What are the contents of the drug instructions for resmetirom?

1, Name:Rezdiffra, resmetirom, resmetirom

2. Indications

Resmetirom - Rezdiffra is approved for the treatment of non-alcoholic steatohepatitis (NASH) in patients with moderate to advanced liver fibrosis (stages F2 to F3). NASH is a liver disease associated with obesity, diabetes, and metabolic syndrome that often results in liver damage and fibrosis. Due to the severity and potential progression of NASH, the use of rismetirol received accelerated approval and is intended to improve patients' quality of life and liver function.

Accelerated approval: Based on the improvement of NASH and fibrosis, this indication received accelerated approval, which means that it showed good efficacy in clinical trials. Conditions for continued approval: The continued approval of rismetirol will depend on the results of subsequent confirmatory trials, which must verify the persistence and effectiveness of its clinical benefits.

Restrictions on use: For patients with decompensated cirrhosis, Rezdiffra should be used with cautionRezdiffra to avoid possible risks and adverse reactions.

3. Usage and dosage

1. Recommended dosage:The dosage of Rezdiffra should be adjusted according to the patient's weight to ensure that each patient can obtain the best therapeutic effect.

For patients whose weight is ≥100kg, it is recommended to take 100mg orally daily.

For patients whose weight is <100kg, it is recommended to take 80mg daily.

Rezdiffra can be taken before or after meals without affecting its efficacy.

2. Dose adjustment: During the use of Rezdiffra, if it is used in combination with certain drugs, the dose may need to be adjusted.

4. Adverse reactions

In clinical studies,the use of Rezdiffra may cause some adverse reactions:

Common adverse reactions: such as diarrhea, nausea, itching, vomiting, constipation, abdominal pain and dizziness.

Reasons for discontinuation: Diarrhea and nausea are the main reasons for patients to discontinue medication. Medical staff should explain possible adverse reactions to patients in detail when prescribing.

5. Storage

Rezdiffra comes as tablets and should be stored in a suitable environment to maintain its stability and effectiveness:

1. Storage conditions: Should be stored at20°C to 25°C (68°F to 77°F), with a deviation of 15°C to 30°C (59°F to 86°F) allowed.

2. Packaging: The medicine is packed in white high-density polyethylene bottles. The bottle has a child-safe sealing design to ensure the safety of the medicine and prevent children from accidentally taking it.

6. Special groups

Special attention should be paid to patients with liver dysfunction. Rezdiffra should be avoided in patients with decompensated cirrhosis (e.g. moderate to severe hepatic impairment) to prevent increased risk of adverse effects. Patients with moderate or severe hepatic impairment (Child-Pugh class B or C) may experience an increase in Cmax and AUC, further increasing the incidence of adverse reactions.

7. Mechanism of action

The main ingredient of Rezdiffra, Resmetirom, is a partial agonist of thyroid hormone receptor beta (THR-β) and has a unique mechanism of action.

1. THR-β activation: The efficacy of Resmetirom shows superiority compared to triiodothyronine (T3), with a maximum response of 83.8% and an EC50 of 0.21µM in the in vitro functional analysis of THR-β activation.

2. The role of THR-α: Compared with THR-β, the efficacy of Resmetirom in the agonistic effect of THR-α is 48.6%, and the EC50 is 3.74µM. This mechanism makes Resmetirom excellent at reducing intrahepatic triglycerides.

3. Distribution of liver and other tissues: In the liver, THR-β is mainly responsible for regulating lipid metabolism, while in other tissues such as the heart and bones, the effects of thyroid hormone are mainly mediated through THR-α. This feature allows Rezdiffra to effectively improve patients' liver health while reducing the risk of systemic adverse reactions.

Reference materials:https://www.drugs.com/monograph/resmetirom.html