Mass balance, metabolic disposition, and pharmacokinetics of a single oral dose of regorafenib in healthy human subjects

• Published in: Cancer chemotherapy and pharmacology Vol. 81; no. 1; pp. 195 - 206
• Main Authors: Gerisch, Michael, Hafner, Frank-Thorsten, Lang, Dieter, Radtke, Martin, Diefenbach, Konstanze, Cleton, Adriaan, Lettieri, John
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer Berlin Heidelberg 01.01.2018; Springer Nature B.V
• Subjects: aerobiosis; Biotransformation; blood; Cancer Research; carbon radioisotopes; Drug dosages; drugs; Excretion; Feces; Hepatocytes; High-performance liquid chromatography; humans; Inhibitor drugs; liquids; males; Medicine; Medicine & Public Health; Metabolism; Metabolites; Oncology; oral administration; Original; Original Article; Oxidative metabolism; Pharmacokinetics; Pharmacology/Toxicology; Plasma; Pyridines; Radioactivity; risk; Targeted cancer therapy; Urine; Human; Regorafenib; Phase I; Metabolism; Biotransformation
• ISSN: 0344-5704; 1432-0843; 1432-0843
• DOI: 10.1007/s00280-017-3480-9

Purpose To evaluate the mass balance, metabolic disposition, and pharmacokinetics of a single dose of regorafenib in healthy volunteers. In addition, in vitro metabolism of regorafenib in human hepatocytes was investigated. Methods Four healthy male subjects received one 120 mg oral dose of regorafe...