The purpose of this trial is to determine the absorption, metabolism, and excretion (AME) of \[14C\] tavapadon.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
12
Participants will receive multiple dose titration of Tavapadon (0.25 mg once daily \[QD\] on Days 1 to 3, 0.5 mg QD on Days 4 to 6, 1.0 mg QD on Days 7 to 9, 1.5 mg QD on Days 10 to 12, and 2.5 mg QD on Days 13 to 15)
Following 15-Day multiple dose titration of Tavapadon, participants will receive a single oral dose of Tavapadon 2.5 mg containing approximately 100 μCi of \[14C\] Tavapadon on Day 16
Covance Clinical Research Unit, Inc.
Madison, Wisconsin, United States
Pharmacokinetics of [14C]-Tavapadon and Metabolites: Area under the radioactivity time curve from zero to infinity (AUCinf) for Tavapadon and Metabolites (PF-06752844), in plasma and whole blood
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon and Metabolites: Area under the radioactivity time curve from time 0 to last quantifiable concentration (AUClast) for Tavapadon and Metabolites (PF-06752844), in plasma and whole blood
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon and Metabolites: Peak radioactivity Cmax) for Tavapadon and Metabolites (PF-06752844), in plasma and whole blood
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon and Metabolites: Time to last measurable radioactivity (Tlast) for Tavapadon and Metabolites (PF-06752844), in plasma and whole blood
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon and Metabolites: Time to maximum radioactivity (Tmax) for Tavapadon and Metabolites (PF-06752844), in plasma and whole blood
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon and Metabolites: elimination half-life (t½) for Tavapadon and Metabolites (PF-06752844), in plasma and whole blood
Time frame: Day 16 up to Day 28
Pharmacokinetics of Tavapadon: Apparent total body clearance (CL/F) for Tavapadon
Time frame: Day 16 up to Day 28
Pharmacokinetics of Tavapadon: Apparent volume of distribution (Vz/F) for Tavapadon
Time frame: Day 16 up to Day 28
Ratio of Plasma AUCinf for Tavapadon to whole blood total Radioactivity AUCinf
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Time frame: Day 16 up to Day 28
Ratio of Plasma AUCinf for Metabolites (PF-06752844) to whole blood total Radioactivity AUCinf
Time frame: Day 16 up to Day 28
Ratio of plasma AUCinf for Metabolites (PF-06752844) to plasma AUCinf for Tavapadon
Time frame: Day 16 up to Day 28
Ratio of whole blood AUCinf for Tavapadon (and metabolites, measured as total radioactivity) to plasma AUCinf for Tavapadon (and metabolites, measured as total radioactivity)
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon: Total radioactivity in urine at different intervals
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon: Cumulative radioactivity excreted in urine (Cumulative Aeu)
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon: Fraction of the dose administered excreted in urine (Feu) for total radioactivity at different intervals
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon: Cumulative fraction of the dose administered excreted in urine (Cumulative Feu) for total radioactivity in urine
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon: Amount eliminated in feces (Aef) for total radioactivity in feces at different intervals
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon: Cumulative amount excreted in feces (Cumulative Aef) for total radioactivity in feces
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon: Fraction of the dose administered excreted in feces (Fef) for total radioactivity in feces at different intervals
Time frame: Day 16 up to Day 28
Pharmacokinetics of [14C]-Tavapadon: Cumulative Fraction of the dose administered excreted in feces (Cumulative Fef) for total radioactivity in feces
Time frame: Day 16 up to Day 28
Number of Subjects with reported Treatment Emergent Adverse Events (TEAEs)
Time frame: Up to Day 28
Number of subjects with Clinically significant changes in Electrocardiogram measures (PR,RR,QT and QTcF)
Time frame: Up to Day 28
Number of subjects with Clinically meaningful changes in Vital signs (Systolic and Diastolic blood pressures, heart rate, respiratory rate and body temperature)
Time frame: Up to Day 28
Number of subjects with clinically significant changes in laboratory measures
Time frame: Up to Day 28
Change from baseline of the Columbia-Suicide Severity Rating Scale (C-SSRS)
The C-SSRS rates an individual's degree of suicidal ideation (SI) on a scale, ranging from "wish to be dead" to "active suicidal ideation with specific plan and intent." The scale identifies SI severity and intensity, which may be indicative of an individual's intent to commit suicide. C-SSRS SI severity subscale ranges from 0 (no SI) to 5 (active SI with plan and intent).
Time frame: At Baseline and up to Day 28