Healthy Subjects, Pharmacokinetics of ASP3652
Conditions
Keywords
Pharmacokinetics, ASP3652, 14C radio-labeled, Phase 1
Brief summary
This study measures how much of the trial drug enters the body and how long it takes for the body to remove it via the feces and urine. In addition, the different breakdown products after a single oral dose of radio-active ASP3652 will be identified.
Detailed description
This is an open-label, one-period, single-dose study with 14C labeled ASP3652. Screening takes place between Day 22 to Day 2, and subjects are admitted to the clinic on Day -1. On the morning of Day 1, each subject receives a single oral dose of 14C-labeled ASP3652. Blood, urine and feces samples for analysis of 14C radioactivity are collected until at least 120 h after dosing. Blood samples for the analysis of ASP3652 and metabolites are collected until 120 h after dosing. The subjects remain in the clinic until Day 6 (or up to Day 13 in case discharge criteria are not met on Day 6) and return for an End of Study Visit (ESV) 7 to 14 days after (early) discharge.
Interventions
DRUGASP3652
oral
Sponsors
Astellas Pharma Europe B.V.
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
35 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Subject is white and of Caucasian origin. * Regular defecation pattern (minimum once per day). * Subject must agree to use a condom during sexual intercourse until 3 months after dosing. In addition to using a condom, subjects must agree to practice an adequate contraceptive method with female sexual partners to prevent pregnancy.
Exclusion criteria
* Known or suspected hypersensitivity to ASP3652 or any components of the formulation used. * Donation of blood or blood products within 3 months prior to admission to the Clinical Unit. * Exposure to radiation for diagnostic reasons (except dental X-rays and plain X-rays of thorax and bony skeleton (excluding spinal column)), during work or during participation in a clinical study in the previous year.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Ratio ASP3652 to 14C-radioactivity for AUCinf | Days 1 to 6 and up to Day 9 | area under the plasma concentration (AUC) - time curve from time zero to infinity (AUCinf) |
| Total radioactivity in plasma | Days 1 to 6 and up to Day 9 | area under the plasma concentration (AUC) - time curve from time zero to infinity (AUCinf), area under the plasma concentration - time curve from time zero to time of last measurable concentration (AUClast), maximum concentration (Cmax), time to attain Cmax (tmax), apparent terminal elimination half-life (t½) |
| Total radioactivity in whole blood | Days 1 to 6 and up to Day 9 | area under the plasma concentration (AUC) - time curve from time zero to infinity (AUCinf), area under the plasma concentration - time curve from time zero to time of last measurable concentration (AUClast), maximum concentration (Cmax), time to attain Cmax (tmax), apparent terminal elimination half-life (t½) |
| Radioactivity ratio of plasma / blood | Days 1 to 6 and up to Day 9 | ratio concentrations per time point and AUC |
| Radioactivity excretion in urine | Urine: Days 1-6 and up to Day 25 | excretion rate and cumulative excretion |
| Radioactivity excretion in feces | Days 1-6 and up to Day 25 | excretion rate and cumulative excretion |
| Radioactivity excretion in urine and feces | Urine: Days 1-6 and up to Day 25 | excretion rate and cumulative excretion |
| ASP3652 in plasma | Days 1 to 6 and up to Day 9 | AUCinf, AUClast, Cmax, tmax, t1/2, apparent clearance after oral administration at steady state (CL/F), volume of terminal phase distribution at steady state (Vz/F) |
| ASP3652 in urine | Days 1-6 and up to Day 25 | cumulative amount of unchanged drug excreted into the urine from time zero to infinity after single dose (Aeinf), cumulative amount of unchanged drug excreted into the urine from time zero to time of last measurable concentration (Aelast), renal clearance of the drug from plasma (CLR), percentage of unchanged drug excreted into the urine from time zero to infinity after single dose % of dose excreted (Aeinf%), percentage of unchanged drug excreted into the urine from time zero to time of last measurable concentration (Aelast%) |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Safety and tolerability after a single dose | Screening (Day 22 to Day 2) to End of Study Visit (7 to 14 days after (early) discharge) | Vital signs, 12-lead ECG, safety laboratory tests, physical examination, occurrence of Adverse Events (AE) |
Countries
United Kingdom
Outcome results
None listed