Clinical trial NCT01598571: Study in Healthy Males to Assess Bioavailability of Single Fostamatinib With iv Micro Tracer Dose
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 type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Keywords: Phase 1
Healthy male volunteers
pharmacokinetics
fostamatinib
Bioavailability
R406 plasma AUC and Cmax
R406 plasma AUC0-t
t1/2λz
tmax
Lead sponsor: AstraZeneca
Sponsor class: INDUSTRY
First posted: 2012-05-15
Enrollment: 37
Sex: MALE
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NON_RANDOMIZED
Intervention model: SINGLE_GROUP
Primary purpose: BASIC_SCIENCE

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

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.

Eligibility criteria: 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

Primary outcomes:
measure: The percent of absolute bioavailability (F) of R406 after oral administration of fostamatinib.
timeFrame: Up to 96 hours post dose
measure: 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.
timeFrame: Up to 96 hours post dose
measure: Pharmacokinetic (PK) profile of a single oral dose of fostamatinib and a radiolabelled intravenous micro tracer dose of [14C] R406.
timeFrame: 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 outcomes:
measure: Number of participants with Adverse Events.
timeFrame: Up to Day 12
measure: Safety profile in terms of vital signs (blood pressure and pulse), clinical laboratory tests, ECGs and physical examination findings.
timeFrame: Up to Day 12
Other outcomes:
Locations:
city: Ruddington
country: United Kingdom
state: Nottingham
Study officials:
affiliation: AstraZeneca, Alderley Park
name: Mark Layton, MD
role: STUDY_DIRECTOR
affiliation: Quotient Clinical Unit
name: Sharan Sidhu, MB CHB, BAO, MRCS
role: PRINCIPAL_INVESTIGATOR
References: