This is a single-center, open-label, non-randomized, single dose study in healthy male subjects designed to assess mass balance recovery, metabolite profile and metabolite identification of radio-labeled SY-5007 administered orally.
The trial will consist of two parts: Pilot Study: Two eligible adult male subjects will be enrolled and admitted to the clinical trial center after passing the inclusion criteria review. They will undergo training on medication administration, urine and feces collection, etc., to ensure compliance with the protocol and standard operating procedures (SOP). Subjects will fast before medication administration and provide urine and feces samples at specified intervals after dosing. Blood samples will also be collected at specified time points. Formal Study: Four to six male subjects will be enrolled, receiving a single dose of SY-5007 160 mg orally containinig roughly 120 µCi \[14C\] SY-5007. Blood, urine and feces samples will be collected at specified time points. Safety monitoring (12-lead ECG, vital signs, blood chemistry and haematology) and adverse events will be monitored throughout the study.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
8
Carbon-14 labeled SY-5007
Beijing Friendship Hospital, Capital Medical University
Beijing, China
Total radioactivity in plasma PK: Cmax
Highest radioactivity observed plasma concentration
Time frame: At pre-dose and up to 2 weeks post-dose
Total radioactivity in plasma PK: Tmax
Time to reach the Cmax
Time frame: At pre-dose and up to 2 weeks post-dose
Total radioactivity in plasma PK: AUC0-t
Defined as area under the single-dose plasma concentration-time curve from Hour 0 to the last quantifiable measurable plasma concentration
Time frame: At pre-dose and up to 2 weeks post-dose
Total radioactivity in plasma PK: t½
Defined as apparent plasma terminal phase disposition half-life
Time frame: At pre-dose and up to 2 weeks post-dose
Total radioactivity in plasma PK: CL/F
Defined as apparent total body clearance
Time frame: At pre-dose and up to 2 weeks post-dose
Whole blood to plasma total radioactivity ratio
To evaluate the extent of distribution of total radioactivity into blood cells
Time frame: At pre-dose and up to 2 weeks post-dose
Cumulative total radioactivity in urine and faeces
Mass balance recovery of total radioactivity in all (urine, faeces) amount excreted (Ae) expressed as a percentage of the administered dose (%Ae)
Time frame: At pre-dose and up to 2 weeks post-dose
Metabolic profiling in plasma, urinary and fecal excretion
To characterize the metabolic profile and identify circulating and excreted metabolites of SY-5007 using liquid chromatography with mass spectral detection.
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Time frame: At pre-dose and up to 2 weeks post-dose
Cmax of SY-5007 and its metabolites
Defined as maximum observed plasma concentration
Time frame: At pre-dose and up to 2 weeks post-dose
Tmax of SY-5007 and its metabolites
Defined as time to maximum plasma concentration
Time frame: At pre-dose and up to 2 weeks post-dose
AUC0-t of SY-5007 and its metabolites
Defined as area under the single-dose plasma concentration-time curve from Hour 0 to the last quantifiable measurable plasma concentration
Time frame: At pre-dose and up to 2 weeks post-dose
t½ of SY-5007 and its metabolites
Defined as apparent plasma terminal phase disposition half-life
Time frame: At pre-dose and up to 2 weeks post-dose
CL/F of SY-5007 and its metabolites
Defined as apparent total body clearance
Time frame: At pre-dose and up to 2 weeks post-dose
Incidence of adverse events
To evaluate the safety of a single oral dose of 160 mg of SY-5007
Time frame: At pre-dose and up to 2 weeks post-dose