Bempedoicacid/ezetimibe: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on Nov 20, 2023.

1. How it works

• Bempedoic acid/ezetimibe is sold under the brand (trade) name Nexlizet and it is a combination tablet that contains bempedoic acid and ezetimibe which are two medicines that help lower high cholesterol.
• Ezetimibe works by reducing cholesterol absorption from the small intestine. It targets the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols and reduces total and LDL (bad) cholesterol levels in the blood and belongs to the class of medicines known as cholesterol absorption inhibitors.
• Bempedoic acid is a new type of cholesterol-lowering medication that works in the same way as statins - lowering the production of cholesterol by the liver - but is not a statin. Bempedoic acid is a prodrug and is only converted to an active drug once in the liver, not in the muscles. Bempedoic acid belongs to the class of medicines known as adenosine triphosphate-citrate lyase (ACL) inhibitors.
• Bempedoic acid/ezetimibe belongs to the class of medicines known as antihyperlipidemic combinations.

2. Upsides

• Bempedoic acid/ezetimibe is used to lower LDL-C (low-density lipoprotein C) levels in adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease whose LDL-C levels are still high despite maximally tolerated statin treatment and a cholesterol-lowering diet.
• Taken as one tablet, once a day. One tablet of Nexlizet (bempedoic acid/ezetimibe) contains 180 mg of bempedoic acid and 10 mg of ezetimibe.
• Can be taken with or without food.
• Bempedoic acid/ezetimibe can be taken with or without other cholesterol-lowering medications like statins, fenofibrate, or bile-acid sequestrants that also help to lower lipids. These medicines work differently and have a complementary effect to bempedoic acid/ezetimibe. Administer bempedoic acid/ezetimibe at least 2 hours before or at least 4 hours after bile acid sequestrants.
• No dosage adjustments are recommended for people with kidney disease, mild liver disease, or due to advanced age; however, bempedoic acid/ezetimibe has not been studied in people with moderate to severe liver disease and is not recommended in patients with moderate or severe hepatic impairment.
• Bempedoic acid/ezetimibe has not been shown to result in changes in blood pressure.

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:

• Upper respiratory tract infections, muscle spasms, high uric acid levels, pain, elevated liver enzymes, diarrhea, sinusitis, and feeling tired have been reported in people using either bempedoic acid or ezetimibe.
• 11% of people taking bempedoic acid (a component of Nexlizet) discontinued treatment because of side effects. The most common reasons for stopping treatment were muscle spasms, diarrhea, and pain.
• Although bempedoic acid/ezetimibe has been shown to lower LDL-C levels, it will not help you lose weight, nor should you gain weight. While you are taking bempedoic acid/ezetimibe you should also be following a low-fat diet and weight loss may occur if you are eating fewer calories as a result of this diet.
• Bempedoic acid/ezetimibe has not been shown to prevent heart disease or heart attacks.
• Serious allergic reactions can happen in some people. Signs of an allergic reaction may include a rash or hives; swelling of the face, lips, tongue, and/or throat that may cause trouble breathing or swallowing; joint pain and muscle aches; changes in laboratory tests; liver problems; stomach pain; inflammation of the pancreas; nausea; dizziness; tingling sensation; depression; headache; gallstones; inflammation of the gallbladder.
• Bempedoic acid/ezetimibe has not been studied in children and is recommended only for adults over the age of 18.
• Bempedoic acid inhibits renal tubular OAT2 and may increase blood uric acid levels. In some studies, uric acid levels increased in 26% of bempedoic acid-treated patients with normal baseline uric acid values (the average increase after 12 weeks was 0.8 mg/dL), versus 9.5% of those treated with a placebo. In 3.5% of patients increases in uric acid were clinically significant. Increases in uric acid levels usually occurred within the first 4 weeks of starting treatment and persisted throughout treatment. This may increase a person's risk of developing gout. Monitor for gout throughout treatment.
• Bempedoic acid may also slightly increase a person's risk of tendon rupture or injury (0.5% of people treated with bempedoic acid experienced a tendon injury that involved the rotator cuff of the shoulder, biceps tendon, or Achilles tendon, compared with 0% of people assigned placebo). May occur within weeks to months of starting Nexlizet and people over the age of 60, taking corticosteroid or fluoroquinolone drugs, with renal failure, or with previous tendon disorders are more at risk. Discontinue bempedoic acid/ezetimibe immediately if tendon rupture occurs. Consider discontinuing bempedoic acid/ezetimibe if the patient experiences joint pain, swelling, or inflammation. Advise patients to rest at the first sign of tendinitis or tendon rupture and to contact their healthcare provider immediately. Bempedoic acid/ezetimibe may not be the preferred lipid-lowering medicine in those with a history of tendon disorders or tendon rupture.
• Bempedoic acid/ezetimibe may interact with other medications. Combining bempedoic acid/ezetimibe with a statin can cause an increase in statin concentrations and may increase the risk of myopathy. Restrict statin doses, for example, simvastatin to 20 mg or pravastatin to 40mg. See below for a full list of interactions.
• Bempedoic acid/ezetimibe has not been studied in pregnant women but generally, lipid-lowering treatments are not recommended in pregnant women. Discontinue bempedoic acid/ezetimibe when pregnancy is recognized and breastfeeding is not recommended with bempedoic acid/ezetimibe.
• Bempedoic acid/ezetimibe is only available as the branded drug Nexlizet. There is no generic form of bempedoic acid/ezetimibe currently available.

