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sunitinib (Rx)Brand and Other Names:Sutent

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 12.5mg
  • 25mg
  • 50mg
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GI Stromal Tumor, Metastatic Renal Cell Carcinoma

50 mg PO qDay for 4 weeks, THEN 2 weeks drug-free, repeat cycle

Dose modification GI stromal tumor (GIST) or metastic renal cell carcinoma (MRCC)

  • Increase or reduce dose in 12.5-mg increments based on individual safety and tolerability
  • Concurrent CYP3A4 Inhibitors: Consider dose reduction to 37.5 mg qDay
  • Concurrent CYP3A4 Inducers: Consider dose increase not to exceed 87.5 mg qDay (in 12.5 mg increments)
  • Ideally, selection of an alternate concomitant medication with no or minimal enzyme inhibition/induction is recommended

Pancreatic Neuroendocrine Tumors

Indicated for progressive, well-differentiated pancreatic neuroendocrine tumors in patients with unresectable locally advanced or metastatic disease

Standard dose: 37.5 mg PO qDay continuously without a scheduled off-treatment period

Dose modification Pancreatic Neuroendocrine Tumors (PNET)

  • Increase or reduce dose in 12.5-mg increments based on individual safety and tolerability
  • Coadministration with potent CYP4503A4 inhibitors: Consider dose reduction to 25 mg PO qDay
  • Coadministration with CYP4503A4 inducers: Consider dose increase not to exceed 62.5 mg PO qDay
  • Ideally, selection of an alternate concomitant medication with no or minimal enzyme inhibition/induction is recommended

Renal Impairment

No dose adjustment necessary

Hepatic Impairment

Mild to moderate impairment: Dose adjustment not necessary for initial dose; monitor subsequent doses

Severe impairment: Not studied

Monitoring

CBC, blood chemistries

Safety and efficacy not established

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Interactions

Interaction Checker

sunitinib and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Dyspepsia (MRCC 46%)

            Altered taste (MRCC 43%; GIST 21%)

            Fatigue (GIST 42%; MRCC 74%)

            Diarrhea (GIST 40%; MRCC 55%)

            Rash (MRCC 38%; GIST 14%)

            Vomiting (MRCC 37%; GIST 24%)

            Constipation (MRCC 34%; GIST 20%)

            Skin discoloration (MRCC 33%; GIST 30%)

            Abdominal pain (GIST 33%; MRCC 20%)

            Nausea (GIST 31%; MRCC 54%)

            Anorexia (MRCC 31%; GIST 33%)

            Mucositis/stomatitis (GIST 29%; MRCC 53%)

            Dyspnea (MRCC 28%; GIST 10%)

            HTN (MRCC 28%; GIST 15%)

            Arthralgia (MRCC 28%; GIST 12%)

            Bleeding (MRCC 26%; GIST 18%)

            Headache (MRCC 25%; GIST 13%)

            Asthenia (GIST 22%)

            Lymphopenia (MRCC 21%)

            Fever (GIST 18%; MRCC 15%),

            Limb pain (MRCC 18%)

            Back pain (MRCC 17%; GIST 11%)

            Myalgia (MRCC 17%; GIST 14%)

            Cough (MRCC 17%; GIST 8%)

            Dry skin (17%)

            Hair color changes (17%)

            Neutropenia (MRCC 13%; GIST 11%)

            Alopecia (MRCC 12%)

            Hand-foot syndrome (MRCC 12%; GIST 14%)

            Dehydration (MRCC 11%)

            1-10%

            Venous thrombotic events

            Hemorrhoids

            Pancreatitis

            Flu-like syndrome

            <1%

            Hepatotoxicity

            Acute renal failure

            Adrenal dysfunction

            Postmarketing Reports

            Blood and lymphatic system disorders: Thrombotic microangiopathy; hemorrhage associated with thrombocytopenia (hold dose, following resolution, treatment may be resumed at the discretion of the treating physician)

            Immune system disorders: Hypersensitivity reactions, including angioedema Infections and infestations: Serious infection (with or without neutropenia); necrotizing fasciitis, including of the perineum; most commonly observed infections include respiratory, urinary tract, skin infections, and sepsis

            Metabolism and nutrition disorders: Tumor lysis syndrome

            Musculoskeletal and connective tissue disorders: Fistula formation, sometimes associated with tumor necrosis and/or regression; osteonecrosis of the jaw, and myopathy and/or rhabdomyolysis with or without acute renal failure

