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WeChat consultation hotline If the call cannot be reached, please add WeChat or [other name] [Indications] Pazopanib is a tyrosine kinase inhibitor suitable for the treatment of patients with advanced renal cell carcinoma. [ ] [Dosage and Administration] Take this medication orally once daily without food (at least one hour before or one hour after a meal). Baseline moderate hepatic impairment – Take orally once daily. Not recommended for patients with severe liver damage. [Dosage form and strength] Tablets. [Mechanism of action] Pazopanib is a vascular endothelial growth factor receptor (R)-, platelet-derived growth factor receptor ()-and-, fibroblast growth factor receptor (R)- and, cytokine receptor , interleukin-receptor-inducible cellular kinase, leukocyte-specific protein tyrosine kinase (PLT), and a multi-tyrosine kinase inhibitor of transmembrane glycoprotein receptor tyrosine kinase. In vitro, pazopanib inhibits ligand-induced autophosphorylation of the receptor, and in vivo, pazopanib inhibits ligand-induced autophosphorylation in mouse lungs, a mouse model of angiogenesis, and Growth of several human tumor xenografts in mice. [Pharmacodynamics and Pharmacokinetics] Increases in blood pressure have been observed and are related to plasma pazopanib steady-state trough concentrations. The prolongation potential of pazopanib was assessed as part of the loss of control. An open-label, dose-escalation study in patients with advanced cancer. Three patients received pazopanib at doses ranging from to, daily. The effect of pazopanib on intervals was evaluated prior to serial collection on day 1 and single dose collection on days 1 and 2 . /3 patients had (r method correction) and 3 patients had > increase from baseline. [See Warnings and Precautions (.).] Absorption: Pazopanib is absorbed orally, with a median time to peak concentration of up to 1 hour after dosing. Daily dosing results in geometric means and are, respectively, / and . / (equal to). There may be no consistent increase when pazopanib doses are exceeded. Administration of a single dose of pazopanib as a crushed tablet increases (-) and approximately times and decreases approximately 10 hours compared to administration of the whole tablet. These results indicate an increase in the bioavailability and rate of oral absorption of pazopanib following administration of mashed tablets relative to administration of whole tablets. Therefore, due to this potential for increased exposure, tablets should not be crushed. The systemic exposure of pazopanib is increased when administered with food. Pazopanib administered with a high-fat or low-fat meal resulted in an approx. Therefore, pazopanib should be administered at least one hour before or one hour after a meal [see Dosage and Administration. (.) Distribution: In vivo binding of pazopanib to human plasma proteins is greater than in the range to/without concentration dependence. In vitro studies suggest that pazopanib is a substrate of beta-glycoprotein and breast cancer resistance protein (B). Metabolism: In vitro studies have demonstrated that pazopanib is metabolized by 3 and with minor contributions. Elimination: The average half-life of pazopanib is 3 hours after the recommended dose. Mainly eliminated through feces, renal elimination accounts for < of the administered dose. [Warnings and Precautions] Editor) Increased serum aminotransferase levels and bilirubin were observed. Severe fatal hepatotoxicity has occurred. Measure liver chemistries before starting treatment and periodically during treatment. (.)) Septal prolongation and torsades de pointes (r) have been observed. Use with caution in patients at higher risk with prolonged interval between occurrences. Monitoring of ECG and electrolytes should be considered. (.) 3) Fatal bleeding events have been reported. It has not been studied in patients with a history of hemoptysis, cerebral palsy, or clinically significant gastrointestinal bleeding within the past months and should not be used in these patients. (.3) ) Arterial thrombotic events and possible fatality have been observed. Use with caution in patients at increased risk for these events. (.) ) Gastrointestinal perforation or fistula has occurred. Fatal perforations have occurred. Use with caution in patients with increased risk of gastrointestinal perforation or fistula. (.) ) Hypertension has been observed. Blood pressure should be adequately controlled when started. Monitor and treat hypertension as needed. ) Treatment interruption is recommended in patients undergoing surgery. (.) ) Hypothyroidism may occur. It is recommended to monitor thyroid function. (.) ) Proteinuria: Monitor urine protein. Interrupt medications for grade proteinuria. (.) ) may harm the fetus when administered to a pregnant woman. Women of pregnancy potential should be advised of the potential harm to the fetus and should avoid pregnancy. (., .)
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