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

An Open Label Study to Evaluate the Pharmacokinetics of ASP3652 After a Single Oral Dose of 14C-labeled ASP3652 in Healthy Caucasian Male Subjects

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.

Study Overview

• Status: Completed
• Conditions: Healthy Subjects; Pharmacokinetics of ASP3652
• Intervention / Treatment: Drug: ASP3652

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.

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • Leeds, United Kingdom, LS2 9LH
    • Covance Clinical Research Unit (CRU) Ltd.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 35 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: 14C labeled ASP3652	Drug: ASP3652; oral

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Total radioactivity in plasma	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)	Days 1 to 6 and up to Day 9
Total radioactivity in whole blood	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)	Days 1 to 6 and up to Day 9
Radioactivity ratio of plasma / blood	ratio concentrations per time point and AUC	Days 1 to 6 and up to Day 9
Radioactivity excretion in urine	excretion rate and cumulative excretion	Urine: Days 1-6 and up to Day 25
Radioactivity excretion in feces	excretion rate and cumulative excretion	Days 1-6 and up to Day 25
Radioactivity excretion in urine and feces	excretion rate and cumulative excretion	Urine: Days 1-6 and up to Day 25
ASP3652 in plasma	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)	Days 1 to 6 and up to Day 9
ASP3652 in urine	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%)	Days 1-6 and up to Day 25
Ratio ASP3652 to 14C-radioactivity for AUCinf	area under the plasma concentration (AUC) - time curve from time zero to infinity (AUCinf)	Days 1 to 6 and up to Day 9

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Safety and tolerability after a single dose	Vital signs, 12-lead ECG, safety laboratory tests, physical examination, occurrence of Adverse Events (AE)	Screening (Day 22 to Day 2) to End of Study Visit (7 to 14 days after (early) discharge)

Collaborators and Investigators

• Sponsor: Astellas Pharma Europe B.V.

Study record dates

Study Major Dates

• Study Start: July 1, 2012
• Primary Completion (Actual): August 1, 2012
• Study Completion (Actual): August 1, 2012

Study Registration Dates

• First Submitted: January 24, 2014
• First Submitted That Met QC Criteria: January 24, 2014
• First Posted (Estimate): January 28, 2014

Study Record Updates

• Last Update Posted (Estimate): January 28, 2014
• Last Update Submitted That Met QC Criteria: January 24, 2014
• Last Verified: January 1, 2014

More Information

Terms related to this study

• Keywords: Pharmacokinetics; Phase 1; ASP3652; 14C radio-labeled
• Other Study ID Numbers: 3652-CL-0003; 2011-004526-10 (EudraCT Number)