Safety, Pharmacokinetic, and Antitumor Activity of SU11248, a Novel Oral Multitarget Tyrosine Kinase Inhibitor, in Patients With Cancer

作者: Sandrine Faivre , Catherine Delbaldo , Karina Vera , Caroline Robert , Stéphanie Lozahic

DOI: 10.1200/JCO.2005.02.2194

关键词: Tyrosine-kinase inhibitorDosingPharmacologyMedicineCancerSunitinibEdemaSunitinib malateAdverse effectPharmacokinetics

摘要: Purpose To establish the safety, pharmacokinetics, and recommended dose of sunitinib, a novel oral multitargeting tyrosine kinase inhibitor with antiangiogenic antitumor properties, in patients advanced malignancies. Patients Methods Sunitinib was given orally for 4 weeks every 6 weeks. Results Twenty-eight received doses ranging from 15 to 59 mg/m2 (ranging 50 mg other day 150 mg/d). Dose-limiting toxicities reported at maximum-tolerated ≥ 75 mg/d were reversible grade 3 fatigue, hypertension, 2 bullous skin toxicity. Therefore, mg/d. At this dose, main adverse effects sore mouth, edema, thrombocytopenia. Hair discoloration yellow coloration observed Pharmacokinetic data indicate that potentially active target plasma concentrations ng/mL can be achieved moderate interpatient variability long half-life compatible single daily dosing. Six o...

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