Nexletol dosage, forms, and strengths

Nexletol is a unique brand-name cholesterol-fighting drug. Approved by the U. S. Food and Drug Administration (FDA) in 2020, Nexletol is added to statin therapy in people with high cholesterol, atherosclerosis, or hereditary high cholesterol not controlled by diet and statin therapy. Its active ingredient, bempedoic acid, helps to decrease low-density lipoprotein cholesterol (LDL-C) by blocking the liver’s ability to make cholesterol. Like statins, Nexletol tablets are taken orally once daily. 

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Nexletol forms and strengths

Nexletol is taken in only one dosage form and one dosage strength. 

• Tablet: 180 mg

Nexletol dosage for adults

Nexletol is a new type of cholesterol drug used solely to lower cholesterol in people who are taking the maximum dose of a statin that they can tolerate. The use of Nexletol is limited to people with atherosclerosis or hereditary high cholesterol called familial hypercholesterolemia.

Nexletol dosage for high cholesterol

Nexletol is a new entrant in treating high cholesterol (hyperlipidemia). Still, its use is limited to people on maximally tolerated statin therapy who are diagnosed either with atherosclerotic cardiovascular disease (ASCVD) or a type of hereditary high cholesterol called heterozygous familial hypercholesterolemia (HeFH). It’s not approved as a stand-alone drug but as an adjunct, or add-on), to statin therapy. In clinical trials, participants taking a daily dose experienced an average reduction in LDL-C cholesterol levels of 18% when used with a statin.

The active ingredient in Nexletol is bempedoic acid. It is the sole member of a drug class called adenosine triphosphate-citrate lyase inhibitors (ACL inhibitors). After the liver converts bempedoic acid into its active form, that active form blocks an enzyme in the liver that is responsible for cholesterol synthesis. The overall result is further lowering LDL-C levels without increasing or decreasing the statin dose. 

Doses are taken by mouth once per day with or without food. The tablet can be taken with the daily statin dose. Doctors do not need to titrate the dose. The starting dose is the maintenance dose.

• Standard Nexletol dosage for high cholesterol: 180 mg tablet taken once per day with a statin 

RELATED: How long does it take to lower cholesterol?

Nexletol dosage for children

Nexletol is only FDA-approved for use in adults 18 and older. It hasn’t been determined if it’s safe or effective in children.

Nexletol dosage restrictions

No dose adjustments are needed for people with kidney disease or liver problems. However, Nexletol is a new drug that has been studied only in people with mild to moderate kidney or liver dysfunction. It has not yet been studied in people with severe renal impairment, end-stage renal failure, or severe hepatic impairment. Dosage restrictions or adjustments have yet to be specified for people with these conditions.

How to take Nexletol

Nexletol is taken as a tablet once per day. It doesn’t matter what time of day it’s taken or whether it’s taken with a meal or on an empty stomach.

• Your doctor will specify how much medicine to use. Use only as directed.

• Read the Patient Information sheet with this medicine before taking the first dose.

• Take one Nexletol tablet daily.

• If Nexletol doses cause stomach upset or similar problems, try taking the dose with food. 

• Store Nexletol tablets in their original bottle at room temperature.

Nexletol dosage FAQs

How long does it take Nexletol to work?

Nexletol’s effects on serum LDL cholesterol take a few weeks to affect blood test results. In placebo-controlled clinical trials, Nexletol produced its best results after 12 weeks of daily dosing, and continued dosing maintained those results for the next nine months.

How long does Nexletol stay in your system?

Bempedoic acid has a half-life of 21 hours, give or take 11 hours. That means it will take four days to a week to clear the last dose of Nexletol from the body.

What happens if I miss a dose of Nexletol?

Ask the prescribing doctor for medical advice about what to do if you miss a dose. Never take more than one dose in a single day.

How long can you take Nexletol?

Nexletol is designed for long-term or even lifelong use. Doctors will prescribe it if it is medically indicated because it is effective and is not known to cause serious side effects. In year-long clinical trials, no side effects due to long-term use were discovered.

How do I stop taking Nexletol?

Nexletol therapy can be stopped at any time without causing withdrawal symptoms. However, if an adequate replacement is not substituted, people may experience increased serum LDL-C levels. In some cases, patients should immediately stop taking the drug and contact the prescriber. These include allergic reactions and tendon rupture.

What is the maximum dosage for Nexletol?

The manufacturer and the FDA have not specified a maximum dosage. Consider the recommended dosage the most you should take in a day. 

Can you overdose on Nexletol?

Because Nexletol is a new medicine, there are no overdose cases that can tell us what kind of problems or symptoms an overdose could cause. If you take too much Nexletol, call a poison control center or go immediately to an emergency room.

What interacts with Nexletol?

