of all the cholesterol within the blood. Fasting was required at least 10 hours before blood sample collection. Baseline was defined as the mean of the last two non-missing measurements collected prior to the first dose of study treatment. Both measurements must be within 10 days prior to the first dose of study treatment; if only one measurement was available 10 days prior to the first dose of study treatment, then that measurement served as the baseline value. (NCT02055976)
Timeframe: Baseline, Day 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141, 155, 169

,,,,,,,,
Interventionmg/dL (Mean)
BaselineDay 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141Day 155Day 169
Atorvastatin + Ezetimibe 10 mg222.84197.77190.19190.50190.64192.41187.55190.86189.18184.14192.91198.82194.05190.27191.73221.18229.50228.86234.95
Atorvastatin + PF-04950615 100 mg210.29154.83137.71137.83119.00133.54113.88128.83112.63116.96121.04119.58128.58114.75124.58176.88202.71203.83212.79
Atorvastatin + PF-04950615 150 mg211.71156.91136.50120.75112.78114.91107.35113.75107.74104.61113.48109.57122.36118.55115.17147.87184.09195.26211.00
Atorvastatin + PF-04950615 50 mg214.16169.20149.72154.20129.28141.04124.12139.40120.04134.16142.13135.52151.24126.40140.63193.96209.75208.32212.96
Atorvastatin + PF-04950615 Placebo222.44219.42222.68221.69218.12217.12217.08214.62215.42208.04218.38208.88216.28212.36201.64219.32216.48221.28221.00
PF-04950615 100 mg243.26203.56184.58165.48152.63153.20147.08151.80145.22148.00146.17141.09149.83142.26146.00176.74217.43227.83245.57
PF-04950615 150 mg244.19199.58186.73165.71153.67150.42144.63147.25144.17135.83142.42134.17139.13139.92134.17166.63192.96208.25227.65
PF-04950615 50 mg245.94211.56202.44198.64176.28176.36163.48171.96161.00158.96174.64165.44178.36167.84169.72223.16247.36250.00254.17
PF-04950615 Placebo242.04249.09254.26251.91253.57256.73244.65254.04246.09236.78243.74231.52249.83241.65236.83249.78253.48246.35258.64

[back to top]

Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-04950615

This outcome measure was to be analyzed in participants who received at least 1 dose of the PF-04950615. (NCT02055976)
Timeframe: Single dose (Day 1: pre-dose, 24, 48, 72, 96, 120, 144, 168 hour (hr) post-dose), Multiple dose (Day 99: pre-dose, 24, 72, 120, 168, 336, 504, 672, 1008 hr post-dose)

,,,,,
Interventionday (Median)
Single doseMultiple dose
Atorvastatin + PF-04950615 100 mg4.972.98
Atorvastatin + PF-04950615 150 mg5.942.97
Atorvastatin + PF-04950615 50 mg4.013.03
PF-04950615 100 mg5.452.98
PF-04950615 150 mg6.944.98
PF-04950615 50 mg5.942.99

[back to top]

Plasma Concentration of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9)

Concentration versus time summary was calculated by setting concentration values below the lower limit of quantification (LLQ =6.99 nanogram per milliliter [ng/mL]) to zero. Summary statistics were not to be presented if number of observations above lower limit of quantification (NALQ) =0. Here, 'Number analyzed' = Participants evaluable for this outcome measure at specified time points. (NCT02055976)
Timeframe: Day 1, 5, 8, 15, 22, 29, 36, 43, 50, 57, 71, 85, 99, 106, 113, 127, 141

,,,,,,,
Interventionng/mL (Mean)
Day 1Day 5Day 8Day 15Day 22Day 29Day 36Day 43Day 50Day 57Day 71Day 85Day 99Day 106Day 113Day 127Day 141
Atorvastatin + PF-04950615 100 mg261.232152.62701.93198.13297.33224.83310.73406.33297.23204.83241.23166.33242.93138.92919.02148.71382.8
Atorvastatin + PF-04950615 150 mg285.961997.72539.53291.93166.53419.83248.53391.93230.93390.63280.53198.93259.62864.02910.33030.72851.0
Atorvastatin + PF-04950615 50 mg266.642292.22711.22539.83451.72844.23446.22900.93394.82779.22889.62727.02915.13326.72727.31429.8736.63
Atorvastatin + PF-04950615 Placebo269.19291.77292.19303.42295275304.75303.54293.38277.69285.81276.31326.08283.67267.71281.40290.16
PF-04950615 100 mg215.501775.42297.73030.82971.63095.53011.23302.53001.33026.43197.12934.13149.32755.73009.82556.01477.0
PF-04950615 150 mg234.421712.02306.72966.72726.72955.62761.43016.92820.32791.92887.62787.92918.92566.52683.92769.72368.7
PF-04950615 50 mg228.801952.52490.42590.63117.43050.03237.03278.93148.52910.63066.82898.73119.23165.72908.41778.91056.5
PF-04950615 Placebo210.22240.41240.22224.43218.82230.09233.09239.13237.40220.13355.17269.61252.13242.23222.05249.8720.043

[back to top]

Percentage of Participants Achieving Low-density Lipoprotein Cholesterol (LDL-C) Less Than (<) 10, 25, 40, 70 and 100 Milligram Per Deciliter

LDL-C is cholesterol in the bloodstream that is carried by low density lipoprotein. Fasting was required at least 10 hours before blood sample collection. (NCT02055976)
Timeframe: Baseline up to Day 113

,,,,,,,
Interventionpercentage of participants (Number)
LDL-C <10 mg/dLLDL-C <25 mg/dLLDL-C <40 mg/dLLDL-C <70 mg/dLLDL-C <100 mg/dL
Atorvastatin + PF-04950615 100 mg4.266.791.7100.0100.0
Atorvastatin + PF-04950615 150 mg0.058.395.8100.0100.0
Atorvastatin + PF-04950615 50 mg0.012.084.096.0100.0
Atorvastatin + PF-04950615 Placebo0.00.00.00.023.1
PF-04950615 100 mg0.00.036.092.0100.0
PF-04950615 150 mg0.020.841.787.5100.0
PF-04950615 50 mg0.00.012.064.092.0
PF-04950615 Placebo0.00.00.00.04.3

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

Triglycerides Before and After Simvastatin/Ezetimibe Administration

Triglyceride concentration were measured by enzymatic assay (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionmg/dl (Median)
Baseline4 weeks8 weeks
Ezetimibe12010581
Simvastatin141117104

[back to top]

Apolipoprotein B Before and After Simvastatin/Ezetimibe Administration

Levels of apolipoprotein B were determined by inmunonephelometry (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionmg/dl (Mean)
Baseline4 weeks8 weeks
Ezetimibe12711079
Simvastatin1399284

[back to top]

High-density Lipoprotein Cholesterol (HDLc) Before and After Simvastatin/Ezetimibe Administration

High-density lipoprotein cholesterol (HDLc) concentration was measured using a direct method (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionmg/dl (Mean)
Baseline4 weeks8 weeks
Ezetimibe535353
Simvastatin475051

[back to top]

Leukocyte Adhesion Before and After Simvastatin/Ezetimibe Administration

Interactions between leukocytes and human umbilical vein endothelial cells were evaluated by flow chamber microscopy. Adhesion was evaluated by counting the number of polymorphonuclear cells that maintained stable contact with human umbilical vein endothelial cells (HUVEC) for 30 seconds. (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionpolymorphonuclear cells/mm2 (Mean)
Baseline4 weeks8 weeks
Ezetimibe25.623.812.5
Simvastatin25.115.010.9

[back to top]

Leukocyte Rolling Flux Before and After Simvastatin/Ezetimibe Administration

Interactions between leukocytes and human umbilical vein endothelial cells were evaluated by flow chamber microscopy. Leukocyte rolling was estimated as the number of leukocytes rolling over 100 μm2 of the endothelial monolayer during a 1-min period. (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionpolymorphonuclear cells/min (Mean)
Baseline4 weeks8 weeks
Ezetimibe421392196
Simvastatin412225147

[back to top]

Leukocyte Rolling Velocity Before and After Simvastatin/Ezetimibe Administration

Interactions between leukocytes and human umbilical vein endothelial cells were evaluated by flow chamber microscopy.The rolling velocity in the field of focus was determined by measuring the time required by 20 consecutive leukocytes to cover a distance of 100 μm. (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionmicrometer/second (Mean)
Baseline4 weeks8 weeks
Ezetimibe524533629
Simvastatin469553608

[back to top]

Levels of E-selectin Before and After Simvastatin/Ezetimibe Administration

E-selectin was evaluated in serum by Luminex® 200™ system (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionng/ml (Mean)
Baseline4 weeks8 weeks
Ezetimibe39.730.524.4
Simvastatin45.138.929.2

[back to top]

Levels of Glutathione (GSH) Before and After Simvastatin/Ezetimibe Administration

Oxidative stress markers (levels of glutathione (GSH)) was measured at baseline and after treatment by fluorometric techniques (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
InterventionFluorescence Units (Mean)
Baseline4 weeks8 weeks
Ezetimibe2.853.797.51
Simvastatin2.685.677.92

[back to top]

Levels of High-sensitive C-reactive Protein (hsCRP) Before and After Simvastatin/Ezetimibe Administration

Levels of high-sensitive C-reactive protein (hsCRP) were analysed by a latex-enhanced inmunonephelometric assay (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionmg/l (Mean)
Baseline4 weeks8 weeks
Ezetimibe4.433.983.31
Simvastatin4.022.822.64

[back to top]

Levels of Intercellular Adhesion Molecule 1 (ICAM-1) Before and After Simvastatin/Ezetimibe Administration

The intercellular adhesion molecule 1 (ICAM-1) was evaluated in serum by Luminex® 200™ system (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionng/ml (Mean)
Baseline4 weeks8 weeks
Ezetimibe160.6114.7108.1
Simvastatin188139.5122.2

[back to top]

Levels of Interleukin-6 (IL-6) Before and After Simvastatin/Ezetimibe Administration

Levels of proinflammatory cytokines (interleukin-6 (IL-6)) were analysed with a Luminex® 200™ system (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionpg/ml (Mean)
Baseline4 weeks8 weeks
Ezetimibe2.943.935.78
Simvastatin2.442.834.43

[back to top]

Levels of Tumor Necrosis Factor α (TNF-α) Before and After Simvastatin/Ezetimibe Administration

Levels of proinflammatory cytokines (tumor necrosis factor α (TNF-α)) were analysed with a Luminex® 200™ system (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionpg/ml (Mean)
Baseline4 weeks8 weeks
Ezetimibe3.015.094.35
Simvastatin3.433.994.43

[back to top]

Levels of Vascular Cell Adhesion Molecule 1 (VCAM-1) Before and After Simvastatin/Ezetimibe Administration

The vascular cell adhesion molecule 1 (VCAM-1) was evaluated in serum by Luminex® 200™ system (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionng/ml (Mean)
Baseline4 weeks8 weeks
Ezetimibe137111661220
Simvastatin131411371074

[back to top]

Low Density Lipoprotein Size Before and After Simvastatin/Ezetimibe Administration

LDL subfractions were separated by high-resolution polyacrylamide gel tubes using the Lipoprint® system. The LDL electrophoretic profile allows 2 patterns to be defined: pattern A or large and buoyant LDL, and pattern non-A or small and dense LDL. (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
InterventionAngström (Mean)
Baseline4 weeks8 weeks
Ezetimibe270.4271.5272.0
Simvastatin268.1270.4271.7

[back to top]

Low-density Lipoprotein Cholesterol (LDLc) Before and After Simvastatin/Ezetimibe Administration

Low-density lipoprotein cholesterol (LDLc) concentration was calculated using the method of Friedewald. (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionmg/dl (Mean)
Baseline4 weeks8 weeks
Ezetimibe17213894
Simvastatin17810698

[back to top]

Membrane Potential Before and After Simvastatin/Ezetimibe Administration

Oxidative stress markers (membrane potential) was measured at baseline and after treatment by fluorometric techniques (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
InterventionFluorescence Units (Mean)
Baseline4 weeks8 weeks
Ezetimibe48.456.767.5
Simvastatin46.662.570.4

[back to top]

Mitochondrial Oxygen (O2) Consumption Before and After Simvastatin/Ezetimibe Administration

Oxidative stress markers (mitochondrial oxygen (O2) consumption) was measured at baseline and after treatment by Clark electrode (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
InterventionNmol O2/min/million cells (Mean)
Baseline4 weeks8 weeks
Ezetimibe1.091.311.67
Simvastatin1.091.541.76

[back to top]

Non-HDL Cholesterol Before and After Simvastatin/Ezetimibe Administration

Non-HDLc concentration was obtained by calculating the difference between total cholesterol and HDLc (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionmg/dl (Mean)
Baseline4 weeks8 weeks
Ezetimibe200162115
Simvastatin208130122

[back to top]

Reactive Oxygen Species (ROS) Production Before and After Simvastatin/Ezetimibe Administration

Oxidative stress markers (Reactive oxygen species (ROS) production) was measured at baseline and after treatment by fluorometric techniques (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
InterventionFluorescence Units (Mean)
Baseline4 weeks8 weeks
Ezetimibe72.863.548.9
Simvastatin74.757.243.3

[back to top]

Total Cholesterol Before and After Simvastatin/Ezetimibe Administration

Total cholesterol concentration was measured by enzymatic assay (NCT02304926)
Timeframe: Baseline, 4 weeks and 8 weeks

,
Interventionmg/dl (Mean)
Baseline4 weeks8 weeks
Ezetimibe253215169
Simvastatin255180173

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Week 12

Baseline value was defined as the last observation before the first dose of the treatment. (NCT02476006)
Timeframe: Baseline, Week 12

Interventionpercent change (Mean)
Alirocumab-38.28

[back to top]

Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol (LDL-C) at Week 12

Calculated LDL-C values were obtained using the Friedewald formula. Calculated LDL-C in mg/dL from Friedewald formula (LDL cholesterol = Total cholesterol - HDL cholesterol - [Triglyceride/5]). Baseline value was defined as the last observation before the first dose of the treatment. (NCT02476006)
Timeframe: Baseline, Week 12

Interventionpercent change (Mean)
Alirocumab-54.84

[back to top]

Percent Change From Baseline in High Density Lipoprotein Cholesterol at Week 12

Baseline value was defined as the last observation before the first dose of the treatment. (NCT02476006)
Timeframe: Baseline, Week 12

Interventionpercent change (Mean)
Alirocumab4.37

[back to top]

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

Baseline value was defined as the last observation before the first dose of the treatment. (NCT02476006)
Timeframe: Baseline, Week 12

Interventionpercent change (Mean)
Alirocumab-45.89

[back to top]

Percent Change From Baseline in Triglycerides at Week 12

Baseline value was defined as the last observation before the first dose of the treatment. (NCT02476006)
Timeframe: Baseline, Week 12

Interventionpercent change (Mean)
Alirocumab-8.28

[back to top]

Percentage of Participants Reaching Calculated LDL-C <100 mg/dL (2.59 mmol/L) at Week 12

LDL-Cholesterol was calculated using the Friedewald formula. Percentage of participants who reached calculated LDL-C <100 mg/dL (2.59 mmol/L) at week 12 were reported. (NCT02476006)
Timeframe: At Week 12

Interventionpercentage of participants (Number)
Alirocumab74.6

[back to top]

Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) and/or >=50% Reduction From Baseline in LDL-C at Week 12

LDL-Cholesterol was calculated using the Friedewald formula. Percentage of participants who reached LDL-C <70 mg/dL at Week 12 and/or >=50% reduction from baseline in LDL-C at Week 12 are reported. (NCT02476006)
Timeframe: At Week 12

Interventionpercentage of participants (Number)
Alirocumab69.1

[back to top]

Percentage of Participants Reaching Calculated LDL-C <70 mg/dL (1.81 mmol/L) at Week 12

