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A Trial to Evaluate the Efficacy and Safety of PQ912 in Patients With Early AD

Phase 2
Terminated
Conditions
Alzheimer Disease
Interventions
Other: Placebo
Registration Number
NCT03919162
Lead Sponsor
Vivoryon Therapeutics N.V.
Brief Summary

This is a phase 2A multi-center, randomized, double blind, placebo-controlled, parallel group study of varoglutamstat, with a stage gate to phase 2B.

In phase 2A there will be adaptive dosing evaluation of three dose levels with exposure to varoglutamstat or placebo for a minimum of 24 weeks, with preliminary evaluation of both cognitive function and pharmacodynamic changes on EEG spectral analysis in approximately 180 participants.

In the event that the stage gate for phase 2B is reached, then phase 2B will assesses efficacy and longer-term safety in a larger study group, i.e., 414.

Detailed Description

The goal of this study is to advance a first-in-class, new small molecule treatment for early Alzheimer's disease (AD). Varoglutamstat (PQ912) is an oral, twice daily medication that addresses a novel and significantly differentiated amyloid target: N-terminal post-translationally modified Ab (pGlu-Ab), a particularly toxic subspecies of amyloid beta (Ab). This study will further evaluate whether varoglutamstat's mechanism of action can result in a measurable therapeutic effect on cognition, function and relevant pharmacodynamic and biological markers in early AD.

The study is a phase 2A multi-center, randomized, double-blind, parallel group trial, with a stage gate to phase 2B. Phase 2A will determine the highest dose that is both safe and well tolerated. During this phase, there is an adaptive dosing evaluation, using a well-defined safety stopping boundary, of three dose levels with exposure to varoglutamstat or placebo for a minimum of 24 weeks to help determine which dose will be carried forward in phase 2B. A sequential dose design will be employed in phase 2A where each of three dose cohorts are randomized equally to placebo or varoglutamstat and treated for at least 8 weeks at the originally assigned full dose. Participants will be randomized 1:1 to varoglutamstat or placebo, and stratified between mild AD and MCI, as well as by site.

Phase 2A also includes preliminary evaluation of both cognitive function and pharmacodynamics changes on electroencephalogram (EEG) spectral analysis.

In the event that the stage gate for phase 2B is reached from data in this phase 2A study, then phase 2B will assess the longer-term efficacy and safety of varoglutamstat in a larger study group, using the highest dose selected in phase 2A. In phase 2B, a composite cognitive and functional measure as well as PD biomarkers will be used to evaluate efficacy during the extended treatment period.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
112
Inclusion Criteria
  • Age 50-89 (inclusive) at screening
  • Diagnosed as having Mild Cognitive Impairment (MCI) due to Alzheimer's disease (AD) or Mild probable AD according to workgroups of the Diagnostic Guidelines of the National Institute on Aging and Alzheimer's Association (NIA-AA)
  • Mini-Mental State Examination (MMSE) score 20-30 inclusive at screening
  • Montreal Cognitive Assessment score (MoCA) < 26 at screening
  • Clinical Dementia Rating global score 0.5 or 1 with memory score of > 0.5 at screening
  • Positive CSF AD biomarker signature
  • A brain MRI scan within 6 months of screening consistent with a diagnosis of Alzheimer's disease
  • Participants must have a study partner who has frequent interaction with them (approximately >3-4 times per week), will be present for all clinic visits, and can assist in compliance with study procedures.

Key

Exclusion Criteria
  • • Significant neurodegenerative diseases and causes of dementia, other than AD, including Parkinson's disease and Huntington's disease, vascular dementia, CJD (Creutzfeldt-Jakob disease), LBD (Lewy Body dementia), PSP (Progressive Supranuclear Palsy), AIDS (Acquired Immunodeficiency Syndrome), or NPH (normal pressure hydrocephalus)
  • Meeting Diagnostic Criteria for Possible AD according to workgroups of the Diagnostic Guidelines of the NIA-AA
  • Hepatic impairment defined as Child-Pugh class A or more severe liver impairment
  • History of moderate or severe skin reactions to medications or current moderate or severe disease of the skin and subcutaneous tissues
  • History of a major depressive episode within the past 6 months of screening
  • History of diagnosis of schizophrenia
  • History of uncontrolled bipolar disorder within past five years of screening
  • History of seizures within past two years of screening
  • Contraindication to lumbar puncture and MRI
  • Participation in another clinical trial for an investigational agent and having taken at least one dose of study drug, unless confirmed as having been on placebo, within 90 days prior to the baseline visit. The end of a previous investigational trial is defined as the date of the last dose of an investigational agent.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
PlaceboPlacebo-
300 mgPQ912First 4 weeks 150 mg BID, week 5-24 300 mg BID
150 mgPQ91224 weeks on 150 mg BID
600 mgPQ912First 4 weeks 150 mg BID, week 5-8 300 mg BID, week 9-24 600 mg BID
Primary Outcome Measures
NameTimeMethod
2A Primary PK: derived mean values of varoglutamstat levels and corresponding calculated target occupancy (TO)24 weeks

