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].
Concizumab 以浓度依赖性方式增加凝血酶峰值[1]。
Concizumab (i.v./s.c.) 阻断 TFPI 与食蟹猴中 FXa 活性位点的相互作用[2]。
| 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. |
[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.
[2]. AgersØ 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.