MedPath

An Efficacy and Safety Study of Ezetimibe (MK-0653, SCH 58235) in Addition to Atorvastatin Compared to Placebo in Participants With Primary Hypercholesterolemia (MK-0653-013)

Registration Number
NCT03867110
Lead Sponsor
Organon and Co
Brief Summary

This is a multicenter, randomized, double-blind, placebo-controlled, balanced-parallel-group, efficacy and safety trial of ezetimibe coadministered with atorvastatin in adult participants with primary hypercholesterolemia. The primary hypothesis is that the coadministration of ezetimibe 10 mg/day with atorvastatin (pooled across all doses: 10 mg, 20 mg, 40 mg, 80 mg) will result in a significantly greater reduction in direct low density lipoprotein-cholesterol (LDL-C) when compared with atorvastatin (pooled across all doses: 10 mg, 20 mg, 40 mg, 80 mg) alone and ezetimibe 10 mg alone.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
628
Inclusion Criteria
  • If female, is not pregnant or breastfeeding, and is either not a woman of childbearing potential (WOCBP), or is a WOCBP who has used a contraceptive consistent with local regulations.
  • Postmenopausal women who are receiving postmenopausal hormonal therapy or raloxifene must be maintained on a stable estrogen (ERT), estrogen/progestin (HRT) or raloxifene regimen during the study period.
  • Primary hypercholesterolemic participants with a plasma LDL-Cholesterol ≥145 mg/dL (3.75 mmol/L) and ≤250 mg/dL (6.48 mmol/L) and plasma triglyceride ≤350 mg/dL (3.99 mmol/L) after adequate drug washout
  • Must be willing to observe the National Cholesterol Education Program (NCEP) Step I diet as determined by a Ratio of Ingested Saturated fat and Cholesterol to Calories (RISCC) score not greater than 24 throughout this study. Ability to complete Diet Diaries needs to be demonstrated.
Exclusion Criteria
  • Has a history of mental instability, drug/alcohol abuse within the past 5 years, or major psychiatric illness not adequately controlled and stable on pharmacotherapy.
  • Underlying disease likely to limit life span to less than 1 year.
  • Participants with hypercholesterolemia in whom withholding of approved lipid-lowering therapy would be inappropriate.
  • Have previously been randomized in any of the studies evaluating Ezetimibe (SCH 58235).
  • Known hypersensitivity or any contraindication to atorvastatin (LIPITOR®).
  • Pregnant or lactating women.
  • Congestive heart failure New York Heart Association (NYHA) Class III or IV.
  • Uncontrolled cardiac arrhythmias.
  • Myocardial infarction, coronary bypass surgery or angioplasty within 6 months of study entry.
  • Unstable or severe peripheral artery disease within 3 months of study entry.
  • Unstable angina pectoris.
  • Disorders of the hematologic, digestive or central nervous systems including cerebrovascular disease and degenerative disease that would limit study evaluation or participation.
  • Uncontrolled or newly diagnosed (within 1 month of study entry) diabetes mellitus.
  • Uncontrolled endocrine or metabolic disease known to influence serum lipids or lipoproteins.
  • Known impairment of renal function (plasma creatinine >2.0 mg/dL), dysproteinemia, nephrotic syndrome or other renal disease.
  • Active or chronic hepatobiliary or hepatic disease.
  • Participants who are known to be Human Immunodeficiency Virus (HIV) positive.
  • Participants with known coagulopathy.
  • Lipid-altering agents, other than study drugs for the whole duration of the study.
  • Oral corticosteroids.
  • Cardiovascular drugs such as: beta blockers, calcium channel blockers, ACE inhibitors, nitrates or α-adrenergic blockers or thiazide diuretics will be allowed, provided the dose remains constant for the duration of the study and the participant has received a stable dose for at least 8 weeks before the initial qualifying LDL-C level is drawn. Aspirin up to 325 mg/day is permitted. In addition, aspirin is allowed as a as needed (prn) concomitant medication.
  • Treatment with psyllium or other fiber-based laxatives unless treated with a stable regimen for at least 4 weeks before initial qualifying lipid determination. Dose must remain constant throughout the study period.
  • Treatment with troglitazone (Rezulin®) unless treated with a stable regimen for at least 6 weeks before initial qualifying lipid determination. Dose must remain constant throughout the study period.
  • Treatment with cyclosporine.
  • Use of any investigational drugs within 30 days of study entry.
  • Treatment with agents with known drug interaction with atorvastatin including antifungal azoles (itraconazole and ketoconazole), macrolide antibiotics (erythromycin and clarithromycin), and nefazodone. In addition, treatment with other agents that may interfere with or induce the CYP3A4 isoenzyme of the cytochrome P450 system should be avoided.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Atorvastatin 10 mgAtorvastatin 10 mgAtorvastatin 10 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Ezetimibe 10 mg + Atorvastatin 20 mgEzetimibe 10 mgEzetimibe 10 mg (MK-0653, SCH 58235) + Atorvastatin 20 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Ezetimibe 10 mg + Atorvastatin 10 mgEzetimibe 10 mgEzetimibe 10 mg (MK-0653, SCH 58235) + Atorvastatin 10 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Ezetimibe 10 mg + Atorvastatin 10 mgAtorvastatin 10 mgEzetimibe 10 mg (MK-0653, SCH 58235) + Atorvastatin 10 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Ezetimibe 10 mg + Atorvastatin 40 mgEzetimibe 10 mgEzetimibe 10 mg (MK-0653, SCH 58235) + Atorvastatin 40 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Atorvastatin 80 mgAtorvastatin 80 mgAtorvastatin 80 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Ezetimibe 10 mgEzetimibe 10 mgEzetimibe 10 mg (MK-0653, SCH 58235) is to be taken orally QD in the morning for 12 consecutive weeks.
Ezetimibe 10 mg + Atorvastatin 80 mgEzetimibe 10 mgEzetimibe 10 mg (MK-0653, SCH 58235) + Atorvastatin 80 mg is to be taken orally QD in the morning for 12 consecutive weeks.
PlaceboPlaceboPlacebo is to be taken orally once a day (QD) in the morning for 12 consecutive weeks.
Ezetimibe 10 mg + Atorvastatin 40 mgAtorvastatin 40 mgEzetimibe 10 mg (MK-0653, SCH 58235) + Atorvastatin 40 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Ezetimibe 10 mg + Atorvastatin 20 mgAtorvastatin 20 mgEzetimibe 10 mg (MK-0653, SCH 58235) + Atorvastatin 20 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Atorvastatin 40 mgAtorvastatin 40 mgAtorvastatin 40 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Atorvastatin 20 mgAtorvastatin 20 mgAtorvastatin 20 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Ezetimibe 10 mg + Atorvastatin 80 mgAtorvastatin 80 mgEzetimibe 10 mg (MK-0653, SCH 58235) + Atorvastatin 80 mg is to be taken orally QD in the morning for 12 consecutive weeks.
Primary Outcome Measures
NameTimeMethod
Percent Change from Baseline at Week 12 of Plasma Low Density Lipoprotein Cholesterol (LDL-C)Baseline and Week 12