As with all prescription drugs, Nexletol can cause problems when combined with some drugs. The prescriber will be familiar with these drug interactions, so make sure to tell the doctor about all prescription drugs, over-the-counter medications, and supplements being taken. If you receive all your medications from the same pharmacy, the pharmacist should look for medication interactions. 

Doctors are most concerned about combining Nexletol with the Zocor (simvastatin) statins or pravastatin. That may seem odd since Nexletol is meant to be taken with statins. These two statins, however, may cause problems. In both cases, Nexletol interferes with the body’s ability to break down these two drugs. As a consequence, Nexletol almost doubles the body’s exposure to these drugs and increases the risk of severe side effects like muscle damage. These two statins aren’t prohibited, but doses may need to be adjusted.

Nexletol can cause similar problems with the cholesterol drug ezetimibe or the gout drug probenecid. Both are relevant drug interactions. Ezetimibe might be prescribed with Nexletol. One brand-name drug, Nexlizet, combines both bempedoic acid and ezetimibe in a single tablet. On the other hand, Probenecid might be used to treat one of the serious side effects of Nexletol: high uric acid levels and gout.

Can Nexletol be taken with other cholesterol-lowering drugs?

Nexletol is not intended as a stand-alone treatment for high cholesterol. It is always combined with a statin in people at their maximally tolerated dose. Other cholesterol-lowering drugs can be used in addition to Nexletol and a statin. One version of Nexletol is Nexlizet, which combines bempedoic acid with ezetimibe, a drug commonly used alone or combined with a statin or fibrate cholesterol medication.

What happens when you mix Nexletol and alcohol?

Drinking is not forbidden or discouraged in people taking Nexletol. The only concern is that drinking too much alcohol injures the liver. Nexletol does not damage the liver but can disrupt its function as measured by liver enzyme levels. 

Is it safe to take Nexletol during pregnancy?

Women taking Nexletol should promptly stop taking Nexletol and inform the prescriber if they get pregnant. Healthcare professionals do not know how risky Nexletol is for pregnant women or the unborn baby because it hasn’t been studied. It is thought that fetal exposure to bempedoic acid may cause fetal harm. Animal studies suggest that bempedoic acid does not cause birth defects. However, the manufacturer and the FDA urge doctors to discontinue Nexletol in women who become pregnant.

Is it safe to take Nexletol while breastfeeding?

Breastfeeding is not recommended if a woman is taking Nexletol. No studies of Nexletol can tell us if Nexletol harms a nursing infant. However, based on Nexletol’s mechanism of action, healthcare professionals believe that the drug probably affects lactation and could produce adverse effects in an infant. 

What should I know about the possible side effects of Nexletol?

As with all prescription drugs, Nexletol can cause side effects. The most commonly experienced are upper respiratory tract infections, muscle spasms, an increase in uric acid (hyperuricemia which can cause gout), back pain, bronchitis, anemia, and elevated liver enzymes. Most people, however, won’t have problems. Only 2–5% of clinical trial participants reported each of these common side effects. 

What should I know about the risks of taking Nexletol?

Nexletol does have significant risks, including causing a gout flare and tendon rupture. 

One out of 66 people in clinical trials developed gout, a buildup of uric acid in the joints. Call the doctor if you notice signs of gout, such as severe foot pain, joint pain, warm joints, swelling, and redness.

Tendon rupture is a more serious problem and occurs in 1 out of 200 participants in clinical trials. It can happen within weeks of starting Nexletol. People who are older than 65, have a history of tendon problems or tendon disorders or are taking drugs like corticosteroids or fluoroquinolone antibiotics are most at risk. The tendons most likely affected are the Achilles tendon, shoulder tendon (rotator cuff), or biceps tendon. Watch for signs such as a sudden popping or snapping in a tendon, bruising around a tendon, pain, and inability to move the joint near the tendon. You must stop taking Nexletol immediately until you see a doctor about the tendon injury. The doctor will most likely discontinue Nexletol and switch to a different cholesterol-lowering drug.

Who should not take Nexletol?

There are no contraindications for Nexletol, so everyone who meets the diagnostic criteria can be prescribed Nexletol. Doctors may discontinue the medicine in some instances, such as during pregnancy or other side effects. 

What are the alternatives to Nexletol?

Healthcare providers have several other drugs that can be added to statin therapy to reduce LDL cholesterol. These include ezetimibe, bile acid sequestrants, Leqvio (inclisiran), and biologic drugs called PCSK9 inhibitors.

Sources

• Bempedoic acid, StatPearls

• Nexletol bempedoic acid tablet prescribing information, NIH National Library of Medicine

• Nexlizet/Nexletol consumer website, Esperion Therapeutics, Inc.

• Nexlizet/Nexletol HCP website, Esperion Therapeutics, Inc.