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Updated: Aug 5, 2026

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
The effect of etophylline clofibrate on HDL subfractions
Insights
Etophylline clofibrate effectively improved lipid profiles in type II hyperlipoproteinemia patients. It increased high-density lipoprotein (HDL) components and significantly reduced low-density lipoprotein (LDL) cholesterol and very-low-density lipoprotein (VLDL) triglycerides.
Area of Science:
- Pharmacology
- Lipid Metabolism
- Cardiovascular Disease
Background:
- Type II hyperlipoproteinemia (HLP) is characterized by elevated levels of certain lipoproteins.
- Effective management of HLP is crucial for reducing cardiovascular risk.
Purpose of the Study:
- To investigate the effects of etophylline clofibrate on lipoprotein metabolism in patients with type II HLP.
- To assess changes in high-density lipoprotein (HDL) subfractions, very-low-density lipoproteins (VLDL), low-density lipoproteins (LDL), and lipolytic enzyme activities.
Main Methods:
- A 12-week treatment period with etophylline clofibrate (750 mg/day) in 14 type II HLP patients.
- Study included washout and placebo periods, and patients followed a low-fat, low-cholesterol diet.
- Measurements included lipids, apolipoproteins, and post-heparin lipolytic activities (PHLA) of lipoprotein lipase (LPL) and hepatic triglyceride lipase (HTGL).
Main Results:
- Etophylline clofibrate significantly increased HDL cholesterol and apoproteins, with distinct changes in HDL2 and HDL3 subfractions over time.
- Significant reductions observed in plasma LDL cholesterol (19%) and VLDL triglycerides (22%).
- VLDL-C apoproteins decreased by 31%, with a relative increase in apo C-II.
Conclusions:
- Etophylline clofibrate demonstrates a beneficial effect on lipid and apolipoprotein profiles in type II HLP.
- The drug effectively lowers atherogenic lipoproteins and modulates HDL metabolism.
- These findings suggest potential therapeutic value in managing dyslipidemias associated with HLP.
Abstract:
The effect of etophylline clofibrate on lipids and apolipoproteins of the high density lipoprotein (HDL) subfractions HDL2 and HDL3 as well as on very low density (VLDL) and low density lipoproteins (LDL) and the post heparin lipolytic activities (PHLA) of lipoprotein lipase (LPL) and hepatic triglyceride lipase (HTGL) has been studied in 14 patients with type II hyperlipoproteinemia (HLP). The study was preceded by a 4-week washout phase, followed by a 6-week placebo period. During the next 12 weeks, the patients received 750 mg etophylline clofibrate per day. Then the drug was again replaced by placebo for another 6 weeks. During the study the patients were on a low fat diet poor in cholesterol with a P/S ratio over 1.0. HDL cholesterol and apoproteins increased significantly during treatment. In the first verum phase this effect was related to the rise in HDL2 components with minor changes in HDL3 concentrations, whereas in the second verum period a distinct increase of the HDL3 components could be detected. This development was accompanied by a significant increase of the LPL activities during the first 6 weeks of treatment, followed by a decrease to initially measured values after 12 weeks. The drug lowered plasma- and LDL-cholesterol levels by 19% and 22%, and plasma and VLDL triglycerides by 22% and 25%, respectively. VLDL-C apoproteins (C-I, C-II, C-III) declined by 31% with a percentage increase of apo C-II compared with apo C-I and apo C-III.
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