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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| [14C] SH-1028 | Experimental | Volunteers will receive 200 mg [14C] SH-1028 containing a nominal 88 μCi activity, administered by mouth, as a solution. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| [14C] SH-1028 | Drug | Volunteer will receive a single oral dose of 200 mg/88 uCi [14C]SH-1028 as a solution on Day 1 |
|
| Measure | Description | Time Frame |
|---|---|---|
| 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. | 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. | 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. | 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 | 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 | Baseline (Day-2) to Day 15 |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Feng Shao, Ph D | Jiangsu Province Hospital Affiliated to Nanjing Madical University of Medicine | Principal Investigator |
| Wei Liu, M.A | Jiangsu Province Hospital Affiliated to Nanjing Madical University of Medicine | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Jiangsu Province Hospital Affiliated to Nanjing Madical University of Medicine | Nanjing | Jiangsu | 210029 | China |
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| ID | Term |
|---|---|
| C000728623 | SH-1028 |
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