LDL-Cholesterol was calculated using the Friedewald formula. Percentage of participants who reached calculated LDL-C <70 mg/dL (1.81 mmol/L) at week 12 were reported. (NCT02476006)
Timeframe: At Week 12

Interventionpercentage of participants (Number)
Alirocumab50.2

[back to top]

Assessment of Participant's Acceptability of Self-Injection Using Self Injection Assessment Questionnaire (SIAQ): Feeling About Injections, Self Confidence, Satisfaction With Self-Injections

Pre-SIAQ: self-completed before first self-injection & Post-SIAQ: self-completed after self-injection. Pre-SIAQ consisted of 7 items grouped into 3 domains:feelings about injections,self-confidence & satisfaction with self-injection. Post-SIAQ consisted of 21 items grouped into 6 domains:feelings about injections,self-image,self-confidence,injection-site reactions,ease of use & satisfaction with self-injection. Participants rated each item on 5-point (or 6-point) semantic Likert-type scale, where lower numbers indicate a worse experience. Item scores were transformed to obtain a score ranging from 0 (worst experience) to 10 (best experience). Transformed scores for items contributing to a domain were then averaged into a domain score. Each domain score ranges from 0 (worst experience) to 10 (best experience), higher score=better acceptability. Domain scores common to the Pre & Post SIAQ were analyzed on participants belonging to Pre & Post-SIAQ population and are reported. (NCT02476006)
Timeframe: Baseline (Pre-SIAQ), Week 4, Week 8, Week 12, Week 24, Week 48, Week 72, Week 96

Interventionunits on a scale (Mean)
Feelings about injections: BaselineFeeling about injections: Week 4Feeling about injections: Week 8Feeling about injections: Week 12Feeling about injections: Week 24Feeling about injections: Week 48Feeling about injections: Week 72Feeling about injections: Week 96Self confidence: BaselineSelf Confidence: Week 4Self Confidence: Week 8Self Confidence: Week 12Self Confidence: Week 24Self Confidence: Week 48Self Confidence: Week 72Self Confidence: Week 96Satisfaction with self injection: BaselineSatisfaction with self-injections: Week 4Satisfaction with self-injections: Week 8Satisfaction with self-injections: Week 12Satisfaction with self-injections: Week 24Satisfaction with self-injections: Week 48Satisfaction with self-injections: Week 72Satisfaction with self-injections: Week 96
Alirocumab8.69.19.19.29.29.29.29.36.98.08.18.18.08.18.38.47.28.58.78.78.68.78.88.8

[back to top]

Assessment of Participant's Acceptability of Self-Injection Using Self Injection Assessment Questionnaire (SIAQ): Self Image, Injection-Site Reactions, Ease of Use

SIAQ: contained 2 modules: Pre-SIAQ and Post-SIAQ. Post-SIAQ: self-completed after self-injection. Post-SIAQ consisted of 21 items grouped into 6 domains: feelings about injections, self-image, self-confidence, injection-site reactions, ease of use & satisfaction with self-injection. Participants rated each item on 5-point (or 6-point) semantic Likert-type scale, where lower numbers indicated a worse experience. Item scores were transformed to obtain a score ranging from 0 (worst experience) to 10 (best experience) for each item. Transformed scores for items contributing to a domain were then averaged into a domain score. Each domain score ranges from 0 (worst experience) to 10 (best experience), higher score=better acceptability. Domain scores which are not in common with Pre-SIAQ were analyzed on the Post-SIAQ population and are reported here. (NCT02476006)
Timeframe: Week 4, Week 8, Week 12, Week 24, Week 48, Week 72, Week 96

Interventionunits on a scale (Mean)
Self Image: Week 4Self Image: Week 8Self Image: Week 12Self Image: Week 24Self Image: Week 48Self Image: Week 72Self Image: Week 96Injection-site reactions: Week 4Injection-site reactions: Week 8Injection-site reactions: Week 12Injection-site reactions: Week 24Injection-site reactions: Week 48Injection-site reactions: Week 72Injection-site reactions: Week 96Ease of use: Week 4Ease of use: Week 8Ease of use: Week 12Ease of use: Week 24Ease of use: Week 48Ease of use: Week 72Ease of use: Week 96
Alirocumab9.49.49.49.39.49.39.49.69.69.69.59.59.59.58.78.78.88.88.99.09.0

[back to top]

Percentage of Participants With Treatment Emergent Adverse Events (TEAEs)

Adverse Event (AE) was defined as any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. Treatment-emergent AEs (TEAEs) were defined as AEs that that developed or worsened or became serious during the TEAE period (time from the first injection of study drug up to the day of the last injection of study drug + 14 days). A Serious Adverse Event (SAE) was any untoward medical occurrence that at any dose: resulted in death, was life-threatening, required inpatient hospitalization or prolongation of existing hospitalization, resulted in persistent or significant disability/incapacity, was a congenital anomaly/birth defect, was a medically important event. (NCT02476006)
Timeframe: From first injection of investigational medicinal product (IMP) up to 2 weeks after last dose of study drug (Week 120)

Interventionpercentage of participants (Number)
Any TEAEAny treatment emergent SAEAny TEAE leading to deathAny TEAE leading to treatment discontinuation
Alirocumab71.616.20.24.5

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in Aspartate Aminotransferase (AST) ≥3 Times ULN

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of AST that were 3 x ULN or greater were recorded. The AST ULN was 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg1.5
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in ALT and/or AST ≥3 Times ULN

Participants had ALT and AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT and/or AST that were 3 x ULN or greater were recorded. The ALT and AST ULNs were 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg1.5
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in ALT ≥5 Times ULN

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had an assessment of ALT that was 5x ULN or greater were recorded. The ALT ULN was 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg1.5
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in ALT ≥10 Times ULN

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had an assessment of ALT that was 10x ULN or greater were recorded. The ALT ULN was 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg0.0
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 12

Participants had LDL-C levels assessed at baseline and after 12 weeks of study drug administration. The change from baseline was calculated. (NCT02550288)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Least Squares Mean)
Ezetimibe 10 mg-19.3
Atorvastatin 10 mg-44.0
Atorvastatin 20 mg-49.1
Ezetimibe 10 mg + Atorvastatin 10 mg-55.6
Ezetimibe 10 mg + Atorvastatin 20 mg-59.2

[back to top]

Percentage of Participants Who Experience 1 or More Allergic Reaction or Rash AEs

Allergic Reaction or Rash AEs included Allergy to Arthropod Sting, Anaphylactoid Reaction, Anaphylactic Reaction, Anaphylatic Shock, Anaphylactoid Shock, Angioedema, Conjunctivitis Allergic, Contrast Media Reaction, Dermatitis, Dermatitis Allergic, Dermatitis Atopic, Dermatitis Bullous, Dermatitis Contact, Dermatitis Psoriasiform, Drug Hypersensitivity, Eczema, Eosinophila, Erythema, Eye Allergy, Face Oedema, Hypersensitivity, Mechanical Urticaria, Palmar Erythema, Periorbital Oedema, Photodermatosis, Photosensitivity Allergic reaction, Photosensitivity Reaction, Pigmentation Disorder, Pruritus, Pruritus Generalised, Rash, Rash Erythematous, Rash Follicular, Rash Generalised, Rash Maculo-Papular, Rash Papulosquamous, Rash Pruritic, Rash Pustular, Rash Vesicular, Rhinitis, Rhinitis Allergic, Rosacea, Skin Exfoliation, Skin Disorder, Skin Hyperpigmentation, Skin Lesion, Skin Mass, Skin Ulcer, Subcutaneous Nodule, Swelling Face, Systemic Lupus Erythematosus Rash, Urticaria. (NCT02550288)
Timeframe: up to 14 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg2.9
Atorvastatin 20 mg2.9
Ezetimibe 10 mg + Atorvastatin 10 mg0.0
Ezetimibe 10 mg + Atorvastatin 20 mg1.4

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) ≥3 Times Upper Limit of Normal (ULN)

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT that were 3 x ULN or greater were recorded. The ALT ULN was 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg1.5
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top] [back to top] [back to top]

Percentage of Participants With Potential Hy's Law Condition

Percentage of Participants with Potential Hy's Law Condition (defined as serum ALT or serum AST elevations >3xULN, with serum alkaline phosphatase <2xULN and total bilirubin (TBL) ≥2xULN) was summarized. The ALT and AST ULNs were 40 U/L. The ULN for alkaline phosphatase was 359 IU/L and the ULN for total bilirubin was 1.2 mg/dL. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg0.0
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percentage of Participants Who Have Elevations in Creatine Kinase (CK) ≥10xULN

Participants had creatine phosphokinase (CK) levels assessed throughout the 12 week treatment period. Participants who had any CK level that was ≥10 x ULN were recorded. The CK ULNs for males and females were 287 IU/L and 163 IU/L, respectively. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg1.4
Ezetimibe 10 mg + Atorvastatin 10 mg0.0
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percentage of Participants Who Have Elevations in CK ≥10xULN With Muscle Symptoms

Participants had CK levels assessed throughout the 12 week treatment period. Participants who had any CK level that was ≥10 x ULN and had associated muscle symptoms present within +/- 7 days were recorded. The CK ULNs for males and females were 287 IU/L and 163 IU/L, respectively. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg0.0
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top] [back to top]

Percentage of Participants Who Have Consecutive Elevations in ALT and/or AST ≥5 Times ULN

Participants had ALT and AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT and/or AST that were 5 x ULN or greater were recorded. The ALT and AST ULNs were 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg1.5
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top] [back to top]

Percentage of Participants Who Have Consecutive Elevations in ALT and/or AST ≥10 Times ULN

Participants had ALT and AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT and/or AST that were 10x ULN or greater were recorded. The ALT and AST ULNs were 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg1.5
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in AST ≥5 Times ULN

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had an assessment of AST that was 5x ULN or greater were recorded. AST ULN was 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg1.5
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in AST ≥10 Times ULN

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of AST that were 10x ULN or greater were recorded. The AST ULN was 40 U/L. (NCT02550288)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Atorvastatin 10 mg0.0
Atorvastatin 20 mg0.0
Ezetimibe 10 mg + Atorvastatin 10 mg1.5
Ezetimibe 10 mg + Atorvastatin 20 mg0.0

[back to top]

Percent Change From Baseline in Triglycerides at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-5.21
Evolocumab-1.73

[back to top]

Percentage of Participants Who Achieved a Mean LDL-C at Weeks 10 and 12 of Less Than 70 mg/dL

Mean low density lipoprotein-cholesterol response was defined as LDL-C < 70 mg/dL [1.8 mol/L]. (NCT02634580)
Timeframe: Weeks 10 and 12

Interventionpercentage of participants (Number)
Ezetimibe0.00
Evolocumab56.41

[back to top]

Percentage of Participants Who Achieved a LDL-C of Less Than 70 mg/dL at Week 12

(NCT02634580)
Timeframe: Week 12

Interventionpercentage of participants (Number)
Ezetimibe0.00
Evolocumab52.63

[back to top]

Percent Change From Baseline in VLDL-C at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-9.06
Evolocumab-1.42

[back to top]

Percent Change From Baseline in VLDL-C at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-4.67
Evolocumab-5.34

[back to top]

Change From Baseline in LDL-C at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionmg/dL (Least Squares Mean)
Ezetimibe-35.6
Evolocumab-113.2

[back to top]

Percent Change From Baseline in Total Cholesterol at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-12.69
Evolocumab-38.52

[back to top]

Percent Change From Baseline in Apolipoprotein B at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-13.23
Evolocumab-48.90

[back to top]

Percent Change From Baseline in Triglycerides at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-9.87
Evolocumab1.92

[back to top]

Change From Baseline in LDL-C at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionmg/dL (Least Squares Mean)
Ezetimibe-33.4
Evolocumab-112.7

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-11.32
Evolocumab-47.91

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A-1 Ratio at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-15.39
Evolocumab-52.46

[back to top]

Percent Change From Baseline in Apolipoprotein B/Apolipoprotein A-1 Ratio at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-15.62
Evolocumab-51.91

[back to top]

Percent Change From Baseline in HDL-C at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe3.10
Evolocumab11.06

[back to top]

Percent Change From Baseline in HDL-C at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe6.45
Evolocumab12.04

[back to top]

Percent Change From Baseline in Lipoprotein(a) at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-5.89
Evolocumab-37.02

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-5.21
Evolocumab-36.41

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at the Mean of Weeks 10 and 12

For all efficacy endpoints the two dosing regimens (every 2 weeks and every month) for each treatment were pooled for analysis. (NCT02634580)
Timeframe: Baseline and Weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-20.39
Evolocumab-59.75

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-19.13
Evolocumab-59.27

[back to top]

Percent Change From Baseline in Total Cholesterol at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-13.80
Evolocumab-39.24

[back to top]

Percent Change From Baseline in Non-HDL-C at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-18.82
Evolocumab-52.35

[back to top]

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

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-18.28
Evolocumab-51.71

[back to top]

Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at the Mean of Weeks 10 and 12

(NCT02634580)
Timeframe: Baseline and weeks 10 and 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-15.73
Evolocumab-44.34

[back to top]

Percent Change From Baseline in the Total Cholesterol/HDL-C Ratio at Week 12

(NCT02634580)
Timeframe: Baseline and week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe-17.34
Evolocumab-44.39

[back to top]

Percent Change From Baseline in Total-C at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-30.9
Usual Care: Intent to Prescribe Fenofibrate-5.7

[back to top]

Percent Change From Baseline in LDL-C Particle Number at Week 24: Overall ITT Analysis

LDL-C particle number was calculated from lipid subfractions by nuclear magnetic resonance (NMR) spectroscopy. Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-41.6
Usual Care-3.9

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 24 : Overall ITT Analysis

Adjusted means and standard errors at Week 24 were obtained from multiple imputation approach followed by robust regression model for handling of missing data. All available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment were included in the imputation model. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-23.7
Usual Care3.7

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum

Adjusted means and standard errors at Week 24 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-18.9
Usual Care: Intent to Prescribe Fenofibrate3.9

[back to top]

Percent Change From Baseline in Apo B at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-38.9
Usual Care: Intent to Prescribe Fenofibrate-3.8

[back to top]

Percent Change From Baseline in Measured LDL-C at Week 12: Overall ITT Analysis

Measured LDL-C values via beta quantification method. Adjusted LS means and standard errors at Week 12 from MMRM model including available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-41.7
Usual Care-7.0

[back to top]

Percent Change From Baseline in Measured LDL-C at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum

Measured LDL-C values via beta quantification method. Adjusted LS means and standard errors at Week 24 from MMRM model including available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-47.0
Usual Care: Intent to Prescribe Fenofibrate8.7

[back to top]

Percent Change From Baseline in Measured Low-Density Lipoprotein Cholesterol (LDL-C) at Week 24: Overall ITT Analysis

Measured LDL-C values via beta quantification method. Adjusted LS means and standard errors at Week 24 from MMRM model including available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-43.3
Usual Care-0.3

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 12: ITT- Intent to Prescribe Fenofibrate Stratum

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-34.7
Usual Care: Intent to Prescribe Fenofibrate-7.3

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 12: Overall ITT Analysis

Adjusted LS means and standard errors at Week 12 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-35.5
Usual Care-9.4

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-41.7
Usual Care: Intent to Prescribe Fenofibrate-8.5

[back to top]

Percent Change From Baseline in Non-HDL-C at Week 24: Overall Intent-to-treat (ITT) Analysis

Adjusted Least-squares (LS) means and standard errors at Week 24 were obtained from a mixed-effect model with repeated measures (MMRM) to account for missing data. All available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment were used in the model (ITT analysis). (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-37.3
Usual Care-4.7

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24 : Overall ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-27.4
Usual Care-2.8

[back to top]

Percent Change From Baseline in Apolipoprotein B (Apo-B) at Week 24: Overall ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-33.8
Usual Care-1.6

[back to top]

Absolute Change From Baseline in Fasting Plasma Glucose (FPG) at Week 12 and 24 : Overall ITT Analysis

Absolute change = FPG value at specified week minus FPG value at baseline. (NCT02642159)
Timeframe: Baseline, Week 12 and 24

