Resmetirom
REZDIFFRA
What it isLiver-selective thyroid-receptor-beta agonist; metabolic dysfunction-associated steatohepatitis with fibrosis.
Why this oneIt was the first therapy specifically approved for MASH, targeting hepatic fat and fibrosis through liver-directed thyroid signaling.
What limits itDiarrhea and nausea occur early. Monitor for hepatotoxicity, and manage its clinically important statin interactions.
FDA-approved for
- MASH/NASH (2024)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Noncirrhotic MASH w/ moderate-advanced fibrosis (F2-F3) | <100 kg | 80 mg QD | 80 mg QD | 80 mg QD |
| Noncirrhotic MASH w/ moderate-advanced fibrosis (F2-F3) | ≥100 kg | 100 mg QD | 100 mg QD | 100 mg QD |
Renal No adjustment needed (mild, moderate, or severe)
Hepatic Mild (Child-Pugh A): no adjustment; avoid in moderate-severe (Child-Pugh B/C) / decompensated cirrhosis
Instructions
- Swallow whole; do not split, crush, or chew
- With or without food
- Missed dose: skip it, resume next scheduled dose
- Moderate CYP2C8 inhibitor: reduce to 60 mg QD (<100 kg) or 80 mg QD (≥100 kg); strong CYP2C8 inhibitor not recommended
Cautions
- Hepatotoxicity, incl. drug-induced autoimmune-like hepatitis; monitor liver tests, discontinue if suspected
- Gallbladder events (cholelithiasis, cholecystitis, gallstone pancreatitis); interrupt for acute events
- Increased statin exposure (atorvastatin, pravastatin, rosuvastatin, simvastatin); monitor for myopathy/rhabdomyolysis
Adverse reactions
- Diarrhea
- Nausea
- Pruritus
- Vomiting
- Constipation
- Abdominal pain
- Dizziness
Pregnancy No human data; animal embryo-fetal toxicity (rabbit) at maternally toxic doses
Lactation No data on presence in human milk or effects on infant
NO BOXED WARNINGS
Principal riskDiarrhea and nausea early
Cost, est. cash$4,000–$4,500/month
Generic entry2038 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Resmetirom ballicule
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Memory aids: mascots and interaction avatars
thyroid gland → binds THR-β thyroid receptors in liver
