Detailed introduction to sunitinib drug instructions

1. Generic name of the drug: Sunitinib, Sunitinib

Product name:SUTENT, Sutent

2. Indications:

1. Gastrointestinal stromal tumor (GIST): Sunitinib (Sunitinib) is suitable for adult patients who have been treated with imatinib mesylate or who do not tolerate it well.

2. Advanced renal cell carcinoma (RCC): It is suitable for adjuvant treatment of adult patients with advanced renal cell carcinoma and patients with high risk of recurrence after nephrectomy.

3. Advanced pancreatic neuroendocrine tumors (pNET): It is suitable for the treatment of adult patients with locally advanced or metastatic unresectable well-differentiated pancreatic neuroendocrine tumors.

3. Usage and dosage:

1. Recommended dosage:

(1) For patients with GIST and advanced RCC, the recommended dose of sunitinib is 50 mg, taken orally once daily, with a treatment course of 4 weeks, followed by a 2-week discontinuation (4/2 course of treatment), until disease progression or serious adverse reactions occur. Can be taken with food or on an empty stomach.

(2) For the adjuvant treatment of RCC, the recommended dose of sunitinib is 50 mg once daily, with a 4-week treatment course followed by 2 weeks off, for a total of 9 6-week cycles.

(3) For patients with advanced pNET, the recommended dose is 37.5 mg orally once daily until disease progression or unacceptable toxicity occurs.

2. Dose adjustment: In order to control adverse reactions,the first dose of GIST and RCC patients can be reduced to 37.5 mg, once a day; the second dose can be reduced to 25 mg; the first dose of pNET patients can be reduced to 25 mg, and if it is intolerable, discontinue use.

(1) Drug interactions: The combination of strong CYP3A4 inhibitors with sunitinib should usually be avoided. If this cannot be avoided, the dose needs to be reduced. If it must be combined with a CYP3A4 inducer, consider increasing the dose to the highest limit, up to 87.5 mg in patients with GIST and RCC; and up to 62.5 mg in patients with pNET.

(2) Hemodialysis patients with end-stage renal disease: The initial dose generally does not need to be adjusted, but drug exposure may be reduced compared with patients with normal renal function, and subsequent doses can be gradually increased to twice the dose based on safety.

4. Adverse reactions:

According to clinical studies, common adverse reactions of sunitinib include fatigue, diarrhea, stomatitis, nausea, loss of appetite, vomiting, abdominal pain, hand-foot syndrome, hypertension, bleeding events, taste changes, indigestion and thrombocytopenia. Common adverse reactions observed after marketing include thrombocytopenic bleeding, esophagitis, cholecystitis, allergic reactions (such as angioedema), serious infection, sepsis, etc.

5. Storage conditions:

Sunitinib capsules are available in four specifications: 12.5 mg, 25 mg, 37.5 mg, and 50 mg. The storage temperature is 20°C to 25°C (68°F to 77°F), and the allowable deviation is 15°C to 30°C (59°F to 86°F).

6. Mechanism analysis:

Sunitinib is a small molecule inhibitor that targets multiple receptor tyrosine kinases (RTKs), some of which are associated with tumor growth, pathological angiogenesis, and cancer metastasis. Its inhibitory effect has been confirmed in multiple biochemical and cellular experiments, and the main metabolite also exhibits similar potency to sunitinib.

7. Precautions for special groups:

1. Female: Since the concentration of sunitinib and its metabolites in mammalian milk is much higher than that in plasma, it is recommended that women avoid breastfeeding during treatment and for at least 4 weeks after the last dose; women of reproductive potential should take effective contraceptive measures during treatment and within 4 weeks after the last dose.

2. Males: Men of reproductive potential should take effective contraceptive measures during treatment with sunitinib and within 7 weeks after the last dose.

Reference materials:https://www.sutent.com/