The purpose of Period 1 of this study is to provide a definitive quantitative characterization of the mass balance, and rates and routes of excretion of enpatoran, and to determine and quantify enpatoran and its metabolites in excreta (urine and feces) and plasma. The purpose of Period 2 of this study is to determine the absolute oral bioavailability of enpatoran. Total minimum duration of study participation for each participant is approximately 50 days.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
7
Participants will receive single oral dose of enpatoran tablet on Day 1
Participants will receive single oral dose of non-labeled enpatoran solution spiked with microtracer of \[14C\]enpatoran on Day 1 of Period 1.
Participants will receive intravenous \[14C\]enpatoran microdose administered at 1.5 hours after the oral dose of enpatoran on Day 1 of Period 2.
PRA Health Sciences
Groningen, Netherlands
Period 1: Percent Urinary Recovery (feurine) of Total Radioactivity per Sampling Interval
Time frame: -24-0 hours (pre-dose), 0-4, 4-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hours after the initiation of the intravenous (IV) dose
Period 1: Percent Fecal Recovery (fefeces) of Total Radioactivity per Sampling Interval
Time frame: -24-0 hours (pre-dose), 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hours after the initiation of the intravenous (IV) dose
Period 1: Percent Total Recovery in Urine and Feces (fetotal) of Total Radioactivity per Sampling Interval
Time frame: Urine: -24-0 hours (pre-dose), 0-4, 4-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hours post-dose; Feces: -24-0 hours (pre-dose), 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hours post-dose of IV injection
Period 1: Pharmacokinetic Plasma and Blood Concentration of Total Radioactivity
Time frame: Pre-dose (Day 1), 15, 30 minutes, 1, 1.5, 2.0, 4.0, 6.0, 8.0, 12, 24, 48, 72, 96, 120, 144, 168 hours post-dose
Period 1: Pharmacokinetic Plasma Concentration of Enpatoran
Time frame: Pre-dose (Day 1), 15, 30 minutes, 1, 1.5, 2.0, 4.0, 6.0, 8.0, 12, 24, 48, 72, 96, 120, 144, 168 hours post-dose
Period 2: Pharmacokinetic Plasma and Blood Concentration of [14C]Enpatoran and Enpatoran
Time frame: [14C]Enpatoran: Pre-dose, 5, 15, 30 minutes, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose; Enpatoran: Pre-dose, 30 minutes, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose
Period 1 and 2: Safety Profile as Assessed by Incidence of Treatment-Emergent Adverse Events (AEs), Serious Adverse Events (SAEs), Laboratory Variables, Vital Signs and Electrocardiogram (ECG) Measurements
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Time frame: Period 1: Baseline up to Day 14; Period 2: Baseline up to Day 4