Nexletol 180mg Tablets
It is used to lower cholesterol.It is used to lower the chance of heart attack and certain heart procedures in some people.
Drug Class
Lipid-modifying agent
Pharmacologic Class
Adenosine triphosphate-citrate lyase (ACL) inhibitor
Pregnancy Category
Not available
FDA Approved
Feb 2020
DEA Schedule
Not Controlled
Overview
What is this medicine?
Nexletol is a medication used to lower 'bad' cholesterol (LDL-C) in your blood. It works by blocking an enzyme in your liver that helps make cholesterol. This helps your liver remove more cholesterol from your blood, reducing your risk of heart problems. It's often used when statins alone aren't enough or if you can't take statins.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food. It's essential to continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry location, avoiding the bathroom. Keep your medication in its original container, and do not remove the antimoisture cube or packet. Ensure that all medications are kept in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food. It's essential to continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry location, avoiding the bathroom. Keep your medication in its original container, and do not remove the antimoisture cube or packet. Ensure that all medications are kept in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Continue to follow a cholesterol-lowering diet as recommended by your doctor or dietitian.
- Engage in regular physical activity as advised by your healthcare provider.
- Maintain a healthy weight.
- Avoid smoking.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
180 mg orally once daily
Dose Range:
180 - 180 mg
Condition-Specific Dosing:
hyperlipidemia:
180 mg orally once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
Limited experience; use with caution. Not studied in patients with eGFR <30 mL/min/1.73 m2 or ESRD on dialysis.
Dialysis:
Not studied in patients on dialysis; use with caution.
Hepatic Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
Not studied; use with caution (Child-Pugh C).
Pharmacology
Mechanism of Action
Bempedoic acid is a prodrug that requires activation by very long-chain acyl-CoA synthetase 1 (ACSVL1) to bempedoyl-CoA. Bempedoyl-CoA inhibits adenosine triphosphate-citrate lyase (ACL), an enzyme upstream of HMG-CoA reductase in the cholesterol biosynthesis pathway. Inhibition of ACL decreases cholesterol synthesis in the liver, which leads to upregulation of LDL receptors and increased uptake of LDL-C from the blood.
Pharmacokinetics
Absorption:
Bioavailability:
Not determined (absolute bioavailability)
Tmax:
3.5 hours (median)
FoodEffect:
No clinically significant effect of food on absorption.
Distribution:
Vd:
18 L (bempedoic acid), 29 L (active metabolite ESP15228)
ProteinBinding:
Approximately 99% (bempedoic acid and active metabolite ESP15228)
CnssPenetration:
Limited (prodrug activated primarily in the liver)
Elimination:
HalfLife:
15-24 hours (bempedoic acid and active metabolite ESP15228)
Clearance:
Not available
ExcretionRoute:
Primarily renal (70% as metabolites), fecal (30%)
Unchanged:
<5% (unchanged drug in urine)
Pharmacodynamics
OnsetOfAction:
Within 2 weeks (LDL-C reduction)
PeakEffect:
Approximately 4 weeks (maximal LDL-C reduction)
DurationOfAction:
Sustained with continued daily dosing
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of gallstones, including:
+ Sudden pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
Feeling extremely tired or weak
Difficulty urinating or changes in urine output
Blood in the urine
High uric acid levels, which may cause:
+ Painful, red, hot, tender, stiff, or swollen joints, particularly in the big toe
Increased risk of tendon tear or injury, especially in people over 60 years old, those taking steroid drugs or certain antibiotics, those with kidney failure, or those with a history of tendon problems. Seek medical attention immediately if you experience:
+ Pain, bruising, or swelling in the back of the ankle, shoulder, arm, or other joints
+ Inability to move or put weight on a joint
+ A snapping or popping sound in a joint
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Signs of a common cold
Flu-like symptoms
Back pain
Stomach pain
Muscle spasms
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of gallstones, including:
+ Sudden pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
Feeling extremely tired or weak
Difficulty urinating or changes in urine output
Blood in the urine
High uric acid levels, which may cause:
+ Painful, red, hot, tender, stiff, or swollen joints, particularly in the big toe
Increased risk of tendon tear or injury, especially in people over 60 years old, those taking steroid drugs or certain antibiotics, those with kidney failure, or those with a history of tendon problems. Seek medical attention immediately if you experience:
+ Pain, bruising, or swelling in the back of the ankle, shoulder, arm, or other joints
+ Inability to move or put weight on a joint
+ A snapping or popping sound in a joint
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Signs of a common cold
Flu-like symptoms
Back pain
Stomach pain
Muscle spasms
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or feeling unwell (could be a sign of muscle damage).
- Sudden, severe joint pain, swelling, or redness (especially in the big toe, ankle, or knee), which could indicate gout.
- Unusual tiredness, loss of appetite, upper belly pain, dark urine, or yellowing of the skin or eyes (signs of liver problems).