,
Interventionmmol/L (Mean)
Change at Week 12Change at Week 24
Alirocumab 75 mg Q2W/Up to 150 mg Q2W0.450.68
Usual Care0.210.03

[back to top]

Absolute Change From Baseline in Hemoglobin A1c (HbA1c) at Week 12 and 24 : Overall ITT Analysis

Absolute change = HbA1c value at specified week minus HbA1c value at baseline. (NCT02642159)
Timeframe: Baseline, Week 12 and 24

,
Interventionmmol/mol (Mean)
Change at Week 12Change at Week 24
Alirocumab 75 mg Q2W/Up to 150 mg Q2W0.592.84
Usual Care0.432.40

[back to top]

Absolute Change From Baseline in Number of Glucose-Lowering Treatments at Week 12 and 24 : Overall ITT Analysis

Glucose lowering treatment was calculated for non-insulin treatments as one for each unique treatment received and for insulin treatment as one in total for all participants who have taken one or more treatments. Absolute change = number of glucose-lowering treatments at specified week minus baseline value. (NCT02642159)
Timeframe: Baseline, Week 12 and 24

,
InterventionGlucose lowering treatments (Mean)
Change at Week 12Change at Week 24
Alirocumab 75 mg Q2W/Up to 150 mg Q2W0.040.07
Usual Care0.040.04

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum

Adjusted means and standard errors at Week 24 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-15.4
Usual Care: Intent to Prescribe Fenofibrate-24.4

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 24: Overall ITT Analysis

Adjusted means and standard errors at Week 24 from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-13.0
Usual Care-8.8

[back to top]

Percent Change From Baseline in HDL-C at Week 24 : Overall ITT Analysis

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W14.5
Usual Care8.2

[back to top]

Percent Change From Baseline in HDL-C at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum

Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W13.5
Usual Care: Intent to Prescribe Fenofibrate12.3

[back to top]

Percent Change From Baseline in LDL-C Particle Number at Week 24: ITT- Intent to Prescribe Fenofibrate Stratum

LDL-C particle number was calculated from lipid subfractions by NMR spectroscopy. Adjusted LS means and standard errors at Week 24 from MMRM model including all available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-45.4
Usual Care: Intent to Prescribe Fenofibrate-2.9

[back to top]

Percent Change From Baseline in Measured LDL-C at Week 12: ITT- Intent to Prescribe Fenofibrate Stratum

Measured LDL-C values via beta quantification method. Adjusted LS means and standard errors at Week 12 from MMRM model including available post-baseline data from Week 8 to Week 24 regardless of status on- or off-treatment in the intent to prescribe fenofibrate stratum. The usual care here corresponds to fenofibrate. (NCT02642159)
Timeframe: From Baseline to Week 24

InterventionPercent change (Least Squares Mean)
Alirocumab 75 mg Q2W/Up to 150 mg Q2W-44.3
Usual Care: Intent to Prescribe Fenofibrate5.4

[back to top]

Percent Change From Baseline in Fasting Triglycerides (TG) at Week 24: ITT Analysis

Adjusted means and standard errors at Week 24 were obtained by using multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent change (Mean)
Ezetimibe 10 mg-14.409
Alirocumab 75 mg Q2W/up to 150 mg Q2W-14.462

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 12: ITT Analysis

Adjusted means and standard errors at Week 12 were obtained by using multiple imputation approach followed by a robust regression model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent change (Mean)
Ezetimibe 10 mg-13.585
Alirocumab 75 mg Q2W/up to 150 mg Q2W-9.965

[back to top]

Percent Change From Baseline in High Density Lipoprotein Cholesterol at Week 12: ITT Analysis

Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg6.1
Alirocumab 75 mg Q2W/up to 150 mg Q2W7.3

[back to top]

Percent Change From Baseline in High Density Lipoprotein Cholesterol at Week 24: ITT Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg6.5
Alirocumab 75 mg Q2W/up to 150 mg Q2W8.3

[back to top]

Percent Change From Baseline in Lipoprotein (a) (Lp[a]) at Week 24: ITT Analysis

Adjusted means and standard errors at Week 24 were obtained from multiple imputation approach followed by robust regression model for handling missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were included in the imputation model. (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent Change (Mean)
Ezetimibe 10 mg3.956
Alirocumab 75 mg Q2W/up to 150 mg Q2W-30.317

[back to top]

Percent Change From Baseline in Lipoprotein (a) at Week 12: ITT Analysis

Adjusted means and standard errors at Week 12 were obtained from multiple imputation approach followed by robust regression model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent Change (Mean)
Ezetimibe 10 mg6.313
Alirocumab 75 mg Q2W/up to 150 mg Q2W-30.064

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24: ITT Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent Change (Least Squares Mean)
Ezetimibe 10 mg-19.4
Alirocumab 75 mg Q2W/up to 150 mg Q2W-47.0

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol at Week 12: ITT Analysis

Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent Change (Least Squares Mean)
Ezetimibe 10 mg-20.7
Alirocumab 75 mg Q2W/up to 150 mg Q2W-47.4

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol at Week 24: On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including all available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first) (on-treatment analysis). (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent Change (Least Squares Mean)
Ezetimibe 10 mg-20.4
Alirocumab 75 mg Q2W/up to 150 mg Q2W-49.1

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24: ITT Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including all available post-baseline data from Week 4 up to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent Change (Least Squares Mean)
Ezetimibe 10 mg-13.8
Alirocumab 75 mg Q2W/up to 150 mg Q2W-33.9

[back to top]

Percent Change From Baseline in Total Cholesterol at Week 12: ITT Analysis

Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent Change (Least Squares Mean)
Ezetimibe 10 mg-14.9
Alirocumab 75 mg Q2W/up to 150 mg Q2W-34.2

[back to top]

Percentage of Participants Reaching Calculated Low Density Lipoprotein Cholesterol <70 mg/dL (1.81 mmol/L) at Week 24: ITT Analysis

Adjusted percentages at Week 24 were obtained from multiple imputation approach for handling of missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were included in the imputation model. (NCT02715726)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Ezetimibe 10 mg40.5
Alirocumab 75 mg Q2W/up to 150 mg Q2W85.1

[back to top]

Percentage of Participants Reaching Calculated Low Density Lipoprotein Cholesterol <70 mg/dL (1.81 mmol/L) at Week 24: On-Treatment Analysis

Adjusted percentages at Week 24 were obtained from multiple imputation approach including all available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first) (on-treatment analysis). (NCT02715726)
Timeframe: Up to Week 24

Interventionpercentage of participants (Number)
Ezetimibe 10 mg42.1
Alirocumab 75 mg Q2W/up to 150 mg Q2W87.0

[back to top]

Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol at Week 24: On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including all available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first) (on-treatment analysis). (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-21.3
Alirocumab 75 mg Q2W/up to 150 mg Q2W-58.7

[back to top]

Percent Change From Baseline in Apolipoprotein A-1 (Apo A-1) at Week 24: ITT Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-0.2
Alirocumab 75 mg Q2W/up to 150 mg Q2W3.2

[back to top]

Percent Change From Baseline in Apolipoprotein A-1 at Week 12 : ITT Analysis

Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg1.1
Alirocumab 75 mg Q2W/up to 150 mg Q2W3.7

[back to top]

Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 24: ITT Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent Change (Least Squares Mean)
Ezetimibe 10 mg-16.2
Alirocumab 75 mg Q2W/up to 150 mg Q2W-43.5

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 12: ITT Analysis

Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent Change (Least Squares Mean)
Ezetimibe 10 mg-16.5
Alirocumab 75 mg Q2W/up to 150 mg Q2W-43.0

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 24: On-Treatment Analysis

Adjusted LS means and standard errors at Week 24 were obtained from MMRM model including all available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first) (on-treatment analysis). (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent Change (Least Squares Mean)
Ezetimibe 10 mg-17.4
Alirocumab 75 mg Q2W/up to 150 mg Q2W-45.2

[back to top]

Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol at Week 12: ITT Analysis

Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including all available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment. (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-22.2
Alirocumab 75 mg Q2W/up to 150 mg Q2W-57.1

[back to top]

Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol at Week 12: On-Treatment Analysis

Adjusted LS means and standard errors at Week 12 were obtained from MMRM model including all available post-baseline on-treatment data from Week 4 to Week 24 (i.e. up to 21 days after last injection or 3 days after the last capsule, whichever came first) (on-treatment analysis). (NCT02715726)
Timeframe: From Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-22.7
Alirocumab 75 mg Q2W/up to 150 mg Q2W-58.1

[back to top]

Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol at Week 24: Intent-to-treat (ITT) Analysis

Adjusted least square (LS) means and standard errors at Week 24 were obtained from mixed models analysis with repeated measures (MMRM) to account for missing data. All available post-baseline data from Week 4 to Week 24 regardless of status on- or off-treatment were used in the model (ITT analysis). (NCT02715726)
Timeframe: From Baseline to Week 24

Interventionpercent change (Least Squares Mean)
Ezetimibe 10 mg-20.3
Alirocumab 75 mg Q2W/up to 150 mg Q2W-56.0

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) and/or Aspartate Aminotransferase (AST) ≥10 Times Upper Normal Limit (ULN)

Participants had ALT and AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT and/or AST that were 10x ULN or greater were recorded. The ALT and AST ULNs were 40 U/L. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top]

Percentage of Participants Who Experience Elevation in Alanine Aminotransferase (ALT) ≥5 Times Upper Normal Limit (ULN)

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had an assessments of ALT that was 5x ULN or greater were recorded. The ALT ULN was 40 U/L. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top]

Percentage of Participants Who Experience Elevation in Alanine Aminotransferase (ALT) ≥10 Times Upper Normal Limit (ULN)

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had an assessments of ALT that was 10x ULN or greater were recorded. The ALT ULN was 40 U/L. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in Aspartate Aminotransferase (AST) ≥3 Times Upper Normal Limit (ULN)

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of AST that were 3 x ULN or greater were recorded. The AST ULN was 40 U/L.. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top]

Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) and/or Aspartate Aminotransferase (AST) ≥3 Times Upper Normal Limit (ULN)

Participants had ALT and AST levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT and/or AST that were 3 x ULN or greater were recorded. The ALT and AST ULNs were 40 U/L. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg1.4
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top] [back to top]

Percentage of Participants Who Experience Consecutive Elevations in Alanine Aminotransferase (ALT) ≥3 Times Upper Normal Limit (ULN)

Participants had ALT levels assessed throughout the 12 week treatment period. Participants who had 2 consecutive assessments of ALT that were 3 x ULN or greater were recorded. The ALT ULN was 40 U/L. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg1.4
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top] [back to top]

Percentage Change From Baseline in Low-density Lipoprotein-cholesterol (LDL-C)

Participants had LDL-C levels assessed at baseline and after 12 weeks of study drug administration. The change from baseline was calculated. Results were reported as a M-estimate. (NCT02741245)
Timeframe: Baseline and Week 12

InterventionPercentage Change (Mean)
Ezetimibe 10 mg-18.7
Rosuvastatin 2.5 mg-39.8
Rosuvastatin 5.0 mg-47.2
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg-54.6
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg-60.5

[back to top]

Percentage of Participants Who Experience 1 or More Allergic Reaction or Rash AEs

Allergic Reaction or Rash AEs included Allergy to Arthropod Sting, Anaphylactoid Reaction, Anaphylactic Reaction, Anaphylatic Shock, Anaphylactoid Shock, Angioedema, Conjunctivitis Allergic, Contrast Media Reaction, Dermatitis, Dermatitis Allergic, Dermatitis Atopic, Dermatitis Bullous, Dermatitis Contact, Dermatitis Psoriasiform, Drug Hypersensitivity, Eczema, Eosinophila, Erythema, Eye Allergy, Face Oedema, Hypersensitivity, Mechanical Urticaria, Palmar Erythema, Periorbital Oedema, Photodermatosis, Photosensitivity Allergic reaction, Photosensitivity Reaction, Pigmentation Disorder, Pruritus, Pruritus Generalised, Rash, Rash Erythematous, Rash Follicular, Rash Generalised, Rash Maculo-Papular, Rash Papulosquamous, Rash Pruritic, Rash Pustular, Rash Vesicular, Rhinitis, Rhinitis Allergic, Rosacea, Skin Exfoliation, Skin Disorder, Skin Hyperpigmentation, Skin Lesion, Skin Mass, Skin Ulcer, Subcutaneous Nodule, Swelling Face, Systemic Lupus Erythematosus Rash, Urticaria. (NCT02741245)
Timeframe: up to 14 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg1.4
Rosuvastatin 5.0 mg4.2
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg2.8
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg2.8

[back to top]

Percentage of Participants With Potential Hy's Law Condition

Percentage of Participants with Potential Hy's Law Condition (defined as serum ALT or serum AST elevations >3xULN, with serum alkalinephosphatase <2xULN and total bilirubin (TBL) ≥2xULN) was summarized. The ALT and AST ULNs were 40 U/L. The ULN for alkaline phosphatase was 359 IU/L and the ULN for total bilirubin was 1.2 mg/dL. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top]

Percentage of Participants Who Had Study Drug Discontinued Due to Adverse Event

An AE was defined as any untoward medical occurrence in a subject which does not necessarily have a causal relationship with the treatment. An AE was any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, whether or not considered related to the medicinal product. The percentage of participants that had study drug discontinued due to an AE was summarized. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg2.8
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg1.4

[back to top] [back to top]

Percentage of Participants Who Experience Elevations in Creatine Kinase (CK) ≥10 Times ULN

Participants had creatine phosphokinase (CK) levels assessed throughout the 12 week treatment period. Participants who had any CK level that was ≥10 x ULN were recorded. The CK ULNs for males and females were 287 IU/L and 163 IU/L, respectively. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top] [back to top]

Percentage of Participants Who Experience Elevation in Aspartate Aminotransferase (AST) ≥10 Times Upper Normal Limit (ULN)

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had an assessments of AST that was 10x ULN or greater were recorded. The AST ULN was 40 U/L. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top]

Percentage of Participants Who Experience Elevation in Aspartate Aminotransferase (AST) ≥5 Times Upper Normal Limit (ULN)

Participants had AST levels assessed throughout the 12 week treatment period. Participants who had an assessments of AST that was 5x ULN or greater were recorded. The AST ULN was 40 U/L. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top]

Percentage of Participants Who Experience at Least 1 Adverse Event (AE)

An AE was defined as any untoward medical occurrence in a subject which does not necessarily have a causal relationship with the treatment. An AE was any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, whether or not considered related to the medicinal product. The percentage of participants that reported at least 1 AE was summarized (NCT02741245)
Timeframe: up to 14 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg31.4
Rosuvastatin 2.5 mg34.7
Rosuvastatin 5.0 mg42.3
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg40.8
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg37.5

[back to top]

Percentage of Participants Who Experience Elevations in Creatine Kinase (CK) ≥10 Times ULN With Muscle Symptoms

Participants had CK levels assessed throughout the 52 week treatment period. Participants who had any CK level that was ≥10 x ULN and had associated muscle symptoms present within +/- 7 days were recorded. The CK ULNs for males and females were 287 IU/L and 163 IU/L, respectively. (NCT02741245)
Timeframe: up to 12 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg0.0
Rosuvastatin 2.5 mg0.0
Rosuvastatin 5.0 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 2.5 mg0.0
Ezetimibe 10 mg+ Rosuvastatin 5.0 mg0.0

[back to top]

Percentage of Participants Who Had Study Drug Discontinued Due to an AE

An AE was any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, regardless of whether or not it was considered related to the medicinal product. The percentage of participants who had study drug discontinued due to an AE was summarized. (NCT02748057)
Timeframe: up to 52 weeks

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg + Rosuvastatin 2.5 mg0.9
Ezetimibe 10 mg + Rosuvastatin 5.0 mg0.0

[back to top]

Percentage Change From Baseline in Low-Density Lipoprotein-Cholesterol (LDL-C)

