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

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

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Fostamatinib; Drug: Fostamatinib

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 Type: Interventional
• Enrollment (Actual): 37
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • Nottingham
    • Ruddington, Nottingham, United Kingdom

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

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

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Non-Randomized
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

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

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
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.	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	Up to 96 hours post dose
Pharmacokinetic (PK) profile of a single oral dose of fostamatinib and a radiolabelled intravenous micro tracer dose of [14C] R406.	PK Parameters: AUC, AUC (0-t), Cmax, t½ λz and MRT	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

Secondary Outcome Measures

Outcome Measure	Time Frame
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

Collaborators and Investigators

• Sponsor: AstraZeneca
• Investigators: Study Director: Mark Layton, MD, AstraZeneca, Alderley Park; Principal Investigator: Sharan Sidhu, MB CHB, BAO, MRCS, Quotient Clinical Unit

Study record dates

Study Major Dates

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

Study Registration Dates

• First Submitted: April 5, 2012
• First Submitted That Met QC Criteria: May 14, 2012
• First Posted (Estimate): May 15, 2012

Study Record Updates

• Last Update Posted (Estimate): August 22, 2012
• Last Update Submitted That Met QC Criteria: August 21, 2012
• Last Verified: August 1, 2012

More Information

Terms related to this study

• Keywords: pharmacokinetics; Phase 1; Healthy male volunteers; fostamatinib; Bioavailability; R406 plasma AUC and Cmax; R406 plasma AUC0-t; t1/2λz; tmax
• Other Study ID Numbers: D4300C00027; QBR112696

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No