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CompletedNCT03440112GABA-AUpdated Jan 10, 2023Results posted

Modulation of GABA-A Receptors in Parkinson Disease-Transdermal Flumazenil Arm

A Phase 1/2 interventional study of Clarithromycin (Not used as of 4/2020) and Placebo (Not used as of 4/2020) in Parkinson Disease, sponsored by Nicolaas Bohnen, MD, PhD. Completed at 1 site in United States. Open to participants aged 50 Years and older. Per ClinicalTrials.gov, last updated 2023-01-10.

Sponsored by Nicolaas Bohnen, MD, PhD · Phase 1/2, Interventional, and Other

Phase
Phase 1/2
Study type
Interventional
Enrollment
34
Allocation
Randomized
Ages
50 Years and older
Sex
All
01

Study summary

The arm of this study evaluates possible GABA-A receptor target engagement effects of the FDA-approved medication, transdermal flumazenil (added 4/2020, replaced clarithromycin), in the setting of Parkinson's disease. Half of the subjects will receive transdermal flumazenil for 7-10 days, and half will receive a placebo. [11C]Flumazenil GABA-A receptor PET imaging will be used to assess target engagement effects. Note [11C]Flumazenil GABA-A receptor PET was not performed as part of the transdermal flumazenil study because of a Covid pandemic research amendment.

Read the detailed description

This study focuses on neurochemical changes in the brain that occur in Parkinson's disease. In particular we will be looking a neurotransmitter called GABA. In some Parkinson's disease patients we see too much GABA activity in the brain. This target engagement study examines the target engagement effect of GABA-A receptor modulation by transdermal flumazenil (previously clarithromycin). [11C]-flumazenil Positron Emission Tomography (PET) imaging results will be used to assess for possible GABA-A receptor target engagement effects of transdermal flumazenil (previously clarithromycin). Note [11C]Flumazenil GABA-A receptor PET was not performed as part of the transdermal flumazenil study because of a Covid pandemic research amendment.

02

Conditions studied

  • Parkinson Disease

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Keywords

  • Gait
  • Balance
  • GABA
  • Transdermal flumazenil (previously Clarithromycin changed 4/2020)
  • PET Imaging
  • MRI
  • Mobility
03

Who can participate

Ages eligible
50 Years and older
Sexes eligible
All
Accepts healthy volunteers
No

Inclusion criteria

  1. Parkinson's disease (PD): PD diagnosis will follow the UK Parkinson's Disease Society Brain Bank Research Center (UKPDSBRC) clinical diagnostic criteria for PD.
  2. Hoehn and Yahr stages 2-4
  3. Absence of dementia confirmed by cognitive testing.
  4. Abnormal 11C-Dihydrotetrabenazine ([11c]-DTBZ) PET study to demonstrate nigrostriatal dopaminergic denervation

Exclusion criteria

Exclusion Criteria:

  1. PD with Dementia (PDD) or dementia with Lewy bodies (DLB).
  2. Other disorders which may resemble PD, such as vascu¬lar dementia, normal pressure hydrocephalus, multiple system atrophy, corticobasal ganglionic dege¬neration, or toxic causes of parkinsonism. Prototypical cases have distincti¬ve clinical profiles, like early and severe dysautonomia or appendicular apraxia, which may differentiate them from idiopathic PD. The use of the UKPDSBRC clinical diagnostic criteria for PD will mitigate the inclusion of subjects with atypical parkinsonism.
  3. Subjects currently on benzodiazepine, GABAB-ergic medications (baclofen, tizanidine), modafinil, neuroleptic, anticholinergic (trihexyphenidyl, benztropine), or cholinesterase inhibitor drugs.
  4. Evidence of a mass lesion on structural brain imaging (MRI).
  5. Participants in whom MRI is contraindicated including, but not limited to, those with a pacemaker, presence of metallic fragments near the eyes or spinal cord, chest, or cochlear implant.
  6. Severe claustrophobia precluding MR or PET imaging.
  7. Subjects limited by participation in research procedures involving ionizing radiation.
  8. Pregnancy (urine or serum pregnancy test within 48 hours of each PET session) or breastfeeding.
  9. History of seizures
  10. Significant anxiety or history of panic disorder.
  11. History of recent suicide attempt or overdose of tricyclic antidepressants or other medications.
  12. History of transient ischemic attack (TIA) or stroke within the last year.
  13. History of systemic lupus erythematosis.
  14. Abnormal liver enzymes (AST or ALT) > 3 times upper limit of normal.
  15. History of atrial fibrillation.
  16. History of retinal branch artery occlusion.
  17. Active dermatitis inner forearms.
  18. Any other medical history determined by investigators to preclude safe participation.

