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
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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.
Commonly reported adverse effects include diarrhea, nausea, vomiting, abdominal pain, dizziness, pruritus, and constipation.
Pregnancy:
There are no adequate data on the use of Resmetirom in pregnant women to assess the risk of major congenital anomalies, miscarriage, or adverse maternal or fetal outcomes.
Lactation:
There is no information regarding the presence of Resmetirom in human or animal milk, its effects on the breastfed infant, or its influence on milk production. The benefits of breastfeeding should be weighed against the mother’s clinical need for Livheal and any potential risks to the infant.
Hepatotoxicity:
Cases of hepatotoxicity have been reported with Livheal use. Patients should be monitored regularly for elevations in liver function tests and signs or symptoms of liver injury. If hepatotoxicity is suspected, treatment should be discontinued and monitoring continued. Re-initiation should be carefully considered after liver parameters return to baseline. Persistent abnormalities should prompt evaluation for drug-induced autoimmune-like hepatitis or autoimmune liver disease.
Gallbladder-Related Events:
Cholelithiasis, acute cholecystitis, and gallstone-related obstructive pancreatitis have been reported in clinical trials. If gallbladder disease is suspected, appropriate diagnostic evaluation and clinical management are required. Livheal therapy should be interrupted during acute gallbladder events until resolution.
Statin Interaction Warning:
Increased exposure to certain statins may occur during concomitant use with Livheal, necessitating dose adjustments to reduce the risk of adverse reactions.
Store below 30°C in a cool, dry place. Protect from light. Keep out of reach of children.
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At ePharma, we’re committed to providing accurate and accessible health information. However, all content is intended for informational purposes only and should not replace medical advice from a qualified physician. Please consult your healthcare provider for personalized guidance. We aim to support, not substitute, the doctor-patient relationship.