Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans - Podoll, Terry; Pearson, Paul G.; Evarts, Jerry; Ingallinera, Tim; Bibikova, Elena; Sun, Hao; Gohdes, Mark; Cardinal, Kristen; Sanghvi, Mitesh; Slatter, J. Greg (Drug metabolism and disposition, 2019)
Keywords: Absorption; Acrylamide; Administration, Oral; Adult; Agammaglobulinaemia Tyrosine Kinase - antagonists & inhibitors; Animals; Antineoplastic Agents - analysis; Antineoplastic Agents - metabolism; Antineoplastic Agents - pharmacology; Benzamide; Benzamides - analysis; Benzamides - metabolism; Benzamides - pharmacology; Bioavailability; Biological Availability; Biotransformation; Blood cells; Bruton's tyrosine kinase; Carbon 14; Conjugation; Covalence; Cytochrome P-450 CYP3A - metabolism; Dogs; Economic conditions; Enzyme inhibitors; Excretion; Feces - chemistry; Female; Glutathione; Half-Life; Healthy Volunteers; Humans; Hydrolysis; Inhibitors; Intestinal Absorption; Intravenous administration; Kinases; Liquid chromatography; Low concentrations; Lymphoma, Mantle-Cell - drug therapy; Male; Mass spectrometry; Mass spectroscopy; Metabolism; Metabolites; Middle Aged; Occupancy; Oxidation; Oxidation-Reduction; Peripheral blood; Protein Kinase Inhibitors - analysis; Protein Kinase Inhibitors - metabolism; Protein Kinase Inhibitors - pharmacology; Pyrazines - analysis; Pyrazines - metabolism; Pyrazines - pharmacology; Pyrrolidine; Radioactive half-life; Radioactivity; Rats; Rats, Sprague-Dawley; Thioethers; Tyrosine; Tyrosine kinase inhibitors; Urine; Urine - chemistry; Young Adult; FDA; MS/MS; AUC; t1/2; ACP-5862; ACP-5461; GSH; LSC; HPLC; BCRP; ADME; MS; AMS; CL; GST; PBMC; CV; HER; LC; Tmax; ACP-5530; ACP-5134; BTK; ACP-5531; PK; TCI; ACP-5197