Bempedoic acid in the treatment of hyperlipidemia: from mechanism of action to therapeutic potential. A literature review

The study aim was to provide an overview of current data on the mechanism of action, clinical efficacy, and safety of bempedoic acid (BA) as a lipid-lowering drug.

The methodological approaches included a literature search of PubMed, Web of Science, and Scopus for studies published before December 19, 2025. The review included randomized controlled trials (RCTs) evaluating the efficacy and safety of BA compared to placebo in patients with hypercholesterolemia, including the Cholesterol Lowering via Bempedoic Acid, an ACL-Inhibiting Regimen (CLEAR) series of studies. Data from metaanalyses and other clinical trials were also considered.

The obtained results demonstrate that BA is the first oral adenosine triphosphate citrate lyase inhibitor, which plays an important role in the treatment of hypercholesterolemia. Due to tissue-specific activation mechanism, BA can be used in patients with statin intolerance. RCT data have demonstrated that when added to maximum-tolerated doses of statins, BA provides an additional reduction in low-density lipoprotein cholesterol (LDL-C) by 15-23%. In monotherapy, in patients with statin intolerance, LDL-C reduction reaches 23-27%. The combination of BA and ezetimibe demonstrated a reduction in LDL-C by 38-45%, and with high doses of statins, BA, and ezetimibe, a reduction of 68%. BA therapy also helps reduce high-sensitivity C-reactive protein levels by 19-32%. Longterm BA use is associated with a 13% reduction in the risk of cardiovascular events compared to placebo, with a favorable safety profile. A subanalysis of the CLEAR studies showed that BA does not increase the incidence of type 2 diabetes.

Thus, BA is an effective and safe lipid-lowering agent that reduces the risk of major cardiovascular events and can be used both as monotherapy and in combination with other lipid-lowering agents.

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