What is Nexletol (bempedoic acid)?

From the Guidelines

Nexletol is a prescription medication containing bempedoic acid that helps lower LDL ("bad") cholesterol in adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease who need additional cholesterol lowering beyond statins. It works by inhibiting an enzyme called ATP-citrate lyase, which is involved in cholesterol production in the liver, thereby reducing the amount of cholesterol your body makes 1. Nexletol is typically taken as an 180 mg tablet once daily, with or without food, and is often prescribed alongside a healthy diet and other cholesterol-lowering medications. Unlike statins, Nexletol is not activated in skeletal muscle, which may make it an option for patients who experience muscle-related side effects with statins. Some key points to consider when prescribing Nexletol include:

• The dose is 180 mg orally once daily, with or without food 1
• Common side effects include upper respiratory tract infections, muscle spasms, back pain, abdominal pain, and elevated liver enzymes 1
• Nexletol should not be taken during pregnancy and is not recommended for people with severe kidney impairment or those on dialysis 1
• It may increase serum uric acid, and patients should be advised to contact their clinician if symptoms of hyperuricemia occur 1
• The medication has been shown to reduce LDL-C levels by approximately 24.5% compared with placebo in patients with statin-associated muscle symptoms on no statin therapy 1

From the FDA Drug Label

NEXLETOL is a prescription medicine used: to lower the risk of heart attack and heart procedures like stent placement or bypass surgery, in adults who are unable to take recommended statin treatment (a cholesterol-lowering medicine), or are not taking a statin, who: have known heart disease, or are at high risk for heart disease but without known heart disease along with diet and other cholesterol-lowering medicines, or alone when use with other cholesterol-lowering medicines is not possible, to reduce low-density lipoprotein (LDL, or bad cholesterol) in adults with high blood cholesterol levels called primary hyperlipidemia, including a type of high blood cholesterol called heterozygous familial hypercholesterolemia (HeFH)

Nexletol (bempedoic acid) is a prescription medicine used to lower the risk of heart attack and heart procedures, and to reduce low-density lipoprotein (LDL, or bad cholesterol) in adults with high blood cholesterol levels. 2

From the Research

What is Nexletol (Bempedoic Acid)?

• Nexletol, also known as bempedoic acid, is a medication used to lower low-density lipoprotein cholesterol (LDL-C) levels in patients with hypercholesterolemia 3, 4, 5, 6, 7.
• It is an oral, once-daily, ATP-citrate lyase inhibitor that works by inhibiting the enzyme adenosine triphosphate (ATP)-citrate lyase, which lies two steps upstream from β-hydroxy β-methylglutaryl-CoA reductase in the cholesterol biosynthesis pathway 5, 6.

Mechanism of Action

• Bempedoic acid is a prodrug that is selectively activated in the liver, which reduces hepatic cholesterol synthesis and increases the uptake of LDL-C from the blood 4, 5, 6.
• This mechanism of action avoids adverse muscle symptoms associated with statins, making it a suitable option for patients who are intolerant to statins 4, 5, 6.

Clinical Use

• Bempedoic acid is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia (HeFH) who require additional lowering of LDL-C 5, 7.
• It is also used in combination with statins (with or without ezetimibe) in patients who do not attain LDL goals despite administration of a statin at the maximum tolerated dose or in case of statin intolerance 6.

Efficacy and Safety

• Bempedoic acid has been shown to significantly lower LDL-C levels and other atherogenic lipoprotein measures, and high-sensitivity C-reactive protein when added to background lipid-lowering therapy in patients with and without statin intolerance 3, 4, 5.
• The safety profile of bempedoic acid is generally well-tolerated, with no clinically meaningful increase in muscle-related symptoms relative to placebo, even in patients taking maximally tolerated statins 3, 4, 5.