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guselkumab   Click here for help

GtoPdb Ligand ID: 7998

Synonyms: CNTO-1959 | Tremfya®
Approved drug Immunopharmacology Ligand
guselkumab is an approved drug (EMA & FDA (2017))
Compound class: Antibody
Comment: Guselkumab is a monoclonal antibody directed against interleukin-23A (IL23A). It is being investigated as a treatment for plaque psoriasis.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
Bioactivity Comments
Results from an earlier clinical trial indicate that 50-100% of guselkumab-treated patients achieved a 75% improvement in psoriasis area severity index scores12 weeks after a single dose treatment. None of the patients receiving placebo showed any improvement [6]. Decreased epidermal thickness and T-cell and dendritic cell expression was observed in lesional and nonlesional skin biopsies from guselkumab-treated patients compared with placebo-treated patients, indicative of improved disease control [6].
Development of guselkumab is claimed in patent US7935344 [1], where it is likely to be the monoclonal identified as 3759EQ/QS, based on peptide sequence identity. The patent provides a graphical representation of 3759EQ/QS displacement of IL-23 binding to IL-23R (in Figure 10), but does not provide a calculated affinity constant or IC50 value for this binding assay.
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-23A Hs Antibody Binding 10.1 pKd - 7
⤷ pKd 10.1 (Kd 7.7x10-11 M) [7]