Plasma LDL-C determined following a standard ultracentrifugation / precipitation (quantification) procedure (direct LDL-C). Participants had LDL-C levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Secondary Outcome Measures
NameTimeMethod
Percent Change from Baseline at Week 12 for High Density-Lipoprotein 2-Cholesterol (HDL2-C)Baseline and Week 12

Participants had HDL2-C levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Percent Change from Baseline at Week 12 for High Density-Lipoprotein 3-Cholesterol (HDL3-C)Baseline and Week 12

Participants had HDL3-C levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Percent Change from Baseline at Week 12 for Calculated Low Density Lipoprotein-Cholesterol (LDL-C)Baseline and Week 12

Participants had LDL-C levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Percent Change from Baseline at Week 12 for Non-High Density-Lipoprotein-Cholesterol (Non-HDL-C)Baseline and Week 12

Participants had Non-HDL-C levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Percent Change from Baseline at Week 12 for Total Cholesterol (TC)Baseline and Week 12

Participants had TC levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Percent Change from Baseline at Week 12 for Apolipoprotein B (Apo B)Baseline and Week 12

Participants had Apo B levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Percent Change from Baseline at Week 12 for High Density-Lipoprotein-Cholesterol (HDL-C)Baseline and Week 12

Participants had HDL-C levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Percent Change from Baseline at Week 12 for Direct Total Cholesterol/High Density-Lipoprotein 3-Cholesterol (TC/HDL-C) RatioBaseline and Week 12

Participants had TC and HDL-C levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline in the TC/HDL-C ratio was calculated.

Percent Change from Baseline at Week 12 for Triglycerides (TG)Baseline and Week 12

Participants had TG levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

Percent Change from Baseline at Week 12 for Direct Low Density-Lipoprotein 3-Cholesterol/High Density-Lipoprotein 3-Cholesterol (LDL-C/HDL-C) RatioBaseline and Week 12

Participants had LDL-C and HDL-C levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline in the LDL-C/HDL-C ratio was calculated.

Percent Change from Baseline at Week 12 for Lipoprotein (a) (Lp[a])Baseline and Week 12

Participants had Lp(a) levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

The Percentage of Participants Achieving National Cholesterol Education Program (NCEP) Adult Treatment Panel (ATP II) Target Goal for Direct Low Density Lipoprotein-Cholesterol (LDL-C)Week 12

LDL cholesterol level goal is \<100 mg per deciliter (2.60 mmol per L)

Percent Change from Baseline at Week 12 for Apolipoprotein A-I (Apo A-I),Baseline and Week 12

Participants had Apo A1 levels assessed at baseline and after 12 weeks of study drug administration. The percent change from baseline was calculated.

© Copyright 2025. All Rights Reserved by MedPath