Bempedoic acid for the treatment of hypercholesterolemia

ABSTRACT

Introduction

Although several lipid-lowering drugs are available, they are not sufficient for some patients. Bempedoic acid is a small molecule adenosine triphosphate-citrate lyase inhibitor indicated for the treatment of adults with hypercholesterolemia.

Areas covered

We performed a systematic review of the literature using PubMed database, and the following keywords were used: ‘bempedoic acid,’ ‘hypercholesterolemia,’ and ‘adenosine triphosphate citrate lyase.’ The chemical property, mechanism of action, pharmacokinetics, clinical efficacy, and safety of bempedoic acid are introduced in this paper.

Expert opinion

Bempedoic acid can modulate the metabolism of cholesterol. Clinical trials indicated that bempedoic acid could significantly reduce low-density lipoprotein cholesterol levels. Bempedoic acid was well tolerated.

KEYWORDS:

• Adenosine triphosphate-citrate lyase
• bempedoic acid
• cardiovascular disease
• hypercholesterolemia
• low-density lipoprotein cholesterol

Article highlights

• Bempedoic acid is an ACL inhibitor.

• C_max is 20.6 µg/mL, AUC is 289.0 µg∙h/mL, the apparent volume distribution is 18 L, plasma protein binding is 99.3%, the half-life is 21 h, clearance is 11.2 mL/min.

• The recommended dose is 180 mg administered orally once daily.

• Common adverse reactions include upper respiratory tract infection, muscle spasms, hyperuricemia, back pain, abdominal pain or discomfort, bronchitis, pain in extremity, anemia, and elevated liver enzymes.

• Clinical trial:

• Phase 2: NCT01262638, NCT01751984, NCT02659397, NCT02072161, NCT01607294.

• Phase 3: NCT02988115, NCT02991118, NCT02666664, NCT03337308,

• NCT03001076

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose. 

Additional information

Funding

This paper was not funded.