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A Study to Assess the Pharmacokinetics, Metabolism and Excretion Routes of ASP3652 in Man, After Administration of 14C Radio Labeled ASP3652

Phase 1
Completed
Conditions
Healthy Subjects
Pharmacokinetics of ASP3652
Interventions
Registration Number
NCT02046798
Lead Sponsor
Astellas Pharma Europe B.V.
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.

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
6
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.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
14C labeled ASP3652ASP3652-
Primary Outcome Measures
NameTimeMethod
Total radioactivity in plasmaDays 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 bloodDays 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 / bloodDays 1 to 6 and up to Day 9

ratio concentrations per time point and AUC

Radioactivity excretion in urineUrine: Days 1-6 and up to Day 25

excretion rate and cumulative excretion

Radioactivity excretion in fecesDays 1-6 and up to Day 25

excretion rate and cumulative excretion

Radioactivity excretion in urine and fecesUrine: Days 1-6 and up to Day 25

excretion rate and cumulative excretion

ASP3652 in plasmaDays 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 urineDays 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%)

Ratio ASP3652 to 14C-radioactivity for AUCinfDays 1 to 6 and up to Day 9

area under the plasma concentration (AUC) - time curve from time zero to infinity (AUCinf)

Secondary Outcome Measures
NameTimeMethod
Safety and tolerability after a single doseScreening (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)

Trial Locations

Locations (1)

Covance Clinical Research Unit (CRU) Ltd.

🇬🇧

Leeds, United Kingdom

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