- To assess the absorption, distribution, metabolism and excretion of R924548 after a single oral dose- To assess the safety and tolerability of R924548 after a single oral dose
ID
Source
Brief title
Condition
- Autoimmune disorders
Synonym
Research involving
Sponsors and support
Intervention
Outcome measures
Primary outcome
- Plasma PK of R507 and R689
- Total concentration radioactivity in plasma and whole blood over time
- Total amount of radioactivity recovered in urine and feces
- Characterized metabolites of R924548 (R548) in plasma, urine, and feces
Secondary outcome
Safety and tolerability: adverse events, vital signs, ECG-parameters,
laboratory parameters, physical examination
Background summary
The study drug to be given, R548, is a new investigational drug that may
eventually be used for the treatment of immunemediated diseases such as
rheumatoid arthritis. R548 is a study drug that will convert in the body into
an inhibitor of Janus kinase 1 (JAK1) and Janus kinase 3 (JAK3), which are
enzymes that contribute to the development of inflammation in rheumatoid
arthritis.
The study medication is not registered as a drug but has been given to humans
before.
Study objective
- To assess the absorption, distribution, metabolism and excretion of R924548
after a single oral dose
- To assess the safety and tolerability of R924548 after a single oral dose
Study design
An open label study in 6 healthy volunteers. The subjects will receive
14C-R924548 as an oral suspension.
Intervention
Study Medication
Active substance: R548
Activity: janus kinase 1 (JAK1) and janus kinase 3 (JAK3)
Dosage form: aqueous suspension or aqueous solution
Treatment:
a single oral dose of 400 mg 14C-R548 aqueous suspension on Day 1
Discharge will occur on Day 8 if the Total Radioactivity Discharge Criteria
are met, or as late as Day 12.
Discharge criteria:
1. The concentration of radioactivity in 2 consecutive whole blood and plasma
timepoints is below the Lower Limit of Quantification (LLOQ) AND
2. * 90% of the administered dose is recovered in the excreta OR
3. * 90% of the dose is recovered in the excreta but the results have shown *
1% of administered radioactive dose is present in the excreta for at least 2
consecutive days.
Study burden and risks
Not applicable
1180 Veterans Boulevard
CA 94080, South San Francisco
US
1180 Veterans Boulevard
CA 94080, South San Francisco
US
Listed location countries
Age
Inclusion criteria
Healthy male volunteers
18-55 years of age
BMI 18.0-31.0 kg/m2
Exclusion criteria
Suffering from: hepatitis B, cancer or HIV/AIDS.
Participation in another drug study within 3 months before the start of this study.
Blood donation within 3 months from the start of this study or in case you have donated more than 1.5 liters of blood in the 10 months before the start of this study.
Design
Recruitment
Followed up by the following (possibly more current) registration
No registrations found.
Other (possibly less up-to-date) registrations in this register
No registrations found.
In other registers
| Register | ID |
|---|---|
| EudraCT | EUCTR2012-002570-31-NL |
| CCMO | NL40981.056.12 |