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Synonyms: Kevzara® | REGN88 | SAR153191
sarilumab is an approved drug (EMA & FDA (2017))
Compound class: Antibody
Comment: Sarilumab is a monoclonal antibody directed against the interleukin 6 receptor (IL6R).
Peptide sequence and structural information for this antibody are available from its IMGT/mAb-db record. Peptide sequence BLAST search using the heavy and light chain variable regions of sarilumab provides 100% matches to sequences covered by patent US7582298 , and to the antibody with designation VQ8F11-21.
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.✖
|No information available.|
|Summary of Clinical Use|
|Sarilumab was granted FDA approval as a treatment for moderate to severe active RA in May 2017 (with EMA approval granted in June 2017), following evaluation in several clinical trials, either as a monotherapy (eg NCT02121210) or in combination with other drugs such as etanercept, methotrexate, tocilizumab and adalimumab.
Click here to link to ClinicalTrials.gov's listing of Phase 3 sarilumab trials. A Phase 2 study for non-infectious uveitis (NCT01900431) has been completed, whereas a Phase 2 extension study (NCT01118728) for ankylosing spondylitis was terminated.
SARS-CoV-2 and COVID-19: Sarilumab was evaluated for potential to reduce exaggerated inflammation in hospitalised patients with COVID-19 in the US. The Phase 2/3 clinical trial (NCT04315298) did not meet its primary or secondary endpoints in these patients and the trial has been terminated. An Italian trial also failed to find mortality benefit . Trials appear to be continuing in other countries.
|Mechanism Of Action and Pharmacodynamic Effects|
|Interleukin 6 (IL6) is a potent pleiotropic cytokine that regulates cell growth and differentiation and plays an important role in the immune response. Dysregulated production of IL6 and its receptor are implicated in the pathogenesis of autoimmune diseases such as RA. Sarilumab blocks the abberant IL6R signalling associated with RA, thereby modulating pathological symptoms.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)