Table 2.
Summary of the effects of investigational antiplatelet agents.
| Agent | Target | Preclinical/Clinical Evidence |
|---|---|---|
| ARC1779 | VWF (A1 domain) |
↓ VWF-induced platelet activation (in vitro) No effect on ADP-, collagen-, or AA-induced platelet activation (in vitro) ↓ platelet activation, dose- and concentration dependent (in humans) ↓ embolic signals proportional to VWF inhibition in carotid endarterectomy (in humans) ↑ Perioperative bleeding in carotid endarterectomy (in humans) |
| TAGX-004 | VWF (A1 domain) |
↑ antiplatelet activity compared to ARC1779 (in vitro) |
| BT200 | VWF (A1 domain) |
↓ ristocetin-induced platelet aggregation (ex vivo and in humans) ↓ VWF activity in patients with an ACS or stroke (in humans) |
| DTRI-031 | VWF (A1 domain) |
↓ collagen- and ADP-induced platelet activation (ex vivo) Prevention of carotid artery thrombosis (in vivo) Induction of recanalization in carotid artery occlusion (in vivo) |
| Anfibatide | GP1b | ↓ ristocetin- and VWF-induced platelet adhesion and aggregation (in vitro and in humans) ↓ thrombosis in VWF-deficient mice (in vivo) ↓ activation of platelets from patients with an ACS, without any effect on revascularization parameters or myocardial injury markers (in humans) No increases in bleeding |
| h6B4-Fab | GP1b | ↓ cyclic flow reductions in stenosed femoral artery (in vivo) |
| Revacept | GPVI | ↓ platelet aggregation (in vivo) Comparable functional outcomes, infarct size, edema to thrombolytic therapy in cerebral ischemia (in vivo) ↑ platelet inhibition of other antiplatelets when used in combination (in vitro) No difference in death or high-sensitivity cardiac troponin increase in patients undergoing elective PCI for CAD (in humans) No increases in bleeding (in humans) |
| Glenzocimab | GPVI | ↓ collagen-induced platelet activation (ex vivo) Thrombus resolution, enhanced by increased wall shear rate (in vitro) Complete inhibition of platelet activation was noted after infusion, 60% platelet inhibition maintained 12 h post infusion (in humans) No increases in bleeding (in humans) |
| Cobalt hematoporphyrin | CLEC2 | ↓ CLEC2-induced platelet activation (in vitro) Prolonged time to occlusion of injured femoral artery (in vivo) |
| 2CP | CLEC2 | ↓ CLEC2-induced platelet activation (in vitro) |
| AYP1 | CLEC2 | ↓ CLEC2-induced platelet activation (in vitro) |
VWF: von Willebrand factor, ADP: adenosine diphosphate, AA: arachidonic acid, ACS: acute coronary syndrome, GP: glycoprotein, PCI: percutaneous coronary intervention, CAD: coronary artery disease. ↓ denotes reduction/inhibition, ↑ denotes increase/stimulation.