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ALIMENTARY TRACT AND METABOLISM › BILE AND LIVER THERAPY › LIVER THERAPY, LIPOTROPICS › Liver therapy
resmetirom
A05BA11
Forms & Strengths
- Oral tablet: 60 mg
- Oral tablet: 80 mg
- Oral tablet: 100 mg
Adult Dosing
- Weight < 100 kg: 80 mg orally once daily
- Weight >= 100 kg: 100 mg orally once daily
- Take with or without food
Pediatric Dosing
- Safety and efficacy in pediatric patients < 18 years have not been established
Indications
- Treatment of adults with noncirrhotic non-alcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis (stages F2 to F3)
- Used in conjunction with diet and exercise
Mechanism of Action
- Liver-directed thyroid hormone receptor-beta (THR-beta) agonist
- Selectively binds to and activates THR-beta in the liver, reducing hepatic fat accumulation and lipotoxicity
Contraindications
- History of decompensated cirrhosis
- Concomitant use with strong CYP2C8 inhibitors (e.g., gemfibrozil)
- Known hypersensitivity to resmetirom or any of its excipients
Adverse Reactions
- Diarrhea
- Nausea
- Pruritus
- Dizziness
- Fatigue
- Abdominal pain
- Constipation
- Increased LDL-C initially or transiently
Drug Interactions
- Strong CYP2C8 inhibitors (e.g., gemfibrozil): Contraindicated due to increased resmetirom exposure
- Moderate or strong CYP2C8 inducers: May decrease resmetirom efficacy
- OATP1B1 and OATP1B3 substrates (e.g., statins): Resmetirom is an inhibitor and may increase their plasma concentrations; monitor for statin toxicity
Curated Content: Needs Vetting Before Put to Clinical Use