This is a single-center, open-label, single-dose phase I study to investigate the absorption, metabolism and excretion of \[14C\] SH-1028 in healthy Chinese male subjects. The study will be conducted into two steps:Firstly, 2 subjects are enrolled in to participate in the pilot study to grope for the collection time of plasma, urine and feces sampling post-dose. Then, the collection time of blood and excreta samples (urine and feces) from the subsequent 2-4 subjects will be adjusted according to the pilot study.
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 transferred to nuclear medical ward. And after an overnight fast of at least 10 h, subjects will receive a single oral dose of 200 mg (88 μCi) of \[14C\]SH-1028 as an oral suspension. Then, after two days of the dosing, subjects will be transferred back to Phase I Clinical Unit ward and confined to this unit until blood or excreta sampling and safety monitoring at the designated time points or intervals are complete.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
OTHER
Masking
NONE
Enrollment
6
Volunteer will receive a single oral dose of 200 mg/88 uCi \[14C\]SH-1028 as a solution on Day 1
Jiangsu Province Hospital Affiliated to Nanjing Madical University of Medicine
Nanjing, Jiangsu, China
The percentage of radioactive dose of [14C] radiolabelled SH-1028 recovered in blood and in total, up to Day 15
The distribution of \[14C\]SH-1028 in the whole blood and plasma and whole radioactive pharmacokinetics following the single orally administered \[14C\]SH-1028 in healthy male volunteers.
Time frame: Blood samples : - 0.5hrs, 1hrs, 2hrs, 3hrs, 4hrs, 6hrs, 8hrs, 12hrs, 24hrs, 48hrs, 72hrs, 120hrs, 168hrs, 216hrs, 264hrs and 336hrs
The percentage of radioactive dose of [14C] radiolabelled SH-1028 recovered in urine, faeces and in total, up to Day 15.
Quantitive analysis of whole radioactivity of excrement of orally administered \[14C\]SH-1028 in healthy volunteers to obtain the mass balance data and the main excretion pathway in human body.
Time frame: Day1 to Day 15
The concentrations of SH-1028, Imp2 and Imp3 in plasma up to Day 15
Quantitive analysis of the concentrations of SH-1028 and Imp2,Imp3 (Metabolites of SH-1028) in plasma using the validated LC-MS/MS to obtain pharmacokinetic data.
Time frame: Blood samples : - 0.5hrs, 1hrs, 2hrs, 3hrs, 4hrs, 6hrs, 8hrs, 12hrs, 24hrs, 48hrs, 72hrs, 120hrs, 168hrs, 216hrs, 264hrs and 336hrs
Proportion of different metabolites
Proportion of different metabolites in healthy volunteers after oral administration of \[14C\]SH-1028
Time frame: Blood samples : - 0.5hrs, 1hrs, 2hrs, 3hrs, 4hrs, 6hrs, 8hrs, 12hrs, 24hrs, 48hrs, 72hrs, 120hrs, 168hrs, 216hrs, 264hrs and 336hrs
Types of adverse events
Types of adverse events assessed by CTCAE v5.0 that occurred during the trial
Time frame: Baseline (Day-2) to Day 15
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