Blood was collected at baseline (predose) and after 52 weeks of treatment to determine LDL-C levels. LDL-C was calculated using the Friedewald equation. If triglycerides (TG) exceeded 400 mg/dL (4.6 mmol/L), LDL-C was determined by beta quantification ultracentrifugation. The percentage change from baseline at Week 52 was summarized. (NCT02748057)
Timeframe: Baseline (predose) and Week 52

InterventionPercentage change (Mean)
Ezetimibe 10 mg + Rosuvastatin 2.5 mg-33.8
Ezetimibe 10 mg + Rosuvastatin 5.0 mg-23.9

[back to top]

Percentage of Participants Who Experience at Least 1 Adverse Event (AE)

An AE was any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, regardless of whether or not it was considered related to the medicinal product. The percentage of participants who reported at least 1 AE was summarized. (NCT02748057)
Timeframe: Up to 2 weeks post last dose of study drug (up to 54 weeks)

InterventionPercentage of Participants (Number)
Ezetimibe 10 mg + Rosuvastatin 2.5 mg72.8
Ezetimibe 10 mg + Rosuvastatin 5.0 mg76.2

[back to top]

Percent Change From Baseline in Fasting Triglyceride at Week 8

Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. The robust regression models included the fixed categorical effect of alirocumab dose/dose regimen. A two-step multiple imputation procedure was used to address missing values in the mITT population (in the two steps respectively; with number of imputations = 1000). In the first step, the monotone missing pattern was induced in the multiply-imputed data. In the second step, the missing data at subsequent visits were imputed using the regression method for continuous variables. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionpercent change (Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-0.4
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-4.0
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-7.4
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg14.5
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg19.3
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg-3.1
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-32.1
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-7.1

[back to top]

Absolute Change From Baseline in Total Cholesterol (Total-C) at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionmg/dL (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-80.1
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-20.8
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-57.1
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-84.4
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-27.2
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg5.3
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-60.7
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-105.1

[back to top]

Percent Change From Baseline in Apolipoprotein (Apo) B at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline value and post-baseline values in at least one of the analysis windows used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionpercent change (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-38.4
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-9.7
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-36.4
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-40.1
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-12.6
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg-0.9
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-27.2
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-51.4

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionpercent change (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-29.0
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-4.1
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-28.6
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-34.2
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-10.7
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg5.2
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-24.0
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-41.8

[back to top]

Percent Change From Baseline in Apolipoprotein A-1 at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionpercent change (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg4.4
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg14.8
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg10.7
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg1.8
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg8.9
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg7.4
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg5.8
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg7.2

[back to top]

Percentage of Participants Achieving Calculated Low Density Lipoprotein Cholesterol (LDL-C) <130 mg/dL (3.37 mmol/L) at Week 8

Combined estimate for percentage of participants was obtained by averaging out all the imputed percentage of participants reaching the level of interest. A two-step multiple imputation procedure was used to address missing values in the mITT population in the two steps respectively; with number of imputations = 1000. In the first step, the monotone missing pattern was induced in the multiply-imputed data. In the second step, the missing data at subsequent visits were imputed using the regression method for continuous variables. (NCT02890992)
Timeframe: At Week 8

Interventionpercentage of participants (Number)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg100.0
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg33.3
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg97.6
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg83.0
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg33.3
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg20.0
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg66.7
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg80.0

[back to top]

Percent Change From Baseline in Calculated LDL-C at Week 12: Cohort 4

Adjusted LS means and standard error at Week 12 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. (NCT02890992)
Timeframe: Baseline, Week 12

Interventionpercent change (Least Squares Mean)
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-29.7
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-49.2

[back to top]

Percent Change From Baseline in Calculated Low Density Lipoprotein Cholesterol (LDL-C) at Week 8

Percent change in calculated LDL-C was defined as 100*(calculated LDL-C value at Week 8 - calculated LDL-C value at baseline)/calculated LDL-C value at baseline. All available baseline and post-baseline calculated LDL-C value during the OLDFI efficacy treatment period & within one of the analysis windows up to Week 8 were used in the model. OLDFI efficacy treatment period was defined as the period from first investigational medicinal product (IMP) injection to last OLDFI IMP injection + 21 days(for Cohorts 1 & 2) or +35 days (for Cohorts 3 & 4). Adjusted Least-squares (LS) mean & standard error (SE) at Week 8 were obtained from mixed-effect model with repeated measures (MMRM) analysis, with fixed categorical effects of alirocumab dose/dose regimen (30 mg Q2W [<50 kg], 40 mg Q2W [<50 kg], 50 mg Q2W [>=50 kg], 75 mg Q2W [>=50 kg], 75 mg Q4W [<50 kg],150 mg Q4W [>=50 kg], 150 mg Q4W [<50 kg] and 300 mg Q4W ([>=50 kg] dose), time point & dose/dose regimen-by-time point interaction. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionpercent change (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-41.1
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-7.9
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-40.6
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-49.8
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-17.5
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg4.0
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-31.9
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-59.8

[back to top]

Percentage of Participants Achieving Calculated LDL-C <110 mg/dL (2.84 mmol/L) at Week 8

Combined estimate for percentage of participants was obtained by averaging out all the imputed percentage of participants reaching the level of interest. A two-step multiple imputation procedure was used to address missing values in the mITT population in the two steps respectively; with number of imputations = 1000. In the first step, the monotone missing pattern was induced in the multiply-imputed data. In the second step, the missing data at subsequent visits were imputed using the regression method for continuous variables. (NCT02890992)
Timeframe: At Week 8

Interventionpercentage of participants (Number)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg0.0
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg0.0
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg93.4
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg65.7
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg16.7
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg20.0
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg66.7
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg80.0

[back to top]

Absolute Change From Baseline in Apolipoprotein A-1 at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionmg/dL (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg4.0
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg17.7
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg11.3
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-0.4
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg10.5
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg8.0
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg7.5
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg11.0

[back to top]

Absolute Change From Baseline in Apolipoprotein B at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionmg/dL (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-51.7
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-18.5
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-35.3
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-53.4
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-15.3
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg-5.4
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-34.2
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-63.5

[back to top]

Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionpercent change (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg9.7
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg16.5
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg14.7
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg10.6
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg5.2
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg13.8
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg4.5
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg2.8

[back to top]

Absolute Change From Baseline in Fasting Triglyceride at Week 8

Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. The robust regression models included the fixed categorical effect of alirocumab dose/dose regimen. A two-step multiple imputation procedure was used to address missing values in the mITT population (in the two steps respectively; with number of imputations = 1000). In the first step, the monotone missing pattern was induced in the multiply-imputed data. In the second step, the missing data at subsequent visits were imputed using the regression method for continuous variables. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionmmol/L (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-0.121
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-0.076
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg0.168
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg0.111
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg0.117
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg-0.045
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-0.402
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-0.107

[back to top]

Absolute Change From Baseline in HDL-C at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionmg/dL (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg5.9
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg7.7
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg5.5
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg4.9
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg2.4
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg5.9
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg2.2
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg1.2

[back to top]

Absolute Change From Baseline in Lipoprotein(a) at Week 8

Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. The robust regression models included the fixed categorical effect of alirocumab dose/dose regimen. A two-step multiple imputation procedure was used to address missing values in the mITT population (in the two steps respectively; with number of imputations = 1000). In the first step, the monotone missing pattern was induced in the multiply-imputed data. In the second step, the missing data at subsequent visits were imputed using the regression method for continuous variables. (NCT02890992)
Timeframe: Baseline, Week 8

Interventiongram/Liter (g/L) (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg0.003
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-0.021
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg0.007
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-0.025
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg0.023
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg-0.031
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-0.002
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-0.120

[back to top]

Absolute Change From Baseline in Calculated Low Density Lipoprotein Cholesterol (LDL-C) at Week 8

Absolute change in LDL-C was calculated by subtracting baseline value from Week 8 value. Adjusted LS means and SE were obtained using MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionmilligram per deciliter (mg/dL) (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-83.7
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-27.6
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-55.5
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-88.3
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-32.4
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg0.1
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-55.9
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-104.3

[back to top]

Absolute Change From Baseline in Ratio Apolipoprotein B/Apolipoprotein A-1 at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionratio (Apo B/Apo A-1) (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-0.363
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-0.262
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-0.370
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-0.402
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-0.190
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg-0.086
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-0.282
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-0.473

[back to top]

Percent Change From Baseline in Lipoprotein(a) at Week 8

Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. The robust regression models included the fixed categorical effect of alirocumab dose/dose regimen. A two-step multiple imputation procedure was used to address missing values in the mITT population in the two steps respectively (with number of imputations = 1000). In the first step, the monotone missing pattern was induced in the multiply-imputed data. In the second step, the missing data at subsequent visits were imputed using the regression method for continuous variables. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionpercent change (Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg4.5
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-26.9
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg1.5
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-25.2
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg2.2
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg-7.7
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg0.1
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-7.7

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein (HDL-C) at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baselines value and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionpercent change (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-39.6
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-7.1
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-39.7
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-43.9
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-14.4
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg3.2
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-31.5
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-54.6

[back to top]

Absolute Change From Baseline in Non-High-Density Lipoprotein (Non-HDL-C) at Week 8

Adjusted LS means and SE at Week 8 were obtained from MMRM analysis, with fixed categorical effects of alirocumab dose/dose regimen, time point and dose/dose regimen-by-time point interaction. All available baseline values and post-baseline values in at least one of the analysis windows up to Week 8 were used in the model. (NCT02890992)
Timeframe: Baseline, Week 8

Interventionmg/dL (Least Squares Mean)
Cohort 1 - Alirocumab 30 mg Q2W: <50 kg-86.1
Cohort 1 - Alirocumab 50 mg Q2W: >=50 kg-28.7
Cohort 2 - Alirocumab 40 mg Q2W: <50 kg-62.7
Cohort 2 - Alirocumab 75 mg Q2W: >=50 kg-88.5
Cohort 3 - Alirocumab 75 mg Q4W: <50 kg-29.5
Cohort 3 - Alirocumab 150 mg Q4W: >=50 kg-0.6
Cohort 4 - Alirocumab 150 mg Q4W: <50 kg-63.1
Cohort 4 - Alirocumab 300 mg Q4W: >=50 kg-106.4

[back to top]

Change in Alanine Aminotransferase (ALT)

Participants will have their ALT levels measured in units per liter (U/L) at baseline and 8 weeks. ALT ranges from 0 to infinity with higher levels of ALT indicating hepatocyte death. The change in ALT levels will be compared among the three intervention groups (i.e., placebo or control cohort, those assigned to 20mg ezetimibe per day, and 40mg ezetimibe per day). (NCT02971033)
Timeframe: 8 weeks

Interventionunits per Liter (Mean)
Placebo-75
20mg/Day Ezetimibe-73

[back to top]

Change in Viral Load

Participants will have their HCV-RNA measured in international unit per milliliter at baseline and 8 weeks. HCV RNA international unit per milliliter ranges from 0 to infinity, with higher levels indicating HCV positivity. The change in international unit per milliliter will be compared among the three intervention groups (i.e., placebo or control cohort, those assigned to 20mg ezetimibe per day, and 40mg ezetimibe per day). Change is calculated based on 8 weeks minus baseline (0 weeks). (NCT02971033)
Timeframe: 0 weeks, 8 weeks

Interventioninternational units per milliliter (Mean)
Placebo-4030000
20mg/Day Ezetimibe-5860000

[back to top]

Second Phase Slope

HCV declines in a biphasic manner under HCV treatment. Here we are measuring the slope (i.e., rate) at which HCV is declining during the second slower phase of viral decline. (NCT02971033)
Timeframe: 3 days through 4 weeks

Interventionlog(copies/mL)/day (Mean)
Placebo.90
20mg/Day Ezetimibe.98

[back to top]

Absolute Change From Baseline in Non-High-density Lipoprotein Cholesterol (Non-HDL-C) at Week 36

Adjusted LS mean and SE at Week 36 were obtained from mixed-effect model including all available post-baseline data from Week 4 to Week 36. Model included treatment arm (SoC arm, alirocumab arm), randomization strata (statin at ACS onset [Yes / No]), time point, treatment-by-time point and randomization strata-by-time point interaction as fixed categorical effects, and baseline calculated non-HDL-C value and baseline calculated non-HDL-C value-by-time point interaction as continuous fixed covariates. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmg/dL (Least Squares Mean)
Standard of Care-20.3
Alirocumab-69.2

[back to top]

Absolute Change From Baseline in Lumen Volume at Week 36

Adjusted mean and SE at Week 36 were obtained from robust regression model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and the baseline lumen volume value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmm^3 (Mean)
Standard of Care-1.25
Alirocumab-0.93

[back to top]

Absolute Change From Baseline in Lipoprotein (a) (Lp[a]) at Week 36

Adjusted mean and SE at Week 36 were obtained from robust regression model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effect, and baseline Lp(a) value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmg/dL (Mean)
Standard of Care-10.3
Alirocumab-15.5

[back to top]

Absolute Change From Baseline in High-density Lipoprotein Cholesterol at Week 36

Adjusted LS mean and SE at Week 36 were obtained from mixed-effect model including all available post-baseline data from Week 4 to Week 36. Model included treatment arm (SoC arm, alirocumab arm), randomization strata (statin at ACS onset [Yes / No]), time point, treatment-by-time point and randomization strata-by-time point interaction as fixed categorical effects, and baseline HDL-C value and baseline HDL-C value-by-time point interaction as continuous fixed covariates. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmg/dL (Least Squares Mean)
Standard of Care4.7
Alirocumab8.1

[back to top]

Absolute Change From Baseline in Fasting Triglycerides (TGs) at Week 36

Adjusted mean and SE were obtained from multiple imputation approach followed by robust regression model including fixed categorical effect of treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) and the continuous fixed covariate of baseline fasting TGs value. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmg/dL (Mean)
Standard of Care-26.2
Alirocumab-35.3

[back to top]

Absolute Change From Baseline in External Elastic Membrane (EEM) Volume at Week 36

Adjusted mean and SE at Week 36 were obtained from robust regression model with treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]), as fixed categorical effects, and the baseline EEM volume value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmm^3 (Mean)
Standard of Care-8.23
Alirocumab-10.01

[back to top]

Absolute Change From Baseline in Apolipoprotein B (Apo B) at Week 36

Adjusted LS mean and SE at Week 36 were obtained from ANCOVA model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and baseline Apo B value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmg/dL (Least Squares Mean)
Standard of Care-16.8
Alirocumab-51.0

[back to top]

Absolute Change From Baseline in Apolipoprotein A-1 (Apo A-1) at Week 36

Adjusted LS mean and SE at Week 36 were obtained from ANCOVA model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and baseline Apo A-1 value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmg/dL (Least Squares Mean)
Standard of Care3.8
Alirocumab12.0

[back to top]

Number of Participants With Cardiovascular (CV) Adverse Events

The suspected or confirmed CV events that occurred from randomization until end of the study visit were collected and reported. The various CV events included CV death, myocardial infarction, ischemic stroke, unstable angina requiring hospitalization , congestive heart failure requiring hospitalization, congestive heart failure requiring hospitalization, ischemia-driven coronary revascularization procedure. (NCT02984982)
Timeframe: Up to 36 weeks

,
InterventionParticipants (Count of Participants)
Cardiovascular deathMyocardial infarctionIschemic strokeUnstable angina requiring hospitalizationCongestive heart failure requiring hospitalizationIschemia led coronary revascularization procedure
Alirocumab022004
Standard of Care030002

[back to top]

Percent Change From Baseline in Normalized Total Atheroma Volume (TAV) at Week 36

Least-squares (LS) means and standard errors (SE) at Week 36 were obtained from analysis of covariance (ANCOVA) model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and the baseline normalized TAV as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Least Squares Mean)
Standard of Care-3.14
Alirocumab-4.79

[back to top]

Percent Change From Baseline in Calculated Low-density Lipoprotein Cholesterol at Week 12 and Week 36

