CompletedPhase 1

A Study of RO4602522 in Patients With Alzheimer Disease and in Healthy Volunteers

An Open-Label, Parallel Group Study to Assess the Inhibition of Brain MAO-B by RO4602522 After Repeated Dosing in Patients With Alzheimer's Disease and in Healthy Control Subjects

Lead sponsor

Hoffmann-La Roche

Asset

RO4602522

Listed sites

Recruiting sites

Enrollment

actual

Study population

Alzheimer’s disease

Key I/E criteria

•Alzheimer's disease•MMSE 17-26•Study partner/caregiver required•Healthy volunteers

Primary endpoints

•Monoamine oxidase (MAO-B) enzyme activity•Plasma concentration of RO4602522

Footprint

Where this trial recruits

Site locations as reported to ClinicalTrials.gov. Site count is not enrollment count; per-site enrollment is not available from source.

Identifiers

Registered as

Org study IDBP28253

NCT IDNCT01701089

Timeline

Milestones

Study start2012-09 (month precision)

Study first posted2012-10-04estimated

Primary completion2013-05actual (month precision)

Study completion2013-05actual (month precision)

Last update posted2016-11-02estimated

Assets

Drug assets

RO4602522

Study populations

Who this study enrolls

Alzheimer’s disease

Eligibility

Who can enroll

Minimum age50 Years

Maximum age80 Years

SexAll

Healthy volunteersAccepted

Inclusion criteria

General:

•Adults between 50-80 years of age. Females must be of non-child-bearing potential or if of child-bearing potential must use an acceptable form of contraception

•Body mass index (BMI) 18.0-32.0 kg/m2 inclusive

Healthy volunteers:

•Healthy, with no clinically relevant finding on physical examination at screening and Day -1

•No suspicion of cognitive impairment/early dementia from neuropsychological battery as judged by the investigator

•Able to participate and willing to give informed consent, and comply with the study restrictions.

Alzheimer Disease (AD) patients:

•Probable Alzheimer's disease, based on the National Institute of Neurological and Communicative

•Disorders and Stroke (NINCDS/ADRDA) and DSM-IV criteria

•Have a MMSE score at screening between 17 and 26 inclusive

•Modified Hachinski Ischemia Scale score of </=4

•A neuroimaging evaluation of the brain by MRI which supports a diagnosis of AD, with no evidence of focal disease to account for dementia or MRI exclusion criteria

•Medications taken for symptomatic treatment of AD must be maintained on a stable dosage regimen for at least 1 month before Day 1.

•Able to participate in all scheduled evaluations

•The patient has an appropriate caregiver or community dwelling with caregiver capable of accompanying subject on all visits to the center as judged by the investigator.

•In the opinion of the investigator the patient and caregiver will be compliant and have a high probability of completing the study.

•Signed and dated written informed consent obtained from the patient, co-signed by the patient's closest relatives and legally authorized representative, as required by national law for patients that are incapable of giving informed consent

Exclusion criteria

General:

•Any active disease of the gastrointestinal (GI) system, liver, or kidneys that could result in altered absorption, excess accumulation, or impaired metabolism or excretion of drugs, including a history of major upper or middle GI tract surgery or current significant chronic disease of the GI tract

•Clinically relevant abnormal history, physical findings, ECG, or laboratory values at the screening assessment

•History of cancer in the past five years, except for fully treated local basal carcinoma, or fully treated carcinoma in situ of cervix

•Any major illness occurring within 1 month prior to the screening examination or febrile illness within 5 days prior to first dose

•History of psychotropic medicine abuse

•At risk of suicide in the opinion of the investigator or having a Yes to question number 4 or 5 of the Suicidal Ideation section of the C-SSRS

•Administration of ionizing radiation or radioisotope for research, diagnostics test or therapy within 12 months prior to the present study which would exceed the local yearly radiation dose exposures for participation in research studies (except for dental x-rays, minimal plain films such as chest and ankle X-rays) or subjects who regularly work with ionizing radiation or radioactive material.

•Participation in a clinical study with an investigational drug within 3 months before screening

•Positive test for hepatitis B, hepatitis C, or HIV at screening

•Loss or donation of more than 450 mL blood in the 4 months before screening or donation of plasma within 14 days of screening.

•History of drug abuse or evidence of drug abuse in urine test performed at screening

•Current alcohol abuse, or regular intake of more than 2 units of alcohol daily

•Coffee (or tea) consumption > 5 cups per day or xanthine containing drinks >/1.5 liter/day

Healthy volunteers:

•Family history of Alzheimer's disease in 1st and 2nd degree relative under 75 years.

•Evidence or history of clinically significant neurological or psychiatric disorders.

AD Patients:

•Any neurological or psychiatric condition not specified in exceptions

•Previous immunization therapy for AD

Endpoints (4)

What's being measured

Protocol endpoints and posted registry outcome measures, grouped into outcome categories. Composite endpoints show their component event types. Standard codes (LOINC, SNOMED CT) are shown where available.

Coverage by outcome category

Safety / tolerability / PK

Other (unclassified)

Safety / tolerability / PK

2 endpoints

Primary/protocol endpoint

Pharmacokinetics: Plasma concentration of RO4602522

Time frame:Days 1, 8, 14, and between Days 15 and 34

concentration, descriptive

Secondary/protocol endpoint

Safety: incidence of adverse events

Time frame:35 days

event count, event

Other (unclassified)

2 endpoints

Primary/protocol endpoint/low confidence

Change in monoamine oxidase (MAO-B) enzyme activity as measured by in vivo positron emission tomography (PET)

Time frame:Days 1, 14, and between days 15 and 34

change from baseline, improvement

Secondary/protocol endpoint/low confidence

Reduction of 11C-L-deprenyl-D2 tracer uptake by in vivo positron emission tomography (PET)

Time frame:Days 1, 14, and between days 15 and 34

descriptive

Provenance

Sources

Trial identity, design, statusClinicalTrials.gov API v2

Snapshot dateJuly 21, 2026

Endpoint classificationDelfa ADRD endpoint taxonomy

Results tableno registry results posted yet

Trial facts come from public ClinicalTrials.gov records. Endpoint categories are Delfa's classification of those records, not a ClinicalTrials.gov field. All figures reflect the July 21, 2026 snapshot.