Bempedoic acid: 7 things you should know

Medically reviewed by Leigh Ann Anderson, PharmD. Last updated on Sep 26, 2023.

1. How it works

• Bempedoic acid works by lowering the production of cholesterol in the liver. It blocks an enzyme needed to make LDL (“bad cholesterol”).
• Bempedoic acid is a prescription medication used along with diet and other lipid-lowering medicines in adults to help lower high cholesterol. It is not a statin drug, but is used alongside statin treatments.
• Bempedoic acid belongs to the class of medicines known as adenosine triphosphate-citrate lyase (ACL) inhibitors. It’s a prodrug and is converted to an active drug in the liver.
• Administration of bempedoic acid with a maximum tolerated dose of a statin (with or without other lipid modifying agents) decreases LDL-C (low density lipoprotein cholesterol or “bad” cholesterol), non-high density lipoprotein cholesterol (non-HDL-C), apolipoprotein B (apo B), and total cholesterol (TC) in patients with hyperlipidemia.

2. Upsides

• Bempedoic acid is used to lower LDL-C (low-density lipoprotein C) levels in adults with heterozygous familial hypercholesterolemia or established heart disease whose LDL-C levels are still high despite maximally tolerated statin treatment and following a cholesterol-lowering diet.
• Taken as one tablet by mouth, once a day. It can be taken with or without food. No dose titration is needed.
• Is used with other cholesterol-lowering medications like statins, fenofibrate, or bile-acid sequestrants that also help to lower lipids.
• No dosage adjustments are recommended for people with mild or moderate kidney impairment, but there is limited experience in people with severe kidney disease or on dialysis.
• No dosage adjustments are recommended for people with mild to moderate liver impairment, but people with severe liver disease have not been studied.
• No dosage adjustments are recommended based on advanced age. No differences in safety or effectiveness were observed between patients 65 years and older, and younger patients. However, greater sensitivity in older patients cannot be ruled out.
• Dosing changes of bempedoic acid are not needed when administered with atorvastatin (Lipitor) or rosuvastatin (Crestor), according to the manufacturer.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Symptoms of the common cold or flu, muscle spasms, back pain, pain in the shoulders, legs or arms, anemia (low red blood cell counts, bronchitis (lung inflammation / infection), increased liver enzymes, or stomach pain. These are listed as some of the most common side effects.
• It is not known if bempedoic acid can decrease problems from high cholesterol, such as heart attacks, stroke, death, or other heart problems.
• It is not known if bempedoic acid is safe and effective in people with severe kidney problems including people with end-stage kidney disease who are on dialysis, severe liver problems, or in children under 18 years of age.
• In some cases, you may not be able to use simvastatin or pravastatin with bempedoic acid based upon your statin dose. Taking simvastatin or pravastatin with bempedoic acid may increase your risk of muscle pain or weakness.
• Tendon rupture has occurred in people using bempedoic acid. You may not be able to use bempedoic acid if you have a history of tendon disorders or tendon rupture. Symptoms of tendon problems may include pain, swelling, inflammation, and tears of tendons including the arm, shoulder, and back of the ankle (Achilles). Stop use of bempedoic acid at the first sign of tendon rupture and contact your doctor right away.
• Elevations in serum uric acid have occurred and may lead to gout. This has happened within 4 weeks of starting treatment and may continue.
• There are no available data on bempedoic acid use in pregnant women to evaluate for a risk of major birth defects, miscarriage, or other side effects in the mother or fetus. However, based on it's mechanism of action, it may cause fetal harm.
• Breastfeeding is not recommended with bempedoic acid.
• There are currently no generic alternatives for bempedoic acid (Nexletol). It can be an expensive medicine if your insurance does cover it, but the manufacturer, Esperion Therapeutics, may be able to offer financial assistance or a Nexletol copay card for eligible patients.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

• Bempedoic acid has been shown in studies to decrease LDL-C (“bad cholesterol”) levels and is given in combination with other cholesterol-lowering treatments. This medicine is usually well-tolerated, but it may infrequently increase your risk of gout or tendon rupture. In studies, the most common reason people stopped treatment was due to muscle spasms, diarrhea, and pain in an extremity, like arms or legs. It is not known if it can lower your risk of death due to heart disease, heart attack or stroke.

