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1312299-39-0

1312299-39-0 Structure

1312299-39-0 Structure
IdentificationBack Directory
[Name]

Concizumab
[CAS]

1312299-39-0
[Synonyms]

Concizumab
Concizumab (anti-TFPI)
Research Grade Concizumab (DHC82802)
Chemical PropertiesBack Directory
[form ]

Liquid
[color ]

Colorless to light yellow
Hazard InformationBack Directory
[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].

1.19Pharmacokinetic parameters after intravenous or subcutaneous administration of Concizumab to cynomolgus monkeys[2].
ParameterUnitEstimate%RSE
CLLmL/h/kg0.146.1
V1mL/kg3334
V2mL/kg33-
QmL/h/kg0.1216
F%937.7
Vmaxμg/h/kg1117
Kmμg/mL0.5452
t1/2(abs)h7232

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
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