A phase 1 healthy volunteer study to assess the excretion and metabolism as well as the absolute bioavailability of oral ONO-5788. The study will be conducted in two parts: Part 1 to assess the absolute bioavailability using ONO-5788 and radiolabelled ONO-5788 as intravenous and oral forms; part 2 will assess the mass balance of ONO-5788 using orally administered radiolabelled ONO-5788
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
12
Investigational Drug
Investigational Drug
PRA-EDS
Groningen, NZ, Netherlands
Absolute bioavailability of ONO-5788 in plasma
Absolute bioavailability is calculated from the AUCs of iv and oral administration
Time frame: 72 hours
Mass balance of ONO-5788
Total recovery of radioactivity in urine and faeces following a single oral dose of \[14C\]-ONO-5788 (expressed as a percentage of the total radioactive dose administered)
Time frame: up to 42 days (until >90% of dose is recovered)
Pharmacokinetics (AUC)
Assessment of the plasma area under the curve of ONO-5788 and \[14C\]-ONO-5788
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)
Pharmacokinetics (t1/2)
Assessment of the total elimination half life of ONO-5788 and \[14C\]-ONO-5788
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)
Pharmacokinetics (CL)
Assessment of the clearance of ONO-5788 (Part 1 only)
Time frame: 24 hours through to 72 hours.
Pharmacokinetics (CL/F)
Assessment of Apparent oral clearance of ONO-5788
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)
Pharmacokinetics (Vz)
Assessment of Volume of distribution at terminal phase (Part 1 only)
Time frame: 24 hours through to 72 hours.
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Pharmacokinetics (Vz/F)
Assessment of Apparent volume of distribution at terminal phase
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)
Pharmacokinetics (CLr)
Assessment of renal clearance (Part 2 only)
Time frame: Part 2: Day 1 to day 42 (depending on recovery of dose)
Treatment emergent adverse events
Number of participants with treatment emergent adverse events by severity
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)
Clinical laboratory abnormalities
Number of participants with abnormalities in clinical laboratory results
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)
Changes in vital signs
Number of participants with clinically significant changes in vital signs including pulse/heart rate, respiratory rate and blood pressure.
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)
ECG abnormalities
Number of participants with ECG abnormalities
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)
Physical examination assessment
A complete physical examination consisting of all body systems (except for genitalia and anus/rectal examinations, which will only be performed if medically indicated). Number of participants with clinically significant changes will be reported
Time frame: Part 1: 24 hours through to 72 hours. Part 2: Day 1 to day 42 (depending on recovery of dose)