            Renal and urinary disorders: Renal impairment and/or failure; proteinuria; rare cases of nephrotic syndrome (discontinue treatment)

            Respiratory disorders: Pulmonary embolism; pulmonary hemorrhage

            Skin and subcutaneous tissue disorders: Pyoderma gangrenosum, including positive dechallenges

            Vascular disorders: Arterial thromboembolic events, most frequent events included CVA, TIA, cerebral infarction

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            Warnings

            Black Box Warnings

            Hepatotoxicity has been observed in clinical trials (7/2281) and post-marketing experience (0.3%)

            Hepatotoxicity may be severe and deaths have been reported

            Monitor liver function tests (ALT, AST, bilirubin) before treatment initiation, during each treatment cycle, and as clinically indicated

            Interrupted for Grade 3 or 4 drug-related hepatic related adverse events and discontinued if there is no resolution

            Do not restart if subsequently experience severe changes in liver function tests or other signs and symptoms of liver failure emerge

            Safety in patients with ALT or AST >2.5 x ULN or, if due to liver metastases, >5 x ULN has not been established

            Use and handle product with caution

            Contraindications

            Hypersensitivity

            Renal impairment

            Cautions

            Hepatotoxicity, including liver failure, observed; monitor liver function tests before initiation of treatment, during each cycle of treatment, and as clinically indicated; interrupt therapy for Grade 3 or 4 drug-related hepatic adverse events and discontinue if no resolution; do not restart if patient subsequently experiences severe changes in liver function tests or have other signs and symptoms of liver failure (see Black Box Warning)

            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

            Hemorrhagic events including tumor-related hemorrhage reported; perform serial complete blood counts and physical examinations

            Adrenal hemorrhage observed in animal studies; monitor adrenal function in case of stress such as surgery, trauma or severe infection

            Monitor urine protein; interrupt treatment for 24-hr urine protein ≥3 g; discontinue for repeat episodes of protein ≥3 g despite dose reductions or nephrotic syndrome

            Hypothyroidism reported; measure baseline thyroid function in patients with hypothyroidism or hyperthyroidism and treat per standard medical practice prior to initiating therapy

            Avoid concurrent St John's Wort and other metabolic inducers

            Impaired wound healing reported; temporary interruption of therapy recommended if undergoing major surgical procedures

            Severe cutaneous reactions have been reported, including cases of erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis, some of which were fatal; necrotizing fasciitis, including fatal cases, also reported

            Advise women of childbearing potential of potential hazard to fetus and to avoid becoming pregnant

            Prolonged QT intervals and Torsade de Pointes reported; use caution in patients at higher risk for developing QT interval prolongation; consider monitoring with on-treatment ECG and electrolytes; hypertension may occur; monitor blood pressure and treat as needed

            Cases of tumor lysis syndrome (TLS) reported in atients with RCC and GIST with high tumor burden; monitor closely and treat as necessary

            Thrombotic microangiopathy, including thrombotic thrombocytopenic purpura and hemolytic uremic syndrome, sometimes leading to renal failure or fatal outcome reported in clinical trials and post-marketing experience

            Hypoglycemia may occur; monitor blood glucose levels regularly and assess if anti-diabetic drug dose modifications necessary

            Osteonecrosis of the jaw reported; consider preventive dentistry prior to treatment; avoid, if possible, invasive dental procedures, particularly in patients receiving intravenous bisphosphonate therapy

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            Pregnancy & Lactation

            Pregnancy Category: D

            Lactation: Unknown if excreted in human milk; a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother

            Bosutinib and/or its metabolites were excreted in the milk of lactating rats; radioactivity was present in the plasma of suckling offspring 24-48 hr after lactating rats received a single oral dose of radioactive bosutinib

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Multikinase inhibitor (including VEGF & PDGF receptor tyrosine kinases) some of which are implicated in tumor growth, angiogenesis, and metastasis

            Pharmacokinetics

            Bioavailability: Not affected by food

            Peak plasma time: 6-12 hr

            Half-life elimination: 40-60 hr

            Vd: 2230 L

            Protein bound: Sunitinib 95%; primary active metabolite: 90%

            Metabolism: by CYP3A4 to a primary active metabolite which is further metabolized by CYP3A4

            Excretion: Feces (61%); urine (16%)

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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