Assess Pharmacokinetics of Fostamatinib in Fed and Fasted State in Combination With Ranitidine to Assess Bioavailability

An Open-label, Single-center, 2-Part, Randomized Study to Assess the Pharmacokinetics of R406 in Healthy Subjects When Fostamatinib 150 mg is Administered Alone in Fed and Fasted State and in Combination With Ranitidine in Fasted State, and to Assess the Relative Bioavailability of Process Variants of Tablets

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01682408

Acronym

PK Combination

Enrollment

Registered

2012-09-10

Start date

2012-09-30

Completion date

2012-12-31

Last updated

2012-12-28

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Pharmacokinetics

Keywords

R406,, Fostamatinib,, Phase I,, Healthy Subjects,, Pharmacokinetics,, Fed/Fasted

Brief summary

Study to Assess the Pharmacokinetics of R406 in Healthy Subjects when Fostamatinib 150 mg is Administered Alone in Fed and Fasted state and in Combination with Ranitidine in Fasted State, and to Assess the Relative Bioavailability of Process Variants of Tablets

Detailed description

An Open-label, Single-center, 2-Part, Randomized Study to Assess the Pharmacokinetics of R406 in Healthy Subjects when Fostamatinib 150 mg is Administered Alone in Fed and Fasted state and in Combination with Ranitidine in Fasted State, and to Assess the Relative Bioavailability of Process Variants of Tablets

Interventions

DRUGFostamatinib - 1 x 150mg mannitol-based 38% drug-loaded tablet(orange reference)

1 x 150mg mannitol-based 38% drug-loaded tablet(orange reference)

DRUGFostamatinib - 3 x 50mg microcrystalline cellulose-based 13% drug loaded tablets,(blue) fed

3 x 50mg microcrystalline cellulose-based 13% drug loaded tablets,(blue) fed

DRUGFostamatinib - 1 x 150mg mannitol based 38% drug-loaded tablet (batch variant A)

1 x 150mg mannitol based 38% drug-loaded tablet (batch variant A)

DRUGFostamatinib - 1 x 150mg mannitol based 38% drug loaded tablet (batch variant B)

1 x 150mg mannitol based 38% drug loaded tablet(batch variant B)

DRUGRanitidine

150 mg ranitidine

Study design

Allocation

RANDOMIZED

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* Provision of signed and dated, written informed consent prior to any study-specific procedures including the genetic sampling and analyses * Volunteers will be males or females aged 18 to 55 years (inclusive) and with a weight of at least 50 kg and body mass index (BMI) between 18 and 30 kg/m2 inclusive. * Provision of signed, written, and dated informed consent for optional genetic research. If a volunteer declines to participate in the genetic component of the study, there will be no penalty or loss of benefit to the volunteer. * Male volunteers should be willing to use barrier contraception, ie, condoms from the day of first dosing until 2 weeks after dosing with the IP in Treatment Period 5. * Females must have a negative pregnancy test at screening and on admission to the CPU (including check-in at each treatment period), must not be lactating and must be of non childbearing potential, confirmed at screening

Exclusion criteria

* History of any clinically significant disease or disorder which, in the opinion of the Investigator, may either put the volunteer at risk because of participation in the study, or influence the results or the volunteer's ability to participate in the study * 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 IP * Any clinically significant abnormalities in clinical chemistry, hematology, or urinalysis results as judged by the Investigator * Any positive result on screening for serum hepatitis B surface antigen, hepatitis C antibody, and human immunodeficiency virus (HIV)

Design outcomes

Primary

Measure	Time frame
Pharmacokinetics profile of R406 in terms of maximum observed plasma concentration (Cmax) and area under the plasma concentration-time curve from time zero extrapolated to infinity (AUC).	Day 1 (predose) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, and 96 hours postdose

Secondary

Measure	Time frame
Pharmacokinetic profile of R406 in terms of area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration [AUC(0-t)], time to Cmax (tmax), terminal half-life (t1/2λz), terminal rate constant (λz).	Day 1 (predose) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, and 96 hours postdose
Description of the safety profile in terms of frequency of adverse events.	up to 3 - 5 days after discharge
Description of the safety profile in terms of severity of adverse events.	up to 3 - 5 days after discharge

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026