Mass balance and metabolite profiling of ¹⁴C-guadecitabine in patients with advanced cancer.

ABSTRACT: Purpose The objective of this mass balance trial was to determine the excretory pathways and metabolic profile of the novel anticancer agent guadecitabine in humans after administration of a ¹⁴C-radiolabeled dose of guadecitabine. Experimental design Included patients received at least one cycle of 45 mg/m² guadecitabine subcutaneously as once-daily doses on Days 1 to 5 of a 28-day cycle, of which the 5th (last) dose in the first cycle was spiked with ¹⁴C-radiolabeled guadecitabine. Using different mass spectrometric techniques in combination with off-line liquid scintillation counting, the exposure and excretion of ¹⁴C-guadecitabine and metabolites in the systemic circulation, excreta, and intracellular target site were established. Results Five

SUBMITTER: Roosendaal J 

PROVIDER: S-EPMC7340650 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature