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Updated: Jun 16, 2026

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
Current strategies and recent advances in the therapy of hypercholesterolemia
E Windler1, B-Chr Zyriax, Chr Bamberger
1Endokrinologie und Stoffwechsel des Alterns, University Medical Center Hamburg-Eppendorf, Martinistr. 52, 20246 Hamburg, Germany. windler@uke.uni-hamburg.de
Insights
Lipid therapy effectively prevents atherosclerotic vascular disease. New drugs like colesevelam, niacin/laropiprant, and mipomersen offer improved efficacy and tolerability for lowering LDL-cholesterol and raising HDL-cholesterol.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Background:
- Atherosclerotic vascular disease prevention relies on lipid therapy.
- Optimal LDL-cholesterol levels are below 100 mg/dl, necessitating potent lipid-lowering drugs.
- Current strategies focus on inhibiting cholesterol synthesis and absorption.
Purpose of the Study:
- To review advancements in lipid therapy for atherosclerotic vascular disease.
- To highlight novel therapeutics enhancing efficacy and tolerability.
- To discuss new agents for lowering LDL-cholesterol and raising HDL-cholesterol.
Main Methods:
- Review of current and emerging lipid-lowering and HDL-raising therapeutics.
- Discussion of drug mechanisms, efficacy, and tolerability profiles.
- Comparison of novel agents with existing therapies and apheresis.
Main Results:
- Colesevelam, a bile-acid sequestrant, offers improved tolerability.
- Niacin combined with laropiprant significantly raises HDL-cholesterol with reduced flushing.
- Mipomersen demonstrates substantial reduction in apolipoprotein B-100, challenging apheresis.
Conclusions:
- New pharmacological developments promise enhanced lipid management for cardiovascular disease.
- Combination therapies and novel agents like mipomersen represent significant progress.
- These advancements aim to achieve lower LDL-cholesterol and improved HDL-cholesterol levels more effectively and safely.
Abstract:
Lipid therapy is an option for preventing atherosclerotic vascular disease that has been intensively studied and proved to be effective independent of the underlying risk factors. Since the optimal LDL-cholesterol appears to lie well below 100 mg/dl most potent lipid lowering drugs and adjunctive HDL-raising therapeutics are mandatory. Inhibition of cholesterol synthesis and absorption is currently the preferred measure. However, new developments may substantially increase the efficacy of lipid therapy. One is add-on colesevelam, a synthetic bile-acid sequestrant with increased binding affinity which allows smaller dosages for better tolerability. Alternatively HDL-cholesterol may be increased by 25% using niacin with improved tolerability due to the combination with laropiprant, an inhibitor of the receptor for prostaglandin D2-receptor, which minimizes flushing close to placebo level. Mipomersen, a specific oligonucleotide capable to reduce apolipoprotein B-100 up to 70%, is certainly the most advanced approach to challenge even apheresis as the most effective measure to lower exceptionally elevated cholesterol levels.
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