In vitro analyses of mAb 2021
| mAb 2021 . | . | . |
|---|---|---|
| TFPI binding (SPR) | TFPI, n = 3 | 25 ± 8pM |
| KD | (ka [1/Ms]: 4.48E+06 ± 1.7E+06) | |
| (kd [1/s]: 1.01E−04 ± 4.1E−06) | ||
| KPI-2 domain binding (SPR) | KPI-2 domain, n = 3 | 73 ± 13pM |
| KD | ||
| Cellular TFPI binding | HUVEC, n = 5 | 123 ± 32pM |
| KD | ||
| Neutralization of TFPI inhibition of FVIIa/TF/FXa | TFPI (1nM), FVIIa, TF (Innovin), FX | 1.20 ± 0.07nM |
| EC50 | n = 5 | |
| Neutralization of TFPI inhibition of FVIIa/TF/FXa on cellular surface (HUVEC) | FVIIa, FX, n = 3 | 0.11nM |
| EC50 | ||
| Clot time (FVIII-deficient plasma) | Plasma, n = 3 | 0.58 ± 0.07nM |
| Dilute prothrombin time | ||
| EC50 | ||
| Clot time (FIX-deficient plasma) | Plasma, n = 3 | 0.91 ± 0.18nM |
| Dilute prothrombin time | ||
| EC50 | ||
| Clot development (hemophilic whole blood) | Blood, n = 4 | 2.00 ± 0.59nM |
| Thrombelastography MTG | ||
| EC50 |
| mAb 2021 . | . | . |
|---|---|---|
| TFPI binding (SPR) | TFPI, n = 3 | 25 ± 8pM |
| KD | (ka [1/Ms]: 4.48E+06 ± 1.7E+06) | |
| (kd [1/s]: 1.01E−04 ± 4.1E−06) | ||
| KPI-2 domain binding (SPR) | KPI-2 domain, n = 3 | 73 ± 13pM |
| KD | ||
| Cellular TFPI binding | HUVEC, n = 5 | 123 ± 32pM |
| KD | ||
| Neutralization of TFPI inhibition of FVIIa/TF/FXa | TFPI (1nM), FVIIa, TF (Innovin), FX | 1.20 ± 0.07nM |
| EC50 | n = 5 | |
| Neutralization of TFPI inhibition of FVIIa/TF/FXa on cellular surface (HUVEC) | FVIIa, FX, n = 3 | 0.11nM |
| EC50 | ||
| Clot time (FVIII-deficient plasma) | Plasma, n = 3 | 0.58 ± 0.07nM |
| Dilute prothrombin time | ||
| EC50 | ||
| Clot time (FIX-deficient plasma) | Plasma, n = 3 | 0.91 ± 0.18nM |
| Dilute prothrombin time | ||
| EC50 | ||
| Clot development (hemophilic whole blood) | Blood, n = 4 | 2.00 ± 0.59nM |
| Thrombelastography MTG | ||
| EC50 |
FIX indicates Factor IX; FVIIa, Factor VIIa; FVIII, Factor VIII; FX, Factor X; FXa, Factor Xa; ka, association rate constant; kd, dissociation rate constant; KD, binding constant; KPI, Kunitz-type protease inhibitor; MTG, maximum thrombus generator; SPR, surface plasmon resonance; TF, tissue factor; and TFPI, tissue factor pathway inhibitor.