Adjusted LS mean and SE at Week 12 and Week 36 were obtained from mixed-effect model including all available post-baseline data from Week 4 to Week 36. Model included treatment arm (SoC arm, alirocumab arm), randomization strata (statin at ACS onset [Yes / No]), time point, treatment-by-time point and randomization strata-by-time point interaction as fixed categorical effects, and baseline calculated LDL-C value and baseline calculated LDL-C value-by-time point interaction as continuous fixed covariates. (NCT02984982)
Timeframe: Baseline, Week 12, Week 36

,
Interventionpercent change (Least Squares Mean)
Week 12Week 36
Alirocumab-64.53-63.94
Standard of Care-7.57-13.40

[back to top]

Absolute Change From Baseline in Calculated Low-density Lipoprotein Cholesterol at Week 12 and Week 36

Adjusted LS mean and SE at Week 12 and Week 36 were obtained from mixed-effect model including all available post-baseline data from Week 4 to Week 36. Model included treatment arm (SoC arm, alirocumab arm), randomization strata (statin at ACS onset [Yes / No]), time point, treatment-by-time point and randomization strata-by-time point interaction as fixed categorical effects, and baseline calculated LDL-C value and baseline calculated LDL-C value-by-time point interaction as continuous fixed covariates. (NCT02984982)
Timeframe: Baseline, Week 12, Week 36

,
Interventionmg/dL (Least Squares Mean)
Week 12Week 36
Alirocumab-62.4-63.2
Standard of Care-9.6-15.5

[back to top]

Percent Change From Baseline in Total Cholesterol at Week 36

Adjusted LS mean and SE at Week 36 were obtained from mixed-effect model including all available post-baseline data from Week 4 to Week 36. Model included treatment arm (SoC arm, alirocumab arm), randomization strata (statin at ACS onset [Yes / No]), time point, treatment-by-time point and randomization strata-by-time point interaction as fixed categorical effects, and baseline TC value and baseline TC value-by-time point interaction as continuous fixed covariates. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Least Squares Mean)
Standard of Care-7.59
Alirocumab-35.43

[back to top]

Percent Change From Baseline in Non-High-density Lipoprotein Cholesterol at Week 36

Adjusted LS mean and SE at Week 36 were obtained from mixed-effect model including all available post-baseline data from Week 4 to Week 36. Model included treatment arm (SoC arm, alirocumab arm), randomization strata (statin at ACS onset [Yes / No]), time point, treatment-by-time point and randomization strata-by-time point interaction as fixed categorical effects, and baseline calculated non-HDL-C value and baseline calculated non-HDL-C value-by-time point interaction as continuous fixed covariates. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Least Squares Mean)
Standard of Care-14.06
Alirocumab-54.50

[back to top]

Percent Change From Baseline in Lumen Volume at Week 36

Adjusted mean and SE at Week 36 were obtained from robust regression model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effect, and the baseline lumen volume value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Mean)
Standard of Care1.20
Alirocumab-0.86

[back to top]

Percent Change From Baseline in Lipoprotein (a) at Week 36

Adjusted mean and SE at Week 36 were obtained from robust regression model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effect, and baseline Lp(a) value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Mean)
Standard of Care-17.23
Alirocumab-55.76

[back to top]

Percent Change From Baseline in High-density Lipoprotein Cholesterol at Week 36

Adjusted LS mean and SE at Week 36 were obtained from mixed-effect model including all available post-baseline data from Week 4 to Week 36. Model included treatment arm (SoC arm, alirocumab arm), randomization strata (statin at ACS onset [Yes / No]), time point, treatment-by-time point and randomization strata-by-time point interaction as fixed categorical effects, and baseline HDL-C value and baseline HDL-C value-by-time point interaction as continuous fixed covariates. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Least Squares Mean)
Standard of Care12.19
Alirocumab21.04

[back to top]

Percent Change From Baseline in Fasting Triglycerides at Week 36

Adjusted mean and SE were obtained by multiple imputation approach followed by robust regression model included fixed categorical effect of treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) and the continuous fixed covariate of baseline fasting TGs value. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Mean)
Standard of Care-8.85
Alirocumab-18.37

[back to top]

Percent Change From Baseline in External Elastic Membrane Volume at Week 36

Adjusted mean and SE at Week 36 were obtained from robust regression model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and the baseline EEM volume value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Mean)
Standard of Care-0.86
Alirocumab-3.18

[back to top]

Percent Change From Baseline in Apolipoprotein B at Week 36

Adjusted LS mean and SE at Week 36 were obtained from ANCOVA model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and baseline Apo B value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Least Squares Mean)
Standard of Care-16.61
Alirocumab-55.13

[back to top]

Percent Change From Baseline in Apolipoprotein A-1 at Week 36

Adjusted LS mean and SE at Week 36 were obtained from ANCOVA model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and baseline Apo A-1 value as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent change (Least Squares Mean)
Standard of Care4.61
Alirocumab11.75

[back to top]

Absolute Change From Baseline in Total Cholesterol (TC) at Week 36

LS mean and SE at Week 36 were obtained from mixed-effect model including all available post-baseline data from Week 4 to Week 36. Model included treatment arm (SoC arm, alirocumab arm), randomization strata (statin at ACS onset [Yes / No]), time point, treatment-by-time point and randomization strata-by-time point interaction as fixed categorical effects, and baseline calculated TC value and baseline calculated TC value-by-time point interaction as continuous fixed covariates. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionmg/dL (Least Squares Mean)
Standard of Care-15.2
Alirocumab-61.7

[back to top]

Absolute Change From Baseline in Percent Atheroma Volume (PAV) at Week 36

LS mean and SE at Week 36 were obtained from ANCOVA model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and the baseline PAV as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventionpercent atheroma volume (Least Squares Mean)
Standard of Care-1.28
Alirocumab-1.42

[back to top]

Absolute Change From Baseline in Normalized Total Atheroma Volume at Week 36

LS mean and SE at Week 36 were obtained from ANCOVA model including treatment arm (SoC arm, alirocumab arm) and randomization strata (statin at ACS onset [Yes / No]) as fixed categorical effects, and the baseline normalized TAV as continuous fixed covariate. (NCT02984982)
Timeframe: Baseline, Week 36

Interventioncubic millimeter (mm^3) (Least Squares Mean)
Standard of Care-4.73
Alirocumab-5.77

[back to top]

Percent Change From Baseline to Weeks 4 and 8 in TGs

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analysed for TGs. Baseline was defined as the mean of the TGs values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: [(TGs value at Week 4 or 8 minus Baseline value) divided by (Baseline Value)] multiplied by 100. Percent change from Baseline in TGs was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. (NCT03001076)
Timeframe: Week 4 and Week 8

,
InterventionPercent change (Least Squares Mean)
Week 4Week 8
Bempedoic Acid5.207.60
Placebo6.007.68

[back to top]

Percent Change From Baseline to Weeks 4 and 8 in Non-HDL-C

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for Non-HDL-C. Baseline was defined as the mean of the Non-HDL-C values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: [(Non-HDL-C value at Week 4 or 8 minus Baseline value) divided by (Baseline Value)] multiplied by 100. Percent change from Baseline in non-HDL-C was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. (NCT03001076)
Timeframe: Week 4 and Week 8

,
InterventionPercent change (Least Squares Mean)
Week 4Week 8
Bempedoic Acid-22.17-20.04
Placebo3.083.71

[back to top]

Percent Change From Baseline to Weeks 4 and 8 in TC

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for TC. Baseline was defined as the mean of the TC values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: [(TC value at Week 4 or 8 minus Baseline value) divided by (Baseline Value)] multiplied by 100. Percent change from Baseline in TC was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. (NCT03001076)
Timeframe: Week 4 and Week 8

,
InterventionPercent change (Least Squares Mean)
Week 4Week 8
Bempedoic Acid-18.33-16.63
Placebo2.081.82

[back to top]

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

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for LDL-C. Baseline was defined as the mean of the LDL-C values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: ([LDL-C value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. Bempedoic Acid = BA. Percent change from Baseline in LDL-C was analyzed using an analysis of covariance (ANCOVA) model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. In the ANCOVA model, missing LDL-C data at Week 12 were imputed using multiple imputation method taking into account adherence to treatment. (NCT03001076)
Timeframe: Week 12

Interventionpercent change (Least Squares Mean)
Placebo4.99
Bempedoic Acid-23.46

[back to top]

Percent Change From Baseline to Week 12 in Non-high-density Lipoprotein Cholesterol (Non-HDL-C)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analysed for non-HDL-C. Baseline was defined as the mean of the non-HDL-C values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: ([non-HDL-C value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. Percent change from Baseline in non-HDL-C was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. In the ANCOVA model, missing non-HDL-C data at Week 12 were imputed using multiple imputation method taking into account adherence to treatment. (NCT03001076)
Timeframe: Week 12

Interventionpercent change (Least Squares Mean)
Placebo5.19
Bempedoic Acid-18.38

[back to top]

Percent Change From Baseline to Week 12 in Total Cholesterol (TC)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analysed for TC. Baseline was defined as the mean of the TC values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: ([TC value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. Percent change from Baseline in TC was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. In the ANCOVA model, missing TC data at Week 12 were imputed using multiple imputation method taking into account adherence to treatment. (NCT03001076)
Timeframe: Week 12

InterventionPercent change (Least Squares Mean)
Placebo2.88
Bempedoic Acid-15.11

[back to top]

Percent Change From Baseline to Week 12 in Triglycerides (TGs)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for TGs. Baseline was defined as the mean of the TGs values from the last two non-missing values on or prior to D 1. Percent change from baseline was calculated as: [(TGs value at Week 12 minus Baseline value) divided by (Baseline Value)] multiplied by 100. Percent change from Baseline in TGs was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. (NCT03001076)
Timeframe: Week 12

InterventionPercent change (Least Squares Mean)
Placebo9.23
Bempedoic Acid4.70

[back to top]

Absolute Change From Baseline to Weeks 4, 8, and 12 in LDL-C

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analysed for LDL-C. Baseline was defined as the mean of the LDL-C values from the last two non-missing values on or prior to Day 1. Absolute change from baseline was calculated as: LDL-C value at Week 4, 8, or 12 minus Baseline value. (NCT03001076)
Timeframe: Week 4, Week 8 and Week 12

,
Interventionmilligrams per deciliter (mg/dL) (Geometric Mean)
Change from Baseline at Week 4Change from Baseline at Week 8Change from Baseline at Week 12
Bempedoic Acid-37.4-34.5-32.9
Placebo3.63.95.3

[back to top]

Number of Participants With Treatment-emergent Adverse Events (TEAEs)

TEAEs, defined as an adverse events (AEs) that began or worsened in severity after the first dose of double-blind study drug and prior to the last dose of double-blind study drug + 30 days, were collected and reported. (NCT03001076)
Timeframe: Up to approximately 16 weeks

,
InterventionParticipants (Number)
TEAEsNon-serious TEAEsSerious TEAEsDeaths
Bempedoic Acid884650
Placebo391830

[back to top]

Percent Change From Baseline to Weeks 4 and 8 in HDL-C

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analysed for HDL-C. Baseline was defined as the mean of the HDL-C values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: [(HDL-C value at Week 4 or 8 minus Baseline value) divided by (Baseline Value)] multiplied by 100. Percent change from Baseline in HDL-C was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. (NCT03001076)
Timeframe: Week 4 and Week 8

,
InterventionPercent change (Least Squares Mean)
Week 4Week 8
Bempedoic Acid-7.73-7.75
Placebo0.85-1.33

[back to top]

Percent Change From Baseline to Weeks 4 and 8 in LDL-C

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for LDL-C. Baseline was defined as the mean of the LDL-C values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: [(LDL-C value at Week 4 or 8 minus Baseline value) divided by (Baseline Value)] multiplied by 100. Percent change from Baseline in LDL-C was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. (NCT03001076)
Timeframe: Week 4 and Week 8

,
InterventionPercent change (Least Squares Mean)
Week 4Week 8
Bempedoic Acid-28.04-25.51
Placebo3.053.61

[back to top]

Percent Change From Baseline to Week 12 in High-sensitivity C-reactive Protein (hsCRP)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analysed for hsCRP. Baseline was defined as the last non-missing value on or prior to Day 1. Percent change from baseline was calculated as: [(hsCRP value at Week 12 minus Baseline value) divided by (Baseline Value)] multiplied by 100. (NCT03001076)
Timeframe: Week 12

InterventionPercent change (Median)
Placebo2.088
Bempedoic Acid-32.521

[back to top]

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

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for HDL-C. Baseline was defined as the mean of the HDL-C values from the last two non-missing values on or prior to Day 1. Percent change from baseline was calculated as: [(HDL-C value at Week 12 minus Baseline value) divided by (Baseline Value)] multiplied by 100. Percent change from Baseline in HDL-C was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. (NCT03001076)
Timeframe: Week 12

Interventionpercent change (Least Squares Mean)
Placebo-1.38
Bempedoic Acid-7.27

[back to top]

Percent Change From Baseline to Week 12 in Apolipoprotein B (apoB)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analysed for apoB. Baseline was defined as the last non-missing value on or prior to Day 1. Percent change from baseline was calculated as: [(apoB value at Week 12 minus Baseline value) divided by (Baseline Value)] multiplied by 100. Percent change from Baseline in apoB was analyzed using an ANCOVA model with percent change from Baseline as the dependent variable, treatment as a fixed effects and Baseline as a covariate. In the ANCOVA model, missing apoB data at Week 12 were imputed using multiple imputation method taking into account adherence to treatment. (NCT03001076)
Timeframe: Week 12

InterventionPercent change (Least Squares Mean)
Placebo4.74
Bempedoic Acid-14.58

[back to top]

Percent Change From Baseline in Lipid Profile Parameters at Week 6

Percent change from Baseline is calculated as the ([post-Baseline value minus the Baseline value] divided by the Baseline value ) x 100. Baseline is defined as the mean of the values from Week -1 (Screening Visit 2) and predose Day 1/Week 0 (Treatment Visit 1). Baseline apolipoprotein B (apoB) was measured only at predose/Day 1. Percent change from Baseline was analyzed using analysis of covariance (ANCOVA) with treatment group as a factor and Baseline value as a covariate. Missing values were imputed using LOCF, with only post-Baseline values carried forward. non-HDL-C, non-high-density lipoprotein cholesterol; TC, total cholesterol; TG, triglycerides; HDL-C, high-density lipoprotein cholesterol. (NCT03051100)
Timeframe: Baseline; Week 6

,
Interventionpercent change (Least Squares Mean)
non-HDL-CTCapoBTGHDL-C
Placebo-1.3-1.10.68.90.4
Triplet Therapy-60.0-47.1-53.5-27.4-1.1

[back to top]

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C) at Week 6

Percent change from Baseline is calculated as the ([post-Baseline value minus the Baseline value] divided by the Baseline value ) x 100. Baseline is defined as the mean of the values from Week -1 (Screening Visit 2) and predose Day 1/Week 0 (Treatment Visit 1). Percent change from Baseline in LDL-C was analyzed using analysis of covariance (ANCOVA) with treatment group as a factor and Baseline value as a covariate. Missing LDL-C values were imputed using last observation carried forward (LOCF), with only post-Baseline values carried forward. If LDL-C was measured (i.e., if TG was >400 mg/dL or LDL-C was <50 mg/dL), the measured values were used in the analysis. (NCT03051100)
Timeframe: Baseline; Week 6

Interventionpercent change (Least Squares Mean)
Placebo-3.1
Triplet Therapy-63.6

[back to top]

Percent Change From Baseline in High-sensitivity C-reactive Protein (Hs-CRP) at Week 6

Percent change is calculated as the ([post-Baseline value minus the Baseline value] divided by the Baseline value ) x 100. Baseline is defined as the predose Day 1/Week 0 (Treatment Visit 1) value. If only one value is available either at Week -1 (Screening Visit 2) or Week 0 (Treatment Visit 1), then that value is used as Baseline. Missing values were imputed using LOCF, with only post-Baseline values carried forward. (NCT03051100)
Timeframe: Baseline; Week 6

