Drug intelligence / Profile preview

bempedoic acid + evolocumab

Development stage
Unknown
Lead developer
Esperion Therapeutics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Subcutaneous
01

Overview

**Bempedoic acid + evolocumab** is a combination therapy of an oral small-molecule ATP-citrate lyase inhibitor (bempedoic acid) and a subcutaneous monoclonal antibody PCSK9 inhibitor (evolocumab), indicated primarily for lowering low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia, especially those intolerant to statins or not reaching LDL-C targets with other therapies. - **Bempedoic acid** acts by inhibiting hepatic ATP-citrate lyase, blocking the cholesterol biosynthesis pathway upstream of HMG-CoA reductase, and activating AMP-activated protein kinase (AMPK), which also reduces gluconeogenesis and exerts anti-inflammatory effects via downregulation of C-reactive protein and other proinflammatory markers[2][4]. - **Evolocumab** is a monoclonal antibody targeting proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 normally binds LDL receptors on hepatocytes and promotes their degradation; inhibition leads to increased receptor recycling and greater removal of LDL-C from plasma[3]. Combining these agents provides additive LDL-C lowering, as demonstrated in clinical studies, and is considered for patients unable to achieve target lipid levels with monotherapy[1][5].

02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)PCSK9 (Proprotein convertase subtilisin/kexin type 9)ACLY (ATP-citrate synthase)

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