Bempedoic acid/ezetimibe

What is Bempedoic acid/ezetimibe?

• Bempedoic acid/ezetimibe (Nexlizet), contains an adenosine triphosphate-citrate lyase (ACL) inhibitor and a cholesterol absorption inhibitor.

Bempedoic acid

Ezetimibe

What are the uses of this medicine?

Bempedoic acid/ezetimibe (Nexlizet), is a prescription medicine that contains 2 cholesterol lowering medicines, bempedoic acid and ezetimibe. Nexlizet is used along with diet and other lipid-lowering medicines in the treatment of adults with:

• heterozygous familial hypercholesterolemia (HeFH). HeFH is an inherited condition that causes high levels of "bad" cholesterol called low density lipoprotein (LDL).
• known heart disease who need additional lowering of "bad" cholesterol (LDL-C) levels.

Limitations of use:

• It is not known if Nexlizet can decrease problems from high cholesterol, such as heart attacks, stroke, death, or other heart problems.
• It is not known if Nexlizet is safe and effective in people with severe kidney problems including people with end-stage kidney disease who are on dialysis.
• It is not known if Nexlizet is safe and effective in people with moderate to severe liver problems.

How does this medicine work?

• Nexlizet contains bempedoic acid and ezetimibe. Nexlizet reduces elevated LDL-C through inhibition of cholesterol synthesis in the liver and absorption in the intestine.

Bempedoic acid:

• Bempedoic acid is an adenosine triphosphate-citrate lyase (ACL) inhibitor that lowers low-density lipoprotein cholesterol (LDL-C) by inhibition of cholesterol synthesis in the liver.
• Bempedoic acid and its active metabolite, ESP15228, require coenzyme A (CoA) activation by very long-chain acyl-CoA synthetase 1 (ACSVL1) to ETC-1002-CoA and ESP15228-CoA, respectively.
• ACSVL1 is expressed primarily in the liver.
• Inhibition of ACL by ETC-1002-CoA results in decreased cholesterol synthesis in the liver and lowers LDL-C in blood via upregulation of low-density lipoprotein receptors.

Ezetimibe:

• Ezetimibe (e zet' i mibe) is a synthetic azetidinone that inhibits cholesterol absorption from the intestine.
• Ezetimibe acts by binding to and inhibiting the Niemann-Pick C1-like 1 protein (NPC1), the major transporter of cholesterol in the intestinal brush border.
• Ezetimibe by itself lowers serum cholesterol, but the inhibition of cholesterol absorption is usually followed by a compensatory increase in hepatic cholesterol synthesis, a response that can be blocked by hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors [statins].
• For this reason, ezetimibe is commonly used in combination with a statin.
• Addition of ezetimibe to a maximized dose of statins generally lowers LDL-cholesterol levels by 22% to 24%.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to ezetimibe tablets.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• simvastatin or pravastatin (other cholesterol lowering medicines). Taking simvastatin or pravastatin with Nexlizet may increase your risk of developing muscle pain or weakness (myopathy).
• cyclosporine (often used in organ transplant patients)
• fibrates (used to lower cholesterol)
• cholestyramine (used to lower cholesterol)

Is this medicine FDA approved?

• The combination was approved for medical use in the United States in February 2020, and in the European Union in March 2020.

How should this medicine be used?

Recommended dosage:

• The recommended dosage of Nexlizet, in combination with maximally tolerated statin therapy, is one tablet orally once daily. One tablet of Nexlizet contains 180 mg of bempedoic acid and 10 mg of ezetimibe.
• After initiation of Nexlizet, analyze lipid levels within 8 to 12 weeks.

Administration:

• Take Nexlizet exactly as your healthcare provider tells you to take it. Check with your healthcare provider or pharmacist if you are not sure.
• Take 1 Nexlizet tablet by mouth each day.
• Swallow the Nexlizet tablet whole. Do not cut, chew, or crush the tablet.
• You may take Nexlizet with or without food.
• If you take a medicine that lowers cholesterol by binding bile acids, such as colesevelam or cholestyramine, take Nexlizet at least 2 hours before or 4 hours after you take bile acid binding medicines. Ask your healthcare provider if you are not sure if you take these medicines.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 180 mg bempedoic acid/10 mg ezetimibe

This medicine is available in fallowing brand namesː

• Nexlizet

What side effects can this medication cause?

The most common side effects of this medicine may include:

• symptoms of the common cold, flu, or flu-like symptoms
• back pain
• bronchitis
• anemia
• diarrhea
• muscle spasms
• stomach pain
• pain in shoulder, legs, or arms
• increased liver enzymes
• fatigue

Less common, but serious side effects may include:

• hyperuricemia
• tendon rupture or injury

What special precautions should I follow?

• Bempedoic acid, a component of Nexlizet, inhibits renal tubular OAT2 and may increase blood uric acid levels. Advise patients to contact their healthcare provider if symptoms of hyperuricemia occur. Assess serum uric acid when clinically indicated. Monitor patients for signs and symptoms of hyperuricemia, and initiate treatment with urate-lowering drugs as appropriate.
• Bempedoic acid, a component of Nexlizet, is associated with an increased risk of tendon rupture or injury. Discontinue Nexlizet immediately if the patient experiences rupture of a tendon. Consider discontinuing Nexlizet 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 if tendinitis or tendon rupture symptoms occur. Consider alternative therapy in patients with a history of tendon disorders or tendon rupture.
• Advise patients to notify their healthcare provider(s) if they are taking, or plan to take simvastatin or pravastatin. The risk of myopathy occurring with the use of simvastatin or pravastatin may be increased when taken with Nexlizet.
• Advise pregnant women of the potential risk to a fetus based on Nexlizet's mechanism of action. Advise females to inform their healthcare provider of a known or suspected pregnancy.
• It is not known if Nexlizet passes into your breast milk. You and your healthcare provider should decide if you will take Nexlizet or breastfeed. You should not do both.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• There is no clinical experience with Nexlizet overdosage.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Discontinue Nexlizet when pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus.
• Tell your healthcare provider right away if you become pregnant while taking Nexlizet.
• You and your healthcare provider will decide if you should take Nexlizet while you are pregnant.
• If you are pregnant during Nexlizet treatment, you are encouraged to call Esperion at 1-833-377-7633 to share information about the health of you and your baby.

Can this medicine be used in children?

• It is not known if Nexlizet is safe and effective in children under 18 years of age.

What are the active and inactive ingredients in this medicine?

• Active ingredients: bempedoic acid and ezetimibe
• Inactive ingredients: colloidal silicon dioxide, hydroxy propyl cellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone K30, sodium lauryl sulfate, sodium starch glycolate
• Tablet coating: FD&C Blue #1/Brilliant Blue FCF Aluminum Lake, FD&C Blue #2/Indigo Carmine Aluminum Lake, glyceryl monocaprylocaprate, partially hydrolyzed polyvinyl alcohol, sodium lauryl sulfate, talc, and titanium dioxide

Who manufactures and distributes this medicine?

Manufactured by:

• Piramal Pharma Limited
• Madhya Pradesh, India

Manufactured for:

• Esperion Therapeutics, Inc.
• 3891 Ranchero Drive, Suite 150
• Ann Arbor, MI

What should I know about storage and disposal of this medication?

• Store Nexlizet in the original package at room temperature between 68ºF to 77ºF (20ºC to 25ºC).
• Protect from heat and moisture.
• Do not throw away the packet that helps to keep your medicine dry (desiccant).
• Nexlizet comes in a bottle with a child-resistant cap.

• Dailymed label info on Bempedoic acid/ezetimibe
• FDA Bempedoic acid/ezetimibe

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