Resmetirom

Aka: Resmetirom, Rezdiffra

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II. Background

  1. Resmetirom is a specialty medication, first in class for NASH treatment, released in 2024
  2. Expensive at time of release ($4000/month) in 2024

III. Indications

  1. Nonalcoholic Steatohepatitis (NASH, MASH)
    1. Refractory to lifestyle and comorbidity management and moderate to severe Hepatic Fibrosis

IV. Mechanism

  1. Activates hepatic Thyroid Hormone Receptor Beta
  2. Increases hepatic Fat Metabolism and decreases hepatic fat deposition

V. Dosing

  1. Weight <100 kg: Resmetirom 80 mg orally once daily
  2. Weight >100 kg: Resmetirom 100 mg orally once daily

VI. Medications

  1. Resmetirom 60 mg, 80 mg, 100 mg

VII. Adverse Effects

  1. Gastrointestinal (common)
    1. Diarrhea
    2. Nausea
  2. Acute Gallbladder dysfunction (uncommon)
  3. Hepatotoxicity
    1. Monitor Liver Function Tests

VIII. Safety

  1. Unknown safety in pregnancy
  2. Unknown safety in Lactation

IX. Drug Interactions

  1. Statins
    1. Limit Simvastatin to 20 mg/day
    2. Limit Rosuvastatin to 20 mg/day
    3. Limit Pravastatin to 40 mg/day
    4. Limit Atorvastatin to 40 mg/day
  2. Moderate to Strong CYP2C8 Inhibitors (e.g. Gemfibrozil)
    1. Avoid in combination with Resmetirom
  3. OATP1B1 and OATP1B3 Inhibitors (e.g. Cyclosporine)
    1. Avoid in combination with Resmetirom

X. Efficacy

  1. Resolves NASH with Fibrosis after 12 months of use when combined with diet and Exercise (NNT 6)

XI. Resources

  1. Resmetirom (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e67ea09f-a840-439c-86c8-f98585f978b2

XII. References

  1. (2024) Presc Lett 31(7): 39

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