Pharm

Resmetirom

search

Resmetirom, Rezdiffra

  • 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
  • Indications
  1. Nonalcoholic Steatohepatitis (NASH, MASH)
    1. Refractory to lifestyle and comorbidity management and moderate to severe Hepatic Fibrosis
  • Mechanism
  1. Activates hepatic Thyroid Hormone Receptor Beta
  2. Increases hepatic Fat Metabolism and decreases hepatic fat deposition
  • Dosing
  1. Weight <100 kg: Resmetirom 80 mg orally once daily
  2. Weight >100 kg: Resmetirom 100 mg orally once daily
  • Medications
  1. Resmetirom 60 mg, 80 mg, 100 mg
  • Adverse Effects
  1. Gastrointestinal (common)
    1. Diarrhea
    2. Nausea
  2. Acute Gallbladder dysfunction (uncommon)
  3. Hepatotoxicity
    1. Monitor Liver Function Tests
  • Safety
  1. Unknown safety in pregnancy
  2. Unknown safety in Lactation
  • 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
  • Efficacy
  1. Resolves NASH with Fibrosis after 12 months of use when combined with diet and Exercise (NNT 6)
  • References
  1. (2024) Presc Lett 31(7): 39