5. Tips

• Contact your doctor if you have any side effects that bother you or do not go away.
• Tell your doctor if you have ever had a serious allergic reaction this medicine; it has been reported to cause angioedema (swelling), wheezing, rash, and urticaria (hives).
• Your healthcare provider will schedule a laboratory appointment to analyze your blood lipid levels within 8 to 12 weeks after you start bempedoic acid treatment.
• If you have or have ever had gout, high uric acid levels or problems with your tendons, tell your healthcare provider before you start treatment. Let your doctor know if you have severe kidney or liver problems before you start taking bempedoic acid.
• Call your healthcare provider if you have the following symptoms of high uric acid and gout, such as severe foot pain especially in the toe joint; tender joints; warm joints; joint redness or joint swelling.
• Stop taking bempedoic acid and get emergency help right away if you have any signs or symptoms of a tendon rupture, such as you hear or feel a snap or pop in a tendon area, you have bruising right after an injury in a tendon area, or you are unable to move the affected area or put weight on the affected area.
• You may be at a higher risk of tendon rupture if you are over 60 years of age, take corticosteroids (like prednisone), are taking antibiotics (like a fluoroquinolone, which includes ciprofloxacin, levofloxcin and others), have kidney problems, have had tendon problems (like in your shoulder or ankle).
• Let your doctor know if you are pregnant or planning a pregnancy before treatment starts. Tell your healthcare provider right away if you become pregnant while taking this medicine. If you become pregnant during treatment, you and your doctor will decide if you should continue this medicine. If you are pregnant during bempedoic acid (Nexletol) treatment, you are encouraged to call Esperion at 1-833-377-7633 to share information about the health of you and your baby.
• If you are breastfeeding or plan to breastfeed, tell your doctor before treatment. It is not known if bempedoic acid passes into your breast milk.
• This medicine may be taken at any time of the day or night; however, you should try to take your medicine at the same time each day.
• Taking statins with bempedoic acid may increase your risk of muscle injury. Contact your doctor if you experience muscle pain.
• You will need to follow a cholesterol-lowering diet and exercise plan while taking this medicine. Ask your doctor if you need information on a diet plan or food choices. If you smoke, discuss options for a smoking cessation plan to help you quit. This may include medicine and group therapy.
• If you cannot afford this medicine, the manufacturer, Esperion Therapuetics, may be able to help you lower your costs. You can call them at 1-833-639-5386, Monday-Friday, 8:00 AM-8:00 PM ET.
• Do not stop using any medications without first talking to your doctor.

6. Response and effectiveness

• In two 52-week long, placebo-controlled studies with over 3,000 patients, bempedoic acid was evaluated in adults with heterozygous familial hypercholesterolemia or established heart disease whose LDL-C levels were still high despite statin treatment at the highest tolerated dose, alone or with other lipid-lowering therapies.
• In study 1, Nexletol was added to the maximally tolerated statin dose, either alone (with only the statin) or with other lipid-lowering therapies. At 12 weeks, bempedoic acid lowered LDL-C levels by a mean of 18% compared to placebo, a statistically significant effect.
• In study 2, bempedoic acid was added to the maximally tolerated statin dose (including no statin at all) either alone or with other lipid-lowering therapies. At 12 weeks, bempedoic acid lowered LDL-C levels by a mean of 17% compared to placebo, a statistically significant effect.
• In both trials, the maximum LDL-C lowering effects occurred at Week 4. Your healthcare provider will check your lipid levels 8 to 12 weeks after you start treatment.

7. Interactions

• Medicines that interact with bempedoic acid may either decrease its effect, increase its side effects, or change how other medicines work. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor or pharmacist about how drug interactions should be managed.
• Do not use bempedoic acid with doses of simvastatin (Zocor) greater than 20 mg or with doses of pravastatin greater than 40 mg. This may cause an increase in the statin level and may cause or worsen myopathy (muscle damage).
• There are no known food or beverage interactions with bempedoic acid, but because it may used alongside a statin or other cholesterol-lowring drug, there may interactions with those medicines (for example, grapefruit juice).
• Caution is advised if bempedoic acid is used concomitantly with drugs that are substrates of OATP1B1 or 1B3, particularly those with a narrow therapeutic range.
• Concomitant administration of bempedoic acid may potentiate the risk of tendon rupture or injury associated with fluoroquinolones (for example: ciprofloxacin or levofloxacin) and corticosteroids (such as prednisone, dexamethasone or methylprednisolone).
• Check with your pharmacist and doctor to review your medications for possible drug interactions with bempedoic acid. Tell your healthcare providers about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal or dietary supplements.

Note that this list is not all-inclusive and includes only common medications that may interact with bempedoic acid. Refer to the prescribing information for a complete list of interactions.

References

• Nexletol (bempedoic acid) prescribing information. Esperion Therapeutics. Ann Arbor, MI. Revised June 2023. Accessed Sept. 26, 2023 at https://pi.esperion.com/nexletol/nexletol-pi.pdf
• Nexletol.com. Esperion Therapeutics. Ann Arbor, MI. Accessed Sept 26, 2023 at https://www.nexlizethcp.com/nexletol-efficacy-safety-dosing
• Drug Safety-related Labeling Changes (SrLC). FDA. Nexlizet. Accessed Sept 26, 2023 at https://www.accessdata.fda.gov/scripts/cder/safetylabelingchanges/index.cfm?event=searchdetail.page&DrugNameID=2850

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use bempedoic acid only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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