Sunitinib is a multi-target tyrosine kinase inhibitor (TKI) that selectively inhibits signaling pathways such as platelet-derived growth factor receptor (PDGFR α/β), vascular endothelial growth factor receptor (VEGFR1/2/3), stem cell factor receptor (KIT), and Fms like tyrosine kinase-3 (FLT3) to block tumor angiogenesis and cell proliferation.

1、 Drug name

Common name: Sunitinib Malate

Product Name: SUTENT ®

2、 Indications

Adult gastrointestinal stromal tumors, suitable for patients with disease progression or intolerance after imatinib treatment.

Adult advanced renal cell carcinoma.

Adjuvant therapy for high-risk postoperative recurrence of adult renal cell carcinoma.

Adult unresectable locally advanced or metastatic pancreatic neuroendocrine tumors.

3、 Specifications

Hard gelatin capsules, 12.5 milligrams.

4、 Main components

Active ingredient: Sunitinib malate.

5、 Usage and dosage

Gastrointestinal stromal tumors and advanced renal cell carcinoma: The recommended dose is 50 milligrams orally once daily, taken continuously for 4 weeks and stopped for 2 weeks (4/2 regimen) until disease progression or intolerable toxicity occurs.

Adjuvant therapy for renal cell carcinoma: The recommended dosage is 50 milligrams orally once daily, using a 4/2 regimen, for a maximum of 9 cycles.

Pancreatic neuroendocrine tumors: The recommended dose is 37.5 milligrams orally once daily until disease progression or intolerable toxicity occurs.

Medication time: can be taken with food or on an empty stomach.

6、 Dose adjustment

Adverse reaction dose adjustment:

First dose reduction: Reduce to 37.5 milligrams once daily for gastrointestinal stromal tumors/renal cell carcinoma; Reduce pancreatic neuroendocrine tumors to 25 milligrams once daily.

Second dose reduction: Reduce to 25 milligrams once daily for gastrointestinal stromal tumors/advanced renal cell carcinoma.

Drug interaction dose adjustment:

Combined with potent CYP3A4 inhibitors: reduce to 37.5 milligrams once daily for gastrointestinal stromal tumors/renal cell carcinoma; Reduce pancreatic neuroendocrine tumors to 25 milligrams once daily.

Combined with potent CYP3A4 inducers: gastrointestinal stromal tumors/renal cell carcinoma increased to 87.5 milligrams once daily; Pancreatic neuroendocrine tumors increased to 62.5 milligrams once daily.

7、 Medication precautions

Before and after meals: can be taken with food or on an empty stomach.

Missing dose: If the missed dose is less than 12 hours, it should be replenished as soon as possible; If it is more than 12 hours, skip the dose and take the next dose according to the original plan.

Vomiting: If vomiting occurs after taking medication, it is not recommended to take the next dose according to the original plan.

Avoid drinking grapefruit juice or consuming grapefruit during medication.

8、 Medication for special populations

Pregnant women: Prohibited, may cause harm to the fetus.

Breastfeeding period: It is recommended to stop breastfeeding during the discontinuation period and at least 4 weeks after the last administration.

Children: Safety and effectiveness have not yet been established.

Elderly people: The incidence of adverse reactions may be higher in patients over 65 years old.

Liver and kidney dysfunction: Mild to moderate liver injury does not require dose adjustment; Severe liver injury has not been studied. Mild, moderate, and severe kidney injury and hemodialysis patients do not need to adjust the starting dose.

9、 Adverse reactions

Common adverse reactions (≥ 25%) include fatigue/weakness, diarrhea, mucositis/stomatitis, nausea, decreased appetite/anorexia, vomiting, abdominal pain, hand foot syndrome, hypertension, bleeding events, taste changes, indigestion, thrombocytopenia, etc.

Serious adverse reactions include: hepatotoxicity, cardiovascular events, QT interval prolongation, hypertension, bleeding, gastrointestinal perforation, tumor lysis syndrome, thrombotic microvascular disease, proteinuria, skin toxicity, reversible posterior leukoencephalopathy syndrome, thyroid dysfunction, hypoglycemia, mandibular necrosis, wound healing disorders, etc.

10、 Contraindications

There are no known contraindications.

11、 Drug interactions

Strong CYP3A4 inhibitors (such as ketoconazole) may increase the blood concentration of sunitinib, and it is recommended to adjust the dosage or avoid co administration.

Strong CYP3A4 inducers (such as rifampicin) may reduce the blood concentration of sunitinib. It is recommended to adjust the dosage or avoid co administration.

When combined with drugs that prolong the QT interval, it is necessary to strengthen electrocardiogram monitoring.

12、 Storage method

Store at 20 ° C to 25 ° C (68 ° F to 77 ° F), allowing short-term exposure to 15 ° C to 30 ° C (59 ° F to 86 ° F) environment.

Avoid light and moisture, keep out of reach of children.

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