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November 16, 2025
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Brand Name :
Nexletol
Synonyms :
bempedoic acid
Class :
ACL Inhibitors, Lipid-Lowering Agents
Brand Name :
Nexletol
Synonyms :
bempedoic acid
Class :
ACL Inhibitors, Lipid-Lowering Agents
Dosage Forms & Strengths
Tablet
180 mg
Polygenic HypercholesterolemiaÂ
In combination with maximally tolerated statin therapy, take 180 mg orally each day
Dose Adjustments
Dosage Modifications
Renal impairment
No dosage modification required
Hepatic impairment
No dosage modification required
Dosing Considerations
Monitoring: once start taking, examine lipid levels within 8 to 12 weeks
Safety and efficacy not determined
Refer to adult dosing
may enhance the serum concentration
may enhance the serum concentration of ubrogepant
may enhance the serum concentration
may increase the levels of serum concentration of elagolix
OATP1B1/1B3 inhibitors increase the concentration of asunapravir in the serum
OATP1B1/1B3 inhibitors increase the concentration of elagolix in the serum
OATP1B1/1B3 inhibitors increase the concentration of elbasvir and grazoprevir in the serum
OATP1B1/1B3 inhibitors increase the concentration of active metabolites of revefenacin in the serum
OATP1B1/1B3 inhibitors increase the concentration of taurursodiol in the serum
OATP1B1/1B3 inhibitors increase the concentration of voxilaprevir in the serum
may enhance the serum concentration of elbasvir/grazoprevir
OATP1B1/1B3 (SLCO1B1/1B3) inhibitors increase the concentration of asunaprevir in the serum
OATP1B1/1B3 (SLCO1B1/1B3) inhibitors increase the concentration of elbasvir and grazoprevir in the serum
it increases the concentration of OATP1B1/1B3 substrates in the serum
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
bempedoic acid: it may enhance the serum concentration of simvastatin
may increase the levels serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) substrates
eltrombopag increases the concentration of OATP1B1/1B3 substrates in the serum
OATP1B1/1B3 inhibitors increase the concentration of brincidofovir in the serum
OATP1B1/1B3 inhibitors increase the concentration of eluxadoline in the serum
may increase the serum concentration of OAT1/3 substrates
may increase the serum concentration of OAT1/3 substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
it may increase the levels of serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates
Actions and Spectrum:
The liver produces cholesterol via an enzyme called ATP citrate lyase, which bempedoic acid binds to and blocks from working.
bempedoic acid lowers the amount of cholesterol produced in the liver via ATP citrate lyase, which might result in a drop in blood cholesterol levels.
The body’s other metabolic processes or activities are not significantly impacted by bempedoic acid, which only affects the production of cholesterol in the liver.
Frequency defined
<1%
Tendon rupture (0.5%)
1-10%
Upper respiratory tract infection (4.5%)
Bronchitis (3%)
Pain in extremity (3%)
Elevated liver enzymes (2.1%)
Atrial fibrillation (1.7%)
Abdominal pain or discomfort (3.1%)
Anemia (2.8%)
Gout (1.5%)
Benign prostatic hyperplasia (1.3%)
Muscle spasms (3.6%)
Hyperuricemia (3.5%)
Back pain (3.3%)
Black Box Warning
There are no black box warnings for bempedoic acid listed in the FDA-approved information.
Contraindication/Caution:
Contraindication:
Caution:
Particularly in people who are old or on corticosteroids, bempedoic acid may increase the risk of tendon rupture or tendinitis.
Pregnancy warnings:   
Pregnancy category: N/A
Lactation: Excretion into human milk is unknown
Pregnancy Categories:     
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology
The liver quickly transforms bempedoic acid, a small molecule prodrug, into bempedoic acid-CoA, which is the active form. The drug’s active form prevents the formation of cholesterol in the liver by inhibiting the enzyme ATP citrate lyase.
As ATP citrate lyase is blocked by bempedoic acid, the liver produces less cholesterol. Compared to statins, which primarily inhibit HMG-CoA reductase, another enzyme involved in the production of cholesterol, this method of action is distinct.
Pharmacodynamics
bempedoic acid’s pharmacodynamic effects are mostly due to its inhibition of ATP citrate lyase, an enzyme involved in the liver’s synthesis of cholesterol. The major goal of cholesterol-lowering treatment is LDL cholesterol, hence the drug’s main impact is to decrease LDL cholesterol production
By preventing the liver from producing cholesterol, bempedoic acid lowers blood levels of LDL cholesterol.
Pharmacokinetics
Absorption
bempedoic acid is taken orally as a tablet, where it is absorbed in the digestive system. The medication has a 25% bioavailability when taken orally.
Distribution
bempedoic acid is mostly found in the liver, where it is converted to bempedoic acid-CoA, the active form.
Metabolism
The enzyme acyl-CoA synthetase long-chain family member 1 quickly converts bempedoic acid in the liver to its active form, bempedoic acid-CoA. (ACSL1).
The medication that inhibits ATP citrate lyase is bempedoic acid-CoA.
Elimination and excretion
Only a minor quantity of bempedoic acid is eliminated in the urine; the majority is excreted in the feces. The medication’s half-life is about 12 hours.
Administration:
An oral tablet containing bempedoic acid is available and should be taken once a day, with or without meals.
180 mg is the suggested dosage, which is acceptable at any time of day.
Patient information leaflet
Generic Name: bempedoic acid
Why do we use bempedoic acid?
For the treatment of people with primary hyperlipidaemia or mixed dyslipidaemia, bempedoic acid is used as an adjuvant therapy to diet and maximally tolerated statin medication to lower levels of low-density lipoprotein cholesterol (LDL-C).
The medication is used in individuals who need extra LDL-C reduction despite receiving statin therapy that is well tolerated or who are intolerant to statins.
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