Sunitinib malate

What is Sunitinib malate?

• Sunitinib malate (Sutent) is a kinase inhibitor used for the treatment of Gastrointestinal stromal tumor, Pancreatic cancer , and Renal cell carcinoma.

Sunitinib

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What are the uses of this medicine?

Sunitinib malate (Sutent) is a prescription medicine used to treat: a rare cancer of the stomach, bowel, or esophagus called gastrointestinal stromal tumor (GIST) and when:

• you have taken the medicine imatinib mesylate and it did not stop the cancer from growing, or
• you cannot take imatinib mesylate.

• advanced kidney cancer (advanced renal cell carcinoma or RCC).
• adults with kidney cancer that has not spread (localized), and who are at high risk of RCC coming back again after having kidney surgery.

• a type of pancreatic cancer called pancreatic neuroendocrine tumors (pNET), that has progressed and cannot be treated with surgery.

How does this medicine work?

• Sunitinib (soo ni' ti nib) is an inhibitor of several tyrosine kinase receptors which are associated with tumor growth and angiogenesis.
• The tyrosine kinase receptors of cancer cells are often mutated and can cause unregulated cell growth and proliferation.
• Sunitinib is one of several tyrosine kinase receptor inhibitors that have been introduced into cancer chemotherapy and are specially directed at molecular abnormalities that occur in cancer cells.
• Inhibition of the receptor can lead to dramatic reversal of progression the cancer, although sometimes limited by the development of tumor resistance caused by mutations in the kinase.
• Sunitinib has special activity against the abnormal tyrosine kinase (cKit) that is found in gastrointestinal stromal tumors (GIST). Sunitinib also has activity against the receptors for platelet derived growth factor (PDGF) and vascular endothelial growth factor (VEGF).

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Be sure to mention any of the following:

• certain antibiotics such as clarithromycin (Biaxin, in Prevpac), rifampin (Rifadin, Rimactane, in Rifamate, in Rifater), rifabutin (Mycobutin), rifapentine (Priftin), and telithromycin (Ketek)
• certain antifungals such as itraconazole (Onmel, Sporanox), ketoconazole, and voriconazole (Vfend)
• dexamethasone
• medications for diabetes
• certain medications for human immunodeficiency virus (HIV) or acquired immunodeficiency syndrome (AIDS) including atazanavir (Reyataz, in Evotaz), indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir, in Kaletra), and saquinavir (Invirase)
• nefazodone
• certain medications for seizures such as carbamazepine (Carbatrol, Epitol, Equetro, Tegretol, Teril), phenobarbital, and phenytoin (Dilantin, Phenytek).
• Also tell your doctor if you are taking or have taken alendronate (Binosto, Fosamax), etidronate, ibandronate (Boniva), pamidronate, risedronate (Actonel, Atelvia), or zoledronic acid injection (Reclast, Zometa)
• Tell your doctor and pharmacist what herbal products you are taking, especially St. John's wort.
• Do not take St. John's wort while taking sunitinib.

Is this medicine FDA approved?

• Sunitinib received approval for use in the United States in 2006.

How should this medicine be used?

Recommended dosage: Gastrointestinal stromal tumor (GIST) and Advanced renal cell carcinoma (RCC):

• The recommended dosage is 50 mg orally once daily for the first 4 weeks of each 6-week cycle.

Adjuvant Treatment of renal cell carcinoma (RCC):

• The recommended dosage is 50 mg orally once daily for the first 4 weeks of a 6-week cycle (Schedule 4/2) for a maximum of 9 cycles.

Pancreatic neuroendocrine tumors (pNET):

• The recommended dosage is 37.5 mg orally once daily.

Administration:

• Take Sutent 1 time each day with or without food.
• If you take Sutent for GIST or RCC, you will usually take your medicine for 4 weeks (28 days) and then stop for 2 weeks (14 days). This is 1 cycle of treatment. You will repeat this cycle for as long as your healthcare provider tells you to.
• If you take Sutent for pNET, take it 1 time each day until your healthcare provider tells you to stop.
• Do not drink grapefruit juice or eat grapefruit during your treatment with Sutent.
• If you miss a dose of Sutent by less than 12 hours, take the missed dose right away. If you miss a dose of Sutent by more than 12 hours, just take your next dose at your regular time. Do not make up the missed dose.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 12.5 mg, 25 mg, 37.5 mg, 50 mg sunitinib

This medicine is available in fallowing brand namesː

• Sutent

What side effects can this medication cause?

The most common side effects of this medicine include:

• tiredness
• weakness
• diarrhea
• pain, swelling or sores inside of your mouth
• nausea
• loss of appetite
• indigestion
• vomiting
• stomach-area (abdominal) pain
• blisters or rash on the palms of your hands and soles of your feet
• high blood pressure
• taste changes
• low platelet counts
• make your skin look yellow

Sutent may also cause other skin problems including:

• dryness, thickness or cracking of the skin

Sutent may cause serious side effects, including:

• Heart problems
• Abnormal heart rhythm changes
• Severe liver problems
• High blood pressure
• Bleeding problems
• Serious stomach and intestinal problems, that can sometimes lead to death
• Tumor lysis syndrome (TLS)
• Reversible Posterior Leukoencephalopathy Syndrome
• thrombotic thrombocytopenia purpura
• hemolytic uremic syndrome
• Protein in your urine
• Serious skin and mouth reactions
• Thyroid problems
• hypoglycemia
• osteonecrosis
• Wound healing problems

What special precautions should I follow?

