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Alirocumab and Reverse Cholesterol Transport

Phase 1
Completed
Conditions
Atherosclerosis
Coronary Heart Disease
Interventions
Drug: Placebos
Registration Number
NCT03014830
Lead Sponsor
Washington University School of Medicine
Brief Summary

Alirocumab is an injectable treatment for elevated blood cholesterol. The hypothesis of this study is that it also increases cholesterol excretion from the body into the stool, a process sometimes called reverse cholesterol transport. A cholesterol metabolic study will be done before and after 6 weeks of alirocumab treatment. If alirocumab increases reverse cholesterol transport, it is possible that this action provides additional protection from cardiovascular disease.

Detailed Description

This study is a single-site, randomized, placebo-controlled clinical trial in which about 24 subjects are expected to complete an 8-week study period. The performance site is Washington University School of Medicine. Even though alirocumab is an approved drug, the investigators consider this to be a phase I trial because it is a physiological study in which the primary endpoint is change in fecal cholesterol excretion and measures of reverse cholesterol transport. It is not a treatment protocol and uses healthy subjects.

Subjects with greater than ideal cholesterol but not taking cholesterol lowering drugs will be studied. All receive whole body cholesterol metabolism tests before and after treatment for 6 weeks with either alirocumab or placebo. Each test takes 2 weeks. On the first day the subjects receive about 35 mg cholesterol-d7 intravenously and blood samples are obtained in order to measure cholesterol turnover rate, pool size, esterification rate, transfer from HDL to LDL and removal from the plasma compartment. Fecal cholesterol excretion and related parameters are measured on days 13 and 14 after a relative steady-state is obtained. During this time the subjects consume a metabolic kitchen diet controlled in cholesterol and phytosterol content and consume oral tracer capsules consisting of cholesterol-d5 and sitostanol-d4. Plasma and stool samples are analyzed by gas chromatography/tandem mass spectrometry to determine daily percent cholesterol excretion from rapidly-mixing body cholesterol pools, fecal cholesterol mass and percent cholesterol absorption. The cholesterol metabolic test is repeated on day 43 and final measurements are made on day 57. Treatment effect, defined as the difference between active and placebo treatments is then calculated. Based on animal data it is expected that alirocumab will increase the efficiency of cholesterol excretion from body pools and the rate of removal of cholesterol ester from plasma.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
28
Inclusion Criteria
  • Healthy or with stable medical or surgical illnesses
  • LDL>100 mg/dl.
Exclusion Criteria
  • Triglycerides>250
  • Taking drugs affecting lipid metabolism
  • Elevated liver function tests
  • Diabetes mellitus
  • A1c 6.5% or greater
  • Pregnant
  • Breastfeeding
  • Desire for conception in either sex.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
AlirocumabAlirocumabSubjects will receive alirocumab for 6 weeks.
PlacebosPlacebosSubjects will receive placebo for 6 weeks.
Primary Outcome Measures
NameTimeMethod
Change from baseline in removal rate of esterified cholesterol from plasma per day.Measurements made on days 1-3 (baseline) and days 43-45 (on treatment).

The removal rate of esterified cholesterol from plasma per day is defined as fractional removal rate of esterified cholesterol from the plasma in pools/day.

Change from baseline in percent cholesterol excretion per day.Measurements made on days 13-15 (baseline) and days 55-57 (on treatment).

Percent cholesterol excretion per day is defined as the percent of endogenous rapidly-mixing cholesterol pools excreted per day into the stool.

Secondary Outcome Measures
NameTimeMethod
Change from baseline in LDL cholesterolMeasurements made on day 15 (baseline) and day 57 (on treatment).

Reduction in LDL with alirocumab treatment.

Change from baseline in percent cholesterol absorptionMeasurements made on days 13-15 (baseline) and days 55-57 (on treatment).

Percent cholesterol absorption is defined as the percent of intestinal cholesterol absorbed into the body.

Trial Locations

Locations (1)

Washington University School of Medicine

🇺🇸

Saint Louis, Missouri, United States

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