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@ARTICLE{Kutzsche:874644,
author = {Kutzsche, Janine and Jürgens, Dagmar and Willuweit, Antje
and Adermann, Knut and Fuchs, Carola and Simons, Stefanie
and Windisch, Manfred and Hümpel, Michael and Rossberg,
Wolfgang and Wolzt, Michael and Willbold, Dieter},
title = {{S}afety and pharmacokinetics of the orally available
antiprionic compound {PRI}‐002: {A} single and multiple
ascending dose phase {I} study},
journal = {Alzheimer's $\&$ dementia / Translational research $\&$
clinical interventions Translational research $\&$ clinical
interventions [...]},
volume = {6},
number = {1},
issn = {2352-8737},
address = {Amsterdam [u.a.]},
publisher = {Elsevier},
reportid = {FZJ-2020-01563},
pages = {e12001},
year = {2020},
abstract = {IntroductionPRI‐002 is an orally available anti–amyloid
beta (Aβ) prionic compound developed for direct disassembly
of toxic Aβ oligomers relevant to Alzheimer's
disease.MethodsTwo placebo‐controlled clinical phase I
trials with oral dosing of PRI‐002 were conducted in
healthy young subjects: A single ascending dose trial (4,
12, 36, 108, or 320 mg PRI‐002 or placebo) in 40
participants followed by a multiple ascending dose study
with daily 160 mg PRI‐002 for 14 days or 320 mg for 28
days in 24 participants. The main objectives were safety,
tolerability, and evaluation of pharmacokinetic (PK)
parameters.ResultsPRI‐002 was safe and well tolerated
after single and multiple oral administration up to the
highest doses. PRI‐002 was absorbed rapidly and drug
exposure increased proportional to dose. During repeated
daily administration, the drug accumulated by a factor of
about three. Steady‐state conditions were reached after 1
to 2 weeks.ConclusionsThe safety and PK results encourage
further clinical development of PRI‐002.},
cin = {IBI-7 / INM-4},
ddc = {610},
cid = {I:(DE-Juel1)IBI-7-20200312 / I:(DE-Juel1)INM-4-20090406},
pnm = {553 - Physical Basis of Diseases (POF3-553)},
pid = {G:(DE-HGF)POF3-553},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:32211506},
UT = {WOS:000751652300062},
doi = {10.1002/trc2.12001},
url = {https://juser.fz-juelich.de/record/874644},
}