Metabolism, Excretion, and Mass Balance of [¹⁴C]-Rezafungin in Animals and Humans.

ABSTRACT: Rezafungin is a novel echinocandin being developed for treatment of candidemia and invasive candidiasis and for prevention of invasive fungal disease caused by Candida, Aspergillus, and Pneumocystis spp. in recipients of blood and marrow transplantation. Studies using [¹⁴C]-radiolabeled rezafungin were conducted in rats, monkeys, and humans to characterize the mass balance, excretion, and pharmacokinetics of [¹⁴C]-rezafungin and to evaluate relative amounts of rezafungin metabolites compared with parent drug. Fecal excretion was the main route of elimination in rats, monkeys, and humans. Radioactivity was primarily excreted as unchanged drug, with ≥95% average total recovery in rats (through 336 h) and monkeys (through 720 h). In humans, cumulativ

SUBMITTER: Ong V 

PROVIDER: S-EPMC8765310 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature