Sunitinib

Sunitinib is a prescription medication indicated for the treatment of advanced or progressive tumors of the stomach, intestines, esophagus, pancreas, or kidneys.

• Sunitinib is available under the following different brand names: Sutent

Adult dosage

Capsule

• 12.5mg
• 25mg
• 37.5mg
• 50mg

Gastrointestinal Stromal Tumor

Adult dosage

• 50 mg orally every day for 4 weeks, THEN 2 weeks drug-free, repeat cycle
• Continue until disease progression or unacceptable toxicity

Renal Cell Carcinoma

Adult dosage

• 50 mg orally every day  for 4 weeks, THEN 2 weeks drug-free, repeat cycle
• Continue until disease progression or unacceptable toxicity

Pancreatic Neuroendocrine Tumors

Adult dosage

• 37.5 mg orally every day continuously without a scheduled off-treatment period
• Continue until disease progression or unacceptable toxicity

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

Common side effects of Sunitinib include:

• unusual or unpleasant taste in the mouth
• cough
• nausea
• vomiting
• upset stomach
• constipation
• dry skin
• changes in skin or hair color (yellow skin or lighter skin/hair)
• hair loss
• joint pain
• back pain
• fatigue
• tiredness
• weakness
• fever
• diarrhea
• mouth pain/sores
• abdominal pain
• rash or other skin changes such as dry or cracked skin
• blisters or rash on hands or feet
• loss of appetite
• pain or swelling in the arms or legs
• numbness or tingling of the arms or legs
• shortness of breath
• bleeding
• watery eyes
• swelling around the eyes
• chest pain
• general ill feeling, or
• uneven heart rate.

Serious side effects of Sunitinib include:

• headache,
• easy bruising or bleeding,
• swelling ankles or feet,
• unusual weight changes,
• cold or heat intolerance,
• unusual tiredness,
• black or bloody stools,
• vomit that looks like coffee grounds,
• coughing up blood,
• slow wound healing,
• jaw pain,
• toe/joint/back pain,
• painful urination,
• cloudy/pink/bloody urine,
• changes in the amount of urine,
• muscle weakness/cramping/twitching,
• signs of low blood sugar (such as hunger, shakiness, fast heartbeat, sweating),
• mental/mood changes (such as decreased alertness, irritability, nervousness), or
• vision changes (such as decreased vision).

Rare side effects of Sunitinib include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Sunitinib has severe interactions with the following drug:
  • lefamulin
• Sunitinib has serious interactions with at least 66 other drugs.
• Sunitinib has moderate interactions with at least 139 other drugs.
• Sunitinib has minor interactions with the following drugs:
  • azithromycin
  • chloroquine

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Sunitinib?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Sunitinib?”

Cautions

• Fatal liver failure has been observed (see Black Box Warnings)
• Hemorrhagic events, some of which were fatal, have involved the gastrointestinal tract, respiratory tract, tumor, urinary tract, and brain; interrupt therapy for Grade 3 or 4 hemorrhagic events until resolution to Grade less than or equal to 1 or baseline, then resume at a reduced dose; discontinue therapy in patients without resolution of Grade 3 or 4 hemorrhagic events; 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 above 3 g; discontinue for repeat episodes of protein above 3 g despite dose reductions or nephrotic syndrome
• Hyperthyroidism, some followed by hypothyroidism, has been reported; monitor thyroid function at baseline, periodically during treatment, and as clinically indicated; initiate and/or adjust therapies for thyroid dysfunction as appropriate
• Impaired wound healing reported; withhold therapy for at least 3 weeks before elective surgery; do not administer for at least 2 weeks following major surgery and until adequate wound healing; safety of resumption of therapy after resolution of wound healing complications has not been established
• 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 about the childbearing potential of the potential hazard to the fetus
• 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
• Cases of tumor lysis syndrome (TLS) are reported in patients 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 outcomes reported in clinical trials and postmarketing experience; not approved for use in combination with bevacizumab
• Hypoglycemia may occur; monitor blood glucose levels regularly during and after discontinuation treatment; assess if antidiabetic drugs dosage modifications are necessary
• Monitor blood pressure at baseline and as clinically indicated; initiate and/or adjust antihypertensive therapy as appropriate; in cases of Grade 3 hypertension, withhold until resolution to Grade less than or equal to 1 or baseline, then resume at a reduced dose; discontinue therapy in patients who develop Grade 4 hypertension
• Osteonecrosis
  • Osteonecrosis of the jaw was reported; concomitant exposure to other risk factors, such as bisphosphonates or dental disease/invasive dental procedures, may increase the risk of ONJ
  • Perform oral examination before initiation of therapy and periodically during therapy; advise patients regarding good oral hygiene practices
  • Withhold treatment for at least 3 weeks before scheduled dental surgery or invasive dental procedures, if possible; withhold treatment for development of ONJ until complete resolution; the safety of resumption after resolution of osteonecrosis of the jaw not established
• Reversible posterior leukoencephalopathy syndrome (RPLS)
  • RPLS some of which were fatal reported
  • Patients can present with hypertension, headache, decreased alertness, altered mental functioning, and visual loss, including cortical blindness
  • Magnetic resonance imaging is necessary to confirm the diagnosis; withhold therapy until resolution;
  • The safety of reinitiating therapy in patients with RPLS is unknown
• Cardiovascular risks
  • Cardiovascular events (e.g., 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 the 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 above 20% but below 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 for signs and symptoms of congestive heart failure
• Drug interaction overview
  • Coadministration with strong CYP3A4 inhibitors
    • Use an alternative with no or minimal CYP3A4 activity
    • Strong CYP3A4 inhibitors may increase sunitinib concentrations
  • Coadministration with strong CYP3A4 inducers
    • Use an alternative with no or minimal CYP3A4 activity
    • Coadministration with CYP3A4 inducers may decrease sunitinib concentrations
  • Coadministration with QT-prolonging drugs
    • Treatment is associated with QTc interval prolongation; monitor QT interval with ECGs more frequently in patients who require treatment with concomitant medications known to prolong the QT interval

Pregnancy and Lactation

• Based on animal reproduction studies and its mechanism of action, fetal harm may occur when administered to pregnant females
• No data available in pregnant women to inform a drug-associated risk
• Verify pregnancy status of females of reproductive potential before initiating treatment
• Contraception
  • Females of reproductive potential: Use effective contraceptives during treatment and for at least 4 weeks after the final dose
  • Males with female partners of reproductive potential: Use effective contraceptive during treatment and for 7 weeks after the final dose
• Infertility
  • Based on findings in animals, male and female fertility may be impaired
• Lactation
  • There is no information regarding the presence of sunitinib and its metabolites in human milk
  • Sunitinib and its metabolites were excreted in rat milk at concentrations up to 12-fold higher than in plasma
  • Advise females not to breastfeed during treatment and for at least 4 weeks after the final dose