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Kitent (Sunitinib)

Kitent (Sunitinib)

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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). Sunitinib inhibition of the activity of these RTKs has been demonstrated in biochemical and cellular assays, and inhibition of function has been demonstrated in cell proliferation assays. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays.




DOSAGE AND ADMINISTRATION

DOSAGE AND ADMINISTRATION

GIST and Advanced RCC:

 50 mg orally once daily, with or without food, 4 weeks on treatment followed by 2 weeks off.

 

 Adjuvant RCC:

50 mg orally once daily, with or without food, 4 weeks on treatment followed by 2 weeks off for nine 6-week cycles.

 

 pNET:

37.5 mg orally once daily, with or without food, continuously without a scheduled off-treatment period. Dose Modification: Dose interruptions and/or dose adjustments of 12.5 mg recommended based on individual safety and tolerability.

INDICATIONS

Sunitinib is a kinase inhibitor indicated for:

 the treatment of gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate

the treatment of advanced renal cell carcinoma (RCC)

 the adjuvant treatment of adult patients at high risk of recurrent RCC following nephrectomy

 the treatment of progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) in patients with unresectable locally advanced or metastatic disease.


WARNINGS AND PRECAUTIONS

WARNINGS AND PRECAUTIONS

Hepatotoxicity, including fatal liver failure, has been observed. Monitor liver function tests before initiation of treatment, during each cycle of treatment, and as clinically indicated. Interrupt Sunitinib for Grade 3 or 4 drug-related hepatic adverse reactions and discontinue if there is no resolution. Do not restart Sunitinib if patients experience severe changes in liver function tests or have signs and symptoms of liver failure.

 

 Cardiovascular events including myocardial ischemia, myocardial infarction, left ventricular ejection fraction declines to below the lower limit of normal and cardiac failure including death have occurred. Monitor patients for signs and symptoms of congestive heart failure. Discontinue Sunitinib for clinical manifestations of congestive heart failure.

 

 Prolonged QT intervals and Torsade de Pointes have been observed. Monitor patients at higher risk for developing QT interval prolongation. Consider monitoring of electrocardiograms and electrolytes.

 

 Hypertension may occur. Monitor blood pressure and treat as needed.

 

 Hemorrhagic events, including tumor-related hemorrhage, and viscus perforation (both with fatal events) have occurred. Perform serial complete blood counts and physical examinations.

 

 Cases of Tumor Lysis Syndrome (TLS) (some fatal) have been reported primarily in patients with RCC and GIST with high tumor burden. Monitor these patients closely and treat as clinically indicated.

 

 Thrombotic microangiopathy (TMA), including thrombotic thrombocytopenic purpura and hemolytic uremic syndrome, sometimes leading to renal failure or a fatal outcome, has been reported. Discontinue Sunitinib in patients developing TMA.

 

 Proteinuria, including renal failure or a fatal outcome, has occurred. Monitor urine protein. Interrupt treatment for 24-hour urine protein ≥3 grams. Discontinue for repeat episodes of protein 3 grams despite dose reductions or nephrotic syndrome.

 

 Necrotizing fasciitis, erythema multiforme, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN) (some fatal) have occurred. Discontinue Sunitinib if these events occur.

 

 Thyroid dysfunction may occur. Patients with signs and/or symptoms suggestive of hypothyroidism or hyperthyroidism should have laboratory monitoring of thyroid function performed and be treated as per standard medical practice.

 

 Hypoglycemia may occur. Check blood glucose levels regularly and assess if antidiabetic drug dose modifications are required.

 

 Osteonecrosis of the jaw has been reported. Consider preventive dentistry prior to treatment with Sunitinib. If possible, avoid invasive dental procedures, particularly in patients receiving intravenous bisphosphonate therapy.

 

  Wound Healing: Impaired wound healing has occurred with Sunitinib . Temporary interruption of therapy with SUTENT is recommended in patients undergoing major surgical procedures.

 

 Embryo-Fetal Toxicity: Can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception.


DRUG INTERACTIONS

DRUG INTERACTIONS

­CYP3A4 Inhibitors: Consider dose reduction of Sunitinib when administered with strong CYP3A4 inhibitors.

 CYP3A4 Inducers: Consider dose increase of sunitinib when administered with CYP3A4 inducers.


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