Pharmacokinetics, absorption, metabolism, and excretion of [14C]ivosidenib (AG-120) in healthy male subjects

• Published in: Cancer chemotherapy and pharmacology Vol. 83; no. 5; pp. 837 - 848
• Main Authors: Prakash, Chandra, Fan, Bin, Altaf, Syed, Agresta, Sam, Liu, Hua, Yang, Hua
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer Berlin Heidelberg 01.05.2019; Springer Nature B.V
• Subjects: Administration, Oral; Adult; Area Under Curve; Blood levels; Cancer Research; Carbon Radioisotopes; Chromatography, Liquid; CYP2D6 protein; Cytochrome P450; Erythrocytes; Excretion; Feces; Feces - chemistry; Genotypes; Glycine - administration & dosage; Glycine - analogs & derivatives; Glycine - blood; Glycine - pharmacokinetics; Glycine - urine; Healthy Volunteers; High-performance liquid chromatography; Humans; Isocitrate dehydrogenase; Isocitrate Dehydrogenase - antagonists & inhibitors; Limit of Detection; Male; Medicine; Medicine & Public Health; Metabolic Clearance Rate; Metabolism; Metabolites; Middle Aged; Oncology; Oral administration; Original Article; Pharmacokinetics; Pharmacology/Toxicology; Pyridines - administration & dosage; Pyridines - blood; Pyridines - pharmacokinetics; Pyridines - urine; Radioactivity; Tandem Mass Spectrometry; Tissue Distribution; Urine; Isocitrate dehydrogenase-1 (IDH1); Excretion; Absorption; Ivosidenib (AG-120); Metabolites; Cytochrome P450; Metabolism; LC–MS/MS

Purpose Pharmacokinetics, absorption, metabolism, and excretion of ivosidenib, a mutant isocitrate dehydrogenase-1 inhibitor, were determined in healthy male subjects. Methods In this open-label phase I study, a single dose of [ 14 C]ivosidenib (500 mg, 200 µCi/subject) was orally administered to ei...