Sunitinib

It is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor used for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Sunitinib inhibitis cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptor (VEGF-R).Sunitinib also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, sunitinib inhibits other RTKs including RET, CSF-1R, and fit3.

Indications

Advanced renal cell carcinoma as well as the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate, Advanced Pancreatic Neuroendocrine tumores.

Dosage

Oral; 37.5-50 mg once daily for 4 weeks and according to regimen.

Contra-Indications

Hypersensitivity.

Special Precautions

Paediatric: Safety not established. Pregnancy: Category D; not safe during pregnancy. Lactation: Potential to cause adverse effects in infants. Elderly: Can be used.

Side Effects

Fatigue, asthenia, fever, diarrhea, nausea, mucositis/stomatitis, vomiting, dyspepsia, abdominal pain, constipation, hypertension, peripheral edema, rash hand-foot syndrome, skin discoloration, dry skin, hair color changes, altered taste, headache, back pain, arthralgia, extremity pain, cough, dyspnea, anorexia, and bleeding. The potentially serious adverse reactions of hepatotoxicity, left ventricular dysfunction, QT interval prolongation, hemorrhage, hypertension, thyroid dysfuction, and adren

Drug Interactions

CYP3A4 inhibitors may increase its concentration while CYP3A4 inducers may decrease its concentration.