• Sutent is a brand (trade) name for sunitinib which is a medication that may be used to treat certain types of renal cell carcinoma (RCC) and other advanced cancers.
• Sutent (sunitinib) works by inhibiting multiple receptor tyrosine kinases (RTKs). RTKs are receptors on the surface of cells that are involved in mediating cell-to-cell communication and controlling a wide range of complex biological functions, such as cell growth, motility, differentiation, and metabolism. Activation of some of these receptors is associated with tumor growth, angiogenesis (the formation of new blood vessels from existing blood vessels), and metastatic progression of cancer. Sunitinib inhibits the activity of multiple kinases such as 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). By inhibiting the phosphorylation of these kinases, Sutent inhibits tumor growth and spread.
• Sutent belongs to the class of medicines known as multikinase inhibitors. It may also be called a VEGF/VEGFR inhibitor.

• Sutent may be used to treat adults with gastrointestinal stromal tumor (GIST) that has progressed despite imatinib or who are intolerant to imatinib.
• Sutent may also be used to treat adults with metastatic (advanced) renal cell carcinoma (RCC) that has not been previously treated or used as adjuvant treatment in those at high risk of recurrent RCC following a kidney removal.
• Sutent is approved to treat progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) (a type of pancreatic cancer) in adults that have progressed and cannot be treated with surgery.
• Sutent is an oral capsule that is usually taken once daily or for a scheduled period (such as 4 weeks on and 2 weeks off for a set number of cycles depending on the cancer being treated).
• No dose adjustment is required for people with mild, moderate, or severe kidney disease or mild or moderate liver disease (Child-Pugh Class A or B). Sutent has not been studied in people with severe liver disease.
• Sutent may be taken with or without food.

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Diarrhea, mouth ulcers, constipation, decreased appetite, lack of energy, skin discoloration, rash, hand-foot syndrome, altered taste, high blood pressure, and muscle or limb pain are the most common side effects reported. Insomnia, depression, cough, shortness of breath, pain, yellowing of the skin, and lightening of the hair have also been reported.
• Laboratory test abnormalities are common. Changes in neutrophils, lymphocytes, platelets, hemoglobin, and liver function tests were reported in more than 10% of trial participants. Decreases in potassium and sodium were also seen, as well as increases in creatinine and renal dysfunction. Over 10% reported a decrease in LVEF.
• 29% of trial participants experienced high blood pressure (BP) with Sutent. This included 7% with Grade 3 and 0.2% with Grade 4. Blood pressure should be monitored at baseline and as indicated. If necessary, withhold Sutent until BP is controlled.
• Bleeding events, affecting the gastrointestinal tract, respiratory tract, tumor, urinary tract, or brain have been reported in about 30% of people taking Sutent; Grade 3 or 4 events were reported in 4.2% of patients, some of which were fatal. Nose bleeds were the most common bleeding event and gastrointestinal hemorrhage was the most common Grade ≥3 event. Perform baseline and periodic complete blood counts (CBCs) and physical examinations as necessary.
• Consider temporarily stopping Sutent or reducing the dosage by 12.5 mg increments in patients who experience adverse reactions.
• The dosage of Sutent may need to be increased gradually up to two-fold in those with end-stage renal disease (ESRD) on hemodialysis.
• Sutent can cause severe liver toxicity that may cause liver failure or death. Symptoms may include jaundice (yellow skin), high transaminases or bilirubin levels, encephalopathy, coagulopathy, or kidney failure. Monitor liver function tests ( such as alanine aminotransferase, aspartate aminotransferase, and bilirubin) when starting Sutent, during each cycle, and when indicated. Interrupt Sutent for Grade 3 or 4 hepatotoxicities until resolution; if resolution does not occur then discontinue Sutent in patients without resolution of Grade 3 or 4 hepatotoxicities, in people who subsequently experience severe changes in liver function tests, and in people who have other signs and symptoms of liver failure. Use of Sutent in people with ALT or AST values >2.5 × the upper limit of normal (ULN) or with >5 × ULN and liver metastases has not been established.
• Sutent can cause cardiovascular events, such as heart failure, cardiomyopathy, myocardial ischemia, and a heart attack, some of which were fatal. Consider monitoring LVEF at baseline and periodically as clinically indicated. Carefully monitor patients for clinical signs and symptoms of congestive heart failure. Discontinue Sutent in people with symptoms of CHF, or reduce the dosage of Sutent in those who have an ejection fraction of greater than 20% but less than 50% below baseline or below the lower limit of normal if baseline ejection fraction was not obtained.
• Sutent can prolong the QT interval leading to an increased risk for ventricular arrhythmias including Torsade de Pointes. The risk is higher in those taking higher dosages of Sutent, with a history of QT interval prolongation; taking antiarrhythmics, strong CYP3A4 inhibitors, or other drugs known to prolong the QT interval; or with relevant pre-existing cardiac disease, bradycardia, or electrolyte disturbances. Consider periodic monitoring of electrocardiograms and electrolytes (such as magnesium and potassium) during treatment with Sutent.
• Tumor Lysis Syndrome (TLS), which may lead to death, has been reported, mostly in patients with RCC or GIST, particularly those with a high tumor burden before treatment. Monitor.
• Sutent has been associated with other serious events, such as thrombotic microangiopathy (results in blood clots in the capillaries and arterioles), proteinuria and nephrotic syndrome, severe skin reactions (such as erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis, necrotizing fasciitis), and reversible posterior leukoencephalopathy syndrome (symptoms may include high blood pressure, headache, decreased alertness, and visual loss). Discontinue Sutent if any of these occur.
• Reports of hyperthyroidism, sometimes followed by hypothyroidism, have been reported in people taking Sutent. Monitor thyroid function at baseline and periodically during treatment.
• Sutent can result in symptomatic hypoglycemia, which may lead to loss of consciousness, or require hospitalization.
• Low blood glucose levels (hypoglycemia) have occurred in 2% of people treated with Sutent for advanced RCC and GIST and in approximately 10% of people treated for pNET (Study 6). People with diabetes may be at higher risk. Check blood glucose levels at baseline and then regularly during treatment. In people with diabetes, antidiabetic treatments may need to be adjusted.
• Sutent may increase the risk of developing osteonecrosis of the jaw (ONJ). The risk is higher in those taking bisphosphonates, with dental disease, or who have undergone invasive dental procedures. Perform an oral examination before starting Sutent and regularly thereafter. Advise patients regarding good oral hygiene practices. Withhold Sutent treatment for at least 3 weeks before scheduled dental surgery or invasive dental procedures, if possible. Withhold Sutent for development of ONJ until complete resolution.
• Sutent may impair wound healing and should be withheld 3 weeks before surgery.
• It is not known if Sutent is safe and effective in children.
• Sutent may harm a developing fetus. Advise women of childbearing potential to use effective contraception during Sutent treatment and for 4 weeks following the final dose. There is also no data about the effects of Sutent on a newborn when breastfeeding. Advise women not to breastfeed during treatment with Sutent and for at least 4 weeks after the last dose. Sutent may impair male and female fertility.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