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
If you are currently taking pravastatin or simvastatin, as these medications may interact with this drug.
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing treatments and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
If you are currently taking pravastatin or simvastatin, as these medications may interact with this drug.
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing treatments and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. If you have a history of gout, be sure to discuss this with your doctor. If you become pregnant or suspect you may be pregnant while taking this drug, contact your doctor immediately to discuss the potential risks and necessary precautions.
Overdose Information
Overdose Symptoms:
- No specific symptoms of overdose have been reported in clinical trials. In case of overdose, general supportive measures should be taken.
What to Do:
Contact your local poison control center (e.g., 1-800-222-1222) or seek emergency medical attention immediately.
Drug Interactions
Moderate Interactions
- Simvastatin (do not exceed 20 mg daily)
- Pravastatin (do not exceed 40 mg daily)
- Atorvastatin (monitor for adverse effects)
- Rosuvastatin (monitor for adverse effects)
- Lovastatin (monitor for adverse effects)
Monitoring
Baseline Monitoring
Lipid Panel (LDL-C, non-HDL-C)
Rationale: To establish baseline lipid levels and assess need for therapy.
Timing: Prior to initiation of therapy
Liver Enzymes (ALT, AST)
Rationale: To establish baseline liver function, as transaminase elevations have been reported.
Timing: Prior to initiation of therapy
Uric Acid
Rationale: To establish baseline uric acid levels, especially in patients with a history of gout or hyperuricemia, as bempedoic acid can increase uric acid.
Timing: Prior to initiation of therapy
Routine Monitoring
Lipid Panel (LDL-C, non-HDL-C)
Frequency: Periodically, typically 4-8 weeks after initiation or dose adjustment, then every 3-6 months
Target: Individualized based on patient risk and treatment goals (e.g., LDL-C <70 mg/dL or <55 mg/dL for high-risk patients)
Action Threshold: If LDL-C goals are not met, consider adherence, dose adjustment of concomitant therapies, or addition of other lipid-lowering agents.
Liver Enzymes (ALT, AST)
Frequency: Periodically, as clinically indicated or if symptoms of liver injury occur
Target: Within normal limits
Action Threshold: If persistent elevations >3x ULN occur, consider dose reduction or discontinuation.
Uric Acid
Frequency: Periodically, as clinically indicated, especially in patients with a history of gout or hyperuricemia
Target: Within normal limits or patient-specific target
Action Threshold: If clinically significant hyperuricemia or symptoms of gout develop, consider appropriate management or discontinuation.
Symptom Monitoring
- Muscle pain, tenderness, or weakness (especially if accompanied by fever or malaise)
- Signs and symptoms of gout (e.g., acute onset of severe joint pain, swelling, redness, warmth, particularly in the big toe)
- Symptoms of liver injury (e.g., unusual fatigue, anorexia, right upper quadrant abdominal pain, dark urine, jaundice)
Special Patient Groups
Pregnancy
Contraindicated. Based on animal studies, bempedoic acid may cause fetal harm. Discontinue Nexletol when pregnancy is recognized. There are no available data on Nexletol use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm based on animal data.
Second Trimester:
Potential for fetal harm based on animal data.
Third Trimester:
Potential for fetal harm based on animal data.
Lactation
Not recommended. There are no data on the presence of bempedoic acid in human milk, the effects on the breastfed infant, or the effects on milk production. Due to the potential for serious adverse reactions in a breastfed infant, advise women not to breastfeed during treatment with Nexletol.
Infant Risk:
Unknown, but potential for serious adverse reactions.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly (âĨ65 years) and younger patients. No dose adjustment is necessary based on age.
Clinical Information
Clinical Pearls
- Bempedoic acid is a prodrug that is activated primarily in the liver, leading to liver-specific ACL inhibition and reduced systemic exposure to the active form, which may contribute to its favorable muscle-related side effect profile compared to statins.
- It is typically used in combination with maximally tolerated statin therapy or in patients who are statin-intolerant and require additional LDL-C lowering.
- Patients should be monitored for increases in uric acid levels and symptoms of gout, especially those with a history of hyperuricemia or gout.
- Transient elevations in liver enzymes (ALT/AST) have been observed; monitor periodically.
- When co-administered with simvastatin or pravastatin, specific dose limitations apply due to increased statin exposure.
Alternative Therapies
- Statins (e.g., atorvastatin, rosuvastatin, simvastatin)
- Ezetimibe
- PCSK9 inhibitors (e.g., evolocumab, alirocumab)
- Fibrates (e.g., fenofibrate, gemfibrozil)
- Niacin (nicotinic acid)
- Bile acid sequestrants (e.g., cholestyramine, colesevelam)
Cost & Coverage
Average Cost:
$350-$450 per 30 tablets
Insurance Coverage:
Tier 2 or 3 (Specialty Drug)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to consult with your pharmacist. If you have any questions or concerns about this medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount, and the time it occurred.