Resmetirom (Rezdiffra) is a thyroid hormone receptor-beta agonist approved for marketing by the U.S. FDA in 2024. When used in combination with diet and exercise, this medication is indicated for the treatment of adult patients with non-cirrhotic non-alcoholic steatohepatitis (NASH) accompanied by moderate to advanced liver fibrosis (equivalent to F2 to F3 stage fibrosis).

How to Use Resmetirom (Rezdiffra)

Dosage Selection

For patients with a body weight < 100 kg, the recommended dosage is 80 mg, taken orally once daily.

For patients with a body weight ≥ 100 kg, the recommended dosage is 100 mg, taken orally once daily.

Administration Time and Method

This medication can be taken with or without food, once daily at a fixed time each day.

The medication is available as film-coated tablets in three strengths: 60 mg, 80 mg, and 100 mg. Patients should select the appropriate strength of tablets as prescribed by their doctor.

Long-Term Treatment Management

During the treatment period, continuous monitoring of liver function indicators is required, especially changes in liver biochemical indicators in the early stage of treatment.

At the same time, attention should be paid to whether the patient experiences adverse reactions related to the gallbladder.

Dosage Adjustment of Resmetirom (Rezdiffra)

Routine Dosage Maintenance

For most patients, the initial dosage determined based on body weight should be maintained, and no routine adjustment is needed.

However, dosage adjustment is required under specific circumstances.

Adjustment Due to Drug Interactions

When used concomitantly with moderate CYP2C8 inhibitors (e.g., clopidogrel), the dosage of resmetirom needs to be adjusted.

For patients with a body weight < 100 kg: reduce the dosage to 60 mg once daily.

For patients with a body weight ≥ 100 kg: reduce the dosage to 80 mg once daily.

Concomitant use of resmetirom with strong CYP2C8 inhibitors (e.g., gemfibrozil) is not recommended.

Special Adjustment Scenarios

Concomitant use of resmetirom with OATP1B1 and OATP1B3 inhibitors (e.g., cyclosporine) is also not recommended.

Medication Use in Special Populations for Resmetirom (Rezdiffra)

Patients with Hepatic Impairment

Use of resmetirom should be avoided in patients with moderate to severe hepatic impairment (Child-Pugh Class B or C).

For patients with mild hepatic impairment (Child-Pugh Class A), no dosage adjustment is required.

Patients with Renal Impairment

Patients with mild or moderate renal impairment may use the same recommended dosage as patients with normal renal function.

However, the use of resmetirom in patients with severe renal impairment has not been studied.

Pregnancy and Lactation

Currently, there are no data on the use of resmetirom in pregnant women, so the risk of drug-related major birth defects, miscarriages, or other adverse maternal and fetal outcomes cannot be evaluated.

There is no information on the presence of resmetirom in human or animal milk, nor is it clear about its effects on breastfeeding infants or milk production.