Sunitinib

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Sunitinib (pronounced soo-NI-ti-nib) is a type of tyrosine kinase inhibitor used primarily in the treatment of renal cell carcinoma and gastrointestinal stromal tumor (GIST). It is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA on January 26, 2006.

Etymology

The name "Sunitinib" is derived from the chemical name of the drug, which is N-(2-diethylaminoethyl)-5-[[[Z-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide.

Pharmacology

Sunitinib inhibits cellular signaling by targeting multiple receptor tyrosine kinases (RTKs). These include the vascular endothelial growth factor receptors (VEGFRs) type 1, 2, and 3, and the platelet-derived growth factor receptors (PDGFRs) alpha and beta. Additional targets of sunitinib are the 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).

Clinical Use

Sunitinib is used to treat advanced renal cell carcinoma (RCC) and gastrointestinal stromal tumors (GISTs) that are resistant to treatment with imatinib. It is also used to treat pancreatic neuroendocrine tumors (pNETs).

Side Effects

Common side effects of sunitinib include fatigue, diarrhea, skin discoloration, mouth sores, nausea, altered taste, and hand-foot syndrome. More serious side effects can include high blood pressure, bleeding, heart problems, and liver problems.

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