Study in Healthy Males to Assess Bioavailability of Single Fostamatinib With iv Micro Tracer Dose

Sponsor

AstraZeneca (Industry)

Overall Status

Completed

CT.gov ID

NCT01598571

Collaborator

(none)

Enrollment

Location

Arms

Duration (Months)

12.2

Patients Per Site Per Month

Study Details

Study Description

Brief Summary

Study in healthy males to assess bioavailability of single fostamatinib with iv micro tracer dose.

Condition or Disease	Intervention/Treatment	Phase
Healthy	Drug: Fostamatinib Drug: Fostamatinib	Phase 1

Detailed Description

A Study to Assess the Absolute Bioavailability of a Single Oral Dose of Fostamatinib with Respect to an Intravenous Micro Tracer Dose of [14C] R406 in Healthy Male Volunteers.

Study Design

Study Type:

Interventional

Actual Enrollment :

37 participants

Allocation:

Non-Randomized

Intervention Model:

Single Group Assignment

Masking:

None (Open Label)

Primary Purpose:

Basic Science

Official Title:

A Study to Assess the Absolute Bioavailability of a Single Oral Dose of Fostamatinib With Respect to an Intravenous Micro Tracer Dose of [14C] R406 in Healthy Male Volunteers

Study Start Date :

May 1, 2012

Actual Primary Completion Date :

Aug 1, 2012

Actual Study Completion Date :

Aug 1, 2012

Arms and Interventions

Arm	Intervention/Treatment
Experimental: Fostamatinib 50 mg tablet	Drug: Fostamatinib Fostamatinib 50 mg tablet
Experimental: Fostamatinib 100 μg [14C] R406 intravenous micro tracer dose	Drug: Fostamatinib Fostamatinib 100 μg [14C] R406 intravenous micro tracer dose

Arm

Intervention/Treatment

Experimental: Fostamatinib 50 mg tablet

Drug: Fostamatinib

Fostamatinib 50 mg tablet

Experimental: Fostamatinib 100 μg [14C] R406 intravenous micro tracer dose

Drug: Fostamatinib

Fostamatinib 100 μg [14C] R406 intravenous micro tracer dose

Outcome Measures

Primary Outcome Measures

The percent of absolute bioavailability (F) of R406 after oral administration of fostamatinib. [Up to 96 hours post dose]
Total radioactivity of [14C] R406 after an intravenous infusion of [14C]R406 in terms of AUC, AUC(0-t), Cmax, t1/2λz, MRT, CL, Vz. [Up to 96 hours post dose]
AUC-Area under the plasma concentration time curve; AUC(0-t)-Area under plasma concentration time curve from zero to time of the last measurable concentration; Cmax - max plasma concentration; t½ λz-Terminal half-life; MRT- Mean residence time; CL - Total body clearance; Vz - Volume of distribution during the terminal phase
Pharmacokinetic (PK) profile of a single oral dose of fostamatinib and a radiolabelled intravenous micro tracer dose of [14C] R406. [0, 30min, 1h, 1h 30min, 1h 45min, 1h 50min, 1h 55min, 2, 2h 5min, 2h 10min, 2h 15min, 2h30min, 3, 3h 30min, 5h30min, 9h, 12h, 18h, 24h, 30h, 48h, 72h, 96h post-dose]
PK Parameters: AUC, AUC (0-t), Cmax, t½ λz and MRT

Secondary Outcome Measures

Number of participants with Adverse Events. [Up to Day 12]
Safety profile in terms of vital signs (blood pressure and pulse), clinical laboratory tests, ECGs and physical examination findings. [Up to Day 12]

Eligibility Criteria

Criteria

Ages Eligible for Study:

18 Years to 55 Years

Sexes Eligible for Study:

Male

Accepts Healthy Volunteers:

Yes

Inclusion Criteria:

Healthy male volunteers aged 18 to 55 years (inclusive), with a weight of at least 50 kg and a body mass index (BMI) between 18 and 30 kg/m2 (inclusive)
Male volunteers willing to use barrier contraception ie, condoms with spermicide, from the first day of the investigational product administration until 3 months after the last administration of the investigational product

Exclusion Criteria:

History of any clinically significant disease or disorder
History or presence of GI, hepatic, or renal disease or any other condition known to interfere with absorption, distribution, metabolism, or excretion of drugs
Any clinically significant illness, medical/surgical procedure or trauma within 4 weeks of the first administration of drug
Volunteers who smoke more than 5 cigarettes or the equivalent in tobacco per day
Any clinically significant abnormalities in clinical chemistry, hematology or urinalysis results as judged by the Investigator