Interventionpercent change (Median)
Placebo-2.7
Triplet Therapy-47.7

[back to top]

Number of Participants With LDL-C Reduction ≥50% From Baseline at Week 6

If LDL-C was measured (i.e., if TG was >400 mg/dL or LDL-C was <50 mg/dL), the measured values were used in the analysis. (NCT03051100)
Timeframe: Baseline; Week 6

InterventionParticipants (Count of Participants)
Placebo0
Triplet Therapy39

[back to top]

Number of Participants With LDL-C <70 mg/dL at Week 6

Analysis was based on LOCF values. If LDL-C was measured (i.e., if TG was >400 mg/dL or LDL-C was <50 mg/dL), the measured values were used in the analysis. (NCT03051100)
Timeframe: Week 6

InterventionParticipants (Count of Participants)
Placebo0
Triplet Therapy37

[back to top]

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

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for HDL-C. Baseline was defined as the mean of the HDL-C values from Week -2 and predose Day 1/Week 0. Percent change from baseline was calculated as: ([HDL-C value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. (NCT03337308)
Timeframe: Baseline; Week 12

InterventionPercent change (Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-5.59
Bempedoic Acid 180 mg-5.40
Ezetimibe 10 mg-2.11
Placebo-0.54

[back to top]

Percent Change From Baseline to Week 12 in Apolipoprotein B (Apo B)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for apo B. Baseline was defined as the predose Day 1/Week 0 value. Percent change from baseline in apo B was analyzed using ANCOVA with treatment group and randomization stratification as a factors and baseline apo B as a covariate. Percent change from baseline was calculated as: ([apo B value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. (NCT03337308)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-24.6
Bempedoic Acid 180 mg-11.8
Ezetimibe 10 mg-15.3
Placebo5.5

[back to top]

Percent Change From Baseline to Week 12 in High-sensitivity C-reactive Protein (hsCRP)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for hsCRP. Baseline was defined as the predose Day 1/Week 0 value. Percent change from baseline in hsCRP was analyzed using a non-parametric analysis. Percent change from baseline was calculated as: ([hsCRP value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. (NCT03337308)
Timeframe: Baseline; Week 12

InterventionPercent Change (Median)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-35.1
Bempedoic Acid 180 mg-31.9
Ezetimibe 10 mg-8.2
Placebo21.6

[back to top]

Percent Change From Baseline to Week 12 in Low-density Lipoprotein Cholesterol (LDL-C)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for LDL-C. Baseline was defined as the mean of the LDL-C values from Week -2 and predose Day 1/Week 0. Percent change from baseline in LDL-C was analyzed using analysis of covariance (ANCOVA) with treatment group and randomization stratification as a factors and baseline LDL-C as a covariate. Percent change from baseline was calculated as: ([LDL-C value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. For LDL-C, if measured LDL-C value was available, measured LDL-C was used. (NCT03337308)
Timeframe: Baseline; Week 12

InterventionPercent Change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-36.2
Bempedoic Acid 180 mg-17.2
Ezetimibe 10 mg-23.2
Placebo1.8

[back to top]

Percent Change From Baseline to Week 12 in Triglycerides (TGs)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for TGs. Baseline was defined as the mean of the TGs values from Week -2 and predose Day 1/Week 0. Percent change from baseline was calculated as: ([TGs value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. (NCT03337308)
Timeframe: Baseline; Week 12

InterventionPercent change (Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-7.90
Bempedoic Acid 180 mg7.94
Ezetimibe 10 mg-2.46
Placebo5.47

[back to top]

Percent Change From Baseline to Week 12 in Total Cholesterol (TC)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for TC. Baseline was defined as the mean of the TC values from Week -2 and predose Day 1/Week 0. Percent change from baseline in TC was analyzed using ANCOVA with treatment group and randomization stratification as a factors and baseline TC as a covariate. Percent change from baseline was calculated as: ([TC value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. (NCT03337308)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-26.4
Bempedoic Acid 180 mg-12.1
Ezetimibe 10 mg-16.0
Placebo0.7

[back to top]

Percent Change From Baseline to Week 12 in Non-high-density Lipoprotein Cholesterol (Non-HDL-C)

Blood samples were drawn after a minimum 10-hour fast (water was allowed) at pre-specified intervals. Samples were collected and analyzed for non-HDL-C. Baseline was defined as the mean of the non-HDL-C values from Week -2 and predose Day 1/Week 0. Percent change from baseline in non-HDL-C was analyzed using ANCOVA with treatment group and randomization stratification as a factors and baseline non-HDL-C as a covariate. Percent change from baseline was calculated as: ([non-HDL-C value at Week 12 minus Baseline value] divided by [Baseline Value]) multiplied by 100. (NCT03337308)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-31.9
Bempedoic Acid 180 mg-14.1
Ezetimibe 10 mg-19.9
Placebo1.8

[back to top]

Percent Change From Baseline in Apolipoprotein (Apo) B at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted LS means and standard errors were obtained from the MMRM model to account for missing data using all available post-baseline data from Week 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionpercent change (Least Squares Mean)
Week 12Week 24Week 48
Alirocumab-4.2-11.80.9

[back to top]

Percent Change From Baseline in Fasting Triglycerides (TG) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted means and standard errors were obtained from a multiple imputation approach followed by a robust regression model including all available post-baseline data from Week 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionpercent change (Mean)
Week 12Week 24Week 48
Alirocumab2.85.210.0

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol at Week 12: On-treatment Analysis

Adjusted LS means and standard errors were obtained from the MMRM model to account for missing data using all available post-baseline on-treatment data from Week 4 to Week 48 (on-treatment Analysis). (NCT03510715)
Timeframe: Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Alirocumab-4.1

[back to top]

Percent Change From Baseline in High Density Lipoprotein Cholesterol (HDL-C) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted LS means and standard errors were obtained from the MMRM model to account for missing data using all available post-baseline data from Weeks 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionpercent change (Least Squares Mean)
Week 12Week 24Week 48
Alirocumab13.08.910.1

[back to top]

Percent Change From Baseline in Lipoprotein a (Lp) (a) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted means and standard errors were obtained from a multiple imputation approach followed by a robust regression model including all available post-baseline data from Week 4 to Week 48 regardless of status on-or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionpercent change (Mean)
Week 12Week 24Week 48
Alirocumab7.4-5.2-6.4

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol at Weeks 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted LS means and standard errors were obtained from the MMRM model to account for missing data using all available post-baseline data from Week 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 24 and 48

Interventionpercent change (Least Squares Mean)
Week 24Week 48
Alirocumab-10.14.2

[back to top]

Absolute Change From Baseline in LDL-C Level at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted LS means and standard errors were obtained from the MMRM model to account for missing data using all available post-baseline data from Week 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionmg/dL (Least Squares Mean)
Week 12Week 24Week 48
Alirocumab-33.4-43.0-15.0

[back to top]

Number of Participants With Tanner Staging at Baseline, Weeks 12, 24 and 48

Tanner stage defines physical measurements of development in children and adolescent based on external primary and secondary sex characteristics. Participants were evaluated for pubic hair distribution, breast development (only females) and genital development (only males), and classified in 3 categories as: Prepubescent (defined as a person just before start of the development of adult sexual characteristics), Pubescent (defined as a person at or approaching the age of puberty), Postpubescent (sexually mature or a person who has completed puberty). (NCT03510715)
Timeframe: Baseline, Weeks 12, 24 and 48

,
InterventionParticipants (Count of Participants)
Baseline: PrepubescentBaseline: PubescentBaseline: Post-pubescentWeek 12: PrepubescentWeek 12: PubescentWeek 12: Post-pubescentWeek 24: PrepubescentWeek 24: PubescentWeek 24: Post-pubescentWeek 48: PrepubescentWeek 48: PubescentWeek 48: Post-pubescent
Alirocumab 150 mg Q2W090081081072
Alirocumab 75 mg Q2W/up to 150 mg Q2W360360260170

[back to top]

Percent Change From Baseline in Apolipoprotein A1 (Apo A1) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted LS means and standard errors were obtained from the MMRM model to account for missing data using all available post-baseline data from Week 4 to 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionpercent change (Least Squares Mean)
Week 12Week 24Week 48
Alirocumab11.314.611.3

[back to top]

Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C) at Week 12: Intent-to-Treat (ITT) Analysis

Adjusted least square (LS) means and standard errors were obtained from the mixed model analysis with repeated measures (MMRM) to account for missing data using all available post-baseline data from Week 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). (NCT03510715)
Timeframe: Baseline to Week 12

Interventionpercent change (Least Squares Mean)
Alirocumab-4.1

[back to top]

Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Weeks 12, 24 and 48 - ITT Analysis/On-treatment Analysis

Adjusted LS means and standard errors were obtained from the MMRM model to account for missing data using all available post-baseline data from Week 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionpercent change (Least Squares Mean)
Week 12Week 24Week 48
Alirocumab-3.9-9.25.7

[back to top]

Percent Change From Baseline in Total Cholesterol (Total-C) at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted LS means and standard errors were obtained from the MMRM model to account for missing data using all available post-baseline data from Weeks 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionpercent change (Least Squares Mean)
Week 12Week 24Week 48
Alirocumab-1.9-6.35.5

[back to top]

Percentage of Participants Reporting >=15 Percent (%) Reduction in LDL-C Level at Weeks 12, 24 and 48: ITT Analysis/On-treatment Analysis

Adjusted Percentage were obtained from a multiple imputation approach for handling of missing data including all available post-baseline data from Week 4 to Week 48 regardless of status on- or off-treatment used in the model (ITT analysis). Although separate analyses of all available data (ITT analysis) and only data collected within a defined time window (On-treatment analysis) were planned, if all values used in the ITT approach were within the on-treatment time window, the on-treatment analysis would be identical to the ITT analysis, thus the results would be identical and a single outcome measure presenting the results for both types of analysis would be provided. (NCT03510715)
Timeframe: Baseline to Weeks 12, 24 and 48

Interventionpercentage of participants (Number)
Week 12Week 24Week 48
Alirocumab50.050.039.0

[back to top]

DB Period: Percentage of Participants Who Achieved Low Density Lipoprotein Cholesterol Level <130 mg/dL (3.37 mmol/L) at Week 12: ITT Estimand

Adjusted percentages at Week 12 were obtained from multiple imputation approach for handling of missing data. All available post-baseline data up to Week 12 were included in the imputation model. (NCT03510884)
Timeframe: At Week 12

Interventionpercentage of participants (Number)
DB Period: Placebo Q2W16.4
DB Period: Alirocumab Q2W70.6
DB Period: Placebo Q4W12.9
DB Period: Alirocumab Q4W72.6

[back to top]

DB Period: Percentage of Participants Achieving Low Density Lipoprotein Cholesterol <110 mg/dL (2.84 mmol/L) at Week 24: ITT Estimand

Adjusted percentages at Week 24 were obtained from multiple imputation approach for handling of missing data. All available post-baseline data up to Week 24 were included in the imputation model. (NCT03510884)
Timeframe: At Week 24

Interventionpercentage of participants (Number)
DB Period: Placebo Q2W4.0
DB Period: Alirocumab Q2W57.2
DB Period: Placebo Q4W9.0
DB Period: Alirocumab Q4W67.2

[back to top]

DB Period: Percentage of Participants Achieving Low Density Lipoprotein Cholesterol <110 mg/dL (2.84 mmol/L) at Week 12: ITT Estimand

Adjusted percentages at Week 12 were obtained from multiple imputation approach for handling of missing data for Q4W. All available post-baseline data up to Week 12 were included in the imputation model. For Q2W, adjusted percentages at Week 12 were obtained from last observation carried forward approach (LOCF) to handle missing on-treatment LDL-C values as well as missing post-treatment LDL-C values in participants who discontinued treatment due to the coronavirus disease-2019 pandemic. Other post-treatment missing values were considered as failure. (NCT03510884)
Timeframe: At Week 12

Interventionpercentage of participants (Number)
DB Period: Placebo Q2W0.0
DB Period: Alirocumab Q2W61.2
DB Period: Placebo Q4W4.3
DB Period: Alirocumab Q4W57.0

[back to top]

DB Period: Percent Change From Baseline in Total Cholesterol at Week 12: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model including all available post-baseline data. All post-baseline data available up to Week 12 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 12

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W7.5
DB Period: Alirocumab Q2W-25.3
DB Period: Placebo Q4W0.9
DB Period: Alirocumab Q4W-27.0

[back to top]

DB Period: Percent Change From Baseline in Total Cholesterol (Total-C) at Week 24: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model including all available post-baseline data. All post-baseline data available up to Week 24 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 24

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W7.4
DB Period: Alirocumab Q2W-23.4
DB Period: Placebo Q4W-4.4
DB Period: Alirocumab Q4W-27.7

[back to top]

DB Period: Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol at Week 12: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model including all available post-baseline data. All post-baseline data available up to Week 12 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 12

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W9.8
DB Period: Alirocumab Q2W-33.0
DB Period: Placebo Q4W2.8
DB Period: Alirocumab Q4W-34.7

[back to top]

DB Period: Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol (Non-HDL-C) at Week 24: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model including all available post-baseline data. All post-baseline data available up to Week 24 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 24

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W9.7
DB Period: Alirocumab Q2W-31.0
DB Period: Placebo Q4W-3.7
DB Period: Alirocumab Q4W-35.6

[back to top]

DB Period: Percent Change From Baseline in Low Density Lipoprotein Cholesterol at Week 12: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model including all available post-baseline data. All post-baseline data available up to Week 12 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 12

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W10.7
DB Period: Alirocumab Q2W-34.8
DB Period: Placebo Q4W2.3
DB Period: Alirocumab Q4W-39.2

[back to top]

DB Period: Percent Change From Baseline in Low Density Lipoprotein Cholesterol (LDL-C) at Week 24: Intent-to-treat (ITT) Estimand

Adjusted least square (LS) means and standard errors (SE) were obtained from mixed-effect model with repeated measures (MMRM) model. All post-baseline data available up to Week 24 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 24

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W9.7
DB Period: Alirocumab Q2W-33.6
DB Period: Placebo Q4W-4.4
DB Period: Alirocumab Q4W-38.2

[back to top]

DB Period: Percent Change From Baseline in Lipoprotein (a) at Week 24: ITT Estimand

Adjusted means and standard errors were obtained from a multiple imputation approach followed by a robust regression model including all available post-baseline data up to Week 24. Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. (NCT03510884)
Timeframe: Baseline, Week 24

Interventionpercent change (Mean)
DB Period: Placebo Q2W0.5
DB Period: Alirocumab Q2W-14.7
DB Period: Placebo Q4W2.5
DB Period: Alirocumab Q4W-22.4

[back to top]

DB Period: Percent Change From Baseline in Lipoprotein (a) at Week 12: ITT Estimand

Adjusted means and standard errors were obtained from a multiple imputation approach followed by a robust regression model including all available post-baseline data up to Week 12. Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. (NCT03510884)
Timeframe: Baseline, Week 12

Interventionpercent change (Mean)
DB Period: Placebo Q2W-7.1
DB Period: Alirocumab Q2W-12.7
DB Period: Placebo Q4W-2.5
DB Period: Alirocumab Q4W-16.0

[back to top]

DB Period: Percent Change From Baseline in High-Density Lipoprotein Cholesterol at Week 12: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline data available up to Week 12 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 12

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W-2.2
DB Period: Alirocumab Q2W3.5
DB Period: Placebo Q4W-3.5
DB Period: Alirocumab Q4W4.0

[back to top]

DB Period: Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) at Week 24: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline data available up to Week 24 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 24

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W-0.8
DB Period: Alirocumab Q2W5.6
DB Period: Placebo Q4W-1.1
DB Period: Alirocumab Q4W3.4

[back to top]

DB Period: Percent Change From Baseline in Fasting Triglycerides (TG) at Week 24: ITT Estimand