• Sutent is taken orally, once a day. It may be taken with or without food. Store it at room temperature, between 68°F to 77°F (20°C to 25°C).
• Sutent may be taken every day, or it may be taken on a 4:2 schedule, which means you take it for 4 weeks and then have 2 weeks off taking it. Talk to your doctor if you are not sure how frequently you should be taking Sutent.
• If you miss a dose of Sutent, and it has been less than 12 hours since your last dose, take the missed dose right away. If it has been more than 12 hours, then just take the next scheduled dose at its regular time. Do not double up on doses.
• Keep your appointments with your healthcare provider. They must be able to monitor your response to Sutent. Your healthcare provider may do blood tests before each cycle of treatment to check you for side effects.
• Do not drink grapefruit juice or eat grapefruit products while you are taking Sutent as this may increase levels of Sutent in your body.
• Sutent has been associated with some uncommon but serious side effects. Seek emergency medical help or call your doctor immediately if you experience any unusual bleeding, severe headache, yellow skin, severe upper right abdominal pain, chest pain, edema, shortness of breath, heart palpitations, itchy skin or skin reactions, dark urine, or other worrying side effects.
• If you have diabetes, you will need to monitor your blood sugar levels more frequently while taking Sutent. Talk to your doctor if your blood sugar levels are consistently low.
• Sutent may cause thyroid problems in some people. Tell your healthcare provider if you experience persistent tiredness, loss of appetite, problems with heat, anxiety, tremors, sweating, nausea or vomiting, diarrhea, fast heart rate, weight gain or weight loss, depression, menstrual problems, or hair loss.
• Sutent may cause skin discoloration (yellow skin), dryness, thickness, or cracking of the skin; and lighten the hair. These are not all of the possible side effects of Sutent. For more information, ask your healthcare provider or pharmacist.
• See your doctor regularly for routine monitoring of your blood pressure, liver function, blood counts, and other vital signs.
• Sutent may increase your risk of developing problems in your jaw bone, particularly if you are already taking bisphosphonates, have dental disease, or have previously undergone invasive dental procedures. Brush your teeth and floss twice a day and see your dentist regularly. Tell your dentist you are taking Sutent and temporarily discontinue Sutent for at least 3 weeks before scheduled dental surgery or invasive dental procedures, if possible.
• Tell all healthcare professionals that you are taking Sutent. Sutent can impair wound healing and should be withheld for at least 3 weeks before elective surgery, and not administered for at least 2 weeks following major surgery or until the wound has adequately healed.
• Your healthcare provider should do a pregnancy test before you start treatment with Sutent. Use effective contraception while receiving Sutent and for 4 weeks after the last dose. If you inadvertently become pregnant, see your doctor immediately. Males with female partners who can become pregnant should use effective birth control (contraception) during treatment and for 7 weeks after their last dose of Sutent. Sutent may affect your fertility. Talk to your doctor about this. You should also not breastfeed while taking Sutent and for at least 4 weeks (1 month) after the last dose.