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

• The combination of bempedoic acid and ezetimibe decreases LDL-C levels by more than either drug alone. It is usually given in combination with other cholesterol-lowering treatments. Bempedoic acid/ezetimibe is only available as the branded drug, Nexlizet. Bempedoic acid/ezetimibe is usually well-tolerated, but it may increase a person's risk of gout or tendon rupture, and it is unknown if it reduces the risk of dying from cardiovascular disease.

5. Tips

• Take one tablet, once daily, with or without food. May be taken at any time of the day (morning or night); however, it is best to be consistent with the time you take your tablets.
• Take your medicine exactly as directed by your doctor. Do not change your dose or stop treatment unless recommended by your doctor.
• If you are taking another medicine to help control your cholesterol, your doctor should have let you know if you can take it at the same time as you take bempedoic acid/ezetimibe. If they haven't, ask them. Taking statins such as pravastatin or simvastatin with bempedoic acid/ezetimibe may increase your risk of muscle injury. Be alert for muscle pain.
• You will need to follow a cholesterol-lowering diet and exercise plan while on this medicine. Ask your doctor if you need diet information. If you smoke, ask your doctor how you can quit.
• Contact your doctor immediately if you notice any yellowing of your skin or eyes, shortness of breath, unexplained cough, severe muscle pain, tenderness, or weakness. Ask your doctor how to recognize liver problems.
• If you are a female of childbearing age you should use an effective method of birth control to prevent pregnancy while using bempedoic acid/ezetimibe.
• Bempedoic acid/ezetimibe may increase your risk of developing gout because it can increase uric acid levels. Tell your doctor if you develop any painful joint swelling. The risk is higher in people who have had gout before.
• Bempedoic acid/ezetimibe may increase your risk of rupturing a tendon and you should tell your doctor immediately and rest if you experience joint pain, swelling, inflammation, or tendon rupture.
• It is important to tell your doctor and pharmacist about all other medications you use, including prescription drugs, over-the-counter (OTC medicines) vitamins, herbs, and dietary supplements. Do not stop using any medications without first talking to your doctor.

6. Response and effectiveness

• The effectiveness of bempedoic acid/ezetimibe was investigated in 301 patients with heterozygous familial hypercholesterolemia, established atherosclerotic cardiovascular disease, or multiple risk factors for cardiovascular disease on maximally tolerated statin therapy. After 12 weeks, the mean LDL-C level decreased by 36% in those taking bempedoic acid/ezetimibe, compared with 17% in those taking only bempedoic acid alone, and by 23% in those taking ezetimibe alone. In those assigned to placebo, LDL-C levels increased by 2%.
• After initiating bempedoic acid/ezetimibe, analyze lipid levels within 8 to 12 weeks.
• More studies are needed to determine if taking bempedoic acid/ezetimibe reduces your risk of cardiovascular disease or dying from cardiovascular disease.

7. Interactions

Medicines that interact with bempedoic acid/ezetimibe 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.

No specific drug interaction studies have been conducted with bempedoic acid/ezetimibe in combination. The following are interactions that have been reported with either bempedoic acid or ezetimibe:

• Atogepant for migraine (may increase blood levels)
• Bile acid sequestrants: Take bempedoic acid/ezetimibe either 2 hours before or 4 hours after taking a bile acid sequestrant (such as cholestyramine). Taking these medicines at the same time may reduce the absorption and effectiveness of bempedoic acid/ezetimibe
• Cyclosporine: Combining bempedoic acid/ezetimibe with cyclosporine may increase the blood levels of ezetimibe and cyclosporine and worsen side effects for one or both drugs. Speak to your doctor before you combine these two medicines. Your blood levels of cyclosporine may need to be monitored
• Fexofenadine (may increase blood levels)
• Fibrates: Coadministration of bempedoic acid/ezetimibe with fibrates other than fenofibrate is not recommended until further studies are completed
• Methotrexate (may increase blood levels)
• Nalidixic acid for urinary tract infections (may increase the risk of tendon rupture)
• Quinolone antibiotics, such as ciprofloxacin, may increase the risk of tendon rupture
• Steroids, such as betamethasone or budesonide may increase the risk of tendon rupture
• Red yeast rice (may increase side effects such as liver damage and rhabdomyolysis)
• Statins (may increase blood levels)
• Valsartan
• Warfarin: If you take the blood thinner warfarin with bempedoic acid/ezetimibe, your doctor will monitor your INR closely.

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

References

• Bempedoic acid and ezetimibe. Updated 07/2023. Cerner Multum. https://www.drugs.com/mtm/bempedoic-acid-and-ezetimibe.html

Further information

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

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

Copyright 1996-2024 Drugs.com. Revision date: November 20, 2023.

Medical Disclaimer