Table 3.
Currently developed VWF inhibitors and their mechanisms of action.
| VWF INHIBITOR | TARGET | MECHANISM | CLINICAL TRIAL | REF | |
|---|---|---|---|---|---|
| AJVW-2 | Murine anti-human VWF monoclonal antibody | Directed against VWF A1 domain | Blocks VWF- GPIbα- interaction | No | [150] |
| AJW200 | IgG4 humanized version of AJvW-2 | Directed against VWF A1 domain | Blocks VWF- GPIbα- interaction | Yes | [151] |
| ANFIBATIDE (AGKICETIN) | Snake venom-derived GPIb antagonist | Binds to GPIbα | Blocks VWF- GPIbα- interaction | No | [152] |
| ARC15105 | Second-generation anti-VWF aptamer | Binds to VWF A1 domain | Blocks VWF- GPIbα- interaction | No | [153] |
| ARC1779 (ARC | Second-generation PEG-conjugated aptamer | Binds to activated VWF A1 domain | Blocks VWF- GPIbα- interaction | Yes | [154] |
| BT200 | Third-generation anti-VWF aptamer | Binds to the A1 domain of VWF. | Blocks VWF- GPIbα- interaction | No | [155] |
| CAPLACIZUMAB/CABLIVI (ALX-0081 OR ALX-0681) | Humanized anti-VWF bivalent nanobody | Binds to the A1 domain of VWF. | Blocks VWF- GPIbα- interaction | Yes | [134] |
| 82D6A3 | Monoclonal anti-VWF antibody | Binds to the VWF A3 domain. | Inhibits VWF-collagen type I and III interactions | No | [156] |
| H82D6A3 | Humanized version of 82D6A3 | Binds to the VWF A3 domain. | Inhibits VWF-collagen type I and III interactions | No | [157] |
| DTRI-031 | Anti-VWF aptamer | Binds to VWF | Inhibits VWF-platelet interaction | No | [158] |
| H6B4-FAB | Fab-fragment of a humanized monoclonal antibody | Targets GPIbα. | Inhibits binding of VWF to GPIbα | No | [159] |
| GPG-290 | Recombinant chimeric protein. | Contains gain-of-function GPIbα fragment that binds to VWF A1 domain | Inhibits binding of VWF to GPIbα | No | [160] |
| KB-VWF-006BI | Anti-VWF nanobody | Recognizes an epitope located within human and mouse VWF A1 domain | Blocks VWF- GPIbα- interaction | No | [15] |
| MA-16N7C2 | Recombinant mouse antibody | Recognizes human GPIIbIIIa | Blocks VWF-GPIIbIIIa interaction | No | [161] |
| TAGX-0004 | DNA aptamer | Recognizes the VWF A1 domain | No | [162] | |