The pharmacokinetics (PK) endpoints in Phase 2A are the derived mean values of varoglutamstat levels in plasma and the correspondingcalculated TO in CSF, for each dose.

2B Primary efficacy: The within-participant change from baseline to week 72 in the Clinical Dementia Rating Scale Sum of Boxes (CDR-SB) score, compared between active arm and placebo.72 weeks

The CDR-SB evaluates cognition and everyday functioning incorporating both informant input and direct assessment of performance. It is scored on a five-point scale a five point scale with following five possible scores: 0 = Normal 0.5 = Very Mild Dementia

1. = Mild Dementia

2. = Moderate Dementia

3. = Severe Dementia

2A Primary efficacy: The within-participant change from baseline to week 24 in the composite sum of standardized scores from the ADNI Battery Composite (ABC, 9-item) compared between active arm and placebo.24 weeks

The ABC is a set of ADNI neuropsychological test measures, including: Category Fluency (Animals and Vegetables), Trail Making A and B, Digit Symbol Substitution, Boston Naming Test, Rey's Auditory and Verbal Learning Test (RAVLT, Immediate and Delayed), Digit Span Forward and Backward.

2A Primary efficacy:The within-participant change from baseline to week 24 in quantitative EEG (global relative theta wave power)24 weeks

The within-participant change frombaseline to week 24 of the global relative theta wave power (4-8 Hz) compared between active arm and placebo.

2A Primary safety: proportion of participants who experience any adverse event of interest (AE-I).24 weeks

The primary endpoint in phase 2A is the proportion of participants, for each dose, who experience any adverse event of interest (AE-I) during the safety reporting period, from first dose to completion of 8 weeks at the full originally assigned dose.

Secondary Outcome Measures
NameTimeMethod
Key secondary efficacy: CFC2, a cognitive-functional composite72 weeks

The key secondary objective in phase 2B is to evaluate the efficacy of PQ912 as measured by CFC2, a cognitive-functional composite, over a 72-week treatment period.

Trial Locations

Locations (22)

Northwestern University Feinberg School of Medicine

🇺🇸

Chicago, Illinois, United States

Ohio State University

🇺🇸

Columbus, Ohio, United States

The Neuron Clinic

🇺🇸

Chula Vista, California, United States

Barrow Neurological Institute

🇺🇸

Phoenix, Arizona, United States

OHSU Neurology Clinic

🇺🇸

Portland, Oregon, United States

Banner Sun Health Research Institute

🇺🇸

Sun City, Arizona, United States

UCSD Alzheimer's Disease Research Center

🇺🇸

La Jolla, California, United States

Northern Light Acadia Hospital

🇺🇸

Bangor, Maine, United States

SUNY Upstate Medical University

🇺🇸

Syracuse, New York, United States

UT Health San Antonio

🇺🇸

San Antonio, Texas, United States

USF Health Byrd Alzheimer's Center and Research Institute

🇺🇸

Tampa, Florida, United States

Emory University

🇺🇸

Atlanta, Georgia, United States

University of California

🇺🇸

Irvine, California, United States

PCND Neurology

🇺🇸

Poway, California, United States

Cedars-Sinai Center

🇺🇸

Los Angeles, California, United States

NYU Langone Health Tisch Hospital

🇺🇸

New York, New York, United States

Abington Neurological Associates

🇺🇸

Abington, Pennsylvania, United States

Georgetown University Medical Center

🇺🇸

Washington, District of Columbia, United States

Lowcountry Center for Veterans Research (LCVR)

🇺🇸

Charleston, South Carolina, United States

The University of Kentucky Sanders-Brown Center on Aging

🇺🇸

Lexington, Kentucky, United States

The University of Iowa Carver College of Medicine

🇺🇸

Iowa City, Iowa, United States

Rhode Island Hospital

🇺🇸

Providence, Rhode Island, United States

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