dupilumab   Click here for help

GtoPdb Ligand ID: 7574

Synonyms: Dupixent® | REGN668 | SAR231893
Approved drug Immunopharmacology Ligand
dupilumab is an approved drug (EMA & FDA (2017))
Compound class: Antibody
Comment: Dupilumab is fully human monoclonal antibody against the α subunit of the IL4 receptor.
Peptide sequences for this antibody are available from its IMGT/mAb-db record. Dupilumab was produced using Regeneron's genetically engineered VelocImmune® mice which have humanized immunoglobulin gene loci and produce human:mouse hybrid antibodies that can rapidly be converted to fully human antibodies [3].
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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.

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View interactive charts of activity data across species
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Summary of Clinical Use Click here for help
Dupilumab was originally evaluated as a treatment for atopic allergic conditions, including asthma [4], atopic dermatitis (AD) and nasal polyposis [1]. A list of trials registered at ClinicalTrials.gov is available here.
The first full regulatory approval for dupilumab was granted by the FDA in March 2017 and this was for the treatment of moderate-to-severe eczema (atopic dermatitis). The EMA granted this same approval in August 2017. In October 2018, FDA approval was expanded to encompass the treatment of patients with eosinophilic type or oral corticosteroid-dependent moderate-to-severe asthma. June 2019 saw FDA approval expanded to include treatment of patients with uncontrolled chronic rhinosinusitis with nasal polyposis.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Dupilumab is an IL-4 receptor α subunit (IL4Rα) inhibitor. IL4Rα is a component of the receptors which bind both interleukin (IL)-4 and IL-13. Interleukins 4 and 13 are released in response to Th2 cell activation in inflammatory reactions. By inhibiting both of these signalling pathways dupilumab effects a reduction of airway inflammation, as originally confirmed by results from clinical trials in patients with moderate-to-severe asthma [4].