To evaluate the absorption, metabolism, and excretion of 86550-106 in healthy males.
The purpose of this study is to determine the absorption, metabolism, and excretion of a single oral dose of 400 mg (4x100 mg tablets) of INCB086550 followed by an oral dose solution of approximately 100 μCi (3.7 MBq) \[14C\]-INCB086550 and to characterize and determine the metabolites present in plasma, urine, and, where possible, feces in healthy male participants .
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
7
INCB086550 will be administered orally, followed approximately 10 minutes later by an oral dose solution of radio labeled INCB086550.
Covance Leeds Cru
Leeds, United Kingdom
Total recovery of radioactivity from urine and feces.
To determine the route of elimination and mass balance of \[14C\]-INCB086550 following administration of a single oral dose of 400 mg of INCB086550 followed by an oral dose solution of approximately 100 μCi (3.7 MBq) \[14C\]-INCB086550.
Time frame: Approximately 2 weeks
Percentage of total radioactive dose in Plasma, Urinary and Fecal Excretion
To characterize the metabolic profile and identify circulating and excreted metabolites of INCB086550 following administration of a single oral dose of 400 mg of INCB086550 followed by an oral dose solution of approximately 100 μCi (3.7 MBq) \[14C\]-INCB086550 using liquid chromatography with mass spectral detection.
Time frame: Up to approximately 2 months
PK for plasma INCB086550: Cmax
Maximum Observed Plasma Concentration of INCB086550 to evaluate the PK of total radioactivity and parent compound following administration of a single oral dose of 400 mg of INCB086550 followed by an oral dose solution of approximately 100 μCi (3.7 MBq) \[14C\]-INCB086550.
Time frame: Pre dose and Post dose on Day 1, Post dose Day 2, post dose Day 3, post dose Day 4, post dose Day 5
PK for plasma INCB086550: tmax
Time to reach maximum (peak) Plasma concentration of INCB086550
Time frame: Pre dose and Post dose on Day 1, Post dose Day 2, post dose Day 3, post dose Day 4, post dose Day 5
PK for plasma INCB086550: AUC0-t
Area under the single-dose plasma concentration-time curve from Hour 0 to the last quantifiable measurable plasma concentration of INCB086550
Time frame: Pre dose and Post dose on Day 1, Post dose Day 2, post dose Day 3, post dose Day 4, post dose Day 5
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PK for plasma INCB086550: AUC0-∞
area under the single-dose plasma concentration-time curve from Hour 0 to infinity of INCB086550
Time frame: Pre dose and Post dose on Day 1, Post dose Day 2, post dose Day 3, post dose Day 4, post dose Day 5
PK for plasma INCB086550: t½
AUC to the end of dosing period of INCB086550
Time frame: Pre dose and Post dose on Day 1, Post dose Day 2, post dose Day 3, post dose Day 4, post dose Day 5
PK for plasma INCB086550: λz
Terminal elimination rate constant of INCB086550
Time frame: Pre dose and Post dose on Day 1, Post dose Day 2, post dose Day 3, post dose Day 4, post dose Day 5
PK for plasma INCB086550: CL/F
Oral dose clearance of INCB086550
Time frame: Pre dose and Post dose on Day 1, Post dose Day 2, post dose Day 3, post dose Day 4, post dose Day 5
PK for plasma INCB086550: Vz/F
Apparent oral dose volume of distribution of INCB086550
Time frame: Pre dose and Post dose on Day 1, Post dose Day 2, post dose Day 3, post dose Day 4, post dose Day 5
PK for Urine INCB086550: Ae
Cumulative amount of unchanged drug excreted into the urine. Urine will be collected for the following intervals relative to study treatment administration: -12 to 0 hours (predose void \[spot sample\] only) and 0 to 6, 6 to 12, and 12 to 24 hours postdose and continuing in 24-hour intervals until discharge.
Time frame: Pre dose and Post dose daily up to day 11, until study discharge
PK for urine INCB086550: CLR
Renal clearance of the drug from plasma.
Time frame: Pre dose and Post dose daily up to day 11, until study discharge
PK for Urine INCB086550: fe
Fraction of the intravenously administered drug excreted into the urine
Time frame: Pre dose and Post dose daily up to day 11, until study discharge
PK for whole blood and plasma total radioactivity: Cmax
Maximum Observed Plasma Concentration
Time frame: Pre dose and poste dose Day 1, post dose Days 2, 3, 4, 5 and Days 6-11 as needed until study discharge
PK for whole blood and plasma total radioactivity: tmax
Time to reach maximum (peak)
Time frame: Pre dose and post dose Day 1, post dose Days 2, 3, 4, 5 and Days 6-11 as needed until study discharge
PK for whole blood and plasma total radioactivity: t½
To evaluate the PK of total radioactivity and parent compound following administration of a single oral dose of 400 mg of INCB086550 followed by an oral dose solution of approximately 100 μCi (3.7 MBq) \[14C\]-INCB086550.
Time frame: Pre dose and post dose Day 1, post dose Days 2, 3, 4, 5 and Days 6-11 as needed until study discharge
PK for whole blood and plasma total radioactivity: AUC0-t
Area under the single-dose plasma concentration-time curve from Hour 0 to the last quantifiable measurable plasma concentration of INCB086550
Time frame: Pre dose and post dose Day 1, post dose Days 2, 3, 4, 5 and Days 6-11 as needed until study discharge
PK for whole blood and plasma total radioactivity: AUC0-∞
To evaluate the PK of total radioactivity and parent compound following administration of a single oral dose of 400 mg of INCB086550 followed by an oral dose solution of approximately 100 μCi (3.7 MBq) \[14C\]-INCB086550.
Time frame: Pre dose and post dose Day 1, post dose Days 2, 3, 4, 5 and Days 6-11 as needed until study discharge
Incidence of AEs, ECGs, vital signs, and clinical laboratory evaluation.
To evaluate the safety of a single oral dose of 400 mg of INCB086550 followed by an oral dose solution of approximately 100 μCi (3.7 MBq) \[14C\]-INCB086550.
Time frame: up to approximately 3 months