Livheal 100

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.