Pazopanib

Pazopanib structure

Information about Pazopanib

Pazopanib is a multi-kinase inhibitor active against vascular endothelial growth factor receptors-1, -2 and -3 that is used in the therapy of advanced renal cell carcinoma and soft tissue sarcomas.

Liver safety of Pazopanib

Pazopanib therapy is commonly associated with transient elevations in serum aminotransferase during therapy and has been linked to rare, but occasionally severe and even fatal cases of clinically apparent acute liver injury.   

Mechanism of action of Pazopanib

Pazopanib (paz oh’ pa nib) is an orally available, multi-kinase inhibitor, most potently inhibiting the tyrosine kinase receptors of vascular endothelial growth factor (VEGF) 1, 2 and 3 which are associated with tumor growth and angiogenesis.  Pazopanib also has activity against c-KIT (an abnormal tyrosine kinase found in gastrointestinal stromal tumors) and the platelet derived growth factor (PDGF) receptor.  Clinical trials of pazopanib in malignant diseases in humans have shown activity against renal cell carcinoma and soft tissue sarcoma and promising effects in ovarian and thyroid cancer. 

FDA approval information for Pazopanib

Pazopanib received approval for use in the United States in 2012 and current indications include advanced renal cell cancer and soft tissue sarcomas. 

Dosage and administration for Pazopanib

Pazopanib is available in tablets of 200 and 400 mg under the brand name Votrient.  The typical dose is 800 mg once daily.  Lower doses are recommended for patients with moderate-to-severe liver disease (200 mg daily) and the dose can be reduced to 400 mg daily for toxicity. 

Side effects of Pazopanib

Common side effects include fatigue, diarrhea, hypertension, hair color changes, anorexia, nausea, and bone marrow suppression.  Uncommon, but potentially severe side effects include prolonged QTc intervals, hemorrhages, arterial thrombosis and visceral perforations and fistulae.  

 

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