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ABT-335 (Choline Fenofibrate) Reverse Cholesterol Transport (RCT) Study

Phase 1
Completed
Conditions
Dyslipidemia
Interventions
Registration Number
NCT00673881
Lead Sponsor
Radiant Research
Brief Summary

The objectives of the study are:

1. To evaluate the effect of ABT-335 (choline fenofibrate) on several parameters of RCT (reverse cholesterol transport) in men and post-menopausal women diagnosed with dyslipidemia (i.e., low high-density lipoprotein \[HDL\] cholesterol levels and elevated triglyceride \[TG\] concentrations).

2. To evaluate longitudinal changes in several parameters of RCT in subjects with low HDL.

3. To obtain pilot data for power calculations for subsequent comparative study.

Detailed Description

This trial assesses the effects of ABT-335 on RCT as measured by cholesterol efflux or rate of appearance of cholesterol (Ra in mg/kg/hr), cholesterol excretion (%/day), RCT efflux (mg/kg/day) and de novo cholesterol synthesis (%) during a baseline period (7 days) and during a treatment period (94 days).

The goal of using RCT to reverse atherosclerosis is to increase the rate of cholesterol export or "efflux" from the tissues and plaques. An increase in this cholesterol efflux rate should shrink arterial plaques by decreasing their static accumulation of cholesterol. While some currently marketed drugs have a positive impact on RCT by increasing the rate of cholesterol excretion from the body, no drug has yet been approved to increase the rate of cholesterol efflux from the tissues

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
25
Inclusion Criteria
  1. Male, non-smoker, 21 - 75 years of age inclusive.
  2. Female, non-smoker, 40 - 75 years of age inclusive.
  3. Post-menopausal women, as defined by lack of menses for at least 2 years and age > 55, OR history of documented bilateral surgical oophorectomy, confirmed with an elevated follicle-stimulating hormone (FSH) at screening.
  4. HDL concentration (≤ 50 mg/dl women, ≤ 40mg/dl men)
  5. TG concentration 150-500 mg/dl, inclusive
  6. Ability to give informed consent
Exclusion Criteria
  1. Subject has history of diabetes mellitus, active hepatitis, gall bladder disease, gastric bypass surgery, or clinically significant abnormalities on screening (prestudy) physical examination or laboratory tests.
  2. Screening laboratory tests with hematocrit <30%, aspartate aminotransferase (AST)/alanine aminotransferase (ALT) > 2X upper limit of normal, abnormal thyroid-stimulating hormone (TSH), fasting glucose ≥126 mg/dl.
  3. Renal impairment with creatinine clearance < 80 ml/min.
  4. Treatment within the last 6 months with drugs known to alter lipid metabolism including beta blockers, thiazide diuretics, bile acid resins, ezetimibe, fibrates, niacin, and fish oils (see Appendix 1). Washout of fibrates is not permitted.
  5. Treatment with drugs known to interact with ABT-335, e.g., warfarin (see Appendix 1).
  6. Treatment with HMG CoA reductase inhibitors (statins) within the past 4 weeks (see Appendix 1).
  7. History of allergy to egg or soy products.
  8. History of coronary heart disease (CHD), stroke or revascularization procedure in the six months prior to Visit 1.
  9. Current or recent history (past 12 months) of drug abuse or alcohol abuse. Alcohol abuse will be defined as >14 drinks per week (1 drink = 12 oz beer, 5 oz wine, or 1.5 oz hard liquor).
  10. Participation in another clinical trial or exposure to any investigational agent within 30 days before visit 1.
  11. Individual has a condition the Principal Investigator believes would interfere with his/her ability to provide informed consent, comply with study instructions, or which might confound the interpretation of the study results or put the subject at undue risk.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Abt-335choline fenofibrateABT-335 (choline fenofibrate)
Primary Outcome Measures
NameTimeMethod
Mean Change in Calculated Low Density Lipoprotein Cholesterolbaseline to 12 weeks

Mean change in calculated LDL, baseline (average Day 0, 1 10) to end-of-treatment (12 weeks treatment,average Day 95)

Mean Change in Plasma Triglyceridesbaseline to 12 weeks

Change in plasma triglyceride, baseline (average Day 0, 1 10) to end-of-treatment (12 weeks treatment,Day 95)

Mean Change in High Density Lipoprotein CholesterolBaseline to 12 weeks

Mean change in plasma high density plasma lipoprotein cholesterol (HDL-C)baseline (average Day 0, 1 10) to end-of-treatment (12 weeks treatment,Day 95)

Total Cholesterol12 weeks

Mean Change in total cholesterol from baseline to End-of-treatment (Day 95)

Secondary Outcome Measures
NameTimeMethod
Plasma Cholesterol Efflux12 weeks

Change in efflux rate from baseline to end-of-treatment. The efflux rate of cholesterol from peripheral tissues into the plasma was measured as mg/kg/hr. An IV infusion of \[13C2\] cholesterol mixed in 10% Intralipid® or Liposyn® and 10 % ethanol was given piggy-backed into normal saline over 24 hours. This was used to determine rate of appearance (Ra) cholesterol, 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 traced into biliary sterols.

Change in Plasma Cholesterol Ester Fractional Catabolic Rate (FCR)Baseline to 12 weeks

Change in FCR from baseline to end-of-treatment (12 weeks)

Percent Change in de Novo Cholesterol SynthesisBaseline to 12 weeks

Plasma DNC was measured three times from blood draws on the 3 visits in the 10 day period following the isotope infusion at baseline and again at end-of-treatment at 12 weeks, and expressed in percent. Change from baseline to end-of-treatment expressed as percent.

Change in Neutral Sterol Excretionbaseline to 12 weeks

The excretion rate of fecal neutral and acidic sterols was measured as mg/day, for each individual three times during the 10 day period following the isotope infusions at baseline and end-of-treatment.

Change in Bile Acid ExcretionBaseline to 12 weeks

Change in bile acid excretion from baseline to end-of-treatment

Neutral Sterol Endogenous Excretion12 weeks

Change in neutral sterol endogenous excretion from baseline to end-of-treatment

Endogenous Bile Acid Excretion12 weeks

Change in endogenous bile acid excretion from baseline to end-of-treatment

Trial Locations

Locations (1)

Radiant Research, 515 N State St, #2700

🇺🇸

Chicago, Illinois, United States

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