Key result
Administration of [14C]-GCC-4401C resulted in a mean total recovery of 87.3% in urine and feces, with the parent drug contributing 58% to total plasma radioactivity.
Why the study?
What are the pharmacokinetics, excretion, and metabolism of the factor Xa inhibitor GCC-4401C in humans?
What are the pharmacokinetics, excretion, and metabolism of the factor Xa inhibitor GCC-4401C in humans?
The study successfully characterized the pharmacokinetics, metabolism, and excretion of the factor Xa inhibitor GCC-4401C in humans, identifying oxidation and dehydrogenation as major metabolic routes.
Answers are grounded in this paper and cite their sources.
Informs early ADME profiling of GCC-4401C; leaves open clinical translation and dosing in target populations.
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.
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Roffel et al. (2017) studied this question. [14C]-GCC-4401C was evaluated on Pharmacokinetics, excretion and metabolism. Administration of [14C]-GCC-4401C resulted in a mean total recovery of 87.3% in urine and feces, with the parent drug contributing 58% to total plasma radioactivity.
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