• Fatal liver failure has been observed. Monitor liver function tests at baseline, during each cycle, and as clinically indicated. Interrupt Sutent for Grade 3 hepatotoxicity until resolution to Grade ≤1 or baseline and resume Sutent at a reduced dose; discontinue if no resolution. Discontinue Sutent in patients with Grade 4 hepatoxicity, in patients who have subsequent severe changes in liver function tests or other signs and symptoms of liver failure.
• Myocardial ischemia, myocardial infarction, heart failure, cardiomyopathy, and decreased left ventricular ejection fraction (LVEF) to below the lower limit of normal including death have occurred. Monitor for signs and symptoms of congestive heart failure and consider monitoring LVEF at baseline and periodically during treatment. Discontinue Sutent for clinical manifestations of congestive heart failure. Interrupt and/or dose reduce for decreased LVEF.
• Sutent can cause QT interval prolongation in a dose-dependent manner, which may lead to an increased risk for ventricular arrhythmias including Torsade de Pointes. Monitor patients at higher risk for developing QT interval prolongation. Consider monitoring of electrocardiograms and electrolytes.
• Monitor blood pressure at baseline and as clinically indicated. Initiate and/or adjust antihypertensive therapy as appropriate. Interrupt Sutent for Grade 3 hypertension until resolution to Grade ≤1 or baseline, then resume Sutent at a reduced dose. Discontinue Sutent in patients who develop Grade 4 hypertension.
• Tumor-related hemorrhage and viscus perforation (both with fatal events) have occurred. Perform serial complete blood counts and physical examinations. Interrupt Sutent for Grade 3 or 4 hemorrhagic events until resolution to Grade ≤1 or baseline, then resume at a reduced dose; discontinue if no resolution.
• TLS (some fatal) has been reported primarily in patients with RCC and GIST. Monitor these patients and treat as clinically indicated.
• Thrombotic microangiopathy (TMA), including thrombotic thrombocytopenic purpura and hemolytic uremic syndrome, sometimes leading to renal failure or a fatal outcome, has been reported. Discontinue Sutent for TMA.
• Proteinuria and nephrotic syndrome have been reported. The safety of continued Sutent treatment in patients with moderate to severe proteinuria has not been evaluated.
• Renal failure or a fatal outcome has occurred. Monitor urine protein. Interrupt treatment for 24-hour urine protein of 3 or more grams. Discontinue for repeat episodes of 24-hour urine protein of 3 or more grams despite dose reductions or nephrotic syndrome.
• Necrotizing fasciitis, erythema multiforme, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN) (some fatal) have occurred. Discontinue Sutent for these events.
• Reversible posterior leukoencephalopathy syndrome (RPLS) (some fatal) has been reported. Monitor for signs and symptoms of RPLS. Withhold Sutent until resolution.
• Hyperthyroidism, some followed by hypothyroidism, have been reported. Monitor thyroid function at baseline, periodically during treatment, and as clinically indicated. Initiate and/or adjust therapy for thyroid dysfunction as appropriate.
• Sutent can result in symptomatic hypoglycemia, which may lead to loss of consciousness, or require hospitalization. Check blood glucose levels regularly and assess if antidiabetic drug dose modifications are required.
• Osteonecrosis of the Jaw (ONJ) occurred in patients treated with Sutent. Withhold Sutent for at least 3 weeks prior to invasive dental procedure and for development of ONJ until complete resolution.
• Impaired wound healing has been reported in patients who received Sutent. Withhold Sutent for at least 3 weeks prior to elective surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing. The safety of resumption of Sutent after resolution of wound healing complications has not been established.
• Sutent Can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception.
• Advise women not to breastfeed during treatment with Sutent and for at least 4 weeks after the last dose.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• Cases of accidental overdose have been reported; these cases were associated with adverse reactions consistent with the known safety profile of Sutent, or without adverse reactions.

Management of overdosage:

• Treatment of overdose with Sutent should consist of general supportive measures.
• There is no specific antidote for overdosage with Sutent.
• If indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage.

Can this medicine be used in pregnancy?

• Based on animal reproduction studies and its mechanism of action, Sutent can cause fetal harm when administered to a pregnant woman.
• Advise females of reproductive potential of the potential risk to a fetus.

Can this medicine be used in children?

• The safety and effectiveness of Sutent in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• sunitinib malate

Inactive ingredients: mannitol, croscarmellose sodium, povidone (K-25), and magnesium stearate.

• Orange gelatin capsule shells: titanium dioxide, and red iron oxide.
• Caramel gelatin capsule shells: titanium dioxide, red iron oxide, yellow iron oxide, and black iron oxide.
• Yellow gelatin capsule shells: titanium dioxide and yellow iron oxide.
• White printing ink: shellac, propylene glycol, sodium hydroxide, povidone, and titanium dioxide.
• Black printing ink: shellac, propylene glycol, potassium hydroxide and black iron oxide.

Who manufactures and distributes this medicine?

Packager: Pfizer Laboratories Div Pfizer Inc

What should I know about storage and disposal of this medication?

• Store Sutent at room temperature, between 68°F to 77°F (20°C to 25°C).

• Dailymed label info on Sunitinib malate
• FDA Sunitinib malate

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