A Human Proof of Concept Study for [11C]-RO5011232 as Radiotracer and Study of the Binding of RO4917523 to Human mGlu5 Brain Receptor at Steady-State in Healthy Volunteers

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT01483469
Recruitment Status : Completed
First Posted : December 1, 2011
Last Update Posted : November 2, 2016
Information provided by (Responsible Party):
Hoffmann-La Roche

Brief Summary:
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.

Condition or disease Intervention/treatment Phase
Healthy Volunteer Drug: RO4917523 Drug: RO5011232 Phase 1

Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 56 participants
Allocation: Non-Randomized
Intervention Model: Parallel Assignment
Masking: None (Open Label)
Official Title: Human Proof of Concept Positron Emission Tomography Study to Investigate [11C]-RO5011232 as a Radiotracer for Brain mGlu5 Receptor Occupancy and to Investigate the Binding of RO4917523 to Human mGlu5 Brain Receptor at Steady-state.
Study Start Date : December 2011
Actual Primary Completion Date : October 2013
Actual Study Completion Date : October 2013

Arm Intervention/treatment
Active Comparator: Concept Proof Drug: RO5011232
[11C]-RO5011232 intravenously
Experimental: Receptor Occupancy Drug: RO4917523
orally daily, 14 days
Drug: RO5011232
[11C]-RO5011232 intravenously

Primary Outcome Measures :
  1. Part I: mGlu5 receptor binding of [11C]-RO5011232 radiotracer in human brain, assessed by positron emission tomography (PET) [ Time Frame: approximately 6 months ]
  2. Part II: Dosimetry/radiation safety of [11C]-RO5011232 assessments by whole body PET scan [ Time Frame: approximately 6 months ]
  3. Part III: Measurement of test-retest precision of PET images of regions of interest in the human brain [ Time Frame: approximately 6 months ]
  4. Part IV: Correlation between RO4917523 plasma concentration and R04917523 binding to mGlu5 receptor in brain [ Time Frame: approximately 6 months ]

Secondary Outcome Measures :
  1. Safety of [11C]-RO5011232 administered intravenously at microdose level: Incidence of adverse events [ Time Frame: approximately 6 months ]
  2. Part IV: In vitro binding potential (reference region with no specific binding of radiotracer) assessed by PET [ Time Frame: approximately 6 months ]
  3. Part IV: Safety of 14-day treatment with RO4917523: Incidence of adverse events [ Time Frame: approximately 6 months ]

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 65 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Healthy male and female volunteers as determined by medical history, physical examination, 12-lead ECG, and routine clinical laboratory measurements
  • Age 18 to 65 years inclusive
  • Body mass index (BMI) between 18 to30 kg/m2 inclusive and body weight at least 50 kg
  • Appropriate body size (less than 195 cm [6 feet and 5 inches]) in order to accommodate the whole body scanning

Exclusion Criteria:

  • History of or presence of clinically significant psychiatric condition, as evaluated by a psychiatrist before enrolment
  • History of head trauma with prolonged loss of consciousness (>10 minutes) or any neurological condition or a history of migraine headaches
  • Contraindications to MRI procedures (Part I, III and IV)
  • Subjects suffering from claustrophobia or who would be unable to undergo magnetic resonance imaging (MRI) or PET scanning
  • Positive pregnancy test at screening or on any day preceding a PET scan
  • Lactating women
  • Positive for hepatitis B, hepatitis C or HIV infection
  • Any history of alcohol or drug abuse within the last 6 months
  • Regular smoker or nicotine user (>10 cigarettes per day)
  • Participation in an investigational drug or device study within three months prior to screening

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT01483469

United States, Maryland
Baltimore, Maryland, United States, 21224
Baltimore, Maryland, United States, 21225
Sponsors and Collaborators
Hoffmann-La Roche
Study Director: Clinical Trials Hoffmann-La Roche

Responsible Party: Hoffmann-La Roche Identifier: NCT01483469     History of Changes
Other Study ID Numbers: BP27890
First Posted: December 1, 2011    Key Record Dates
Last Update Posted: November 2, 2016
Last Verified: November 2016