Open-label, single-dose study to assess the absorption, metabolism, excretion and mass balance of \[C14\] CT1812
Open-label, single-dose study to assess the absorption, metabolism, excretion and mass balance of \[C14\] CT1812 in 8 healthy male subjects Subjects will be screened 28-days prior to dosing to determine eligibility. Eligible subjects will be admitted to the clinical research unit (CRU) on Day -1. On Day 1, subjects will receive a single dose of CT1812 with a microtracer dose of \[14C\] CT1812. Whole blood, plasma, urine and fecal samples will be collection during the confinement period. Safety will be monitored throughout the study by repeated clinical and laboratory evaluations. Subjects will be and discharged from the CRU following completion of procedures 168 hours post dose (Day 8)
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
8
Single dose of 300 mg CT1812 with microtracer dose of \[C14\]
Celerion
Lincoln, Nebraska, United States
Plasma CT1812 Concentration at 96 Hours Timepoint
Plasma concentrations of CT1812 were determined using a validated liquid chromatography with tandem mass spectrometry (LC-MS/MS) following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects.
Time frame: Predose through 96 hours postdose
Plasma M6/CP199 Concentration at 144 Hours Timepoint
Plasma concentrations of M6/CP199 were determined using a validated liquid chromatography with tandem mass spectrometry (LC-MS/MS) following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects.
Time frame: Predose through 144 hours postdose
Plasma Total Radioactivity (TRA) Concentration CT1812-Equivalents at 168 Hours Timepoint
Plasma Total Radioactivity Concentration of CT1812-Equivalents was performed using Liquid Scintillation Counting (LSC) method following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects.
Time frame: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168 hours postdose
Whole Blood Total Radioactivity (TRA) Concentration CT1812-Equivalents at 144 Hours Timepoint
The analysis of Whole Blood Total Radioactivity Concentration of CT1812-Equivalents was performed using combustion followed by Liquid Scintillation Counting (LSC) method following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects.
Time frame: Predose through 144 hours postdose
Cumulative Percentage of Radioactive Dose (Cum%Dose) Excreted in the Urine
Cumulative radioactive dose (Cum%Dose) excreted in the urine was determined using Liquid Scintillation Counting (LSC) following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects.
Time frame: Predose and 0 to 4, 4 to 8, 8 to 12, and 12 to 24 hours postdose, and every 24 hours (pooled) until Day 8 (168 hours postdose).
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Cumulative Percentage of Radioactive Dose (Cum%Dose) Excreted in the Feces
Cumulative radioactive dose (Cum%Dose) excreted in the feces was performed using combustion followed by Liquid Scintillation Counting (LSC) method following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects.
Time frame: Predose, 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168 hours postdose
CT1812 Plasma Exposure According to AUC0-last Pharmacokinetic Parameter
Plasma CT1812 Concentration were measured using the area under the concentration-time curve, from time 0 to the last observed non-zero concentration, as calculated by the linear trapezoidal method following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects. Plasma concentrations of CT1812 were determined using a validated liquid chromatography with tandem mass spectrometry (LC-MS/MS).
Time frame: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168 hours postdose
M6/CP199 Plasma Exposure According to AUC0-last Pharmacokinetic Parameter
M6/CP199 Plasma Concentration was measured using the area under the concentration-time curve, from time 0 to the last observed non-zero concentration, as calculated by the linear trapezoidal method following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects. M6/CP199 plasma concentrations were determined using a validated liquid chromatography with tandem mass spectrometry (LC-MS/MS).
Time frame: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168 hours postdose
Plasma Total Radioactivity According to AUC0-last Pharmacokinetic Parameter
Plasma Total Radioactivity was measured using the area under the concentration-time curve, from time 0 to the last observed non-zero concentration, as calculated by the linear trapezoidal method following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects. Plasma Total Radioactivity Concentration of CT1812-Equivalents was performed using Liquid Scintillation Counting (LSC).
Time frame: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168 hours postdose
Whole Blood Total Radioactivity According to AUC0-last Pharmacokinetic Parameter
Whole Blood Total Radioactivity was measured using the area under the concentration-time curve, from time 0 to the last observed non-zero concentration, as calculated by the linear trapezoidal method following a single oral dose of 300 mg (\~1 μCi) \[14C\]-CT1812 administered in healthy adult male subjects. Plasma Total Radioactivity Concentration of CT1812-Equivalents was performed using Liquid Scintillation Counting (LSC)
Time frame: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168 hours postdose
Whole Blood:Plasma Total Radioactivity Partitioning Ratios Over Time up to 144 Hours Timepoint
This measure describes the percentage of TRA in whole blood relative to plasma. The fraction of \[14C\]-radioactivity associated with whole blood and plasma and with red blood cells and other cellular components of whole blood was determined by using the concentration of \[14C\]-radioactivity in whole blood and plasma.
Time frame: Predose through 144 hours postdose
Number of TEAEs, Related TEAEs, SAEs, and Related SAEs
Incidence and Severity of Adverse Events. All AEs that occurred during this clinical trial were coded using the Medical Dictionary for Regulatory Activities (MedDRA®), Version 24.1.
Time frame: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168 hours