Pharmacokinetics of current and emerging treatments for hypercholesterolemia

Brian Tomlinson, Paul Chan, Yuzhen Zhang, Zhongmin Liu, Christopher Wai Kei Lam

Research output: Contribution to journalReview articlepeer-review

9 Citations (Scopus)


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-interfering RNA inclisiran has the notable advantage that a single subcutaneous administration may be effective for up to 6 months. The CV outcome trial results and long term safety data are eagerly awaited for these new agents.

Original languageEnglish
Pages (from-to)371-385
Number of pages15
JournalExpert Opinion on Drug Metabolism and Toxicology
Issue number5
Publication statusPublished - May 3 2020


  • bempedoic acid
  • ezetimibe
  • gemcabene
  • inclisiran
  • LDL-C-lowering
  • pemafibrate
  • pradigastat
  • proprotein convertase subtilisin/kexin type 9 inhibitors
  • statins
  • volanesorsen

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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