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@ARTICLE{Kutzsche:1043479,
author = {Kutzsche, Janine and Cosma, Nicoleta Carmen and Kauselmann,
Gunther and Fenski, Friederike and Bieniek, Christine and
Bujnicki, Tuyen and Pils, Marlene and Bannach, Oliver and
Willbold, Dieter and Peters, Oliver},
title = {{O}ral {PRI}-002 treatment in patients with {MCI} or mild
{AD}: a randomized, double-blind phase 1b trial},
journal = {Nature Communications},
volume = {16},
number = {1},
issn = {2041-1723},
address = {[London]},
publisher = {Springer Nature},
reportid = {FZJ-2025-02882},
pages = {4180},
year = {2025},
abstract = {Self-replicating amyloid beta (Aβ) oligomers are
considered as one of the major drivers for disrupted
synaptic function and plasticity, leading to impaired
neuronal viability and progression of Alzheimer’s disease
(AD). Here, we investigated the safety, tolerability and
pharmacokinetics of the anti-oligomeric peptide PRI-002,
which was developed to disassemble toxic Aβ oligomers into
non-toxic monomers. In a randomized, double-blind,
single-center phase 1b trial, 20 patients aged between 50
and 80 years, with mild neurocognitive impairment (MCI) or
mild dementia due to AD were recruited. Eligible patients
were randomly assigned (1:1) to receive 300 mg PRI-002
once daily (q.d.) or placebo for 28 days. During treatment,
study visits were performed on baseline (Day 1), Day 14, Day
28 and an additional follow-up visit on Day 56. Safety
assessments were carried out at all visits to determine the
primary endpoints. On Day 7 and Day 21 additional phone
visits were carried out to assess concomitant meds and AEs.
Primary endpoints were nature, frequency, severity, and
timing of adverse and serious adverse events (AE/SAEs) and
treatment discontinuation. Furthermore, standard laboratory
values, electrocardiogram (ECG), electroencephalogram (EEG),
magnetic resonance imaging (MRI), and vital signs were
assessed. Secondary endpoints included the evaluation of
pharmacokinetic characteristics of PRI-002 in plasma and the
determination of cerebrospinal fluid (CSF) concentrations of
PRI-002. The trial is registered in EudraCT 2020-003416-27
and clinicaltrials.gov NCT04711486. In the study, 19 out of
20 patients were randomly assigned to PRI-002 (n = 9) or
placebo (n = 10) and completed the study. One patient
withdrew informed consent before randomization. All primary
endpoints were met. Overall, the study drug was well
tolerated. In total n = 16 AEs were reported in the
verum group, while n = 27 AEs were noted in the placebo
group. No SAEs were reported. No significant changes in
clinical chemistry, hematology or hematoserology were
detected. ECG, EEG and MRI revealed no changes and in detail
no ARIA were observed. Pharmacokinetic parameters were
unrelated to sex, age, and weight. Furthermore, no
significant changes were detected in p-tau, t-tau, Aβ 1-40,
Aβ 1-42 and Aβ oligomers in CSF. Patients receiving
PRI-002 performed significantly better than those receiving
placebo in the CERAD word list at Day 56 (P ≤ 0.05).
In conclusion, 28 days of treatment with 300 mg q.d.
PRI-002 was well tolerated in patients with MCI or mild
dementia due to AD.},
cin = {IBI-7},
ddc = {500},
cid = {I:(DE-Juel1)IBI-7-20200312},
pnm = {5244 - Information Processing in Neuronal Networks
(POF4-524)},
pid = {G:(DE-HGF)POF4-5244},
typ = {PUB:(DE-HGF)16},
pubmed = {40324978},
UT = {WOS:001482771100001},
doi = {10.1038/s41467-025-59295-z},
url = {https://juser.fz-juelich.de/record/1043479},
}