Sunitinib – Uses, and Side Effects

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What is Sunitinib?

Sunitinib (pronounced sue-nit-i-nib) is a targeted cancer drug and is also known by its brand name Sutent.

It is a possible treatment for:

  1. Advanced kidney cancer
  2. A rare type of sarcoma called a gastrointestinal stromal tumor (GIST)
  3. pancreatic neuroendocrine tumors

Sunitinib uses

Sutent is used to treat gastrointestinal stromal tumors (GISTs) if:

  1. The tumors have worsened after you’ve taken a drug called imatinib (Gleevec), or
  2. Your body can’t tolerate imatinib (side effects from the drug made it very hard or unsafe for you to take)
  3. Advanced renal cell carcinoma. Renal cell carcinoma (RCC) is a kind of kidney cancer. “Advanced” refers to cancer that has started to grow or spread.
  4. Sutent is used for localized RCC that was treated with a nephrectomy (surgical removal of a kidney). “Localized” means that cancer hasn’t spread. There’s a high risk the RCC will return. And Sutent is approved as an adjuvant treatment for RCC.
  5. Advanced pancreatic neuroendocrine tumors. Sutent is approved to treat pancreatic neuroendocrine tumors (pNETs). The pNETs must be well-differentiated, which means they’re slow-growing and their cells look more like normal cells. The pNETs must also be unresectable (can’t be removed with surgery). In addition, they must also be either:
      1. Locally advanced (grown or spread near the pancreas), or
      2. Metastatic (spread to other parts of the body)

Mechanism of action

Sunitinib is a small molecule that inhibits multiple RTKs, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRa and PDGFRb), 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). Sunitinib inhibition of the activity of these RTKs has been demonstrated in biochemical and cellular assays, and inhibition of function has been demonstrated in cell proliferation assays. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays.

Dosage

Metastatic renal cell carcinoma, Unresectable, metastatic malignant gastrointestinal stromal tumors.

Adult: 50 mg once daily for 4 wk followed by a 2-wk rest period to comprise a complete 6-wk cycle. May be adjusted in increments or decrements of 12.5 mg based on individual tolerability. Min: 25 mg daily. Max: 75 mg daily.

 

Malignant tumor of the endocrine pancreas, advanced

Adult: 37.5 mg once daily, given continuously. May be adjusted in increments or decrements of 12.5 mg, based on individual tolerability. Max: 50 mg daily.

Administration

Oral administration:

  1. Take with or without food
  2. Do not drink grapefruit juice or eat grapefruit during your treatment.

 

Missed dose:

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

Sunitinib side effects

Sutent may cause serious side effects including:

  1. Hives
  2. Difficulty breathing
  3. Swelling of your face, lips, tongue, or throat
  4. Fever
  5. Sore throat
  6. Burning in your eyes
  7. Skin pain
  8. Red or purple skin rash that spreads and causes blistering and peeling
  9. Loss of appetite
  10. Stomach pain on the upper right side
  11. Tiredness
  12. Itching
  13. Dark urine
  14. Clay-colored stools
  15. Yellowing of the skin or eyes (jaundice)
  16. Decreased urination
  17. Nosebleeds
  18. Pain, redness, numbness, and peeling skin or your hands or feet
  19. Easy bruising
  20. Unusual bleeding
  21. Purple or red spots under your skin
  22. Painful skin sores
  23. Sores in your mouth or on your lips
  24. Jaw pain or numbness
  25. Red or swollen gums
  26. Loose teeth
  27. Slow healing after dental work
  28. Confusion
  29. Thinking problems
  30. Vision loss
  31. Seizure
  32. Swelling
  33. Rapid weight gain
  34. Fast or pounding heartbeats
  35. Fluttering in your chest
  36. Shortness of breath
  37. Sudden dizziness
  38. Lightheadedness
  39. Severe headache
  40. Blurred vision
  41. Pounding in your neck or ears
  42. Headache
  43. Hunger
  44. Sweating
  45. Fast or slow heart rate
  46. Feeling jittery
  47. Changes in your mental state
Sunitinib

Interaction with other diseases

  1. Liver disease
  2. Lung toxicity
  3. Adrenal toxicity
  4. Cardiovascular Events
  5. Dermatologic toxicities
  6. Hemorrhagic events
  7. Hypertension
  8. Hypoglycemia
  9. ONJ
  10. Proteinuria
  11. QT prolongation
  12. Thyroid abnormality

Precautions/ safety information

Before using this medication, tell your doctor your medical history, especially of: bleeding problems, heart problems (such as heart attack), high blood pressure, liver problems, kidney disease, thyroid disease, diabetes, blood vessel problems (such as an aneurysm or a tear/break in the aorta or other blood vessels).

Sunitinib may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using sunitinib, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/”water pills”) or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using sunitinib safely.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F)

Contraindications

This medicine is not right for everyone. Do not use it if you had an allergic reaction to sunitinib, or if you are pregnant.

Pregnancy or breastfeeding

Use should be avoided. If used during pregnancy or if pregnancy occurs, apprise the patient of potential hazard to the fetus. As angiogenesis is a critical component of embryonic and fetal development, this drug is expected to cause fetal harm if administered to pregnant women.

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