-5%
Pazocent is indicated for the treatment of:
- Advanced renal cell carcinoma (RCC).
- Advanced soft tissue sarcoma (STS) in patients who have previously received chemotherapy.
The efficacy of Pazocent for adipocytic STS or gastrointestinal stromal tumors has not been demonstrated.
Pazopanib is a multi-tyrosine kinase inhibitor targeting various receptors, including:
- VEGFR-1, VEGFR-2, VEGFR-3 (vascular endothelial growth factor receptors)
- PDGFR-α and PDGFR-β (platelet-derived growth factor receptors)
- FGFR-1 and FGFR-3 (fibroblast growth factor receptors)
- Kit, Itk, Lck, and c-Fms (cytokine and protein tyrosine kinases).
Pazopanib works by inhibiting the autophosphorylation of several growth factor receptors, thereby exerting its anti-cancer effects.
Absorption
Pazopanib is absorbed orally, reaching peak concentration in 2 to 4 hours. When administered at 800 mg daily, the geometric mean AUC (Area Under the Curve) is 1,037 mcg/mL and C max is 58.1 mcg/mL.
Distribution
Pazopanib binds to plasma proteins in humans with an in vivo binding of greater than 99%, unaffected by concentration over the range of 10 to 100 mcg/mL.
Metabolism
Pazopanib is metabolized primarily by CYP3A4, with some contributions from CYP1A2 and CYP2C8.
Elimination
The drug has a half-life of 30.9 hours after an 800 mg dose. The majority is eliminated via feces, with less than 4% excreted renally.