Adjusted means and standard errors were obtained from a multiple imputation approach followed by a robust regression model including all available post-baseline data up to Week 24. Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. (NCT03510884)
Timeframe: Baseline, Week 24

Interventionpercent change (Mean)
DB Period: Placebo Q2W7.7
DB Period: Alirocumab Q2W11.9
DB Period: Placebo Q4W12.2
DB Period: Alirocumab Q4W-6.8

[back to top]

DB Period: Percentage of Participants Who Achieved Low Density Lipoprotein Cholesterol Level Lower Than (<) 130 mg/dL (3.37 mmol/L) at Week 24: ITT Estimand

Adjusted percentages at Week 24 were obtained from multiple imputation approach for handling of missing data. All available post-baseline data up to Week 24 were included in the imputation model. (NCT03510884)
Timeframe: At Week 24

Interventionpercentage of participants (Number)
DB Period: Placebo Q2W8.0
DB Period: Alirocumab Q2W73.3
DB Period: Placebo Q4W22.2
DB Period: Alirocumab Q4W76.3

[back to top]

DB Period: Percent Change From Baseline in Fasting Triglycerides (TG) at Week 12: ITT Estimand

Adjusted means and standard errors were obtained from a multiple imputation approach followed by a robust regression model including all available post-baseline data up to Week 12. Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. (NCT03510884)
Timeframe: Baseline, Week 12

Interventionpercent change (Mean)
DB Period: Placebo Q2W6.5
DB Period: Alirocumab Q2W-2.2
DB Period: Placebo Q4W7.8
Db Period: Alirocumab Q4W-0.3

[back to top]

DB Period: Percent Change From Baseline in Apolipoprotein B at Week 12: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model including all available post-baseline data. All post-baseline data available up to Week 12 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 12

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W8.9
DB Period: Alirocumab Q2W-30.0
DB Period: Placebo Q4W1.1
DB Period: Alirocumab Q4W-31.7

[back to top]

DB Period: Percent Change From Baseline in Apolipoprotein B (Apo B) at Week 24: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model including all available post-baseline data. All post-baseline data available up to Week 24 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 24

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W10.4
DB Period: Alirocumab Q2W-27.4
DB Period: Placebo Q4W-3.6
DB Period: Alirocumab Q4W-34.3

[back to top]

DB Period: Percent Change From Baseline in Apolipoprotein A1 at Week 12: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline data available up to Week 12 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 12

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W-0.1
DB Period: Alirocumab Q2W-1.7
DB Period: Placebo Q4W-0.7
DB Period: Alirocumab Q4W5.0

[back to top]

DB Period: Percent Change From Baseline in Apolipoprotein A1 (Apo A1) at Week 24: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline data available up to Week 24 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Week 24

Interventionpercent change (Least Squares Mean)
DB Period: Placebo Q2W-0.1
DB Period: Alirocumab Q2W1.0
DB Period: Placebo Q4W-4.5
DB Period: Alirocumab Q4W4.4

[back to top]

DB Period: Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) at Weeks 12 and 24: On-treatment Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline on-treatment data available up to Week 12 and Week 24 were used for the MMRM model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for who stopped IMP before switch to Q2W regimen, + 21 day otherwise. MMRM model was run on participants with a Baseline value and at one on-treatment post-baseline value for a timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Weeks 12, and 24

,,,
Interventionpercent change (Least Squares Mean)
Week 12Week 24
DB Period: Alirocumab Q2W3.55.6
DB Period: Alirocumab Q4W4.03.4
DB Period: Placebo Q2W-2.2-0.8
DB Period: Placebo Q4W-3.5-1.1

[back to top]

Number of Participants With Tanner Staging at Baseline and Weeks 24, 68 and 104

Tanner stage defines physical measurements of development in children and adolescent based on external primary and secondary sex characteristics. Participants were evaluated for pubic hair distribution, breast development (only females) and genital development (only males) and classified in 3 categories as: Prepubescent (defined as a person just before start of the development of adult sexual characteristics), Pubescent (defined as a person at or approaching the age of puberty), Postpubescent (sexually mature or a person who has completed puberty). (NCT03510884)
Timeframe: Baseline, Weeks 24, 68 and 104

,,,
InterventionParticipants (Count of Participants)
Baseline: Boys - PrepubescentBaseline: Boys - PubescentBaseline: Boys - PostpubescentBaseline: Girls - PrepubescentBaseline: Girls - PubescentBaseline: Girls - PostpubescentWeek 24: Boys - PrepubescentWeek 24: Boys - PubescentWeek 24: Boys - PostpubescentWeek 24: Girls - PrepubescentWeek 24: Girls - PubescentWeek 24: Girls - PostpubescentWeek 68: Boys - PrepubescentWeek 68: Boys - PubescentWeek 68: Boys - PostpubescentWeek 68: Girls - PrepubescentWeek 68: Girls - PubescentWeek 68: Girls - PostpubescentWeek 104: Boys - PrepubescentWeek 104: Boys - PubescentWeek 104: Boys - PostpubescentWeek 104: Girls - PrepubescentWeek 104: Girls - PubescentWeek 104: Girls - Postpubescent
Alirocumab Q2W41324161031134159196314918601011
Alirocumab Q4W01447131401252169096116908711711
Placebo/Alirocumab Q2W11331610134152074061067042
Placebo/Alirocumab Q4W543186173165153155152155

[back to top]

DB Period: Percentage of Participants Who Achieved Low Density Lipoprotein Cholesterol < 130 mg/dL (3.37 mmol/L) at Weeks 12 and 24: On-treatment Estimand

Adjusted percentages at Weeks 12 and 24 were obtained from multiple imputation approach for handling of missing data followed by logistic regression model. All available post-baseline on-treatment data up to Week 12 and Week 24 were included in the imputation model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for those who stopped IMP before switch to Q2W regimen, + 21 days otherwise. (NCT03510884)
Timeframe: Weeks 12 and 24

,,,
Interventionpercentage of participants (Number)
Week 12Week 24
DB Period: Alirocumab Q2W70.673.3
DB Period: Alirocumab Q4W72.676.3
DB Period: Placebo Q2W16.48.0
Db Period: Placebo Q4W12.922.2

[back to top]

DB Period: Percentage of Participants Who Achieved Low Density Lipoprotein Cholesterol < 110 mg/dL (2.84 mmol/L) at Weeks 12 and 24: On-treatment Estimand

Adjusted percentages at Weeks 12 and 24 were obtained from multiple imputation approach for handling of missing data followed by logistic regression model. All available post-baseline on-treatment data up to Week 12 and Week 24 were included in the imputation model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for those who stopped IMP before switch to Q2W regimen, + 21 days otherwise. (NCT03510884)
Timeframe: Weeks 12 and 24

,,,
Interventionpercentage of participants (Number)
Week 12Week 24
DB Period: Alirocumab Q2W61.757.2
DB Period: Alirocumab Q4W57.067.2
DB Period: Placebo Q2W0.14.0
DB Period: Placebo Q4W4.39.0

[back to top]

DB Period: Percentage of Participants Who Achieved at Least 50% Reduction in Low Density Lipoprotein Cholesterol Level From Baseline at Weeks 12 and 24: On-treatment Estimand

Adjusted percentages at Weeks 12 and 24 were obtained from multiple imputation approach for handling of missing data followed by logistic regression model. All available post-baseline on-treatment data up to Week 12 and Week 24 were included in the imputation model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for those who stopped IMP before switch to Q2W regimen, + 21 days otherwise. (NCT03510884)
Timeframe: At Weeks 12 and 24

,,,
Interventionpercentage of participants (Number)
Week 12Week 24
DB Period: Alirocumab Q2W25.221.6
DB Period: Alirocumab Q4W31.932.4
DB Period: Placebo Q2W0.00.0
DB Period: Placebo Q4W0.19.1

[back to top]

DB Period: Percentage of Participants Who Achieved at Least 50% Reduction in Low Density Lipoprotein Cholesterol Level From Baseline at Weeks 12 and 24: ITT Estimand

Adjusted percentages at Weeks 12 and 24 were obtained from multiple imputation approach for handling of missing data followed by logistic regression model. All available post-baseline on-treatment data up to Week 12 and Week 24 were included in the imputation model. (NCT03510884)
Timeframe: At Weeks 12 and 24

,,,
Interventionpercentage of participants (Number)
Week 12Week 24
DB Period: Alirocumab Q2W25.221.6
DB Period: Alirocumab Q4W31.932.4
DB Period: Placebo Q2W0.00.0
DB Period: Placebo Q4W0.19.1

[back to top]

DB Period: Percentage of Participants Who Achieved at Least 30 Percent (%) Reduction in Low Density Lipoprotein Cholesterol Level From Baseline at Weeks 12 and 24: ITT Estimand

Adjusted percentages at Weeks 12 and 24 were obtained from multiple imputation approach for handling of missing data followed by logistic regression model. All available post-baseline on-treatment data up to Week 12 and Week 24 were included in the imputation model. (NCT03510884)
Timeframe: At Weeks 12 and 24

,,,
Interventionpercentage of participants (Number)
Week12Week 24
DB Period: Alirocumab Q2W65.866.7
DB Period: Alirocumab Q4W70.872.5
DB Period: Placebo Q2W0.84.0
DB Period: Placebo Q4W4.218.5

[back to top]

DB Period: Percentage of Participants Achieved at Least 30% Reduction in Low Density Lipoprotein Cholesterol Level From Baseline at Weeks 12 and 24: On-treatment Estimand

Adjusted percentages at Weeks 12 and 24 were obtained from multiple imputation approach for handling of missing data followed by logistic regression model. All available post-baseline on-treatment data up to Week 12 and Week 24 were included in the imputation model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for those who stopped IMP before switch to Q2W regimen, + 21 days otherwise. (NCT03510884)
Timeframe: At Weeks 12 and 24

,,,
Interventionpercentage of participants (Number)
Week 12Week 24
DB Period: Alirocumab Q2W65.866.7
DB Period: Alirocumab Q4W70.872.5
DB Period: Placebo Q2W0.84.0
DB Period: Placebo Q4W4.218.5

[back to top]

DB Period: Percent Change in Low Density Lipoprotein Cholesterol From Baseline to Weeks 8, 12 and 24: On-treatment Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline on-treatment data available up to Week 8, Week 12 and Week 24 were used for the MMRM model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for who stopped IMP before switch to Q2W regimen, + 21 days otherwise. (NCT03510884)
Timeframe: Baseline to Weeks 8, 12 and 24

,,,
Interventionpercent change (Least Squares Mean)
Week 8Week 12Week 24
DB Period: Alirocumab Q2W-35.4-34.8-33.6
DB Period: Alirocumab Q4W-42.0-39.2-38.2
DB Period: Placebo Q2W7.110.79.7
DB Period: Placebo Q4W-3.82.3-4.4

[back to top]

DB Period: Percent Change in Low Density Lipoprotein Cholesterol From Baseline to Weeks 8, 12 and 24: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline data available up to Week 8, Week 12 and Week 24 were used and missing data were accounted for by the MMRM model. (NCT03510884)
Timeframe: Baseline to Weeks 8, 12 and 24

,,,
Interventionpercent change (Least Squares Mean)
Week 8Week 12Week 24
DB Period: Alirocumab Q2W-35.4-34.8-33.6
DB Period: Alirocumab Q4W-42.0-39.2-38.2
DB Period: Placebo Q2W7.110.79.7
DB Period: Placebo Q4W-3.82.3-4.4

[back to top]

DB Period: Percent Change From Baseline in Total Cholesterol at Weeks 12 and 24: On-treatment Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline on-treatment data available up to Week 12 and Week 24 were used for the MMRM model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for who stopped IMP before switch to Q2W regimen, + 21 days otherwise. MMRM model was run on participants with a Baseline value and at one on-treatment post-baseline value for a timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Weeks 12 and 24

,,,
Interventionpercent change (Least Squares Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-25.3-23.4
DB Period: Alirocumab Q4W-27.0-27.7
DB Period: Placebo Q2W7.57.4
DB Period: Placebo Q4W0.9-4.4

[back to top]

DB Period: Percent Change From Baseline in Non-High Density Lipoprotein Cholesterol at Weeks 12 and 24: On-treatment Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline on-treatment data available up to Week 12 and Week 24 were used for the MMRM model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for who stopped IMP before switch to Q2W regimen, + 21 days otherwise. MMRM model was run on participants with a Baseline value and at one on-treatment post-baseline value for a timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Weeks 12 and 24

,,,
Interventionpercent change (Least Squares Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-33.0-31.0
Db Period: Alirocumab Q4W-34.7-35.6
DB Period: Placebo Q2W9.89.7
DB Period: Placebo Q4W2.8-3.7

[back to top]

DB Period: Percent Change From Baseline in Low Density Lipoprotein Cholesterol at Weeks 12, and 24: On-treatment Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline on-treatment data available up to Week 12 and Week 24 were used for the MMRM model, i.e., for Q2W data: from 1st investigational medicinal product (IMP) injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for who stopped IMP before switch to Q2W regimen, + 21 days otherwise. MMRM model was run on participants with a Baseline value and at one on-treatment post-baseline value for a timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Weeks 12, and 24

,,,
Interventionpercent change (Least Squares Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-34.8-33.6
DB Period: Alirocumab Q4W-39.2-38.2
DB Period: Placebo Q2W10.79.7
DB Period: Placebo Q4W2.3-4.4

[back to top]

DB Period: Percent Change From Baseline in Lipoprotein (a) at Weeks 12 and 24: On-treatment Estimand

Adjusted means and standard errors were obtained from a multiple imputation approach followed by a robust regression model including all available post-baseline on-treatment data up to Week 12 and Week 24, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for those who stopped IMP before switch to Q2W regimen, + 21 days otherwise. Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. (NCT03510884)
Timeframe: Baseline, Weeks 12 and 24

,,,
Interventionpercent change (Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-12.746-14.748
DB Period: Alirocumab Q4W-16.042-22.418
DB Period: Placebo Q2W-7.0990.492
DB Period: Placebo Q4W-2.5452.468

[back to top]

DB Period: Percent Change From Baseline in Fasting Triglycerides at Weeks 12 and 24: On-treatment Estimand

Adjusted means and standard errors were obtained from a multiple imputation approach followed by a robust regression model including all available post-baseline on-treatment data up to Week 12 and Week 24, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for those who stopped IMP before switch to Q2W regimen, + 21 days otherwise. Combined estimates and SE were obtained by combining adjusted means and SE from robust regression model analyses of the different imputed data sets. (NCT03510884)
Timeframe: Baseline, Weeks 12, and 24

,,,
Interventionpercent change (Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-2.211.9
DB Period: Alirocumab Q4W-0.3-6.8
DB Period: Placebo Q2W6.57.7
DB Period: Placebo Q4W7.812.2

[back to top]

DB Period: Percent Change From Baseline in Apolipoprotein B at Weeks 12 and 24: On-treatment Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline on-treatment data available up to Week 12 and Week 24 were used for the MMRM model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for who stopped IMP before switch to Q2W regimen, + 21 days otherwise. MMRM model was run on participants with a Baseline value and at one on-treatment post-baseline value for a timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Weeks 12 and 24

,,,
Interventionpercent change (Least Squares Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-30.0-27.4
DB Period: Alirocumab Q4W-31.7-34.3
DB Period: Placebo Q2W8.910.4
DB Period: Placebo Q4W1.1-3.6

[back to top]

DB Period: Percent Change From Baseline in Apolipoprotein A1 at Weeks 12 and 24: On-treatment Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline on-treatment data available up to Week 12 and Week 24 were used for the MMRM mode, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for who stopped IMP before switch to Q2W regimen, + 21 days otherwise. MMRM model was run on participants with a Baseline value and at one on-treatment post-baseline value for a timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Weeks 12 and 24

,,,
Interventionpercent change (Least Squares Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-1.71.0
DB Period: Alirocumab Q4W5.04.4
DB Period: Placebo Q2W-0.1-0.1
DB Period: Placebo Q4W-0.7-4.5

[back to top]

