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This open label, non-randomized, parallel group study will evaluate [11C]-RO5011232 as radiotracer for brain mGlu5 receptor occupancy and investigate the binding of RO49917523 to human mGlu5 brain receptor at steady-state in healthy volunteers. In Parts I, II and III, positron emission tomography (PET) assessments of specific uptake of the radiotracer and whole body dosimetry will be made after intravenous injection of [11C]-RO5011232. In Part IV, subjects will receive RO4917523 orally daily for 14 days while receiving three single intravenous bolus injections of [11C]-RO5011232. The anticipated time on study treatment is up to 4 weeks.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Concept Proof | Active Comparator |
| |
| Receptor Occupancy | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| RO4917523 | Drug | orally daily, 14 days |
| |
| RO5011232 |
| Measure | Description | Time Frame |
|---|---|---|
| Part I: mGlu5 receptor binding of [11C]-RO5011232 radiotracer in human brain, assessed by positron emission tomography (PET) | approximately 6 months | |
| Part II: Dosimetry/radiation safety of [11C]-RO5011232 assessments by whole body PET scan | approximately 6 months | |
| Part III: Measurement of test-retest precision of PET images of regions of interest in the human brain | approximately 6 months | |
| Part IV: Correlation between RO4917523 plasma concentration and R04917523 binding to mGlu5 receptor in brain | approximately 6 months |
| Measure | Description | Time Frame |
|---|---|---|
| Safety of [11C]-RO5011232 administered intravenously at microdose level: Incidence of adverse events | approximately 6 months | |
| Part IV: In vitro binding potential (reference region with no specific binding of radiotracer) assessed by PET | approximately 6 months |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Clinical Trials | Hoffmann-La Roche | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Baltimore | Maryland | 21224 | United States | |||
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| Drug |
[11C]-RO5011232 intravenously |
|
| Part IV: Safety of 14-day treatment with RO4917523: Incidence of adverse events | approximately 6 months |
| Baltimore |
| Maryland |
| 21225 |
| United States |
| ID | Term |
|---|---|
| C000596770 | 2-chloro-4-(1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl)pyridine |
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