Risimertilo is a highly selective thyroid hormone receptor beta (THR - β) agonist.

1、 Indications

Risimetirol is a thyroid hormone receptor beta (THR - β) agonist that requires a combination of diet and exercise for the treatment of adult non-alcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis (F2-F3 stages). This indication is based on an accelerated approval pathway and requires subsequent clinical trials to validate clinical benefits. Prohibited for patients with decompensated cirrhosis.

2、 Usage and dosage

Recommended dosage: Adjust according to actual weight. For those weighing less than 100kg, take 80mg orally per day, and for those weighing ≥ 100kg, take 100mg orally per day. It can be taken before or after meals.

Dose adjustment:

Combination use of CYP2C8 inhibitors: Strong inhibitors (such as gemfibrozil) are prohibited; Intermediate acting inhibitors (such as clopidogrel) need to be reduced to 60mg (<100kg) or 80mg (≥ 100kg).

Liver dysfunction: Avoid use in patients with moderate to severe liver injury (Child Pugh B/C grade).

Medication precautions: Swallow the entire tablet, no need to supplement if missed, take the next dose according to the original plan.

3、 Side effects

Common adverse reactions (≥ 5%) include diarrhea (14-33%), nausea (9-18%), itching (4-10%), vomiting (4-8%), constipation (4-8%), abdominal pain (4-7%), and dizziness (1-4%). Be alert to the following serious risks:

Hepatotoxicity: May cause drug-induced autoimmune hepatitis (DI-ALH), liver function needs to be monitored, and medication should be stopped immediately if symptoms such as fatigue and jaundice occur.

Gallbladder related events: The incidence of gallstones and cholecystitis increases, and treatment needs to be interrupted during acute attacks.

Drug interactions: Combination with statins may increase the risk of rhabdomyolysis, and statin dosage should be limited (e.g. simvastatin ≤ 20mg/day).

4、 Precautions and taboos

Monitoring requirements:

Regularly check liver function, thyroid function (FT4 may decrease), and gallbladder ultrasound.

Medication should be discontinued before and after surgery: Discontinue medication 24 days before elective surgery, and restart medication after wound healing.

Taboo population: There are no absolute contraindications, but potent CYP2C8 inhibitors (such as gefitolozil) or OATP inhibitors (such as cyclosporine) are contraindicated.

Special populations:

Pregnant woman: Animal experiments have shown embryotoxicity, and contraception should be used until one month after discontinuation.

Breastfeeding period: Avoid breastfeeding during treatment and within one month of discontinuation of medication.

5、 Storage method

Store in a dark place at 20-25 ° C (15-30 ° C is allowed for a short period of time) and keep out of reach of children.

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