The novel antiplatelet agent ACT017 confers reduced risk for bleeding in healthy volunteers and may be a safe and effective alternative for patients with stroke, according to early findings published in Arteriosclerosis, Thrombosis and Vascular Biology.
Christine Voors-Pette, MD, a principal investigator and manager of medical operations at QPS Holdings LLC in the Netherlands, and colleagues evaluated the safety, tolerability, pharmacokinetics and pharmacodynamics of ACT017 (QPS Holdings LLC), a glycoprotein VI antibody, in healthy volunteers.
“There is a clear need for a novel antiplatelet agent that resolves platelet aggregation and clot formation without raising the risk for bleeding,” Martine Jandrot-Perrus, MD, PhD, a scientist at France’s National Institute of Health and Medical Research, said in a press release. “Such a therapy would considerably improve and expand our current therapeutic arsenal for the treatment of acute stroke.”
The researchers analyzed data of six cohorts of eight healthy male and female subjects (aged 18 to 65 years) receiving ascending single doses of ACT017 (six in each cohort) or placebo (two in each cohort). The doses were administered as a 6-hour IV infusion, with one-fourth of the total dose administered within 15 minutes and the remainder administered within 5 hours and 45 minutes.
The investigated doses ranged from 62.5 mg to 2,000 mg, Voors-Pette and colleagues wrote.
No serious adverse events occurred during the study and all doses of ACT017 were tolerated, the researchers wrote.
Template bleeding time was not affected in a clinically significant manner by any of the ACT017 doses, Voors-Pette and colleagues.
There was no change in platelet count, platelet glycoprotein VI (GPVI) expression assessed by flow cytometry or plasma levels of soluble GPVI assessed by enzyme-linked immunosorbent assay (ELISA), the researchers wrote.
Administration of ACT017 inhibited collagen-induced platelet aggregation measured by light transmission aggregometry on platelet-rich plasma, and the extent and duration of the effect were dose-dependent, Voors-Pette and colleagues wrote.
“Our results are quite encouraging because they show the candidate compound is well-tolerated at does even twice as high as the ones targeted for a future treatment and without any signs of bleeding,” Jandrot-Perrus said in the release. “Another encouraging finding is the fact that the drug’s action on platelets is rapid, specific and largely reversable within 24 hours.” – by Earl Holland Jr.
Disclosures: The study was funded by QPC Holdings LLC. Voors-Pette reports being employed by QPC Holdings LLC. Jandrot-Perrus reports she holds equity and received consulting fees in Acticor-Biotech. Please see the study for all other authors’ relevant financial disclosures.
Editor’s Note: This article and headline were updated on April 25, 2019 to clarify that the study was in healthy volunteers, not patients with stroke.