Drugs targeting FXI and FXIa studied in phase 2 trials
| Drug name . | Drug description . | Mechanism of action . | Administration . | Duration of effect . |
|---|---|---|---|---|
| Ionis FXIRx (BAY-2306001) | DNA antisense oligonucleotide with complementary sequence to FXI messenger RNA | Reduces synthesis of FXI in hepatocytes | Subcutaneous or IV | Effect may persist for weeks to months after discontinuation |
| Osocimab | Monoclonal IgG that binds to the catalytic domain of FXIa | Inhibits FXIa catalytic activity through allosteric effects | Subcutaneous or IV | Days to weeks depending on dose. Mean elimination half-life, 30-44 days. |
| Abelacimab | Monoclonal IgG that binds to the catalytic domain of FXI and FXIa | Binds FXI preventing its activation. It also neutralizes FXIa activity | Subcutaneous or IV | Mean elimination half-life, 25-30 days. The IgG becomes saturated with FXI over time. |
| Xisomab (gruticibart) | Monoclonal IgG that binds to the apple 2 domain of FXI and FXIa | Interferes with FXI activation by FXIIa | Subcutaneous or IV | Half-life, 121.5 h with single dose of 5 mg/kg |
| Milvexian | Small molecule inhibitor of the FXIa catalytic active site | Inhibits FXIa catalytic activity by active site binding | Oral | Half-life, 11.4 to 18.1 h when administered daily |
| Asundexian | Small molecule inhibitor of the FXIa catalytic active site | Inhibits FXIa catalytic activity by active site binding | Oral | Dose dependent terminal half-life of 14.2 to 17.4 h |
| Drug name . | Drug description . | Mechanism of action . | Administration . | Duration of effect . |
|---|---|---|---|---|
| Ionis FXIRx (BAY-2306001) | DNA antisense oligonucleotide with complementary sequence to FXI messenger RNA | Reduces synthesis of FXI in hepatocytes | Subcutaneous or IV | Effect may persist for weeks to months after discontinuation |
| Osocimab | Monoclonal IgG that binds to the catalytic domain of FXIa | Inhibits FXIa catalytic activity through allosteric effects | Subcutaneous or IV | Days to weeks depending on dose. Mean elimination half-life, 30-44 days. |
| Abelacimab | Monoclonal IgG that binds to the catalytic domain of FXI and FXIa | Binds FXI preventing its activation. It also neutralizes FXIa activity | Subcutaneous or IV | Mean elimination half-life, 25-30 days. The IgG becomes saturated with FXI over time. |
| Xisomab (gruticibart) | Monoclonal IgG that binds to the apple 2 domain of FXI and FXIa | Interferes with FXI activation by FXIIa | Subcutaneous or IV | Half-life, 121.5 h with single dose of 5 mg/kg |
| Milvexian | Small molecule inhibitor of the FXIa catalytic active site | Inhibits FXIa catalytic activity by active site binding | Oral | Half-life, 11.4 to 18.1 h when administered daily |
| Asundexian | Small molecule inhibitor of the FXIa catalytic active site | Inhibits FXIa catalytic activity by active site binding | Oral | Dose dependent terminal half-life of 14.2 to 17.4 h |