-5%
Resmetirom
The recommended dose of Livheal is determined based on actual body weight:
Patients weighing <100 kg: 80 mg orally once daily
Patients weighing ≥100 kg: 100 mg orally once daily
- Pediatric Patients: Safety and efficacy have not been established.
- Geriatric Patients: No overall differences in effectiveness were observed; however, a numerically higher incidence of adverse reactions has been reported in patients aged 65 years and older.
- Renal Impairment: No dose adjustment is required in patients with mild to moderate renal impairment. Livheal has not been studied in severe renal impairment.
- Hepatic Impairment: Use in patients with decompensated cirrhosis or moderate to severe hepatic impairment (Child-Pugh Class B or C) should be avoided. No dose adjustment is required in mild hepatic impairment (Child-Pugh Class A).
Livheal tablet, in combination with appropriate diet and exercise, is indicated for the treatment of adults with noncirrhotic nonalcoholic steatohepatitis (NASH) associated with moderate to advanced liver fibrosis (corresponding to fibrosis stages F2–F3).
Resmetirom, the active ingredient of Livheal, is a selective partial agonist of the thyroid hormone receptor-beta (THR-β). In in-vitro functional assays, Resmetirom demonstrated 83.8% of the maximum response compared to triiodothyronine (T3), with an EC50 of 0.21 μM for THR-β activation. In contrast, its activity on thyroid hormone receptor-alpha (THR-α) was lower, showing 48.6% efficacy relative to T3, with an EC50 of 3.74 pM.
THR-β is the predominant thyroid hormone receptor subtype in the liver, and its activation plays a key role in reducing intrahepatic triglyceride levels, thereby improving hepatic steatosis and fibrosis.
Effects of Other Drugs on Livheal
CYP2C8 Inhibitors:
Concomitant use of Livheal with strong or moderate CYP2C8 inhibitors may increase the risk of adverse reactions.
Use with strong CYP2C8 inhibitors (e.g., gemfibrozil) is not recommended.
If used with moderate CYP2C8 inhibitors (e.g., clopidogrel), dose reduction is required:
<100 kg: 60 mg once daily
≥100 kg: 80 mg once daily
OATP1B1 and OATP1B3 Inhibitors:
Co-administration with OATP1B1 or OATP1B3 inhibitors (e.g., cyclosporine) may increase Livheal exposure and the risk of adverse reactions; such combinations are not recommended.
Effects of Livheal on Other Drugs
Statins:
Livheal increases plasma concentrations of certain statins (atorvastatin, pravastatin, rosuvastatin, and simvastatin), potentially increasing statin-related adverse effects. Recommended maximum daily doses are:
Rosuvastatin and Simvastatin: 20 mg
Atorvastatin and Pravastatin: 40 mg
CYP2C8 Substrates:
Livheal may increase exposure to CYP2C8 substrates (e.g., pioglitazone). Patients should be closely monitored, particularly when small increases in substrate concentration may result in clinically significant adverse reactions.