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ATP-Citrate Lyase Inhibitor

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ATP-Citrate Lyase Inhibitor, ATP-Citrate Lyase, Bempedoic Acid, Nexletol, Nexlizet

  • See Also
  1. Hyperlipidemia
  2. Hyperlipidemia Management
  • Indications
  1. Hyperlipidemia
    1. Statin Intolerant (e.g. Statin-Induced Myopathy)
    2. Second or third-line adjunct to Statin therapy if LDL not at goal
  • Contraindications
  1. Gouty Arthritis
  • Mechanism
  1. Class prototype, Bempedoic Acid, inhibits the enzyme ATP-Citrate Lyase
    1. ATP-Citrate Lyase is an enzyme key to Fatty Acid biosynthesis
    2. ATP-Citrate Lyase cleaves citrate into oxaloacetate (and acetyl CoA, ADP and orthophosphate)
  2. Lowers LDL Cholesterol as a Statin adjunct or alternative
  3. Does NOT effect Triglycerides or HDL
  • Efficacy
  1. Limited data on longterm cardiovascular outcomes
  2. Lowers LDL Cholesterol 20%
  3. NNT 63 for high Cardiovascular Risk patients to prevent 1 cardiovascular event in 3 years
  • Dosing
  1. Bempedoic Acid (Nexletol)
    1. Take 180 mg orally daily (typically in combination with a Statin)
  2. Bempedoic Acid 180 and Ezetimibe 10 mg (Nexlizet)
    1. Take one tablet orally daily
  • Precautions
  1. Bempedoic Acid (Nexletol) costs $400/month in 2023
  • Adverse Effects
  1. Increased Uric Acid
    1. Gout flare in up to 10% of patients with gout history on Bempedoic Acid (Nexletol)
  2. Gallstones
    1. Occurs in 1% of patients on Bempedoic Acid (Nexletol)
  • Drug Interactions
  1. Pravastatin or Simvastatin
    1. Risk of Statin-Induced Myopathy when used with Bempedoic Acid (Nexletol)
    2. Limit Simvastatin doses to 20 mg orally daily when using Bempedoic Acid
    3. Limit Pravastatin doses to 40 mg orally daily when using Bempedoic Acid
  • Resources
  1. Bempedoic Acid (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=88d06d89-a3da-40b4-b273-8f4f7d56c4c9
  2. Bempedoic Acid and Ezetimibe (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3fa2108c-0300-47b8-9d34-f762af7c93c6
  • References
  1. (2023) Presc Lett 30(4): 19
  2. Feng (2020) Prog Lipid Res +PMID:31499095 [PubMed]