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Serpatinib (Retevmo) is a highly selective and potent kinase inhibitor that works by targeting the mutation or fusion form of the RET (RearrangedDuringTransfection) gene.
1. Generic name: Selpercatinib
2. Trade name: Retevmo™
1. Adult metastatic RET fusion-positive non-small cell lung cancer (NSCLC).
2. Patients aged 12 years and above with advanced or metastatic RET-mutated medullary thyroid cancer (MTC) requiring systemic treatment.
3. Patients aged 12 years and above with advanced or metastatic RET fusion-positive thyroid cancer that require systemic treatment and are refractory to radioactive iodine.
Capsule dosage form: 40mg).
1. Active ingredient: Serpatinib.
2. Excipients: Microcrystalline cellulose, colloidal silica (capsule shell contains gelatin, titanium dioxide, etc.).
1. Conventional dosage of :
≥50kg: 160mg orally, 2 times a day (12 hours apart); <50kg: 120mg orally, 2 times a day.
2. How to take :
Swallow the whole tablet, do not chew or crush it.
It can be taken before or after meals, but if proton pump inhibitors (such as omeprazole) are used in combination, they need to be taken with food.
3. Treatment of missed doses :
If it is >6 hours before the next dose, you can take it again, otherwise skip it.
4. Vomiting treatment :
There is no need to take another dose after vomiting. Take the next dose according to the original plan.
1. Hepatotoxicity : Suspend the administration when AST/ALT rises, and reduce the dose by 2 levels after recovery (such as 160mg → 120mg).
2. Hypertension : Suspend medication for grade 3 hypertension and reduce the dose after control; permanently discontinue medication for grade 4 hypertension.
3. QT prolongation : For grade 3, suspend until recovery, reduce dose; for grade 4, permanently discontinue the drug.
4. Severe liver damage : Reduce the dose by half (such as 160mg → 80mg).
1. Combination restrictions :
Avoid combined use with strong/moderate CYP3A inhibitors (such as itraconazole) or inducers (such as rifampicin).
Antacids should be taken 2 hours apart.
2. Monitoring requirements :
Regularly detect liver function, blood pressure, QT interval, and electrolytes before medication and during treatment.
1. Pregnant women : is embryotoxic and requires contraception until 1 week after stopping the drug.
2. Lactation : Avoid breastfeeding during treatment and within 1 week of stopping the drug.
3. Children : It is safe and effective for ≥12 years old, but there is insufficient data for <12 years old.
4. Liver damage : In severe cases, dose reduction is required.
Common (≥25%) include:
1. Laboratory abnormalities: Elevated AST/ALT, hyperglycemia, low albumin, and low calcium.
2. Clinical symptoms: Dry mouth, diarrhea, high blood pressure, fatigue, rash, edema.
There are no clear contraindications.
1. CYP3A affects : Strong inhibitors increase the efficacy (need to reduce the dosage), while strong inducers decrease the efficacy (avoid combined use).
2. CYP2C8/3A substrate : may increase its plasma concentration (such as repaglinide).
Stored at room temperature (20-25℃), short-term fluctuation of 15-30℃ is allowed.