Synonyms: Cetrotide® | SB-075
cetrorelix is an approved drug (EMA (1999), FDA (2000))
Compound class:
Peptide
Comment: Cetrorelix is a synthetic GnRH receptor antagonist. Natural GnRH is a decapeptide hormone.
![]() Ligand Activity Visualisation ChartsThese 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. ✖ |
|
Immunopharmacology Comments |
Based on evidence which indicates that GnRH regulates immune cell development [8] and has proinflammatory effects [4], and that GnRH antagonists have experimentally proven anti-inflammatory effects in vivo [1,5], GnRH receptor blockade with cetrorelix has been evaluated in Phase 2 clinical trial NCT00667758 for potential anti-inflammatory efficacy in patients with rheumatoid arthritis [6-7]. Whilst this proof-of-concept study did show anti-inflammatory effects the programme was not progressed. |