This phase I study is designed to evaluate absorption, metabolism and excretion (AME) profiles of \[14C\]-DZD8586, to determine the routes, rates of elimination, and mass balance of DZD8586 in healthy adult male participants. Participants will be administered a single oral dose of 50 mg of \[14C\]-DZD8586 (containing radioactive dose \~ 100 μCi) as a suspension.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
6
Carbon-14 labeled DZD8586
Affiliated Hospital of Jiangnan University
Wuxi, Jiangsu, China
Total amount and recovery of the radioactive dose in urine and feces: Ae, Cum Ae, fe and Cum fe
Time frame: All excreted urine and feces samples at specified time points during 0-504 hours after dosing will be collected
Metabolic profiling of relative abundance of [14C]-DZD8586 and metabolite identification of [14C]-DZD8586 in plasma, urine, and feces
Time frame: Conduct testing within 1 month after all subjects collect plasma, urine, and fecal samples at all time points required by the protocol
Peak plasma concentration (Cmax) of DZD8586
Time frame: up to 504 hours post dose
Peak plasma concentration (Cmax) of DZ4581
Time frame: up to 504 hours post dose
Peak concentration (Cmax) of total radioactivity concentration equivalents in plasma and whole blood
Time frame: Conduct testing within 1 month after all subjects collect whole blood and plasma samples at all time points defined by the protocol
Time to Cmax (Tmax) of DZD8586
Time frame: up to 504 hours post dose
Time to Cmax (Tmax) of DZ4581
Time frame: up to 504 hours post dose
Time to Cmax (Tmax) of total radioactivity concentration equivalents in plasma and whole blood
Time frame: Conduct testing within 1 month after all subjects collect whole blood and plasma samples at all time points defined by the protocol
Elimination half-life (t1/2,λz) of DZD8586
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Time frame: up to 504 hours post dose
Elimination half-life (t1/2,λz) of DZ4581
Time frame: up to 504 hours post dose
Elimination half-life (t1/2,λz) of total radioactivity concentration equivalents in plasma and whole blood
Time frame: Conduct testing within 1 month after all subjects collect whole blood and plasma samples at all time points required by the protocol
Area under the concentration-time curve from time zero to the time of the last quantifiable concentration (AUC0-t) of DZD8586
Time frame: up to 504 hours post dose
Area under the concentration-time curve from time zero to the time of the last quantifiable concentration (AUC0-t) of DZ4581
Time frame: up to 504 hours post dose
Area under the concentration-time curve from time zero to the time of the last quantifiable concentration (AUC0-t) of total radioactivity concentration equivalents in plasma and whole blood
Time frame: Conduct testing within 1 month after all subjects collect whole blood and plasma samples at all time points required by the protocol
Area under the concentration-time curve from time zero to infinity (AUC0-inf) of DZD8586
Time frame: up to 504 hours post dose
Area under the concentration-time curve from time zero to infinity (AUC0-inf) of DZ4581
Time frame: up to 504 hours post dose
Area under the concentration-time curve from time zero to infinity (AUC0-inf) of total radioactivity concentration equivalents in plasma and whole blood
Time frame: Conduct testing within 1 month after all subjects collect whole blood and plasma samples at all time points required by the protocol
Apparent oral clearance (CL/F) of DZD8586
Time frame: up to 504 hours post dose
Apparent volume of distribution (Vz/F) of DZD8586
Time frame: up to 504 hours post dose
PK parameters for renal clearance (CLR) for DZD8586 and DZ4581 in urine
Time frame: up to 504 hours post dose
Amount and percentage of DZD8586 recovered in urine
Time frame: up to 504 hours post dose
Plasma DZD8586-to-total plasma radioactivity ratio
Time frame: Conduct testing within 1 month after all subjects collect plasma samples at all time points required by the protocol
Whole blood to plasma total radioactivity ratio
Time frame: Conduct testing within 1 month after all subjects collect whole blood and plasma samples at all time points required by the protocol
Frequency, type and severity of adverse events/serious adverse events
Time frame: Up to 3 weeks
Pulse rate
Time frame: Up to 3 weeks
Blood pressure
Time frame: Up to 3 weeks
Heart rate
Time frame: Up to 3 weeks
RR, PR, QRS, and QT intervals
Time frame: Up to 3 weeks
Number of participants with abnormal laboratory tests results (including blood chemistry, hematology, coagulation function, and urinalysis)
Time frame: Up to 3 weeks
Number of participants with abnormal physical and ophthalmologic examinations findings
Time frame: Up to 3 weeks