Healthy
Conditions
Keywords
Phase 1, Healthy male volunteers, pharmacokinetics, fostamatinib, Bioavailability, R406 plasma AUC and Cmax, R406 plasma AUC0-t, t1/2λz, tmax
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.
Interventions
DRUGFostamatinib
Fostamatinib 50 mg tablet
Sponsors
AstraZeneca
Study design
Allocation
NON_RANDOMIZED
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
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
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| 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
| 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 |
Countries
United Kingdom
Outcome results
None listed