ARC15105 is a potent antagonist of von Willebrand factor mediated platelet activation and adhesion.

ABSTRACT:

Objective

We investigated the stability, pharmacokinetic, and pharmacodynamic profile of the 2(nd) generation anti-von Willeband factor aptamer ARC15105.

Methods and results

Platelet plug formation was measured by collagen/adenosine diphosphate-induced closure time with the platelet function analyzer-100 and platelet aggregation by multiple electrode aggregometry. Platelet adhesion was measured on denuded porcine aortas and in a flow chamber. Aptamer stability was assessed by incubation in nuclease rich human, monkey, and rat serum for up to 72 hours. Pharmacokinetic and pharmacodynamic profiles were tested in cynomolgus monkeys after IV and SC administration. The median IC(100) and IC(50) to prolong collagen/adenosine diphosphate-induced closure timewere 27 nmol/L and 12 nm

SUBMITTER: Siller-Matula JM 

PROVIDER: S-EPMC11586852 | biostudies-literature | 2012 Apr

REPOSITORIES: biostudies-literature