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. Contraindications

  1. Decompensated Cirrhosis
  2. Moderate to severe hepatic imapirment (Child-Pugh Class B or C)

V. Mechanism

  1. Activates hepatic Thyroid Hormone Receptor Beta (THR-B Agonist)
  2. Increases hepatic Fat Metabolism and decreases hepatic fat deposition

VI. Medications

  1. Resmetirom 60 mg, 80 mg, 100 mg

VII. Dosing

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

VIII. Adverse Effects

  1. Gastrointestinal (common)
    1. Diarrhea
    2. Nausea
  2. Acute Gallbladder dysfunction (uncommon)
    1. Includes Cholelithiasis, Cholecystitis, Gallstone Pancreatitis
  3. Hepatotoxicity
    1. Monitor Liver Function Tests
    2. Monitor for hepatotoxicity signs (Nausea, Vomiting, RUQ Abdominal Pain, Jaundice)

IX. Safety

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

X. Drug Interactions

  1. Statins
    1. Resmetirom increases Statin plasma concentrations
    2. Limit Simvastatin to 20 mg/day
    3. Limit Rosuvastatin to 20 mg/day
    4. Limit Pravastatin to 40 mg/day
    5. Limit Atorvastatin to 40 mg/day
  2. Moderate to Strong CYP2C8 Inhibitors
    1. Avoid strong CYP2C8 Inhibitors (e.g. Gemfibrozil) in combination with Resmetirom
    2. Moderate CYP2C8 Inhibitor (e.g. cloipidogrel)
      1. Weight <100 kg: Limit Resmetirom dose to 60 mg
      2. Weight >100 kg: Limit Resmetirom dose to 80 mg
  3. OATP1B1 and OATP1B3 Inhibitors (e.g. Cyclosporine)
    1. Avoid in combination with Resmetirom

XI. Efficacy

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

XII. Resources

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

XIII. References

  1. (2024) Presc Lett 31(7): 39
  2. Harrison (2024) N Engl J Med 390(6):497-509 +PMID: 38324483 [PubMed]

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