concizumab   Click here for help

GtoPdb Ligand ID: 11182

Synonyms: Alhemo® | Anti-TFPI | concizumab-mtci | mab2021 | NN7415
Approved drug
concizumab is an approved drug (Health Canada (2023), FDA (2024))
Compound class: Antibody
Comment: Concizumab is a clinical stage anti-tissue factor pathway inhibitor (TFPI) monoclonal antibody. It is a humanised IgG4 construct that was developed by Novo Nordisk as a novel therapeutic for genetic bleeding disorders [2]. Concizumab binds to the Kunitz-type protease inhibitor (KPI) 2 domain of TFPI and blocks its interaction with the active site of FXa [1]. TFPI is an endogenous anticoagulant protein whose pharmacological inhibition restores hemostasis [7].
Bioactivity Comments
In vitro, concizumab demonstrates binding to cell surface TFPI on EA.hy926 cells and neutralises TFPI inhibition of Factor X activation [3]. It cross-reacts with rabbit TFPI, but not with rat TFPI.
Selectivity at ligand targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
tissue factor pathway inhibitor Hs Antibody Binding 10.6 pKd - 4
⤷ pKd 10.6 (Kd 2.5x10-11 M) [4]