TY  - JOUR
AU  - Kutzsche, Janine
AU  - Jürgens, Dagmar
AU  - Willuweit, Antje
AU  - Adermann, Knut
AU  - Fuchs, Carola
AU  - Simons, Stefanie
AU  - Windisch, Manfred
AU  - Hümpel, Michael
AU  - Rossberg, Wolfgang
AU  - Wolzt, Michael
AU  - Willbold, Dieter
TI  - Safety and pharmacokinetics of the orally available antiprionic compound PRI‐002: A single and multiple ascending dose phase I study
JO  - Alzheimer's & dementia / Translational research & clinical interventions Translational research & clinical interventions [...]
VL  - 6
IS  - 1
SN  - 2352-8737
CY  - Amsterdam [u.a.]
PB  - Elsevier
M1  - FZJ-2020-01563
SP  - e12001
PY  - 2020
AB  - 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.
LB  - PUB:(DE-HGF)16
C6  - pmid:32211506
UR  - <Go to ISI:>//WOS:000751652300062
DO  - DOI:10.1002/trc2.12001
UR  - https://juser.fz-juelich.de/record/874644
ER  -