• Research has shown that Sutent increased the median progression-free survival by 6 months in those with metastatic RCC compared to those treated with interferon alfa (11 months vs. 5 months).
• Health-related quality of life was better with Sutent compared to the interferon alfa group according to quality of life questionnaires filled out by patients.
• When Sutent was used as an add-on treatment for RCC in people who have had a kidney removed, the median disease-free survival was 6.8 years compared to 5.6 years with a placebo. Side effects were more common with Sutent compared with placebo.
• When Sutent was used to treat patients with GIST, it delayed the time to tumor progression by 21 weeks (time to tumor progression was 27.3 weeks with Sutent and 6.4 weeks with placebo). Progression-free survival was 24.1 weeks with Sutent compared to 6.0 with placebo.
• Progression-free survival for patients with pNET was 10.2 months with Sutent and 5.4 months with placebo. The objective response rate was 9.3%.

Medicines that interact with Sutent may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with Sutent. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Sutent interacts with over 380 medications; the majority of these interactions are considered moderate or major. Common medications that may interact with Sutent include:

• amisulpride
• antibiotics such as azithromycin, ciprofloxacin, or norfloxacin
• antidepressants, such as citalopram or clomipramine
• antidiabetics, such as glyburide, glibenclamide, or insulin
• antihistamines such as terfenadine
• antipsychotics, such as clozapine, aripiprazole, or haloperidol
• antiseizure medications such as fosphenytoin, phenytoin, or phenobarbitone
• astemizole
• biologics, such as adalimumab
• bisphosphonates, such as alendronate, etidronate, or zolendronic acid
• cisapride
• corticosteroids, such as dexamethasone
• digoxin
• droperidol
• fingolimod
• grapefruit juice
• heart medications, such as beta-blockers (eg, atenolol, sotalol), digoxin, amiodarone, quinidine, or flecainide (may be associated with severe bradycardia or heart block)
• herbals, such as black cohosh or echinacea
• HIV medications, such as atazanavir or efavirenz
• hydroxychloroquine
• immunosuppressants such as tacrolimus
• interferon
• loperamide
• methotrexate
• mifepristone
• opioids, such as buprenorphine or methadone
• oxytocin
• promethazine
• quinine
• tamoxifen
• warfarin.

Sutent may prolong the QT interval and this risk is higher in people taking other QT-prolonging medications, such as citalopram, chlorpromazine, haloperidol, methadone, or erythromycin.

Strong CYP3A4 enzyme inhibitors, such as ketoconazole, diltiazem, itraconazole, or grapefruit may increase blood concentrations of Sutent and its active metabolite by up to 49% and 51%, respectively.

Strong CYP3A4 enzyme inducers, such as carbamazepine, rifampicin, phenytoin, phenobarbital, and St. John’s wort, have been shown to decrease blood concentrations of Sutent and its metabolite by approximately 23% and 46% respectively. Select an alternate concomitant medication with no or minimal enzyme induction potential if possible. If coadministration cannot be avoided, consider a dose increase for Sutent to a maximum dosage of 87.5 mg orally once daily (Schedule 4/2) for GIST and RCC, and 62.5mg once daily for pNET.

Note that this list is not all-inclusive and includes only common medications that may interact with Sutent. You should refer to the prescribing information for Sutent for a complete list of interactions.