Additional Exclusion Criteria for Flumazenil sub-studies:

  1. Allergy to flumazenil
  2. Significant liver disease
  3. History of alcohol or other substance abuse within past two years.
  4. Subjects currently taking benzodiazepines
04

Study design

Phase
Phase 1 / Phase 2
Primary purpose
Other
Allocation
Randomized
Intervention model
Parallel assignment
Masking
Triple (Participant, Care provider, Investigator)
Enrollment
34 participants (actual)

Study arms

  • Active comparator
    Clarithromycin (Not used anymore as of 4/2020; study aborted)

    Clarithromycin 250mg (1 capsule) will be taken orally twice a day for 3 days and if tolerated will be increased to 500mg (2 capsules) orally twice a day for 4-6 days.

    Drug: Clarithromycin (Not used as of 4/2020)

  • Placebo comparator
    Placebo (Not used anymore as of 4/2020; study aborted)

    Placebo will be taken exactly as the clarithromycin arm: 1 capsule orally twice a day for 3 days and if tolerated will be increased to 2 capsules orally twice a day for 4-6 days.

    Drug: Placebo (Not used as of 4/2020)

  • Active comparator
    Transdermal flumazenil (added 4/2020 as safer alternative for clarithromycin)

    Added in April 2020. Subjects will take 18mg transdermal application every 3-4 hrs dispensed as 3 dispenser bottle clicks of 0.25 ml each, while awake for 3 days then if no side-effects subjects will increase to 36mg transdermal application every 3-4 hrs dispensed as 6 dispenser bottle clicks of 0.25 ml each, while awake.

    Drug: Transdermal flumazenil (Added 4/2020)

  • Placebo comparator
    Placebo cream (added 4/2020)

    Added in April 2020. Placebo will be taken exactly as the transdermal flumazenil arm: Subjects will take 18mg transdermal application every 3-4 hrs dispensed as 3 dispenser bottle clicks of 0.25 ml each, while awake for 3 days then if no side-effects subjects will increase to 36mg transdermal application every 3-4 hrs dispensed as 6 dispenser bottle clicks of 0.25 ml each, while awake.

    Drug: Placebo (Added 4/2020)

Interventions

  • DrugClarithromycin (Not used as of 4/2020)

    Clarithromycin (generic) capsule 250mg each

    Also known as: Biaxin

  • DrugPlacebo (Not used as of 4/2020)

    Lactose in a gel capsule

  • DrugTransdermal flumazenil (Added 4/2020)

    Transdermal flumazenil 24mg/mL

  • DrugPlacebo (Added 4/2020)

    Transdermal placebo

    Also known as: Placebo cream

05

What researchers measure

Primary outcomes

  1. Change in Quantitative Biomechanics 1 (Clinical Motor Ratings MDS-UPDRS)

    We will use the total Movement Disorder Society - Unified Parkinson's Disease Rating Scale (MDS-UPDRS) Part III - motor scale rating scores to assess motor function. Scale from 0-132, higher scores indicate worse motor outcomes. Outcome measure was collected during dopaminergic medication ON state.

