Sunitinib

What it is and how it works

Mechanism of Action Sunitinib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs), some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRα and PDGFRβ), vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET).

Indications

Sunitinib malate capsules are a kinase inhibitor indicated for: treatment of adult patients with gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate. treatment of adult patients with advanced renal cell carcinoma (RCC). adjuvant treatment of adult patients at high risk of recurrent RCC following nephrectomy. treatment of progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) in adult patients with unresectable locally advanced or metastatic disease. Gastrointestinal Stromal Tumor Sunitinib malate capsules are indicated for the treatment of adult patients with gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate. Advanced Renal Cell Carcinoma Sunitinib malate capsules are indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC). Adjuvant Treatment of Renal Cell Carcinoma Sunitinib malate capsules are indicated for the adjuvant treatment of adult patients at high risk of recurrent RCC following nephrectomy.

Dosage and administration (summary)

and Advanced RCC : The recommended dosage is 50 mg orally once daily for the first 4 weeks of each 6-week cycle (Schedule 4/2). Adjuvant Treatment of RCC : The recommended dosage is 50 mg orally once daily for the first 4 weeks of a 6-week cycle (Schedule 4/2) for a maximum of 9 cycles. pNET : The recommended dosage is 37.5 mg orally once daily. Recommended Dosage for GIST and Advanced RCC The recommended dosage of sunitinib malate capsules for gastrointestinal stromal tumor (GIST) and advanced renal cell carcinoma (RCC) is 50 mg taken orally once daily, on a schedule of 4 weeks on treatment followed by 2 weeks off (Schedule 4/2) until disease progression or unacceptable toxicity.

Contraindications

None. None

Warnings and precautions

Hepatotoxicity : Fatal liver failure has been observed. Monitor liver function tests at baseline, during each cycle, and as clinically indicated. Interrupt sunitinib malate for Grade 3 hepatotoxicity until resolution to Grade ≤1 or baseline and resume sunitinib malate at a reduced dose; discontinue if no resolution. Discontinue sunitinib malate in patients with Grade 4 hepatoxicity, in patients who have subsequent severe changes in liver function tests or other signs and symptoms of liver failure.

Pregnancy

Pregnancy Risk Summary Based on animal reproduction studies and its mechanism of action, sunitinib malate can cause fetal harm when administered to a pregnant woman . There are no available data in pregnant women to inform a drug-associated risk.

Storage and supply

12.5 mg capsules Hard gelatin capsule with maroon opaque cap and body, imprinted with TEVA over 8199 on both cap and body in black ink. Available as follows: Bottles of 28 capsules: NDC 42291-901-28 25 mg capsules Hard gelatin capsule with light brown opaque cap and maroon opaque body, imprinted with TEVA over 8224 on both cap and body in black ink…

Source: Sunitinib Malate (Sunitinib Malate) — US FDA prescribing information, 2026-01-16, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.