Select therapeutic use:

Bladder, kidney, and other urologic cancers:

Indications for SUTENT:

Advanced renal cell carcinoma (RCC). Adjuvant treatment of patients at high risk of recurrent RCC following nephrectomy.

Adult:

50mg once daily for 4 weeks on, then 2 weeks off until disease progression or unacceptable toxicity. Adjuvant: treat for nine 6-week cycles. Dose modifications for adverse reactions: see full labeling. Concomitant strong CYP3A4 inhibitors: may reduce dose to 37.5mg daily. Concomitant strong CYP3A4 inducers: may increase to max 87.5mg daily. ESRD on dialysis: may gradually increase subsequent doses up to 2-fold based on response.

Children:

Not established.

Boxed Warning:

Hepatotoxicity.

Warnings/Precautions:

Risk of hepatotoxicity (may be severe). Monitor LFTs at baseline, during each cycle of treatment and as clinically needed; interrupt if Grade 3 or 4 hepatotoxicity occurs and discontinue if no resolution, severe changes in LFTs, or other signs/symptoms of failure. Cardiovascular events: monitor for CHF, LVEF at baseline and periodically; interrupt and/or reduce dose if LVEF >20% but <50% below baseline; discontinue if CHF occurs. History of QT prolongation or pre-existing cardiac disease, bradycardia, electrolyte disturbances; perform periodic ECG, monitor electrolytes. Monitor BP at baseline and as indicated; withhold if hypertension develops until controlled. Not for use in lung cancer patients. Perform serial CBCs and physical exams to assess for hemorrhagic events. Risk of tumor lysis syndrome: monitor closely in RCC and GIST patients with high tumor burden. Permanently discontinue if severe cutaneous reactions (eg, erythema multiforme, SJS, TEN) develop. Monitor for proteinuria; perform baseline and periodic urinalyses; interrupt and reduce dose if 24-hr urine protein ≥3g; discontinue if nephrotic syndrome or repeat urine protein ≥3g persists. Monitor thyroid function at baseline, during treatment, and as indicated. Monitor blood glucose levels at baseline, during and after treatment discontinuation; adjust antidiabetic therapies as needed. Concomitant exposure to other risk factors (eg, bisphosphonates therapy, dental disease/invasive procedures) may increase the risk of osteonecrosis of the jaw (ONJ); withhold Sutent therapy for ≥3 weeks prior to scheduled dental surgery/invasive procedures or for development of ONJ until resolution. Impaired wound healing: withhold for ≥3 weeks prior to elective surgery; do not give for ≥2 weeks after major surgery and until adequate healing. Severe hepatic impairment. Embryo-fetal toxicity. Advise use of effective contraception during and for ≥4 weeks (females) or 7 weeks (males w. female partners) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for ≥4 weeks after the last dose).

Pharmacologic Class:

Kinase inhibitor.

Interactions:

May be potentiated by strong CYP3A4 inhibitors (eg, ketoconazole); use alternatives or consider dose reduction if needed (see Adult dose). May be antagonized by CYP3A4 inducers (eg, rifampin); use alternatives or consider dose increase if needed (see Adult dose). Avoid grapefruit. Caution with concomitant antiarrhythmics. Monitor ECGs more frequently with concomitant drugs known to prolong the QT interval.

Adverse Reactions:

Fatigue/asthenia, diarrhea, mucositis/stomatitis, nausea, decreased appetite/anorexia, vomiting, abdominal pain, hand-foot syndrome, hypertension, bleeding events, dysguesia/altered taste, dyspepsia, thrombocytopenia; ventricular arrhythmias, thrombotic microangiopathy (discontinue if develops), necrotizing fasciitis (discontinue if occurs), reversible posterior leukoencephalopathy syndrome.

Generic Availability:

NO

How Supplied:

Caps—28

Colorectal and other GI cancers:

Indications for SUTENT:

Gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate.

Adult:

50mg once daily for 4 weeks on, then 2 weeks off until disease progression or unacceptable toxicity. Dose modifications for adverse reactions: see full labeling. Concomitant strong CYP3A4 inhibitors: may reduce dose to 37.5mg daily. Concomitant strong CYP3A4 inducers: may increase to max 87.5mg daily. ESRD on dialysis: may gradually increase subsequent doses up to 2-fold based on response.

Children:

Not established.

Boxed Warning:

Hepatotoxicity.

Warnings/Precautions:

Risk of hepatotoxicity (may be severe). Monitor LFTs at baseline, during each cycle of treatment and as clinically needed; interrupt if Grade 3 or 4 hepatotoxicity occurs and discontinue if no resolution, severe changes in LFTs, or other signs/symptoms of failure. Cardiovascular events: monitor for CHF, LVEF at baseline and periodically; interrupt and/or reduce dose if LVEF >20% but <50% below baseline; discontinue if CHF occurs. History of QT prolongation or pre-existing cardiac disease, bradycardia, electrolyte disturbances; perform periodic ECG, monitor electrolytes. Monitor BP at baseline and as indicated; withhold if hypertension develops until controlled. Not for use in lung cancer patients. Perform serial CBCs and physical exams to assess for hemorrhagic events. Risk of tumor lysis syndrome: monitor closely in RCC and GIST patients with high tumor burden. Permanently discontinue if severe cutaneous reactions (eg, erythema multiforme, SJS, TEN) develop. Monitor for proteinuria; perform baseline and periodic urinalyses; interrupt and reduce dose if 24-hr urine protein ≥3g; discontinue if nephrotic syndrome or repeat urine protein ≥3g persists. Monitor thyroid function at baseline, during treatment, and as indicated. Monitor blood glucose levels at baseline, during and after treatment discontinuation; adjust antidiabetic therapies as needed. Concomitant exposure to other risk factors (eg, bisphosphonates therapy, dental disease/invasive procedures) may increase the risk of osteonecrosis of the jaw (ONJ); withhold Sutent therapy for ≥3 weeks prior to scheduled dental surgery/invasive procedures or for development of ONJ until resolution. Impaired wound healing: withhold for ≥3 weeks prior to elective surgery; do not give for ≥2 weeks after major surgery and until adequate healing. Severe hepatic impairment. Embryo-fetal toxicity. Advise use of effective contraception during and for ≥4 weeks (females) or 7 weeks (males w. female partners) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for ≥4 weeks after the last dose).

