Pharmacokinetics, metabolism and excretion of radiolabeled fostemsavir administered with or without ritonavir in healthy male subjects
Published in Xenobiotica, 2022
Peter Gorycki, Mindy Magee, Peter Ackerman, Xiusheng Miao, Katy Moore
This was a non-randomized, open-label, single-dose study in healthy male subjects. A total of 18 subjects were dosed, and the results for 17 subjects are reported (one subject died while receiving RTV prior to FTR administration). Subjects were between 18 and 45 years old with a body mass index (BMI) of 18 to 32 kg/m2. Subjects who met all inclusion and exclusion criteria were assigned by the investigator into 1 of 4 groups. Subjects in Groups A (n = 6) and B (n = 3) received a single dose of 300 mg [14C]-FTR containing 100 µCi (3.7 MBq) of total radioactivity as an oral solution, without RTV, on Day 1 under fasted conditions. Subjects in Groups C (n = 5) and D (n = 3) were administered 100 mg RTV with food each morning and evening on Days 1 to 9. On Day 10, subjects received a single dose of 300 mg [14C]-FTR (100 μCi [3.7 MBq]) oral solution in conjunction with 100 mg RTV under fasted conditions. Subjects then received their last dose of RTV 12 h later with food. A 20 ng/kg intravenous dose of sincalide (Ziessman 2019) was administered to stimulate gallbladder contraction at 7 h post-dose. Dose administration, sample collection, and sample processing were conducted at Clinical Applications Laboratories, Inc., San Diego, CA.