DB Period: Number of Participants With Treatment-Emergent (TE) Positive Anti-Alirocumab Antibodies (ADA) Response

Anti-drug (alirocumab) antibodies samples were analyzed using a validated non-quantitative, titer-based bridging immunoassay. Number of participants with positive ADA during 24-week treatment period is reported. Treatment-emergent positive ADA response was defined as 1) participants with no ADA positive response at baseline but with any positive response in the post-baseline period or 2) participants with a positive ADA response at baseline and at least a 4- fold increase in titer in the post-baseline period. A persistent positive response was defined as a TE ADA positive response detected in at least 2 consecutive post-baseline samples separated by at least a 12-week period. Persistent positive response was only analyzed for participants with positive TE ADA response. (NCT03510884)
Timeframe: Up to 24 weeks

InterventionParticipants (Count of Participants)
TE ADA positive responsePersistent positive response
DB Period: Alirocumab Q2W30

[back to top]

DB Period: Number of Participants With Treatment-Emergent (TE) Positive Anti-Alirocumab Antibodies (ADA) Response

Anti-drug (alirocumab) antibodies samples were analyzed using a validated non-quantitative, titer-based bridging immunoassay. Number of participants with positive ADA during 24-week treatment period is reported. Treatment-emergent positive ADA response was defined as 1) participants with no ADA positive response at baseline but with any positive response in the post-baseline period or 2) participants with a positive ADA response at baseline and at least a 4- fold increase in titer in the post-baseline period. A persistent positive response was defined as a TE ADA positive response detected in at least 2 consecutive post-baseline samples separated by at least a 12-week period. Persistent positive response was only analyzed for participants with positive TE ADA response. (NCT03510884)
Timeframe: Up to 24 weeks

,,
InterventionParticipants (Count of Participants)
TE ADA positive response
DB Period: Alirocumab Q4W0
DB Period: Placebo Q2W0
DB Period: Placebo Q4W0

[back to top]

DB Period: Absolute Change From Baseline in Apo B/Apo A-1 Ratio at Weeks 12 and 24: On-treatment Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline on-treatment data available up to Week 12 and Week 24 were used for the MMRM model, i.e., for Q2W data: from 1st IMP injection up to last IMP injection + 21 days and for Q4W data: from 1st IMP injection up to last IMP injection + 35 days for who stopped IMP before switch to Q2W regimen, + 21 days otherwise. MMRM model was run on participants with a Baseline value and at one on-treatment post-baseline value for a timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Weeks 12, and 24

,,,
Interventionratio (Apo B/Apo A-1) (Least Squares Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-0.2-0.2
DB Period: Alirocumab Q4W-0.3-0.3
DB Period: Placebo Q2W0.10.1
DB Period: Placebo Q4W0.00.0

[back to top]

DB Period: Absolute Change From Baseline in Apo B/Apo A-1 Ratio at Weeks 12 and 24: ITT Estimand

Adjusted LS means and SE were obtained from MMRM model. All post-baseline data available up to Week 12 and Week 24 were used and missing data were accounted for by the MMRM model. MMRM model was run on participants with a Baseline value and a post-baseline value for at least one timepoint used in the model. (NCT03510884)
Timeframe: Baseline, Weeks 12, and 24

,,,
Interventionratio (Apo B/Apo A-1) (Least Squares Mean)
Week 12Week 24
DB Period: Alirocumab Q2W-0.2-0.2
DB Period: Alirocumab Q4W-0.3-0.3
DB Period: Placebo Q2W0.10.1
DB Period: Placebo Q4W0.00.0

[back to top]

Change From Baseline in Cogstate Battery Test - Overall Composite Score at Weeks 24, 68 and 104

Cogstate battery test (cognitive testing system) consisted of detection test (DET), identification test (IDN), one card learning test (OCL) and Groton maze learning test (GML) to assess processing speed, attention, visual learning and executive functioning, respectively. For each test, Z-scores were computed based on participant's age at Baseline and Weeks 24, 68 and 104. Composite score: calculated as mean of Z-scores equally weighted, provided that at least 3 of 4 tests were available and if all of these domains were covered as: attention, through either DET or IDN, visual learning, through OCL and executive function, through GML. There is not minimum/maximum since values were reported as z-score but z-score of 0 means result equals to mean with negative numbers indicating values lower than mean and positive values higher. Positive change in z-score = an improvement in cognition, i.e., a better outcome; and negative change in z-score = worsening in cognition, i.e., a worse outcome. (NCT03510884)
Timeframe: Baseline, Weeks 24, 68 and 104

,,,
InterventionZ-score (Mean)
Week 24Week 68Week 104
Alirocumab Q2W-0.313-0.334-0.439
Alirocumab Q4W-0.136-0.263-0.638
Placebo/Alirocumab Q2W-0.403-0.421-0.601
Placebo/Alirocumab Q4W-0.218-0.272-0.393

[back to top]

OL Period: Percent Change in Low Density Lipoprotein Cholesterol From Baseline to Week 104: On-treatment Estimand

Percent Change in LDL-C from Baseline to Week 104 was reported in this outcome measure. (NCT03510884)
Timeframe: Baseline, Week 104

Interventionpercent change (Least Squares Mean)
OL Period: Placebo/Alirocumab Q2W-22.8
OL Period: Alirocumab Q2W-25.8
OL Period: Placebo/Alirocumab Q4W-27.6
OL Period: Alirocumab Q4W-23.4

[back to top]

OL Period: Percent Change in Low Density Lipoprotein Cholesterol From Baseline to Week 104: ITT Estimand

Percent Change in LDL-C from Baseline to Week 104 was reported in this outcome measure. (NCT03510884)
Timeframe: Baseline, Week 104

Interventionpercent change (Least Squares Mean)
OL Period: Placebo/Alirocumab Q2W-23.3
OL Period: Alirocumab Q2W-22.2
OL Period: Placebo/Alirocumab Q4W-27.1
OL Period: Alirocumab Q4W-23.7

[back to top]

Percent Change From Baseline to Week 12 in Homeostatic Model Assessment of Insulin Resistance (HOMA-IR) Index

The HOMA-IR index was calculated from the fasting glucose and insulin values that were obtained at each clinic visit (Day 1/Visit T1, Week 4/Visit T2, and Week 12/Visit T3) during the double-blind treatment period, using the formula: (fasting glucose [millimoles per milliliter {mmol/ml}] x fasting insulin [micro International Units per milliliter {μIU/ml}]) divided by 22.5. Percent change from Baseline for HOMA-IR index was analyzed using ANCOVA, with treatment as factor and Baseline HOMA-IR index as a covariate. Baseline was defined as the last value prior to the first dose of study drug (on or before T1). Percent change from Baseline for HOMA-IR index was calculated as: ([HOMA-IR index value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC3.0
Ezetimibe 10 mg2.5
Placebo18.9

[back to top]

Percent Change From Baseline to Week 12 in High-sensitivity C-reactive Protein (hsCRP)

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for hsCRP. Baseline was defined as the last value prior to the first dose of investigational medicinal product (IMP). Percent change from Baseline for hsCRP was analyzed using a non-parametric approach. Percent change from Baseline was calculated as: ([hsCRP value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For hsCRP, if a measured hsCRP value was available, measured hsCRP was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Median)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-25.347
Ezetimibe 10 mg2.078
Placebo14.085

[back to top]

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

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for HDL-C. Baseline was defined as the average of HDL-C values at Visit S3 and Visit T1 (last 2 non-missing values on or prior to Day 1). If only 1 value was available, the single value was used as Baseline. Percent change from Baseline for HDL-C was analyzed using ANCOVA, with treatment as factor and Baseline lipid parameter as a covariate. Missing data for HDL-C was imputed using the LOCF method. Percent change from Baseline was calculated as: ([HDL-C value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For HDL-C, if a measured HDL-C value was available, measured HDL-C was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-5.1
Ezetimibe 10 mg2.1
Placebo0.8

[back to top]

Percent Change From Baseline to Week 12 in HbA1c

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for HbA1c. Baseline was defined as the last value prior to the first dose of IMP (on or before Visit T1). Percent change from Baseline for HbA1C was analyzed using ANCOVA, with treatment as factor and Baseline HbA1C value as a covariate. Percent change from Baseline for HbA1c was calculated as: ([HbA1c value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For HbA1c, if a measured HbA1c value was available, measured HbA1c was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC0.1
Ezetimibe 10 mg-0.7
Placebo0.4

[back to top]

Percent Change From Baseline to Week 12 in Fasting Plasma Glucose

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for fasting plasma glucose. Baseline was defined as the last value prior to the first dose of study drug (on or before T1). Percent change from Baseline for fasting plasma glucose was analyzed using ANCOVA, with treatment as factor and Baseline fasting plasma glucose as a covariate. Percent change from Baseline for fasting plasma glucose was calculated as: ([fasting plasma glucose value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For fasting plasma glucose, if a measured fasting plasma glucose value was available, measured fasting plasma glucose was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC4.2
Ezetimibe 10 mg3.7
Placebo1.7

[back to top]

Percent Change From Baseline to Week 12 in Apolipoprotein B (Apo B)

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for apo B. Baseline was defined as the last value prior to the first dose of IMP. Percent change from Baseline for TC was analyzed using ANCOVA, with treatment as factor and Baseline lipid parameter as a covariate. Missing data for apo B was imputed using the LOCF method. Percent change from Baseline was calculated as: ([apo B value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For apo B, if a measured apo B value was available, measured apo B was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-27.5
Ezetimibe 10 mg-14.8
Placebo-0.3

[back to top]

Percent Change From Baseline to Week 12 in 2-hour Post Prandial Plasma Glucose (PPG)

Blood samples were drawn 2 hours ± 5 minutes after the start of the meal. Samples were collected and analyzed for PPG. Baseline was defined as the last value prior to the first dose of study drug (on or before T1). Percent change from Baseline for PPG was calculated as: ([PPG value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For PPG, if a measured PPG value was available, measured PPG was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC1.9
Ezetimibe 10 mg0.2
Placebo2.2

[back to top]

Number of Participants With LDL-C <70 Milligrams Per Deciliter (mg/dL) at Week 12

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for LDL-C. For LDL-C, if a measured LDL-C value was available, measured LDL-C was used. (NCT03531905)
Timeframe: Week 12

InterventionParticipants (Count of Participants)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC21
Ezetimibe 10 mg3
Placebo0

[back to top]

Number of Participants With Any Treatment-emergent Adverse Event (TEAE)

Treatment-emergent adverse events (TEAEs) are defined as adverse events (AEs) that began or worsened in severity on or after the first dose of double-blind IMP through 30 days after the last dose of double-blind IMP. An AE is defined as any untoward medical occurrence in a clinical investigation participant administered a pharmaceutical product, including control, and which does not necessarily have a causal relationship with treatment. An AE is: any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product; any new disease or exacerbation of an existing disease; any deterioration in non-protocol-required measurements of a laboratory value or other clinical test (e.g., electrocardiogram or x-ray) that results in symptoms, a change in treatment, or discontinuation from IMP; or an adverse drug reaction. (NCT03531905)
Timeframe: up to approximately 16 weeks

InterventionParticipants (Count of Participants)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC55
Ezetimibe 10 mg45
Placebo46

[back to top]

Change From Baseline to Week 12 in Hemoglobin A1C (HbA1c)

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for HbA1c. Baseline was defined as the last value prior to the first dose of IMP (on or before Visit T1). Change from Baseline was calculated as the HbA1c value at Week 12 minus the Baseline value. For HbA1c, if a measured HbA1c value was available, measured HbA1c was used. (NCT03531905)
Timeframe: Baseline; Week 12

Interventionmg/dL (Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC0.01
Ezetimibe 10 mg-0.06
Placebo0.03

[back to top]

Percent Change From Baseline to Week 12/EOS in LDL-C (Comparing Ezetimibe With Placebo)

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for LDL-C. Baseline was defined as the average of LDL-C values at Visit S3 and Visit T1 (last 2 non-missing values on or prior to Day 1). If only 1 value was available, the single value was used as Baseline. Percent change from Baseline for LDL-C was analyzed using ANCOVA, with treatment as factor and Baseline lipid parameter as a covariate. Missing data for LDL-C was imputed using the LOCF method. Percent change from Baseline was calculated as: ([LDL-C value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For LDL-C, if a measured LDL-C value was available, measured LDL-C was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Ezetimibe 10 mg-19.2
Placebo0.9

[back to top]

Percent Change From Baseline to Week 12/End of Study (EOS) in Low-density Lipoprotein Cholesterol (LDL-C)

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for LDL-C. Baseline was defined as the average of LDL-C values at the Screening Visit 3 (Visit S3) and the Treatment Visit 1 (Visit T1) (last 2 non-missing values on or prior to Day 1). If only 1 value was available, the single value was used as Baseline. Percent change from Baseline for LDL-C was analyzed using analysis of covariance (ANCOVA), with treatment as factor and Baseline lipid parameter as a covariate. Missing data for LDL-C was imputed using the last observation carried forward (LOCF) method. Percent change from Baseline was calculated as: ([LDL-C value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For LDL-C, if a measured LDL-C value was available, measured LDL-C was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Geometric Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-38.8
Ezetimibe 10 mg-19.2
Placebo0.9

[back to top]

Secondary Outcome Measure: Number of Participants With an LDL-C Reduction of ≥50% From Baseline at Week 12

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for LDL-C. Baseline was defined as the average of LDL-C values at Visit S3 and Visit T1 (last 2 non-missing values on or prior to Day 1). If only 1 value was available, the single value was used as Baseline. LDL-C reduction from Baseline was calculated as the LDL-C value at Week 12 minus the Baseline value. For LDL-C, if a measured LDL-C value was available, measured LDL-C was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionParticipants (Count of Participants)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC22
Ezetimibe 10 mg0
Placebo0

[back to top]

Percent Change From Baseline to Week 12 in Total Cholesterol (TC)

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for TC. Baseline was defined as the average of TC values at Visit S3 and Visit T1 (last 2 non-missing values on or prior to Day 1). If only 1 value was available, the single value was used as Baseline. Percent change from Baseline for TC was analyzed using ANCOVA, with treatment as factor and Baseline lipid parameter as a covariate. Missing data for TC was imputed using the LOCF method. Percent change from Baseline was calculated as: ([TC value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For TC, if a measured TC value was available, measured TC was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-27.3
Ezetimibe 10 mg-13.9
Placebo-0.1

[back to top]

Percent Change From Baseline to Week 12 in Non-high-density Lipoprotein Cholesterol (Non-HDL-C)

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for non-HDL-C. Baseline was defined as the average of non-HDL-C values at Visit S3 and Visit T1 (last 2 non-missing values on or prior to Day 1). If only 1 value was available, the single value was used as Baseline. Percent change from Baseline for non-HDL-C was analyzed using ANCOVA, with treatment as factor and Baseline lipid parameter as a covariate. Missing data for non-HDL-C was imputed using the LOCF method. Percent change from Baseline was calculated as: ([non-HDL-C value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For non-HDL-C, if a measured non-HDL-C value was available, measured non-HDL-C was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Least Squares Mean)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-33.0
Ezetimibe 10 mg-17.8
Placebo0.1

[back to top]

Percent Change From Baseline to Week 12 in Triglycerides (TGs)

Blood samples were drawn after a minimum 10-hour fast at pre-specified intervals. Samples were collected and analyzed for TGs. Baseline was defined as the average of TG values at Visit S3 and Visit T1 (last 2 non-missing values on or prior to Day 1). If only 1 value was available, the single value was used as Baseline. Percent change from Baseline for TGs was analyzed using a non-parametric approach. Percent change from Baseline was calculated as: ([TG value at Week 12 minus Baseline value] divided by [Baseline value]) multiplied by 100. For TGs, if a measured TG value was available, measured TG was used. (NCT03531905)
Timeframe: Baseline; Week 12

InterventionPercent change (Median)
Bempedoic Acid 180 mg + Ezetimibe 10 mg FDC-9.20
Ezetimibe 10 mg-13.59
Placebo-5.11

[back to top]