Resmetirom

Class
Thyromimetics
Subclass
Thyroid hormone receptor-β agonists
Substance name
Resmetirom
Brand names
Rezdiffra®
Common formulations
Tablet
Dosage and administration
Adults patients
Treatment of MASH • Moderate-to-advanced liver fibrosis
Weight < 100 kg
•
80 mg PO daily
Taken with or without food.
Weight ≥ 100 kg
•
100 mg PO daily
Taken with or without food.
Indications for use
Labeled indications
Adults
•
Treatment of MASH (moderate-to-advanced liver fibrosis)
Safety risks
Contraindications
Concomitant use of OATP1B1 or OATP1B3 inhibitors
•
Do not use OATP1B1 or OATP1B3 inhibitors, such as cyclosporine, with resmetirom.
Warnings and precautions
Cholelithiasis, acute cholecystitis, gallstone pancreatitis
•
Maintain a high level of suspicion, as resmetirom has been associated with an increased risk of gallbladder-related adverse reactions.
Hepatotoxicity
•
Maintain a high level of suspicion, as resmetirom has been associated with an increased risk of hepatotoxicity, including elevated liver enzymes and drug-induced autoimmune-like hepatitis. Monitor for liver enzyme elevations and signs or symptoms of hepatotoxicity. Discontinue resmetirom if hepatotoxicity is suspected. Reassess the risks and benefits of restarting therapy if liver function returns to baseline.
Increased serum drug levels
•
Use caution in patients receiving atorvastatin, pravastatin, rosuvastatin, or simvastatin, as resmetirom may increase the plasma levels of these statins. Limit daily doses of rosuvastatin and simvastatin to 20 mg, and pravastatin and atorvastatin to 40 mg.
Increased serum resmetirom levels
•
Use caution in patients receiving moderate CYP2C8 inhibitors, such as clopidogrel. Reduce the resmetirom dose to 60 mg once daily in patients weighing < 100 kg and to 80 mg once daily in patients weighing ≥ 100 kg.
Specific populations
Renal impairment
eGFR ≥ 30 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required.
eGFR < 30 mL/min/1.73 m²
•
No guidance available.
Renal replacement therapy
Any modality
•
No guidance available.
Hepatic impairment
Acute or decompensated chronic liver disease
•
Avoid use.
Child-Pugh A (mild)
•
Use acceptable. No dose adjustment required. Monitor liver function tests.
Child-Pugh B (moderate)
•
Avoid use.
Child-Pugh C (severe)
•
Avoid use.
Pregnancy and breastfeeding
Pregnancy
All trimesters
•
Insufficient evidence. Evidence of fetal harm in animals.
Breastfeeding
Use only if benefits outweigh potential risks.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
•
↑ serum ALT, ↑ serum AST, ↑ serum transaminases, diarrhea, generalized pruritus, nausea
Common 1-10%
•
↑ serum TBIL, ↑ serum TBIL, abdominal pain, constipation, dizziness, loss of appetite, flatulence, change in taste, vertigo, palpitations, skin erythema, depression, abnormal uterine bleeding, ↓ blood glucose, vomiting, tendinopathy
Rare < 0.1%
•
Cholelithiasis, acute cholecystitis, gallstone pancreatitis, urticaria, skin rash
Unknown frequency
•
Drug-induced autoimmune-like hepatitis
Interactions
Drug(s)
Check Interactions
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