Apr 1, 2020

Pharmacokinetics of current and emerging treatments for hypercholesterolemia

Expert Opinion on Drug Metabolism & Toxicology
Brian TomlinsonChristopher Wai Kei Lam

Abstract

Introduction: Reduction of low-density-lipoprotein cholesterol (LDL-C) and other apolipoprotein B (apoB)-containing lipoproteins reduces cardiovascular (CV) events and greater reductions have greater benefits. Current lipid treatments cannot always achieve desirable LDL-C targets and additional or alternative treatments are often needed.Areas covered: In this article, we review the pharmacokinetics of the available and emerging treatments for hypercholesterolemia and focus on recently approved drugs and those at a late stage of development.Expert opinion: Statin pharmacokinetics are well known and appropriate drugs and doses can usually be chosen for individual patients to achieve LDL-C targets and avoid adverse effects and drug-drug interactions. Ezetimibe, icosapent ethyl and the monoclonal antibodies evolocumab and alirocumab have established efficacy and safety. Newer oral agents including pemafibrate and bempedoic acid have generally favorable pharmacokinetics supporting use in a wide range of patients. RNA-based therapies with antisense oligonucleotides are highly specific for their targets and those inhibiting apoB, apoCIII, angiopoietin-like protein 3 and lipoprotein(a) have shown promising results. The small-interferin...Continue Reading

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Mentioned in this Paper

Adverse Effects
Lipoprotein (a)
Agent
Measurement of Serum Lipid Level
Pharmacologic Substance
Acids
Monoclonal Antibodies
Angptl3 protein, mouse
RNA, Small Interfering
Hydroxymethylglutaryl-CoA Reductase Inhibitors

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