    Time frame: Day 1 (before treatment administration), day 7 (after 7 days of treatment), and day 14 (7 days of treatment discontinuation).

Secondary outcomes

  1. Change in Quantitative Biomechanics 2 (MiniBESTest Dynamic Balance Scale Sensory Subscore)

    MiniBEST sensory subscore measures an individual's ability to maintain balance under conditions of sensory constrain and unstable/inclined standing surface. It is is computed as a sum of MiniBEST items 7, 8, and 9.The score ranges from 0 to 6, with 0 indicating inability to balance under all of the condition, and 6 indicating no difficulty in maintaining balance under any of the conditions (lower score indicates worse balance). Outcome measure was collected during dopaminergic medication ON state.

    Time frame: Day 1 (before treatment administration), day 7 (after 7 days of treatment), and day 14 (7 days of treatment discontinuation).

06

Results

Posted Jan 10, 2023
Limitations and caveats
Our participants were predominantly male, which is often the case with Parkinson's disease (PD) patient population since PD is known to affect males at a greater rate. This means that our findings may not generalize as well to population of female PD patients.

Participant flow

Participant flow — Overall Study
MilestoneTransdermal Flumazenil (Active)Placebo CreamOral Clarithromycin (Dropped in 04/2020)
Started11113
Completed11113
Not completed000

Outcome measures

PrimaryChange in Quantitative Biomechanics 1 (Clinical Motor Ratings MDS-UPDRS)

We will use the total Movement Disorder Society - Unified Parkinson's Disease Rating Scale (MDS-UPDRS) Part III - motor scale rating scores to assess motor function. Scale from 0-132, higher scores indicate worse motor outcomes. Outcome measure was collected during dopaminergic medication ON state.

Time frame:
Day 1 (before treatment administration), day 7 (after 7 days of treatment), and day 14 (7 days of treatment discontinuation).
Reported as:
Median · units on a scale
Change in Quantitative Biomechanics 1 (Clinical Motor Ratings MDS-UPDRS)
units on a scaleTransdermal Flumazenil (Active)Placebo CreamClarithromycin (Active or Placebo)
Day 138 (27.5 to 44.5)34 (30 to 47)28 (25.50 to 33.00)
Day 736.75 (29.75 to 52)31.50 (25.375 to 43.375)23.50 (21.25 to 26.75)
Day 1432.75 (26.375 to 47.375)34 (29.5 to 40)22 (19.5 to 23.0)
Statistical analysis
  • Transdermal Flumazenil (Active) vs Placebo Cream · Mixed Models Analysis · p = 0.391 · Chi-squared: 3.0039
SecondaryChange in Quantitative Biomechanics 2 (MiniBESTest Dynamic Balance Scale Sensory Subscore)

MiniBEST sensory subscore measures an individual's ability to maintain balance under conditions of sensory constrain and unstable/inclined standing surface. It is is computed as a sum of MiniBEST items 7, 8, and 9.The score ranges from 0 to 6, with 0 indicating inability to balance under all of the condition, and 6 indicating no difficulty in maintaining balance under any of the conditions (lower score indicates worse balance). Outcome measure was collected during dopaminergic medication ON state.

Time frame:
Day 1 (before treatment administration), day 7 (after 7 days of treatment), and day 14 (7 days of treatment discontinuation).
Reported as:
Mean · units on a scale
Change in Quantitative Biomechanics 2 (MiniBESTest Dynamic Balance Scale Sensory Subscore)
units on a scaleTransdermal Flumazenil (Active)Placebo CreamClarithromycin (Active or Placebo)
Day 15.54 ± 0.696 ± 06 ± 0
Day 75.82 ± 0.406 ± 05.67 ± 0.58
Day 146 ± 05.82 ± 0.606 ± 0
Statistical analysis
  • Transdermal Flumazenil (Active) vs Placebo Cream · Mixed Models Analysis · p = 0.02351 · Chi-squared: 9.4836

