Sunitix Sunitinib Malate 25mg Beacon

[Drug Name] Sunitinib Malate Capsules (Sutent)

[Generic Name] Sunitinib Malate Capsules

[Specification/Model] 25 mg × 28 capsules × 1 bottle

[Manufacturer] Beacon Pharmaceuticals Ltd.

[Drug Type] Western Medicine

[Shelf Life] 24 months

[Indications]

1. Gastrointestinal stromal tumor (GIST) that is refractory to or intolerant of imatinib mesylate treatment;

2. Advanced renal cell carcinoma (RCC) that is not amenable to surgery;

3. Unresectable, metastatic, well-differentiated, advanced pancreatic neuroendocrine tumors (pNET) in adult patients.

[Dosage and Administration] The recommended dose of this product for the treatment of gastrointestinal stromal tumor and advanced renal cell carcinoma is 50 mg, taken orally once daily; the medication is taken for 4 weeks, followed by a 2-week rest period (a 4/2 dosing schedule). It may be taken with or without food.

[Adverse Reactions] Not yet established.

[Precautions] Adequate clinical study data in the Chinese population are currently lacking; therefore, it is recommended that this product be used under the guidance of a physician experienced in its use. Left Ventricular Dysfunction: If clinical signs of congestive heart failure (CHF) appear, it is recommended to discontinue the use of this product. Patients with no clinical evidence of congestive heart failure but whose ejection fraction is less than 50%, as well as those whose ejection fraction has decreased by more than 20% from baseline, should also discontinue treatment with this product and/or undergo dose reduction. Among patients treated with sunitinib, a higher number of patients experienced a decrease in left ventricular ejection fraction compared to the placebo group or the IFN-α group. In Study A involving gastrointestinal stromal tumor (GIST) patients, 22 out of 209 patients (11%) in the sunitinib group and 3 out of 102 patients (3%) in the placebo group experienced a treatment-related decrease in left ventricular ejection fraction (LVEF) below the lower limit of normal (LLN). Among the 22 patients in the sunitinib group who experienced changes in LVEF, 9 recovered spontaneously without intervention; 5 patients returned to normal levels following treatment (1 patient underwent dose reduction, while 4 patients received additional treatment with antihypertensive agents or diuretics); and 6 patients completed the study with no recorded recovery status. Furthermore, 3 patients (1%) in the sunitinib group experienced Grade 3 decline in left ventricular systolic function, with LVEF dropping below 40%; of these, 2 patients died without receiving further treatment with the study drug. No patients in the placebo group experienced a Grade 3 decline in LVEF. In Gastrointestinal Stromal Tumor (GIST) Study A, one patient in each of the two groups... (Sunitinib group... Please read the package insert carefully and use as directed by a physician.)

[Contraindications] Contraindicated in patients with severe hypersensitivity to this product or to any of its inactive ingredients.

[Packaging Unit] Box

[Active Ingredient] Sunitinib Malate. Chemical Name: (Z)-N-[2-(Diethylamino)ethyl]-5-[(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-3-carbamoyl-1H-pyrrole malate. Molecular Formula: C22H27FN4O2 · C4H6O5. Molecular Weight: 532.6.

[Description] This product is a capsule; the contents consist of yellow to orange granules.

[Use in Pregnancy and Lactation] Pregnancy Category D. Since angiogenesis is critical to embryonic and fetal development, and sunitinib inhibits angiogenesis, it may cause adverse effects on pregnancy. There are no adequate and well-controlled studies of this product in pregnant women. If this product is used during pregnancy, or if the patient becomes pregnant while receiving treatment with this product, the patient should be apprised of the potential hazard to the fetus. Women of childbearing potential should use effective contraception while receiving treatment with this product. The effects of sunitinib on the embryo were evaluated in pregnant rats (at doses of 0.3, 1.5, 3.0, and 5.0 mg/kg/day) and pregnant rabbits (at doses of 0.5, 1, 5, and 20 mg/kg/day). At a dose of 5 mg/kg/day (approximately 5.5 times the AUC at the recommended human daily dose [RDD]), a significant increase in the incidence of embryonic death and developmental abnormalities was observed in rats. In rabbit studies, a significant increase in the incidence of embryonic death was observed at a dose of 5 mg/kg/day; furthermore, at doses ≥ 1 mg/kg/day (approximately 0.3 times the AUC at the recommended human daily dose of 50 mg/day... ...times) developmental abnormalities were observed. Effects on development included an increased incidence of skeletal malformations—specifically in the ribs and vertebrae—in rat fetuses. In rabbit studies, cleft lip was observed at a dose of 1 mg/kg/day, while both cleft lip and cleft palate were observed at a dose of 5 mg/kg/day (approximately 2.7 times the AUC of the recommended daily human dose). In rat studies, no fetal abortions or malformations were observed at doses ≤ 3 mg/kg/day (approximately 2.3 times the recommended daily human dose). Lactating Women:

[Pediatric Use] No clinical studies have been conducted to establish the safety and efficacy of this product in pediatric patients.

[Geriatric Use] Of the 825 patients treated with this product for Gastrointestinal Stromal Tumor (GIST) and Advanced/Metastatic Renal Cell Carcinoma (MRCC), 277 (34%) were aged 65 years or older. No differences in safety or efficacy were observed between younger and older patients.

[Storage] Store at 25°C.

Product Specifications

Product Name: Sunitinib 25 mg * 28 Capsules — Sunitix (Sunitinib Malate) 25 mg (Beacon Pharmaceuticals)

Common Name: Sunitinib Malate Capsules

Composition: Sunitinib Malate

Dosage Form: Capsules

Specification: 25 mg * 28 capsules * 1 bottle

Manufacturer: Beacon Pharmaceuticals Co., Ltd.

Indications: 1. Gastrointestinal Stromal Tumor (GIST) in patients whose disease has progressed on or who are intolerant to imatinib mesylate therapy;

2. Advanced Renal Cell Carcinoma (RCC) in patients unsuitable for surgery;

3. Unresectable, metastatic, well-differentiated, progressive pancreatic neuroendocrine tumors (pNET) in adult patients.

Dosage and Administration: The recommended dose for the treatment of GIST and advanced RCC is 50 mg taken orally once daily; the medication is taken for 4 weeks, followed by a 2-week off-period (a 4/2 dosing schedule). It may be taken with or without food.