guselkumab

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Ligands
guselkumab

GtoPdb Ligand ID: 7998

Synonyms: CNTO-1959 | Tremfya®

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 3759^EQ/QS, based on peptide sequence identity. The patent provides a graphical representation of 3759^EQ/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.

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 3759^EQ/QS, based on peptide sequence identity. The patent provides a graphical representation of 3759^EQ/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

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