Serpatinib usage guidelines and detailed instructions

Indications:

Non-small cell lung cancer: Suitable for the treatment of adult patients with RET fusion gene-positive locally advanced or spread non-small cell lung cancer. The drug blocks the growth and spread of tumors, providing a new treatment option for these patients.

Medullary thyroid cancer: Serpatinib is also used to treat adults and pediatric patients 12 years and older who have advanced or disseminated RETmutant medullary thyroid cancer. These patients usually require systemic therapy to control the disease.

RETFusion-positive thyroid cancer: Serpatinib has also shown promising results in adults and pediatric patients 12 years of age and older with advanced or metastatic RETfusion-positive thyroid cancer that requires systemic therapy and is radioactive iodine refractory (if applicable).

Mechanism of action:

Selpatinib specifically binds to the active site of RET kinase and inhibits its tyrosine kinase activity. RETGene mutations or rearrangements can lead to abnormal activation, which in turn drives cell proliferation and tumor growth. By inhibiting RET kinase, serpatinib effectively interrupts signal transduction pathways related to cell proliferation and survival. This intervention can reduce the ability of tumor cells to proliferate. When the RET signaling pathway is inhibited, the survival signal of tumor cells is weakened. In multiple clinical trials, serpatinib has shown good efficacy in patients with RET mutation-positive patients, significantly improving the disease remission rate and overall survival, and playing a positive role in improving the quality of life of patients.

Medication method:

1.＜50kg, twice a day, each time120mg.

2.≥50kg, 160mg twice daily.

Side effects:

Common side effects: include swelling (edema) of the arms, legs, hands, and feet, diarrhea, fatigue, dry mouth, high blood pressure, stomachache (abdominal pain), constipation, rash, nausea, and headache. These side effects are usually mild, tolerated by most patients, and can be managed with medication dose adjustments or supportive care.

Laboratory test abnormalities: Serpatinib may also cause abnormalities in some laboratory test indicators, such as reduced white blood cell count, reduced sodium and calcium levels in the blood, etc. These changes require close monitoring and appropriate treatment if necessary.

Severe side effects: including hepatotoxicity (such as liver damage or jaundice), lung inflammation, severe hypertension, heart rhythm changes (such asQT interval prolongation), bleeding problems, allergic reactions, and tumor lysis syndrome (TLS). These serious side effects may threaten the patient's life and require prompt medical treatment.

Warnings and precautions:

Hepatotoxicity warning: The use of serpatinib may cause liver damage, so liver function needs to be monitored regularly before and during use, such as ALT and ASTlevels should be monitored every 2weeks, especially during the first 3months of use.

Cardiovascular risks: The drug may cause hypertension and prolongation of the QT interval. Patients should monitor blood pressure and ECG regularly.

Bleeding risk: Serpatinib may increase the risk of bleeding, and patients should be closely monitored for bleeding tendencies.

Allergic reaction: Be alert to the occurrence of hypersensitivity reaction. Once it occurs, the drug should be stopped immediately and appropriate treatment should be given.

Impaired wound healing: Use of this drug should be suspended before and after surgery to avoid affecting wound healing.

Drug interactions:

Potential interactions with other drugs, especially those that affect liver metabolic enzymes (such asCYP3A4). Concomitant use with strong CYP3A4 inhibitors may increase the plasma concentration of serpatinib, while use with strong inducers may reduce its efficacy.

Medication for special populations:

Please use caution during pregnancy, lactation, and those with liver and kidney dysfunction.

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References:

https://www.drugs.com/dosage/selpercatinib.html