ArticlemAbs
Design, development and characterization of ACT017, a humanized Fab that blocks platelet's glycoprotein VI function without causing bleeding risks.
Article in mAbs. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 90 citations in OpenAlex.
- Trial
- Targeting GPVI with glenzocimab in COVID-19 patients: Results from a randomized clinical trial.PloS one · 2024Trial
- Partial downregulation of platelet glycoprotein VI by low affinity antibodies confers sustained and safe antithrombotic protection.Signal transduction and targeted therapy · 2026Article
- Glycoprotein VI inhibitors: glenzocimab and EMA601 two inhibitory Fabs.European heart journal · 2025Article
- Comparative Effects of Glenzocimab and Eptifibatide on Bleeding Severity in 2 Mouse Models of Intracranial Hemorrhage.Journal of the American Heart Association · 2025Article
- The Role of Thrombo-inflammation in Ischemic Stroke: Focus on the Manipulation and Clinical Application.Molecular neurobiology · 2025Review
- GPVI-mediated thrombus stabilization of shear-induced platelet aggregates in a microfluidic stenosis.Biophysical journal · 2025Article
- A naphthalimide derivative exerts potent antiplatelet and antithrombotic activities without a bleeding tendency.Frontiers in pharmacology · 2025Article
- The humanized platelet glycoprotein VI Fab inhibitor EMA601 protects from arterial thrombosis and ischaemic stroke in mice.European heart journal · 2024Article
- GPVI inhibition: Advancing antithrombotic therapy in cardiovascular disease.European heart journal. Cardiovascular pharmacotherapy · 2024Review
- Platelets favor the outgrowth of established metastases.Nature communications · 2024Article
- Ultra-high throughput-based screening for the discovery of antiplatelet drugs affecting receptor dependent calcium signaling dynamics.Scientific reports · 2024Article
- Article
- Current concepts and novel targets for antiplatelet therapy.Nature reviews. Cardiology · 2023Review
- Targeting platelet GPVI with glenzocimab: a novel mechanism for inhibition.Blood advances · 2023Article
- Luteolin inhibits GPVI-mediated platelet activation, oxidative stress, and thrombosis.Frontiers in pharmacology · 2023Article
- Novel strategies in antithrombotic therapy: targeting thrombosis while preserving hemostasis.Frontiers in cardiovascular medicine · 2023Review
- Novel Antithrombotic Agents in Ischemic Cardiovascular Disease: Progress in the Search for the Optimal Treatment.Journal of cardiovascular development and disease · 2022Review
- Anti-GPVI nanobody blocks collagen- and atherosclerotic plaque-induced GPVI clustering, signaling, and thrombus formation.Journal of thrombosis and haemostasis : JTH · 2022Article
- Modulation of Glycoprotein VI and Its Downstream Signaling Pathways as an Antiplatelet Target.International journal of molecular sciences · 2022Review
Corrections and comments
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Authors and funding
5 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glycoprotein VI is a platelet-specific collagen receptor critical for in vivo formation of arterial thrombosis. It is also considered as an attractive target for the development of anti-thrombotic drugs because blocking glycoprotein (GP)VI inhibits platelet aggregation without inducing detrimental effects on physiologic hemostasis. Here, we present data on the identification, in vitro and ex vivo pharmacology of a humanized Fab fragment designated as ACT017. ACT017 was selected out of 15 humanized variants based upon structural and functional properties. It was produced under GMP-like conditions followed by detailed physico-chemical analysis and functional characterization indicating high antigen-binding specificity and affinity. In addition, we demonstrate, in a dose-escalation study, that ACT017 has a high capacity to specifically inhibit collagen-induced platelet aggregation ex vivo after injection to the macaque without inducing thrombocytopenia, GPVI depletion or bleeding side effects as is the case for conventional anti-platelets. Therefore, ACT017 is a promising therapeutic candidate for the development of a new generation of safe and efficient anti-thrombotic drugs.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.