Chemical Properties
| form | Liquid |
| color | Colorless to light yellow |
Concizumab Chemical Properties,Usage,Production
Uses
Concizumab is an anti-TFPI monoclonal antibody (IgG4 type) that binds to the Kunitz-type protease inhibitor (KPI) 2 structural domain of TFPI, thereby blocking the interaction of this structural domain with the FXa active site. Concizumab can be used in the study of haemophilia[1][2].in vivo
Concizumab (i.v./s.c.) blocks the TFPI interaction with the active site of FXa in cynomolgus monkeys[2].
| Parameter | Unit | Estimate | %RSE |
| CLL | mL/h/kg | 0.14 | 6.1 |
| V1 | mL/kg | 33 | 34 |
| V2 | mL/kg | 33 | - |
| Q | mL/h/kg | 0.12 | 16 |
| F | % | 93 | 7.7 |
| Vmax | μg/h/kg | 11 | 17 |
| Km | μg/mL | 0.54 | 52 |
| t1/2(abs) | h | 72 | 32 |
CLL: the linear part of the clearance.
V1: the volume of the central compartment.
V2: the volume of the peripheral compartment.
Vmax: the maximum amount of anti-TFPI cleared per time unit via binding to TFPI.
Km: the concentration at which the target mediated elimination rate is 50% of the maximum value (Vmax).
T1/2(abs): the absorption half-life, describing the rate of absorption after sc administration.
%RSE: residual standard error.
| Animal Model: | Cynomolgus monkeys (target mediated drug disposition (TMDD) model)[2]. |
| Dosage: | 20mg/kg or 200 mg/kg |
| Administration: | Intravenous injection/subcutaneous injection |
| Result: | Showed a high bioavailability (93%) and the absorption half-life is estimated to be 72 h. |
References
[1] Kjalke M, et al. Thrombin generation potential in the presence of concizumab and rFVIIa, APCC, rFVIII, or rFIX: In vitro and ex vivo analyses. J Thromb Haemost. 2021 Jul;19(7):1687-1696. DOI:10.1111/jth.15323[2] Agers H, et al. Pharmacokinetics of an anti-TFPI monoclonal antibody (concizumab) blocking the TFPI interaction with the active site of FXa in Cynomolgus monkeys after iv and sc administration. Eur J Pharm Sci. 2014 Jun 2;56:65-9. DOI:10.1016/j.ejps.2014.02.009
Concizumab Suppliers
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