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Effectiveness of Treatment of Hypercholesterolemia With Rosuvastatin and Ezetimibe

Phase 4
Completed
Conditions
Hypercholesterolemia
Interventions
Registration Number
NCT02772640
Lead Sponsor
Collegium Medicum w Bydgoszczy
Brief Summary

The aim of the study is to demonstrate, whether the time of day of administration of the study drug (containing rosuvastatin and ezetimibe) has an impact on the effectiveness of lipid-lowering therapy.

Detailed Description

The current guidelines recommend statins as drugs of first choice in the treatment of hypercholesterolemia. If the target LDL cholesterol is not achieved, combination of a statin with a cholesterol absorption inhibitor -ezetimibe may be considered.

According to meta-analyzes of studies assessing statins, each 1.0 mmol / L (\~ 40 mg / dL) reduction in LDL-C corresponds to a 10% reduction in all-cause mortality and a 20% reduction in the number of deaths from coronary artery disease. Each 1 mmol / L (40 mg / dL) reduction in LDL-C also translates into a 23% and 17% reduction of the risk of major coronary events and stroke, respectively. Similar results concerning the efficacy and safety of lipid-lowering therapy using statins were obtained in meta-analyzes of studies on primary prevention. Statins are a heterogenous group of drugs with respect to their LDL-C reduction power. So far, the most potent statin is rosuvastatin. Despite intensive statin therapy provided, a large group of patients still does not reach therapeutic goals. Statin dose titration seems to be less effective compared with the combined therapy with statin and ezetimibe. The combination of statin with ezetimibe reduces the LDL-C by additional 15-20%.

Tablets comprising both of these drugs (statin and ezetimibe) simplify the drug administration and increase the probability of drug compliance. This may increase the probability for achieving therapeutic goals in hypercholesterolemia treatment.

Taking into account the metabolism of cholesterol and possible drug-drug interactions it is recommended to administer simvastatin in the evening. Rosuvastatin may be administer at any time of the day.

The study is designed as an open-label, single-center, cross-over study evaluating the effectiveness of combined therapy with rosuvastatin and ezetimibe for hypercholesterolemia depending on timing of the day of administration of the study treatment. After enrollment the participants will be allocated into two arms, each receiving rosuvastatin and ezetimibe. The study drug (rosuvastatin with ezetimibe) will be given: 1) in the morning (8:00) for 6 weeks and then in the evening for the next 6 weeks; 2) in the evening (20:00) for the first 6 weeks and then in the morning for the following 6 weeks. The change in total cholesterol and LDL-cholesterol at 6 and 12 weeks of the tested therapy will be measured as the primary outcome of the study. Moreover, other parameters including: HDL-cholesterol, triglycerides, apolipoprotein B (ApoB), ApoAI, nonHDL-cholesterol, sd-LDL-cholesterol, lipoprotein (a), glucose, HBA1c, high sensitivity C reactive protein (hsCRP), ALT, aspartate aminotransferase (AST), creatine kinase (CK ) will be assessed as secondary outcomes.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
83
Inclusion Criteria
  1. Hypercholesterolemia
  2. Ineffectiveness of statin monotherapy in the treatment of hypercholesterolemia after at least 6 weeks
Exclusion Criteria
  1. Active liver disease
  2. Unexplained persistent increase in serum transaminase levels, including more than 3 times the upper limit of normal activity of one of them
  3. Severe renal impairment (creatinine clearance <30 ml / min)
  4. Myopathy
  5. Concomitant treatment with cyclosporine, gemfibrozil
  6. Pregnancy
  7. Lactation
  8. Women of childbearing age not using effective methods of contraception
  9. Symptoms of muscle damage after using statins or fibrates in the past.
  10. The activity of creatine kinase> 5 times the upper limit of normal

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
ARM II: R+E evening->morningRosuvastatin and Ezetimibe morning or evening administrationRosuvastatin and Ezetimibe evening or morning administration: Rosuvastatin (R) plus Ezetimibe (E) administration in the evening (20:00) for 6 weeks. After 6 weeks - intervention - change of the timing of study drug administration to the morning hours (8:00).
Arm I: R+E morning->eveningRosuvastatin and Ezetimibe morning or evening administrationRosuvastatin and Ezetimibe morning or evening administration: Rosuvastatin (R) plus Ezetimibe (E) administration in the morning (8:00) for 6 weeks. After 6 weeks - intervention - change of the timing of study drug administration to the evening hours (20:00).
Primary Outcome Measures
NameTimeMethod
Change in total cholesterol and LDL-Cholesterol6 and 12 weeks

Change in total cholesterol and LDL-Cholesterol at 6 and 12 weeks of study drug treatment (combination of ezetimibe and rosuvastatin), depending on the time of day of study drug administration

Secondary Outcome Measures
NameTimeMethod
Change in lipoprotein (a)6 and 12 weeks

Change in lipoprotein (a) at 6 and 12 weeks of study drug treatment (combination of ezetimibe and rosuvastatin), depending on the time of day of study drug administration

Change in HDL-Cholesterol6 and 12 weeks

Change in HDL-Cholesterol at 6 and 12 weeks of study drug treatment (combination of ezetimibe and rosuvastatin), depending on the time of day of study drug administration

Change in non - HDL-Cholesterol6 and 12 weeks

Change in non - HDL-Cholesterol at 6 and 12 weeks of study drug treatment (combination of ezetimibe and rosuvastatin), depending on the time of day of study drug administration

Change in sd-LDL-Cholesterol6 and 12 weeks

Change in sd-LDL-Cholesterol at 6 and 12 weeks of study drug treatment (combination of ezetimibe and rosuvastatin), depending on the time of day of study drug administration

Assessment of hsCRPBaseline, 6 and 12 weeks

Assessment hsCRP at baseline and at 6 and 12 weeks of treatment with study drug

Assessment of ASTBaseline, 6 and 12 weeks

Assessment AST at baseline and at 6 and 12 weeks of treatment with study drug

Change in apolipoproteins ApoB, APO AI6 and 12 weeks

Change in apolipoproteins ApoB, APO AI at 6 and 12 weeks of study drug treatment (combination of ezetimibe and rosuvastatin), depending on the time of day of study drug administration

Assessment of change of glucose concentrationBaseline, 6 and 12 weeks

Assessment of glucose at baseline and at 6 and 12 weeks of treatment with study drug

Assessment of ALTBaseline, 6 and 12 weeks

Assessment ALT at baseline and at 6 and 12 weeks of treatment with study drug

Change in triglycerides6 and 12 weeks

Change in triglycerides at 6 and 12 weeks of study drug treatment (combination of ezetimibe and rosuvastatin), depending on the time of day of study drug administration

Assessment of HbA1cBaseline, 6 and 12 weeks

Assessment of HbA1c at baseline and at 6 and 12 weeks of treatment with study drug

Assessment of CKBaseline, 6 and 12 weeks

Assessment CK at baseline and at 6 and 12 weeks of treatment with study drug

Assessment of plasma fluorescence using stationary and time-resolved spectrofluorimetryBaseline, 6 and 12 weeks

Assessment of plasma fluorescence using stationary and time-resolved spectrofluorimetry at baseline, at 6 and 12 weeks of treatment with study drug

Trial Locations

Locations (1)

Cardiology Department, Dr. A. Jurasz University Hospital

🇵🇱

Bydgoszcz, Kujawsko-Pomorskie, Poland

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