varokibart   Click here for help

GtoPdb Ligand ID: 12187

Immunopharmacology Ligand
Compound class: Antibody
Comment: Varokibart is an IgG4λ, fully human anti-IL-5 monoclonal antibody that was developed for potential anti-inflammatory action. The '-bart' stem indicates that it is an engineered antibody. The amino acid sequences for varokibart's heavy and light chains are claimed in Cephalon, Inc.'s patent WO2018119016A1, as SEQ IDs 20 and 19 respectively [1]. These two peptide chains generate the antibody disclosed as 3A5.046 therein.
Teva acquired Cephalon in 2011, and from review of Teva's development pipeline it is possible that varokibart is their clinical candidate TEV-48574. Although the mechanism of action of TEV-48574 has not been formally declared, it was initially tested for anti-asthma efficacy, which is a predictable indication for an anti-IL-5 agent.
Bioactivity Comments
Antibody 3A5.046 is a more potent inhibitor of IL-5-driven proliferation and differentiation of TF-1-derived myeloid progenitor cells than the approved anti-IL-5 mAb mepolizumab in in vitro assays [1]. The cells used (TF-1.6G4) were selected and subcloned based on their enhanced surface expression of IL5RA, and their reliable proliferative response to hIL-5.
Selectivity at ligand targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
IL-5 Hs Antibody Binding ~10.7 pKd - 1
⤷ pKd ~10.7 (Kd ~2x10-11 M) [1]
Description: Binding affinity for hIL-5 determined by SPR