Primary:* To determine the absolute oral bioavailability and further characterize the PK of RO5186582 using a stable isotope technique.* To explore the routes and rates of elimination of [14C] labelled RO5186582.Secondary:* To identify and quantify…
ID
Source
Brief title
Condition
- Chromosomal abnormalities, gene alterations and gene variants
Synonym
Research involving
Sponsors and support
Intervention
Outcome measures
Primary outcome
Plasma levels of RO5186582 and its metabolites as appropriate, will be
determined. Plasma concentrations will be determined by a validated assay. The
stable isotope [13C]-labelled RO5186582 and RO5271857 will be measured in
plasma by a specific LC/MS-MS method.
Radioactivity concentrations in blood, plasma, urine and feces will be
determined by conventional methods and AMS as appropriate.
Secondary outcome
adverse events, vital signs, ECG-parameters, laboratory parameters, physical
examination, C-SSRS and Leeds Sleep Questionnaire
Background summary
RO5186582 is a new investigational compound that may eventually be used for the
treatment of cognitive, functional, and/or adaptive behavioural deficits in
individuals with Down syndrome (DS) aged 6 to 30 years. The studymedication
influences a receptor protein (GABAA *5) involved in the learning functions.
Study objective
Primary:
* To determine the absolute oral bioavailability and further characterize the
PK of RO5186582 using a stable isotope technique.
* To explore the routes and rates of elimination of [14C] labelled RO5186582.
Secondary:
* To identify and quantify circulating and excreted metabolites of RO516582 in
plasma and fecal samples based on radioactive metabolic profiling, using
conventional analytical methods and AMS if necessary.
* To investigate the safety and tolerability of 28 days of twice-daily dosing
of RO5186582
Study design
open label with [14C] and [13C] labeled study medication
Intervention
Oral Treatments:
Days 1-27
160mg RO5186852
orally as 4x40mg tablets twice daily (Day 1: evening only)
Day 1 morning only
160mg RO5186852 single dose
as capsule [14C]-labelled RO5186582 containing 2.80MBq
Intravenous Treatments:
Day 1 and Day 28
0.1mg [13C]-labelled RO5186852
as solution by constant rate infusion over 15 minutes
All these doses will be administered within 10 minutes after completion of a
standard meal or snack.
Study burden and risks
During this study several assessments will be performed that may be considered
a burden.
Falcon Way 6
Welwyn Garden City AL7 1TW
GB
Falcon Way 6
Welwyn Garden City AL7 1TW
GB
Listed location countries
Age
Inclusion criteria
healthy male
30-55 yrs, inclusive
BMI: 18.0-30.0 kg/m2, inclusive
non-smoking or smoking < 5 cigarettes/day
Exclusion criteria
Suffering from hepatitis B, hepatitis C, cancer or HIV/AIDS. In case of participation in another drug study within 90 days before the start of this study or being a blood donor within 60 days from the start of the study. In case of donating more than 1.5 liters of blood in the 10 months prior 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 | EUCTR2012-001434-34-NL |
| CCMO | NL41103.056.12 |