Bempedoic Acid-Ezetimibe

Bempedoic Acid-Ezetimibe is a combination medication used as an adjunct to diet and maximally tolerated statin therapy for adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease who require additional lowering of low-density lipoprotein cholesterol (LDL-C).

• Bempedoic Acid-Ezetimibe is available under the following different brand names: Nexlizet

Common side effects of Bempedoic Acid-Ezetimibe include:

• upper respiratory tract infection
• muscle spasms
• high uric acid in the blood (hyperuricemia)
• back pain
• abdominal pain or discomfort
• bronchitis
• pain in extremities
• anemia
• elevated liver enzymes
• diarrhea
• joint pain
• sinusitis
• fatigue
• influenza
• increased risk of tendon rupture
• increased risk of gout

Serious side effects of Bempedoic Acid-Ezetimibe include:

• hives 
• rash
• severe itching
• skin redness or swelling
• wheezing, difficulty breathing
• feeling lightheaded; fast or pounding heartbeats; swelling of your face, lips, tongue, or throat
• tendon rupture—sudden pain, swelling, bruising, tenderness, stiffness, movement problems, or a snapping or popping sound in any of your joints (rest the joint until you receive medical care or instructions)
• low red blood cells (anemia)—pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands, and feet
• symptoms of gout—joint pain or swelling, warmth or redness around your joints, severe foot, or toe pain

Rare side effects of Bempedoic Acid-Ezetimibe include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 180 mg/10 mg

Hypercholesterolemia

Adult dosage

• 1 tablet (bempedoic acid 180 mg/ezetimibe 10 mg) orally once a day

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Bempedoic Acid-Ezetimibe has severe interactions with no other drugs
• Bempedoic Acid-Ezetimibe has serious interactions with the following drugs:
  • cyclosporine
  • leniolisib
  • trofinetide
  • zavegepant intranasal
• Bempedoic Acid-Ezetimibe has moderate interactions with the following drugs:
  • apalutamide
  • cholestyramine
  • encorafenib
  • fostemsavir
  • glecaprevir/pibrentasvir
  • letermovir
  • pravastatin
  • simvastatin
  • sofosbuvir/velpatasvir
• Bempedoic Acid-Ezetimibe has minor interactions with the following drugs:
  • fenofibrate
  • fenofibrate micronized
  • fenofibric acid
  • gemfibrozil
  • voclosporin

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Known hypersensitivity to ezetimibe, including anaphylaxis, angioedema, rash, and urticaria

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Bempedoic Acid-Ezetimibe?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Bempedoic Acid-Ezetimibe?”

Cautions

• Hyperuricemia
  • Bempedoic acid inhibits renal tubular OAT2 and may increase blood uric acid levels
  • Elevated uric acid levels usually occur within the first 4 weeks of treatment initiation and persist throughout treatment; elevated blood uric acid may lead to gout
• Tendon rupture
  • Bempedoic acid is associated with an increased risk of tendon rupture or injury
  • Tendon rupture occurred within weeks to months of initiating
  • May occur more frequently in patients aged 60 years and older
    • Discontinue immediately if tendon rupture occurs
• Consider discontinuing joint pain, swelling, or inflammation
• Drug interaction overview
• Simvastatin or pravastatin
  • Bempedoic acid increases simvastatin or pravastatin serum concentrations which, may increase simvastatin/pravastatin-related myopathy
  • Avoid use with simvastatin doses of more than 20 mg
  • Avoid use with pravastatin doses of more than 40 mg
  • Atorvastatin and rosuvastatin: Elevations of 1.7-fold in AUC of atorvastatin, rosuvastatin, and/or their major metabolites were observed with bempedoic acid coadministration, suggesting a weak interaction; these elevations were generally within the individual statin exposures and do not affect dosing recommendations
• Cyclosporine
  • Coadministration of cyclosporine and ezetimibe increases both cyclosporine and ezetimibe concentrations
  • If coadministered, monitor cyclosporine concentrations
• Fibrates
  • Both fenofibrate and ezetimibe may increase cholesterol excretion into the bile, leading to cholelithiasis
  • Coadministration of ezetimibe with fibrates other than fenofibrate is not recommended
  • If cholelithiasis is suspected, gallbladder studies are indicated
  • Consider alternative lipid-lowering therapies
• Cholestyramine
  • Coadministration of cholestyramine and ezetimibe decreases ezetimibe concentration, which may lead to reduced efficacy
  • Administer ezetimibe-containing products at least 2 hours before or 4 hours after bile acid sequestrants

Pregnancy and Lactation

• Discontinue Bempedoic Acid-Ezetimibe when pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus
• Decreases cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol; therefore, Bempedoic Acid-Ezetimibe may cause fetal harm when administered to pregnant women based on the mechanism of action
• No available data regarding use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
• NOTE: Statins are contraindicated in pregnant women
• Clinical considerations
  • Treatment of hyperlipidemia is not generally necessary during pregnancy
  • Cholesterol and cholesterol derivatives are needed for normal fetal development
• Lactation
  • Data are not available regarding the drug presence of bempedoic acid in human or animal milk, its effects on breastfed infants, or its effects on milk production; ezetimibe is present in rat milk, and therefore is likely present in human milk
  • Since bempedoic acid and ezetimibe decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, these actions may cause harm to the breastfed infant
  • Based on the mechanism of action, advise patients that breastfeeding is not recommended during treatment