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Resmetirom

Brand and Other Names: Rezdiffra
Mechanism of Action:

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 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 of 3.74 μM. THR-β is the major form of THR in the liver, and stimulation of THR-β in the liver reduces intrahepatic triglycerides, whereas actions of thyroid hormone outside the liver, including in heart and bone, are largely mediated through THR-α. 

Indications:

REZDIFFRA is a thyroid hormone receptor-beta (THR-beta) agonist 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).

This indication is approved under accelerated approval based on improvement of NASH and fibrosis.

Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials. 

Limitations of Use: Avoid use of REZDIFFRA in patients with decompensated cirrhosis.

Route: Oral
Dose:

The recommended dosage of REZDIFFRA is based on actual body weight. For patients weighing:

  • < 100 kg, the recommended dosage is 80 mg orally once daily.
  • ≥ 100 kg, the recommneded dosage is 100 mg orally once daily.

Administer REZDIFFRA with or without food.

See full prescribing information for REZDIFFRA dosage modifications with concomitant use of moderate CYP2C8 inhibitors. 

Adverse Reactions:

The most common adverse reactions with REZDIFFRA (reported in at least 5% of patients and higher compared to placebo) are: diarrhea, nausea, pruritus, vomiting, constipation, abdominal pain, and dizziness.

Contraindication:
None.
Warnings and Precautions:
  • Hepatotoxicity: Monitor patients during treatment with REZDIFFRA for elevations in liver tests and for the development of liver-related adverse reactions. Discontinue REZDIFFRA and continue to monitor the patient if hepatotoxicity is suspected.
  • Gallbladder-Related Adverse Reactions: Cholelithiasis and cholecystitis were observed more often in REZDIFFRA-treated patients. If cholelithiasis is suspected, gallbladder diagnostic studies and appropriate clinical follow-up are indicated. If an acute gallbladder event such as acute cholecystitis is suspected, interrupt REZDIFFRA treatment until the event is resolved. 
See package insert for full prescribing information.