Phase 1 safety, tolerability and pharmacokinetics of 3K3A-APC in healthy adult volunteers.

ABSTRACT:

Background and purpose

Activated Protein C (APC) stimulates multiple cytoprotective pathways via the protease activated receptor-1 (PAR-1) and promotes anticoagulation. 3K3A-APC was designed for preserved activity at PAR-1 with reduced anticoagulation. This Phase 1 trial characterized pharmacokinetics and anticoagulation effects of 3K3A-APC.

Methods

Subjects (n=64) were randomly assigned to receive 3K3A-APC (n=4) at 6, 30, 90, 180, 360, 540 or 720 µg/kg or placebo (n=6) and were observed for 24 hr. After safety review additional subjects received drug every 12 hr for 5 doses (n=6 per group) at 90, 180, 360, or 540 µg/kg or placebo (n=8) and were observed for 24 hr.

Results

All subjects returned for safety assessments at 72 hours and 15 days. We found few adverse event

SUBMITTER: Lyden P 

PROVIDER: S-EPMC4040367 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature