Indications

Resmetirom tablet is indicated in conjunction with diet and exercise for the treatment of adults with noncirrhotic nonalcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis (consistent with stages F2 to F3 fibrosis).

Composition

Pharmacology

Resmetirom is a partial agonist of the thyroid hormone receptor-beta (THR-β). Resmetirom produced 83.8% of the maximum response compared to triiodothyronine (T3), with an EC 50 of 0.21 μM in an in vitro functional assay for THR-β activation. The same functional assay for thyroid hormone receptor alpha (THR-α) agonism showed 48.6% efficacy for Resmetirom relative to T3, with an EC 50 of 3.74 pM. THR-p is the major form of THR in the liver, and stimulation of THR-β in the liver reduces intrahepatic triglycerides.

Dosage & Administration

The recommended dose of Resmetirom is based on actual body weight. For patients weighing: <100 kg, the recommended dose is 80 mg orally once daily. >100 kg, the recommended dose is 100 mg orally once daily. Resmetirom can be administered with or without food.

Contraindications

Side Effects

The common side effects of Resmetirom are: Diarrhea, Nausea, Vomiting, Abdominal pain, Dizziness, Pruritus, Constipation.

Pregnancy & Lactation

Pregnancy : There are no available data on Resmetirom use in pregnant women to evaluate for a drug associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. Lactation : There is no information regarding the presence of Resmetirom in human or animal milk, the effects on the breast-fed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for Resmetirom and any potential adverse effects on the breastfed infant from Resmetirom or from the underlying maternal condition.

Precautions & Warnings

Hepatotoxicity : Hepatotoxicity has been observed with use of Resmetirom. Monitoring of patient is required during treatment with Resmetirom for elevations in liver tests, for the development of liver-related adverse reactions and for sign & symptoms of hepatotoxicity. If hepatotoxicity is suspected, Resmetirom should be discontinued and monitoring of the patient should be continued. If laboratory values return to baseline, the potential risks against the benefits of restarting Resmetirom should be considered. If laboratory values do not return to baseline, DI-ALH or autoimmune liver disease should be considered in the evaluation of elevations in liver tests. Gallbladder-Related Adverse Reactions : In clinical trials, cholelithiasis, acute cholecystitis, and obstructive pancreatitis (gallstone) were observed in Resmetirom-treated patients. If cholelithiasis is suspected, gallbladder diagnostic studies and appropriate clinical follow-up are indicated , If an acute gallbladder event is suspected, Resmetirom treatment should be interrupted until the event is resolved. Drug Interaction with Certain Statins : An increase in exposure of Atorvastatin, Pravastatin, Rosuvastatin and Simvastatin was observed when concomitantly administered with Resmetirom, which may increase the risk of adverse reactions related to these drugs. Dosage adjustment for certain statins is recommended.

Therapeutic Class

Storage Conditions

Store below 30°C, in a cool and dry place. Keep away from light. Keep out of the reach of children.