Adverse events

Collected over Up to 14 days.. Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Transdermal Flumazenil (Active)0/11 (0%)0/11 (0%)0/11 (0%)
Placebo Cream0/11 (0%)0/11 (0%)0/11 (0%)
Oral Clarithromycin (Dropped in 04/2020)0/3 (0%)0/3 (0%)0/3 (0%)

Baseline characteristics

Parkinson's disease patients age 50 years or older. Some, but not all, participants in the Clarithromycin arm were randomized, and only few completed study procedures because of premature termination of the trial due to an FDA safety risk warning of Clarithromycin, precluding any meaningful analysis. Consequently, this study arm was replaced by the transdermal Flumazenil arm.

Age, Continuous
Age, Continuous(years)Transdermal Flumazenil (Active)Placebo CreamOral Clarithromycin (Active or Placebo)Total
Mean72.09 ± 4.4170.27 ± 3.8066.33 ± 5.1370.6 ± 4.43
Sex: Female, Male
Sex: Female, Male(Participants)Transdermal Flumazenil (Active)Placebo CreamOral Clarithromycin (Active or Placebo)Total
Female3115
Male810220
Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)Transdermal Flumazenil (Active)Placebo CreamOral Clarithromycin (Active or Placebo)Total
Hispanic or Latino0000
Not Hispanic or Latino1111325
Unknown or Not Reported0000
Race (NIH/OMB)
Race (NIH/OMB)(Participants)Transdermal Flumazenil (Active)Placebo CreamOral Clarithromycin (Active or Placebo)Total
American Indian or Alaska Native0000
Asian0000
Native Hawaiian or Other Pacific Islander0000
Black or African American0000
White1111325
More than one race0000
Unknown or Not Reported0000
Region of Enrollment
Region of Enrollment(participants)Transdermal Flumazenil (Active)Placebo CreamOral Clarithromycin (Active or Placebo)Total
United States1111325
MiniBEST Sensory Subscore
MiniBEST Sensory Subscore(units on a scale)Transdermal Flumazenil (Active)Placebo CreamOral Clarithromycin (Active or Placebo)Total
Mean5.27 ± 1.15.81 ± 0.406 ± 05.6 ± 0.82
Movement Disorder Society - Unified Parkinson's Disease Rating Scale (MDS-UPDRS) Part III
Movement Disorder Society - Unified Parkinson's Disease Rating Scale (MDS-UPDRS) Part III(units on a scale)Transdermal Flumazenil (Active)Placebo CreamOral Clarithromycin (Active or Placebo)Total
Median45 (38.5 to 57)41.5 (37 to 49.25)40.50 (33.00 to 45.25)43.5 (36.00 to 51.50)
07

Study locations

1 site
  • University of Michigan Health System Functional Neuroimaging, Cognitive and Mobility Laboratory
    Ann Arbor, Michigan 48106, United States
08

References and documents

Study documents

  • Study protocol · Dec 14, 2020
  • Statistical analysis plan · Sep 12, 2022

Documents are hosted by the registry — open the source record to download them.

Individual participant data

Plan to share: No

09

Registry details

Key details

Study ID
NCT03440112
Lead sponsor
Nicolaas Bohnen, MD, PhD
Collaborators
National Institute of Neurological Disorders and Stroke (NINDS)
Responsible party
Nicolaas Bohnen, MD, PhD (Professor of Radiology and Neurology, University of Michigan) — Sponsor-investigator
First posted
Feb 20, 2018
Start date
Jan 29, 2018
Primary completion
Dec 8, 2021
Completion
Dec 8, 2021
Results posted
Jan 10, 2023
Last update
Jan 10, 2023

Study contacts

Nicolaas I Bohnen, MD, PhD
principal investigator · University of Michigan

Oversight

Data monitoring committee
Yes
FDA-regulated drug
Yes
FDA-regulated device
No
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