sunitinib (Rx)

Brand and Other Names:Sutent
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 12.5mg
  • 25mg
  • 50mg
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Gastrointestinal Stromal Tumor

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

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

Renal Cell Carcinoma

Indicated for treatment of advanced renal cell carcinoma (RCC)

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

Adjuvant treatment of RCC

  • Indicated for the adjuvant treatment of adult patients at high risk of recurrent RCC following nephrectomy
  • 50 mg PO qDay for 4 weeks, THEN 2 weeks drug-free, repeat cycle for a total of nine 6-week cycles

Pancreatic Neuroendocrine Tumors

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

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

Dosage Modification Renal Impairment

Dose interruption and/or dose modification in 12.5 mg increments or decrements is recommended based on individual safety and tolerability

Maximum dose administered in the pNET study was 50 mg daily

In the adjuvant RCC study, the minimum dose administered was 37.5 mg

Coadministration with CYP3A4 inhibitors or inducers

  • Strong CYP3A4 inhibitors
    • Strong CYP3A4 inhibitors may increase sunitinib plasma concentrations
    • Select an alternate concomitant medication with no or minimal enzyme inhibition potential is recommended
    • Reduce dose for sunitinib to a minimum of 37.5 mg (GIST and RCC) or 25 mg (pNET) daily should be considered
  • CYP3A4 inducers
    • CYP3A4 inducers may decrease sunitinib plasma concentrations
    • Selection of an alternate concomitant medication with no or minimal enzyme inhibition is recommended
    • Increase dose for sunitinib to a maximum of 87.5 mg (GIST and RCC) or 62.5 mg (pNET) daily should be considered if coadministered with a CYP3A4 inducer cannot be avoided
    • If dose is increased, the patient should be monitored carefully for toxicity

Renal impairment

  • No dose adjustment necessary with any degree of renal impairment in patients not on dialysis
  • ESRD on hemodialysis: No adjustment to the starting dose is required; however, compared to patients with normal renal function, the sunitinib exposure is 47% lower in patients with ESRD on hemodialysis; may require gradual dose increase (up to 2-fold) based on safety and tolerability

Hepatic impairment

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

Dosing Considerations

Monitor CBC count, blood chemistries

Safety and efficacy not established

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Interactions

Interaction Checker

and sunitinib

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    No Interactions Found
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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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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)

            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

            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 (see Pregnancy)

            Prolonged QT intervals and Torsade de Pointes may occur in a dose-dependent manner; 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 during and after discontinuation treatment; assess if antidiabetic drugs dosage modifications are 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

            Monitor patients for hypertension and treat as needed with standard antihypertensive therapy; in cases of severe hypertension, temporary suspend treatment until hypertension is controlled

            Drug interactions overview

            • See Dosage Modifications
            • Coadministration with strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole) may increase sunitinib concentrations
            • Coadministration with CYP3A4 inducers (eg, dexamethasone, phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital, St. John’s Wort) may decrease sunitinib concentrations

            Cardiovascular risks

            • Cardiovascular events (eg, heart failure, cardiomyopathy, myocardial ischemia, and myocardial infarction), some of which were fatal, have been reported
            • Increased risk for heart failure and high grade heart failure; discontinue treatment if patient presents with signs or symptoms of congestive heart failure (CHF); interrupt and/or reduce dose in patients without clinical evidence of CHF who either have an ejection fraction (EF) of >20% but <50% below baseline or below the lower limit of normal if baseline EF is not obtained
            • Cardiac dysfunction occurs 28 to 180 days after sunitinib initiation and most commonly after the third cycle
            • Heart failure risk is associated with preexisting hypertension and coronary artery disease
            • Monitor patients for signs and symptoms of congestive heart failure
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            Pregnancy & Lactation

            Pregnancy

            No available data established in pregnant women to inform a drug-associated risk In animal developmental and reproductive toxicology studies, oral administration of sunitinib to pregnant rats and rabbits throughout organogenesis resulted in teratogenicity (embryolethality, craniofacial and skeletal malformations) at 5.5 and 0.3 times the AUC in patients administered the recommended daily doses (RDD), respectively

            Advise pregnant women or females of reproductive potential of the potential hazard to a fetus

            Females of reproductive potential should have a pregnancy test before initiating treatment

            Advise females of reproductive potential to use effective contraception during treatment and for at least 4 weeks after the last dose

            Based on findings in animal reproduction studies, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 7 weeks after the last dose

            Based on findings in animals, male and female fertility may be compromised by treatment

            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

            Parent drug 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

            Because of the potential for serious adverse reactions in breastfed infants from sunitinib, advise a lactating woman not to breastfeed during treatment with sunitinib and for at least 4 weeks after the last dose

            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 and 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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            Administration

            Oral administration

            Take with or without food

            Do not drink grapefruit juice or eat grapefruit during your treatment

            Missed dose

            • Missed dose <12 hr: Take the missed dose right away
            • Missed dose >12 hr: Take next dose at regular time
            • Do not make up missed dose

            Storage

            Tablets: Store at room temperature at 68-77°F (20-25°C)

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

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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.
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            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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.