Study to Evaluate the Mass Balance and Biotransformation of Single Dose\[14C\] AST2818 in Chinese Healthy Male Volunteers
A Phase I Mass Balance and Biotransformation Study of Orally Administered \[14C\]-Alflutinib Mesylate (AST2818) in Chinese Healthy Male Volunteers
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
OTHER
Masking
NONE
Enrollment
6
Volunteer will receive a single oral dose of 80 mg /100 u Ci \[14C\]-AST2818 as a solution on Day 1
First Affiliated Hospital of Soochow University
Suzhou, Jiangsu, China
The distribution of AST2818 in the whole blood and plasma and whole radioactive pharmacokinetics following the single orally administered [14C]-AST2818 in healthy male volunteers.
The percentage of radioactive dose of \[14C\] radiolabelled AST2818 recovered in blood and in total, up to Day 85(p.s:The administration time on the first day is 7:30 am)
Time frame: Blood samples (hrs) - 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, every 24 to 504, 672, 840, 1008, 1176, 1344, 1512, 1680, 1848 and 2016.
Quantitive analysis of whole radioactivity of excrement of orally administered [14C]-AST2818 in healthy volunteers to obtain the mass balance data and the main excretion pathway in human body.
The percentage of radioactive dose of \[14C\] radiolabelled AST2818 recovered in urine, faeces and in total, up to Day 85(p.s:The administration time on the first day is 7:30 am)
Time frame: Urine and faeces (hrs): 0-4, 4-8, 8-12, 12-24, every 24 to 504, 624-672, 792-840, 960-1008, 1128-1176, 1296-1344, 1464-1512, 1632-1680, 1800-1848 and 1968-2016.
Quantitive analysis of the concentrations of AST2818 and AST5902 (Metabolite of AST2818) in plasma using the validated LC-MS/MS to obtain pharmacokinetic data;
The concentrations of AST2818 and AST5902 in plasma up to Day 85(p.s:The administration time on the first day is 7:30 am)
Time frame: Blood samples (hrs) - 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, every 24 to 504, 672, 840, 1008, 1176, 1344, 1512, 1680, 1848 and 2016.
Proportion of different metabolites in healthy volunteers after oral administration of [14C]-AST2818
Proportion of different metabolites
Time frame: Blood samples (hrs) - 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, every 24 to 504, 672, 840, 1008, 1176, 1344, 1512, 1680, 1848 and 2016.
Types of adverse events assessed by CTCAE v5.0 that occurred during the trial
Types of adverse events
Time frame: Baseline (Day-1) to Day 85(p.s:The administration time on the first day is 7:30 am)
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