Sunitinib
Sunitinib was approved by the FDA in 2006 to treat two different types of cancers: gastrointestinal stromal tumors (GIST) after disease progression on imatinib mesylate (Gleevec®) or when the patient is intolerant of imatinib in the case of metastaticThe term for a cancer that has spread beyond its point of origin. Metastatic disease is responsible for the majority of cancer deaths. renal cell carcinomaCancer of epithelial cells, the cells that cover the outside and inside of body surfaces. This is the most common form of cancer. (MRCC). Sunitinib is administered orally, with or without food.
Sunitinib (Sutent®) is a small molecule that functions as a receptor tyrosine kinaseAn enzyme that adds phosphate groups to target molecules. Often the targets of these enzymes are proteins that control the cell division process, so the enzymes play a key role in cell division. See also, kinase. (RTK) inhibitor. These receptors are proteins found on the surface of cells and are involved in cellular signaling. The drug inhibits several different receptor proteins including vascular endothelial growth factorA substance that stimulates cell division. Growth factors are usually small proteins or steroid hormones. They may be secreted by the same cells on which they act or by cells that reside in a different part of the body than the target cells. Some examples of growth factors include estrogen, a growth factor for breast cells, and VEGF, a growth factor that causes the development of blood vessels. Several different anti-cancer treatments are designed to inhibit the activity of growth factors. receptor (VEGFR), platelet derived growth factor receptor (PDGFR), and stem cellCells capable of developing into more than one cell type. All of the cells in a human body come from the division and subsequent differentiation of a single cell, formed from the fusion of an egg and sperm. This original cell has the capability to form any cell type and is called totipotent. As tissues develop the cells lose the ability to form all other tissues, and become 'committed' to forming only one or a few cell types. These stem cells are called pluripotent. An example are bone marrow cells that form many different kinds of blood cells. Stem cell replacement allows for the pluripotent stem cells in bone marrow to be replaced after high doses of chemotherapy. Many fully differentiated cells are not capable of cell division and are replaced when they die by the division of stem cells in that tissue. Many forms of cancer are thought to be the result of abnormal division of stem cells. factor receptor (KIT). Inhibition of these receptors prevents the formation of signals that result in tumor growth, angiogenesisThe formation of blood vessels. This process is required for a tumor to grow past a small size since the blood delivers nutrients to the cells in the tumor mass. and metastasis.1
The diagram below shows the 3D molecular structure of Sunitinib.
Common side effects include fatigue, swelling, taste changes, nausea, vomiting, high blood pressure, mouth pain/irritation, upset stomach, constipation, diarrhea, skin changes (yellowing, dry, cracking), bleeding (nose bleeds, excessive bleeding from cuts). Possible serious side effects include heart problems - inform your doctor if you fell extremely tired, short of breath, or experience swelling in the feet or ankles, hole in the stomach or bowels or bleeding from the tumor (both very rare) - inform your doctor if you experience pain or swelling it the abdomen, are vomiting blood or having abnormally black bowel movements. Be sure to inform your doctor about all your pre-existing medical conditions before taking sunitinib. Also, tell your doctor about any prescription medications, over-the-counter drugs, supplements, vitamins, and herbal products. 1
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