This non-randomized, single group, open-label study will investigate the mass balance, routes of elimination, pharmacokinetics, metabolism, safety and tolerability of a single oral dose of \[14C\]XZP-3621 in healthy volunteers.
This open-label, radiolabeled, single 400-mg dose study in approximately 6 healthy male volunteers has been designed to further the understanding of human metabolism of XZP-3621. Subjects who had signed informed consent and meet inclusion criteria and no exclusion criteria are admitted to Phase I Clinical Unit two days prior to dosing (D-2). On the morning of Day 1 before dosing, subjects will be performed baseline examination and trained on procedures such as medicine-taking, PK blood collection, urine and fecal collection, etc., to ensure that the procedures can be performed according to the protocols and standard operating procedures. And after an overnight fast of at least 10 h, 30 minutes afer a standard meal, subjects will receive a single oral dose of 400 mg (200 μCi) of \[14C\]XZP-3621 as an oral suspension. Water will be banned from 1 hour pre-dose to 1 hour post-dose (excluding when taking the medicine) and food will be banned within 4 hours post-dose. Metabolic profiling of radiolabeled components will be performed on pooled plasma samples as well as on cumulative urine and feces excreted until Day 14 postdose or until one of the early release criteria is met. The early release criteria are: 1) recovery in excreta of at least 80% of administered radioactivity, or 2) less than 1% of administered radioactivity being recovered in excreta from two consecutive days (ie, total for urine + feces should be \<1% on 2 consecutive days).
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
6
Extemporaneously compounded oral suspension solution of \[14C\]XZP-3621 (400 mg/200 µCi)
The First Affiliated Hospital of Suzhou Universiy
Suzhou, Jiangsu, China
Total recovery of radioactivity in urine and feces
Calculate the total radioactivity in urine and feces based on the radioactivity concentration of each sample.
Time frame: Assessments will be made up to 19 days post dose
Radioactivity concentration of each plasma sample
Use liquid scintillation counter to evaluate Radioactivity concentration of each plasma(DPM/ml) sample
Time frame: Assessments will be made up to 19 days post dose
Metabolic profiling for XZP-3621 will be determined in plasma, urine and fecal samples
Percent (%) of each radiolabeled drug-related material (parent and each metabolite) will be determined in plasma, urine and feces.
Time frame: Assessments will be made up to 19 days post dose
Maximum exposure in plasma will be determined for XZP-3621, XZP-5089 metabolite and total radioactivity
Cmax (maximum observed plasma concentration) will be reported directly from each analyte's data
Time frame: Assessments will be made up to 19 days post dose
The overall exposure in plasma will be determined for XZP-3621, metabolite and total radioactivity
AUC0-∞ (Area under the plasma concentration time profile from time 0 extrapolated to infinite time) will be determined, using Linear/Log trapezoidal method, from plasma concentration data for each analyte
Time frame: Assessments will be made up to 19 days post dose
The terminal elimination half life in plasma will be estimated from plasma profiles over time for XZP-3621, metabolite and total radioactivity
t1/2 (apparent terminal elimination half life) will be estimated for each analyte from the terminal portion of its plasma concentration versus time plot
Time frame: Assessments will be made up to 19 days post dose
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Number of participants with treatment-related adverse events as assessed by CTCAE v5.0
According to CTCAE v5.0, the number and frequency of adverse events after a single dose of \[14C\]XZP-3621 were assessed.
Time frame: Assessments will be made up to 28 days post dose