CFZ533   

GtoPdb Ligand ID: 9802

Synonyms: CFZ-533 | iscalimab (proposed INN) | NVP-CFZ533 | OM11-62MF
Compound class: Antibody
Comment: CFZ533 is an anti-CD40 monoclonal antibody that is designed exhibit no agonist activity and is non-depleting (no ADCC activity for an improved safety profile, particularly in non-oncologic indications). It is claimed in Novartis' patent WO2012065950 [1] as mAb1 (based on peptide sequence alignments between the INN record for iscalimab and patented sequences retrieved from a BLAST search). Blocking CD40-mediated inflammatory responses is a well advanced mechanism being expoited for potential to treat autoimmune and inflammatory disorders and/or for preventing/reducing graft rejection following organ transplant.
Bioactivity Comments
CFZ533 (mAb1) shows no agonist activity in an in vitro assay using isolated human PBMCs, blocks CD40 ligand-mediated PBMC proliferation (IC50 58 ng/ml), inhibits CD40L-mediated TNF-α release from human monocyte derived dendritic cells (IC50 40 ng/ml), and has ADCC activity of < 1% (measuring specific lysis) [1].
Selectivity at catalytic receptors
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
CD40 Hs Antibody Binding 9.2 pKd - 1
pKd 9.2 (Kd 6.9x10-10 M) [1]
Description: Measured using a Biacore assay.