Pharmacologic Class:

Kinase inhibitor.

Interactions:

May be potentiated by strong CYP3A4 inhibitors (eg, ketoconazole); use alternatives or consider dose reduction if needed (see Adult dose). May be antagonized by CYP3A4 inducers (eg, rifampin); use alternatives or consider dose increase if needed (see Adult dose). Avoid grapefruit. Caution with concomitant antiarrhythmics. Monitor ECGs more frequently with concomitant drugs known to prolong the QT interval.

Adverse Reactions:

Fatigue/asthenia, diarrhea, mucositis/stomatitis, nausea, decreased appetite/anorexia, vomiting, abdominal pain, hand-foot syndrome, hypertension, bleeding events, dysguesia/altered taste, dyspepsia, thrombocytopenia; ventricular arrhythmias, thrombotic microangiopathy (discontinue if develops), necrotizing fasciitis (discontinue if occurs), reversible posterior leukoencephalopathy syndrome.

Generic Availability:

NO

How Supplied:

Caps—28

Pancreatic, thyroid, and other endocrine cancers:

Indications for SUTENT:

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

Adult:

37.5mg once daily until disease progression or unacceptable toxicity. Dose modifications for adverse reactions: see full labeling. Concomitant strong CYP3A4 inhibitors: may reduce dose to 25mg daily. Concomitant strong CYP3A4 inducers: may increase to max 62.5mg daily. ESRD on dialysis: may gradually increase subsequent doses up to 2-fold based on response.

Children:

Not established.

Boxed Warning:

Hepatotoxicity.

Warnings/Precautions:

Risk of hepatotoxicity (may be severe). Monitor LFTs at baseline, during each cycle of treatment and as clinically needed; interrupt if Grade 3 or 4 hepatotoxicity occurs and discontinue if no resolution, severe changes in LFTs, or other signs/symptoms of failure. Cardiovascular events: monitor for CHF, LVEF at baseline and periodically; interrupt and/or reduce dose if LVEF >20% but <50% below baseline; discontinue if CHF occurs. History of QT prolongation or pre-existing cardiac disease, bradycardia, electrolyte disturbances; perform periodic ECG, monitor electrolytes. Monitor BP at baseline and as indicated; withhold if hypertension develops until controlled. Not for use in lung cancer patients. Perform serial CBCs and physical exams to assess for hemorrhagic events. Risk of tumor lysis syndrome: monitor closely in RCC and GIST patients with high tumor burden. Permanently discontinue if severe cutaneous reactions (eg, erythema multiforme, SJS, TEN) develop. Monitor for proteinuria; perform baseline and periodic urinalyses; interrupt and reduce dose if 24-hr urine protein ≥3g; discontinue if nephrotic syndrome or repeat urine protein ≥3g persists. Monitor thyroid function at baseline, during treatment, and as indicated. Monitor blood glucose levels at baseline, during and after treatment discontinuation; adjust antidiabetic therapies as needed. Concomitant exposure to other risk factors (eg, bisphosphonates therapy, dental disease/invasive procedures) may increase the risk of osteonecrosis of the jaw (ONJ); withhold Sutent therapy for ≥3 weeks prior to scheduled dental surgery/invasive procedures or for development of ONJ until resolution. Impaired wound healing: withhold for ≥3 weeks prior to elective surgery; do not give for ≥2 weeks after major surgery and until adequate healing. Severe hepatic impairment. Embryo-fetal toxicity. Advise use of effective contraception during and for ≥4 weeks (females) or 7 weeks (males w. female partners) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for ≥4 weeks after the last dose).

Pharmacologic Class:

Kinase inhibitor.

Interactions:

May be potentiated by strong CYP3A4 inhibitors (eg, ketoconazole); use alternatives or consider dose reduction if needed (see Adult dose). May be antagonized by CYP3A4 inducers (eg, rifampin); use alternatives or consider dose increase if needed (see Adult dose). Avoid grapefruit. Caution with concomitant antiarrhythmics. Monitor ECGs more frequently with concomitant drugs known to prolong the QT interval.

Adverse Reactions:

Fatigue/asthenia, diarrhea, mucositis/stomatitis, nausea, decreased appetite/anorexia, vomiting, abdominal pain, hand-foot syndrome, hypertension, bleeding events, dysguesia/altered taste, dyspepsia, thrombocytopenia; ventricular arrhythmias, thrombotic microangiopathy (discontinue if develops), necrotizing fasciitis (discontinue if occurs), reversible posterior leukoencephalopathy syndrome.

Generic Availability:

NO

How Supplied:

Caps—28