Concizumab

• CAT Number: I042255
• CAS Number: 1312299-39-0
• Purity: ≥95%

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 increases thrombin peak in a concentration- dependent manner[1].
Concizumab (i.v./s.c.) blocks the TFPI interaction with the active site of FXa in cynomolgus monkeys[2].

1.19

Pharmacokinetic parameters after intravenous or subcutaneous administration of Concizumab to 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.

Reference

[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.
 [Content Brief]

[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.
 [Content Brief]