Seputinib is a highly selective RET kinase inhibitor that can accurately bind to and inhibit the phosphorylation process of RET protein, interfere with downstream cancer-promoting signaling pathways (such as MAPK, PI3K-AKT, etc.), and inhibit tumor cell proliferation and survival.
Indications and efficacy
Non-small cell lung cancer: Suitable for patients with locally advanced or metastatic RET fusion-positive NSCLC. Clinical trials have shown that its objective response rate (ORR) can reach about 85%, and it also shows a certain effect on patients with brain metastases. 1.
Thyroid cancer: 2.
Medullary thyroid cancer: For patients with RET mutations, the ORR is about 69%;
Differentiated thyroid cancer: Effective for patients with RET fusion-positive, the ORR is about 79%.
Adverse reactions and treatment
Common side effects: elevated liver enzymes, hypertension, dry mouth, fatigue, constipation, etc., which can usually be relieved by adjusting the dose or symptomatic treatment;
Serious risks: interstitial lung disease, prolonged QT interval, bleeding risk, etc., need to stop the drug immediately and seek medical attention;
Liver function, blood pressure and electrocardiogram should be monitored regularly during medication.
Precautions for medication
RET mutation must be confirmed through genetic testing to avoid blind medication; 1.
Adjust the dose according to the doctor’s instructions: the standard dose is 160 mg twice a day, but it needs to be adjusted individually according to side effects or combined medication; 2.
Drug interactions: Avoid combined use with strong CYP3A4 inhibitors (such as clarithromycin) or inducers (such as rifampicin), which may affect blood drug concentrations; 3.
It is forbidden to use during pregnancy and lactation, which may cause harm to the fetus or infant. 4.
Medical guidance
Sepertib is a prescription drug. Before use, an oncologist must evaluate the genetic test results, overall health status and contraindications of the drug. Close follow-up is required during treatment, and emergency medical treatment is required in case of dyspnea, chest pain or severe allergic reactions.
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