Nexletol: 7 things you should know

Medically reviewed by Leigh Ann Anderson, PharmD. Last updated on April 1, 2024.

1. How it works

• Nexletol (generic name: bempedoic acid) works by lowering the production of cholesterol in your liver. It blocks an enzyme needed to make LDL (“bad cholesterol”) and therefore lowers your cholesterol or other lipid levels.
• Administration of this medicine with a statin and diet may decrease 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 high lipid levels.
• Nexletol 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. Prodrugs are inactive when first taken. Once they are in your system, they are converted to an active medication.

2. Upsides

• Nexletol is a prescription medication used with a cholesterol-lowering diet and other LDL cholesterol-lowering medicines, OR used alone when use with other LDL-C lowering therapy is not possible, to reduce LDL-C ("bad" cholesterol) in adults with high blood cholesterol levels, including heterozygous familial hypercholesterolemia (HeFH). HeFH is an inherited condition that causes high levels of “bad” cholesterol called low density lipoprotein (LDL).
• It is also used to to lower the risk of heart attack and heart procedures like stent placement or bypass surgery, in adults who cannot 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.
• Taken as one tablet by mouth, once a day. It can be taken with or without food. No dose titration is needed.
• 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 differences in safety or effectiveness were observed between patients 65 years and older when compared to younger patients, but greater sensitivity in older patients cannot be ruled out. No dosage adjustments are recommended based on advanced age.
• Dose changes of Nexletol are not needed when administered with atorvastatin (Lipitor) or rosuvastatin (Crestor), based on product labeling, but you may not be able to use Nexletol with some other statins. Check with your doctor.

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 count), bronchitis (inflammation of lung airways), increased liver enzymes, kidney problems, gallstones or stomach pain are listed as some of the most common side effects.
• It is not known if Nexletol is safe and effective in people with severe kidney problems. This includes people with end-stage kidney disease, those on dialysis, with severe liver problems. Safety and effectiveness in children under the age of 18 years has not been determined.
• Depending on your statin dose, you may not be able to use the statin medications simvastatin (Zocor) or pravastatin with Nexletol. Check with your doctor.
• Tendon rupture has occurred in people using Nexletol. You may not be able to use this medicine if you have a history of tendon disorders or tendon rupture. Tendons are tough cords of tissue that connect muscles to bones. 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 Nexletol at the first sign of tendon rupture and contact your healthcare provider.
• Elevations in serum uric acid have occurred and may lead to gout. It may occur within the first month of 4 of starting treatment and may continue. Your doctor may monitor you regularly for elevated uric acid levels.
• There is no available data on use in pregnant women. The risk of major birth defects, miscarriage, or other side effects in the mother or fetus are unknown. However, based on it's mechanism of action, it may cause fetal harm.
• Breastfeeding is not recommended with Nexletol.
• There are currently no generic alternatives for Nexletol. It can be an expensive medicine if your insurance does not cover it. Prescription coupons may help to offset your cost. The manfacturer, Esperion Therapeutics, may be able to offer a copay card or financial assistance. You can contact them at 1-833-639-5386, Monday-Friday, 8:00 AM-8:00 PM ET.

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

• Nexletol has been shown in studies to decrease LDL-C (“bad cholesterol”) levels and is used in combination with a statin, another type of cholesterol-lowering medicine. Nexletol is an oral medicine and 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 the shoulders, arms or legs. Your healthcare provider will schedule a blood test to check your cholesterol levels 8 to 12 weeks after you start treatment.

5. Tips

• Contact your doctor if you have any side effects that bother you or do not go away.
• Tell your healthcare provider if you have ever had a serious allergic reaction this medicine; it has been reported to cause serious allergic reactions with symptoms such as angioedema (swelling), wheezing, rash, and urticaria (hives). Do not use Nexletol if you have had a previous serious allergic reaction to bempedoic acid or any of the inactive ingredients in Nexletol.
• Your healthcare provider will schedule a laboratory test to analyze your blood lipid levels within 8 to 12 weeks after you start Nexletol treatment.
• Taking statins with Nexletol may increase your risk of muscle injury. Contact your healthcare provider if you experience muscle pain.
• 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).
• 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 kidney or liver problems before you start taking Nexletol.
• Call your doctor 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.
• Tell your healthcare provider right away 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.
• Breastfeeding is not recommended with Nexletol. If you are breastfeeding or plan to breastfeed, tell your doctor before treatment. It is not known if Nexletol 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.
• 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, the best food choices and regular exercise. 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 taking 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, Nexletol was evaluated in adults with heterozygous familial hypercholesterolemia (HeFH) or established heart disease (ASCVD) whose LDL-C levels were still high despite statin treatment at the highest tolerated dose, alone or with other lipid-lowering therapies.
• In one study (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, Nexletol lowered LDL-C levels by a mean of 18% compared to placebo, a statistically significant effect. In another study (Study 2), Nexletol was added to the maximally tolerated statin dose (including no statin at all) either alone or with other lipid-lowering therapies. At 12 weeks, Nexletol 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 Nexletol might decrease its intended effect, increase its side effects, or change how well 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 Nexletol with doses of simvastatin greater than 20 mg or doses of pravastatin greater than 40 mg. This may cause an increase in the statin level and may cause or worsen myopathy (a type of muscle damage, which can be serious).
• There are no known food or beverage interactions with Nexletol, 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 Nexletol is used concomitantly with drugs that are substrates of OATP1B1 or 1B3, particularly those with a narrow therapeutic range.
• Concomitant administration of Nexletol 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 Nexletol. 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 Dec. 2023. Accessed Sept. 27, 2023 at https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/211616s015lbl.pdf
• Nexletol.com. Esperion Therapeutics. Ann Arbor, MI. Accessed Sept 27, 2023 at https://www.nexlizethcp.com/nexletol-efficacy-safety-dosing
• Drug Safety-related Labeling Changes (SrLC). FDA. Nexlizet. Accessed Sept 27, 2023 at https://www.accessdata.fda.gov/scripts/cder/safetylabelingchanges/index.cfm?event=searchdetail.page&DrugNameID=2850
• U.S. FDA Updates LDL-C Lowering Indication for Esperion’s Nexletol (bempedoic acid) Tablet and Nexlizet (bempedoic acid and ezetimibe) Tablet. Dec. 13, 2023. Drugs.com. Accessed Dec. 20, 2023 at https://www.drugs.com/newdrugs/u-s-fda-updates-ldl-c-lowering-indication-esperion-s-nexletol-bempedoic-acid-tablet-nexlizet-6167.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use nexletol 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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