For the treatment of patients with advanced renal cell carcinoma.
藥理
Pazopanib is a multi-tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR)-1, 2, and 3, platelet-derived growth factor receptor α and β, fibroblast growth factor receptor 1 and 3, cytokine receptor (Kit), interleukin-2 receptor inducible T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck), and transmembrane glycoprotein receptor tyrosine kinase (c-Fms).
藥動學
Bioavailability: crushed tablet, increased bioavailability and rate or absorption; Effects of food: increased systemic exposure (2-fold increase in AUC and Cmax);Protein binding: >99%; Metabolism: metabolized by CYP3A4 (major), CYP1A2 and CYP2C8 (minor); Elimination: half-life: 30.9 hours. Dialyzable: No (hemodialysis).
禁忌症
懷孕分類
D
哺乳分類
Avoided.
副作用
Common: Hypertension, Hair color change, Decreased albumin, Hypomagnesemia, Hyponatremia , Hypophosphatemia, Decrease in appetite, Diarrhea , Leukopenia, , Neutropenia, Thrombocytopenia , Alkaline phosphatase raised, ALT/SGPT level raised. Potentially serious adverse reactions: hepatotoxicity, QT prolongation and torsades de pointes, hemorrhagic events, arterial thrombotic events, and gastrointestinal perforation and fistula.
劑量和給藥方法
800 mg orally once daily without food (at least 1 hour before or 2 hours after a meal). The dose of VOTRIENT should not exceed 800 mg. Do not crush tablets due to the potential for increased rate of absorption which may affect systemic exposure. If a dose is missed, it should not be taken if it is less than 12 hours until the next dose.