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Updated: Aug 13, 2026

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
Colesevelam hydrochloride: a non-absorbed, polymeric cholesterol-lowering agent
M H Davidson1, M R Dicklin, K C Maki
1Nutrition and Metabolism Research Unit, Chicago Center for Clinical Research, 515 North State Street, Suite 2700, Chicago, IL 60610, USA. mdavidson@protocare.com
Colesevelam hydrochloride is a safe and effective cholesterol-lowering drug that reduces LDL-cholesterol. It offers a non-systemic option for hypercholesterolemia, with good tolerability and minimal side effects, improving compliance.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
Background:
- Colesevelam hydrochloride (formerly Cholestagel, now WelChol) is a novel polymeric hydrogel.
- It acts as a potent, water-absorbing agent for cholesterol management.
Purpose of the Study:
- To evaluate the safety and efficacy of colesevelam hydrochloride as a cholesterol-lowering agent.
- To assess its lipid-lowering activity in patients with hypercholesterolemia.
Main Methods:
- Clinical evaluation of colesevelam hydrochloride in approximately 1400 subjects.
- Dose-dependent assessment of low-density lipoprotein (LDL)-cholesterol reduction.
- Evaluation of concurrent administration with hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins).
Main Results:
- Colesevelam hydrochloride reduced LDL-cholesterol by up to 20% (median) in hypercholesterolemia patients.
- Effective at once or twice daily dosing; did not affect statin absorption.
- Combination therapy with statins yielded an additional 8-16% LDL-cholesterol reduction.
Conclusions:
- Colesevelam hydrochloride is a safe and effective non-systemic agent for hypercholesterolemia.
- It offers improved tolerability and compliance compared to traditional bile acid sequestrants.
- Represents a valuable therapeutic option for monotherapy or combination therapy alongside diet and exercise.
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