Safety and pharmacokinetics of the orally available antiprionic compound PRI-002: A single and multiple ascending dose phase I study

Alzheimers Dement (N Y). 2020 Mar 20;6(1):e12001. doi: 10.1002/trc2.12001. eCollection 2020.

Abstract

Introduction: PRI-002 is an orally available anti-amyloid beta (Aβ) prionic compound developed for direct disassembly of toxic Aβ oligomers relevant to Alzheimer's disease.

Methods: Two 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.

Results: PRI-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.

Conclusions: The safety and PK results encourage further clinical development of PRI-002.

Keywords: Alzheimer´s disease (AD); MAD; PRI‐002; SAD; anti‐Aβ‐prionic; first‐in‐human (FIH); multiple ascending dose; pharmacokinetics; phase I; safety; single ascending dose.