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Effect of Neflamapimod on Brain Inflammation in Alzheimer's Disease Patients

Phase 2
Completed
Conditions
Alzheimer Disease
Interventions
Drug: placebo
Registration Number
NCT03435861
Lead Sponsor
University Hospital, Toulouse
Brief Summary

For this project, neflamapimod and placebo will be provided free of charge by the EIP company (www.eippharma.com). Neflamapimod is currently tested in 2 clinical trials in AD, one in Europe (The Netherlands) and one in the USA (clinical trials.gov/VX-745). The company commenced in May 2015 dosing in two phase 2a clinical studies in patients with Early AD: one in the Netherlands that is focused on PET amyloid imaging as the primary biomarker of drug effect, and one in the US (California) that is focused on Cerebrospinal fluid (CSF) evaluation to determine CSF drug concentrations and effects on inflammatory markers and disease biomarkers. Pharmacokinetic evaluation in these patients has demonstrated blood drug concentration levels in the predicted therapeutic range; and importantly, the data from the US study demonstrate that the drug achieves target drug concentrations in CSF, thus confirming the drug robustly enters the brain in humans.

The present project offers us a unique chance to test this promising drug in AD patients. The aim of the study is to focus on PET neuroinflammation imaging as the primary biomarker of this drug effect. The chosen biomarker for imaging neuroinflammation in patients is \[1 8F\]-DPA714.

Detailed Description

The present project is an intervention proof of concept study to test the efficacy of neflamapimod in a population of AD patients at an early stage.

To track the impact of this drug in patients, the investigators will use an innovative radiotracer, \[18F\]DPA-714, as a promising ligand of microglial activation targeting the translocator protein (TSPO), specific of microglial activation. The use of \[18F\]DPA-714 will allow to monitor the evolution of neuroinflammation in patients as a function of treatment. The main objective will be to compare the level of inflammation using the \[18F\]DPA-714 in neflamapimod and placebo groups after 12 weeks of treatment. Blood and cerebrospinal fluid (CSF) samples and magnetic resonance imaging (MRI) will also be collected to assess inflammation markers and brain structure respectively in these patients.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
34
Inclusion Criteria
  • A group of 40 AD patients at an early stage (prodromal) will be recruited. Patient's recruitment will follow the most recent research criteria for AD in its "typical form" (Dubois, Feldman et al. 2014):

    • Age 50 - 90 (inclusive)
    • Willing and able to provide informed consent
    • Objective memory impairment corroborated by level of performance on a standardized memory test (Free and Cued Selective Reminding test, (Grober, Hall et al. 2008)) < -1.5 DS according to established norms and
    • Documented cerebral amyloidopathy using CSF analysis or PET amyloid imaging and
    • Early stage of the disease (Mini Mental State Examination > 20) (Folstein, Robins et al. 1983).
Exclusion Criteria
  • • Evidence of neurodegenerative disease other than AD

    • Inability for any reason to undergo MRI scans (e.g. pacemaker). Patients who require sedation for screening procedures such as MRI may receive a short-acting sedative.
    • Psychiatric disorder that would compromise ability to comply with study requirements
    • History of cancer within the last 5 years, except basal cell carcinoma, non-squamous skin carcinoma, prostate cancer or carcinoma in situ with no significant progression over the past 2 years
    • Significant cardiovascular, pulmonary, renal, liver, infectious disease, immune disorder or metabolic/endocrine disorders or other disease that would preclude treatment with p38 MAP kinase inhibitor and/or assessment of drug safety and efficacy
    • Recent (<60 days) changes to AD medications prescribed for cognitive reasons or with the potential to impact cognition
    • Psychotropic drugs taken within 1 month. Anticoagulant drugs taken within 1 week.
    • Participation in a study of an investigational drug less than 6 months or 5 half-lives of the investigational drug, whichever is longer, before enrollment in the study
    • Male subjects with female partner of child-bearing potential who are unwilling or unable to adhere to contraception requirements
    • Female subjects who have not reached menopause or have not had a hysterectomy or bilateral oophorectomy/salpingoophorectomy
    • Positive urine or serum pregnancy test or plans desires to become pregnant during the course of the trial
    • History of alcohol and/or illicit drug abuse within 6 months.
    • Infection with hepatitis A, B or C or HIV.
    • Any factor deemed by the investigator to be likely to interfere with study conduction

