spartalizumab   Click here for help

GtoPdb Ligand ID: 10140

Synonyms: NPV-PDR001 | NPVPDR001 | PDR-001 | PDR001
Immunopharmacology Ligand
Compound class: Antibody
Comment: Spartalizumab (PDR001) is a humanized, IgG4κ anti-PD-1 monoclonal antibody immuno-oncology lead that is being developed by Novartis.
Sequence and structural information about this antibody are available from its IMGT/mAb-DB entry. BLAST analysis of the peptide sequences submitted to the WHO for the INN spartalizumab reveal exact matches with peptide sequences claimed in patent US9683048B2 [1], specifically SEQ ID NO: 91 for the entire heavy chain and SEQ ID NO: 72 for the entire light chain. Sequence IDs 91 and 72 are components of the antibody designated as BAP049-Clone-E which is one of the humanized clones generated in the discovery campaign described in US9683048B2.
Click here for help

Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

✖

View interactive charts of activity data across species
Immunopharmacology Comments
Spartalizumab (PDR001) is an anti-PD-1 monoclonal antibody (immune checkpoint inhibitor) that is in clinical devlopment as an immuno-oncology therapeutic. It binds strongly to purified PD-1 by Biacore analysis and inhibits binding of PD-L1 and PD-L2 to PD-1 in whole cell assays [1]. Functionally spartalizumab modulates PD-1-dependent activities and restores effector T cell functions such as proliferation, IFNγ secretion and cytolytic capacity. In addition, it favourably alters the activity of other immune cells such as regulatory T cells and NK cells, which combined with increased effector T cell activity, brings about an enhanced immune response against cancer cells.