1. Metabolism and excretion of GCC-4401C, a factor Xa inhibitor, in humans
- Author
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HJ Lee, A.F. Roffel, SR Dueker, RG Tiessen, SP van Marle, and S Choi
- Subjects
Chromatography ,medicine.drug_mechanism_of_action ,Chemistry ,Total recovery ,Factor Xa Inhibitor ,Liquid scintillation counting ,Urine ,Metabolism ,030204 cardiovascular system & hematology ,030226 pharmacology & pharmacy ,Excretion ,03 medical and health sciences ,0302 clinical medicine ,Pharmacokinetics ,medicine ,Feces - Abstract
Aim: This study investigated the pharmacokinetics, excretion and metabolism of [14C]-GCC-4401C, a factor Xa inhibitor, using a microtracer approach. Results/methodology: Total [14C] in excreta and plasma, and radiochromatographic profiles were determined using accelerator MS and liquid scintillation counting. LC/MS was used to assess pharmacokinetics and metabolism. The average plasma exposure for [14C] was higher than for GCC-4401C, indicating that metabolites with a longer half-life than GCC-4401C were formed. Mean total recovery of [14C] in urine and feces was 87.3%. GCC-4401C was the primary contributor (58%) to total radioactivity in plasma. A total of 12 metabolites were identified; M11 and M12 were the major circulating metabolites. The major metabolic routes of GCC-4401C in humans were oxidation and dehydrogenation. Discussion/conclusion: The study successfully assessed the elimination and metabolism of GCC-4401C.
- Published
- 2017