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
VX-745VX-745In the present study, VX-745 will be given at the dosage of 40 mg twice a day (1 tab. of 40 mg, twice), orally for 12 weeks
placeboplaceboIn the present study, placebo will be given twice a day (1 tab. , twice), orally for 12 weeks
Primary Outcome Measures
NameTimeMethod
brain inflammation assessed by [18F]-DPA714, Standard Uptake Value (SUV)3 month

To track the impact of this drug in patients, investigators will use an innovative radiotracer, \[18F\]DPA-714, as a promising ligand of microglial activation targeting the translocator protein (TSPO), specific of microglial activation. The use of \[18F\]DPA-714 will allow us to monitor the evolution of neuroinflammation in patients as a function of treatment. the main objective will be to compare the level of inflammation using the \[18F\]DPA-714 in neflamapimod and placebo.

Regional cortical DPA-714 mean SUV will be measured in each subject using a Matlab (The MathWorks®) script. Mean global SUVs will be calculated

brain inflammation assessed by [18F]-DPA714, Standard Uptake Value (SUV) 23 month

SUVs in the five lobes will be calculated.

brain inflammation assessed by [18F]-DPA714, Standard Uptake Value (SUV)33 month

SUVs in specific regions of interest (ROIs: orbitofrontal, anterior cingulate, posterior cingulate and precuneus) will be calculated.

Secondary Outcome Measures
NameTimeMethod
Blood and CSF biomarkers of inflammation 223 month

IL-1b

Blood and CSF biomarkers of inflammation 233 month

IL-12

Blood and CSF biomarkers of inflammation 263 month

IL-27,

Blood and CSF biomarkers of inflammation 203 month

cells count

Neuropsychological assessment to assess the following cognitive functions 1:3 month

Memory: Rey Figure

Neuropsychological assessment to assess the following cognitive functions 2:3 month

Memory: DMS 48,

Neuropsychological assessment to assess the following cognitive functions 2.2:3 month

Language: FAS fluencies,

Neuropsychological assessment to assess the following cognitive functions 3:3 month

o Attention and executive functions: D2

Blood and CSF biomarkers of inflammation 213 month

TNFa

Neuropsychological assessment to assess the following cognitive functions 1.1:3 month

Language: confrontation naming (Gremots),

Neuropsychological assessment to assess the following cognitive functions 4:3 month

o Attention and executive functions: TEA

Neuropsychological assessment to assess the following cognitive functions 5:3 month

o Attention and executive functions: SDMT WAIS

Blood and CSF biomarkers of inflammation13 month

ApoE phenotype

Blood and CSF biomarkers of inflammation 23 month

TSPO phenotype,

Blood and CSF biomarkers of inflammation 33 month

TNFa,

Blood and CSF biomarkers of inflammation 43 month

IL-1b,

Blood and CSF biomarkers of inflammation 53 month

IFNg

Blood and CSF biomarkers of inflammation 63 month

IL-12

Blood and CSF biomarkers of inflammation 73 month

IFNa/b

Blood and CSF biomarkers of inflammation 83 month

IL-10

Blood and CSF biomarkers of inflammation 93 month

IL-6

Blood and CSF biomarkers of inflammation 103 month

IL-8,

Blood and CSF biomarkers of inflammation 113 month

MCP-1,

Blood and CSF biomarkers of inflammation 123 month

GM-CSF

Blood and CSF biomarkers of inflammation 133 month

IL-27

Blood and CSF biomarkers of inflammation 143 month

chimiokines receptors,

Blood and CSF biomarkers of inflammation 153 month

PD-1,

Blood and CSF biomarkers of inflammation 163 month

CD14/16

Blood and CSF biomarkers of inflammation 183 month

abéta42,

Blood and CSF biomarkers of inflammation 253 month

GM-CSF

Blood and CSF biomarkers of inflammation 173 month

p-tau,

Blood and CSF biomarkers of inflammation 193 month

Abeta40,

Blood and CSF biomarkers of inflammation 243 month

MCP-1

Blood and CSF biomarkers of inflammation 273 month

PD-1

Blood and CSF biomarkers of inflammation 283 month

CD14/16

Trial Locations

Locations (1)

CHU Toulouse

🇫🇷

Toulouse, France

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