Absorption, distribution, metabolism and excretion (ADME) of the ALK inhibitor alectinib: results from an absolute bioavailability and mass balance study in healthy subjects

• Published in: Xenobiotica Vol. 47; no. 3; pp. 217 - 229
• Main Authors: Morcos, Peter N., Yu, Li, Bogman, Katrijn, Sato, Mika, Katsuki, Hisakazu, Kawashima, Kosuke, Moore, David J, Whayman, Matt, Nieforth, Keith, Heinig, Katja, Guerini, Elena, Muri, Dieter, Martin-Facklam, Meret, Phipps, Alex
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 04.03.2017
• Subjects: Adult; Biological Availability; Carbazoles - metabolism; Carbazoles - pharmacokinetics; Cross-Over Studies; Healthy Volunteers; Humans; Intravenous; Male; metabolites; microtracer; Middle Aged; pharmacokinetics; Piperidines - metabolism; Piperidines - pharmacokinetics; Protein Kinase Inhibitors - metabolism; Protein Kinase Inhibitors - pharmacokinetics; radiolabelled alectinib; Receptor Protein-Tyrosine Kinases - antagonists & inhibitors; Tissue Distribution; radiolabelled alectinib; pharmacokinetics; Intravenous; metabolites; microtracer
• ISSN: 0049-8254; 1366-5928
• DOI: 10.1080/00498254.2016.1179821

1. Alectinib is a highly selective, central nervous system-active small molecule anaplastic lymphoma kinase inhibitor. 2. The absolute bioavailability, metabolism, excretion and pharmacokinetics of alectinib were studied in a two-period single-sequence crossover study. A 50 μg radiolabelled intraven...