Generic
Resmetirom
22 brands available in the market
At a glance
Resmetirom is a thyroid hormone receptor-beta (THR-β) partial agonist used in conjunction with diet and exercise for the treatment of noncirrhotic nonalcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis (F2-F3).
Description
Resmetirom is a partial agonist of THR-β. It is more selective for THR-β compared to THR-α, which is the major THR form in the liver. Stimulation of THR-β reduces intrahepatic triglycerides. In vitro functional assays showed 83.8% maximum response compared to T3 for THR-β activation.
Indications
- Noncirrhotic nonalcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis (F2-F3)
Therapeutic class
Metabolic Disorder Drugs
Pharmacological class
THR-β Partial Agonist
Pharmacology
Resmetirom is a selective partial agonist of THR-β that activates THR-β receptors in the liver, reducing intrahepatic triglycerides and improving liver fibrosis. It is more selective for THR-β compared to THR-α, reducing cardiovascular effects.
Mechanism of action
Reduces intrahepatic triglycerides and fibrosis by activating THR-β receptors in the liver.
Dosage
Adult Dose (Oral):
- <100 kg: 80 mg once daily
- ≥100 kg: 100 mg once daily
- With moderate CYP2C8 inhibitors (<100 kg): 60 mg/day; (≥100 kg): 80 mg/day
- Can be taken with or without food
Administration
- Take at the same time each day
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Diarrhea
- Nausea
- Vomiting
- Abdominal pain
- Dizziness
- Pruritus
- Constipation
Precautions & warnings
- Hepatotoxicity: Monitor liver tests; discontinue if suspected
- Gallbladder-related adverse reactions (cholelithiasis, acute cholecystitis, obstructive pancreatitis): Interrupt treatment if suspected
- Drug interaction with statins: Dose adjustment needed for atorvastatin, pravastatin, rosuvastatin, simvastatin
Contraindications
- Hypersensitivity to resmetirom or any component
Drug interactions
- Strong or moderate CYP2C8 inhibitors (gemfibrozil): Avoid; dose reduction with moderate inhibitors
- OATP1B1/1B3 inhibitors (cyclosporine): Avoid
- Statins (atorvastatin, pravastatin, rosuvastatin, simvastatin): Increased plasma concentrations; dose adjustment needed (rosuvastatin/simvastatin: 20 mg/day; pravastatin/atorvastatin: 40 mg/day)
- CYP2C8 substrates (pioglitazone): Increased exposure; monitor for adverse reactions
Food interactions
It is not known whether it is safe to consume alcohol with Resmetirom.
Use in pregnancy
Use in Pregnancy: No data on use in pregnant women; consult your doctor.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: No information on presence in human or animal milk; consider developmental and health benefits of breastfeeding.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Numerically higher incidence of adverse reactions in patients 65 years and older; caution required.
Renal / hepatic impairment
Renal Impairment: No dose adjustment needed for mild-moderate renal impairment; not studied in severe renal impairment; consult your doctor.
Hepatic Impairment: Avoid in decompensated cirrhosis (moderate-severe hepatic impairment); no dose adjustment for mild hepatic impairment; consult your doctor.
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Store below 30°C in a cool and dry place, away from light; keep out of reach of children.
Chemical structure
Resmetirom