GPVI/​Glenzocimab
In brief

The development of glenzocimab is rooted in pioneering academic research carried out at INSERM demonstrating that a specific mouse monoclonal antibody fragment (9O12) targeting human platelet GPVI exerted antithrombotic properties without inducing an additional bleeding risk5.

Acticor Biotech then designed and selected a humanized monoclonal antibody fragment (ACT017), later named glenzocimab, with high affinity and selectivity for GPVI6.

Glenzocimab binds specifically to human platelets and disrupts the interaction between GPVI and its major ligands: fibrin, fibrinogen, and collagen. It blocks GPVI-triggered platelet activation in vitro and ex vivo, and the intravenous administration of glenzocimab is antithrombotic in animal models and does not induce bleeding5.

Treatment by glenzocimab prevents recruitment of platelets on a fibrin clot, including during fibrin lysis. This will increase the efficacy on fibrinolytic treatments, preventing the transformation of fibrin rich clot into platelet rich clots. Glenzocimab has also shown in pre-clinical studies the ability to promotes disaggregation of platelets aggregates in a stand-alone treatment. Together, those properties indicate a role for glenzocimab at occlusion site in the vicinity of fibrin clot but also on platelets microaggregates, a key driver of thrombo-inflammation processes.

In a placebo-controlled phase 1 clinical trial in Healthy Volunteers, glenzocimab proved to be safe and well tolerated, with no Safety Adverse Events (SAE), dose or time-related adverse events being reported, and no prolongation of bleeding time7. Its pharmacokinetic/pharmacodynamic properties were characterized and this enabled the definition of doses and dosing regimens for clinical studies of glenzocimab8 in patients.

In July2022, Acticor Biotech was granted Priority Medicines (PRIME) status by theEuropean Medicines Agency for glenzocimab in the treatment of stroke,recognizing the potential clinical benefit of glenzocimab and its relevance tothe unmet medical.