The primary purpose of this study is to determine the routes, rates of elimination, mass balance of total radioactivity and metabolite profiles following a single oral dose of \[14C\]-tebapivat. To characterize the PK of tebapivat and \[13C2,15N3\]-tebapivat and determine the absolute bioavailability following single oral dose of \[14C\]-tebapivat relative to single intravenous microdose of \[13C2,15N3\]-tebapivat to healthy male participants.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
8
Oral Capsule
Intravenous Solution
Taha El-Shahat
Madison, Wisconsin, United States
Percentage of Radioactive Dose Excreted in Urine Over a Time Interval (feut1-t2) of [14C]-Tebapivat
Time frame: Up to Day 42
Percentage of Radioactive Dose Excreted in Feces Over a Time Interval (fef t1-t2) of [14C]-Tebapivat
Time frame: Up to Day 42
Cumulative Percentage of Radioactive Dose Excreted in Urine Over a Time Interval (Cum feut1-t2) of [14C]-Tebapivat
Time frame: Up to Day 42
Cumulative Percentage of Radioactive Dose Excreted in Feces Over a Time Interval (Cum fef t1-t2) of [14C]-Tebapivat
Time frame: Up to Day 42
Percentage of Total Radioactivity in Total Excreta (Feces + Urine) (Cum fe) of [14C]-Tebapivat
Time frame: Up to Day 42
Amount of Drug Excreted in Urine (Aeu) of [14C]-Tebapivat
Time frame: Up to Day 42
Cumulative Amount of Drug Excreted in Urine (Cum Aeu) of [14C]-Tebapivat
Time frame: Up to Day 42
Renal Clearance (CLR) of [14C]-Tebapivat
Time frame: Up to Day 42
Area Under the Concentration-Time Curve (AUC) From Time 0 to 168 Hours Postdose (AUC0-168) in Plasma for [14C]-Tebapivat and [13C2,15N3]-Tebapivat
Time frame: Up to Day 7
AUC0-168 in Plasma and Whole Blood for Total Radioactivity
Time frame: Up to Day 7
AUC From Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t) in Plasma for [14C]-Tebapivat and [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
AUC0-t in Plasma and Whole Blood for Total Radioactivity
Time frame: Up to Day 42
AUC Extrapolated to Infinity (AUC0-inf) in Plasma for [14C]-Tebapivat and [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
(AUC0-inf) in Plasma and Whole Blood for Total Radioactivity
Time frame: Up to Day 42
Maximum Observed Plasma Concentration (Cmax) for [14C]-Tebapivat and [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
Cmax in Plasma and Whole Blood for Total Radioactivity
Time frame: Up to Day 42
Time to Reach Cmax (Tmax) for [14C]-Tebapivat and [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
Tmax in Plasma and Whole Blood for Total Radioactivity
Time frame: Up to Day 42
Terminal Elimination Half-Life (t1/2) in Plasma for [14C]-Tebapivat and [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
T1/2 in Plasma and Whole Blood for Total Radioactivity
Time frame: Up to Day 42
Ratio of AUC0-inf for Tebapivat to AUC0-inf for Total Radioactivity in Plasma
Time frame: Up to Day 42
Ratio of AUC0-inf for Total Radioactivity in Whole Blood to AUC0-inf for Total Radioactivity in Plasma
Time frame: Up to Day 42
Total Clearance Following IV Administration (CL) of [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
Apparent Volume of Distribution During the Terminal Phase Following IV Administration (Vz) of [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
Apparent Volume of Distribution at Steady State Following IV Administration (Vss) of [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
Ratio of Dose-Normalized AUC0-inf of Oral Administration of [14C]-Tebapivat Relative to IV Administration of [13C2,15N3]-Tebapivat
Time frame: Up to Day 21
Quantitation of Major Metabolites of [14C]-Tebapivat in Plasma After Oral Administration
Quantification of major metabolites of \[14C\]-tebapivat in plasma.
Time frame: Up to Day 21
Quantitation of Major Metabolites of [14C]-Tebapivat in Excreta After Oral Administration
Quantification of major metabolites of \[14C\]-tebapivat in excreta.
Time frame: Up to Day 42
Identification of Chemical Structure of Major Metabolites of [14C]-Tebapivat in Plasma After Oral Administration
Identification of the chemical structures of major metabolites of \[14C\]-tebapivat in plasma.
Time frame: Up to Day 21
Identification of Chemical Structure of Major Metabolites of [14C]-Tebapivat in Excreta After Oral Administration
Identification of the chemical structures of major metabolites of \[14C\]-tebapivat in excreta.
Time frame: Up to Day 42
Number of Participants with Adverse Events (AEs) by Type, Severity, and Relationship to Study Drug
Time frame: Up to Day 28
Number of Participants With Clinically Significant Change From Baseline in Clinical Laboratory Assessments
Time frame: Baseline up to Day 28
Number of Participants With Clinically Significant Change From Baseline in Abnormal 12-Lead Electrocardiogram (ECG) Parameters
Time frame: Baseline up to Day 28
Number of Participants With Clinically Significant Change From Baseline in Abnormal Vital Signs Measurements
Time frame: Baseline up to Day 28
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