Sutent

Gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib; Advanced renal cell carcinoma (RCC); Progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) in patients with unresectable, locally advanced, or metastatic disease

GIST and RCC: 50 mg orally once daily on a schedule of 4 weeks on treatment followed by 2 weeks off (Schedule 4/2)
pNET: 37.5 mg orally once daily continuously without a scheduled off-treatment period
Take with or without food

Capsules: 12.5 mg, 25 mg, 37.5 mg, 50 mg

Refer to the complete prescribing information for contraindications. Sutent prescribing should account for patient-specific factors including hypersensitivity to the active ingredient or any excipients.

• Hepatotoxicity: Liver failure (some fatal) reported. Monitor LFTs before each cycle.
• Cardiovascular Events: Decreased LVEF and heart failure reported. Monitor LVEF at baseline and periodically.
• QT Prolongation and Torsades de Pointes: Use with caution in patients at risk. Monitor ECGs and electrolytes.
• Hypertension: Monitor and treat as needed. Suspend for severe uncontrolled hypertension.
• Hemorrhagic Events: Including tumor-related hemorrhage (GI, respiratory tract).
• Thyroid Dysfunction: Hypothyroidism in up to 46% of RCC patients. Monitor thyroid function.
• Adrenal Insufficiency: Monitor for signs/symptoms.
• Jaw Osteonecrosis: Consider preventive dentistry prior to treatment.

Fatigue (62%), diarrhea (61%), nausea (52%), mucositis/stomatitis (47%), vomiting (39%), dyspepsia (34%), decreased appetite (33%), abdominal pain (30%), hypertension (34%), skin discoloration (30%), rash (24%), hand-foot syndrome (29%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Sunitinib is a multi-kinase inhibitor that targets PDGFRα and PDGFRβ, VEGFR1-3, KIT, FLT3, CSF-1R, and RET. It inhibits tumor cell proliferation and angiogenesis by blocking receptor tyrosine kinase signaling. The anti-tumor activity results from inhibition of multiple receptor tyrosine kinases involved in tumor growth, pathologic angiogenesis, and metastatic progression.

Tmax: 6-12 hours. Half-life: 40-60 hours (active metabolite: 80-110 hours). Protein binding: 95% (sunitinib), 90% (metabolite). Metabolized primarily by CYP3A4. Primarily excreted in feces (61%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• Sunitinib RCC — Sunitinib vs. interferon-α in 1L metastatic RCC. Phase III, n=750.
  🔬 NCT00098657 ↗ 📄 Primary Publication ↗

Sutent has FDA-approved indications across the following cancer types covered on PipelineEvidence: