- Guide to PHARMACOLOGY
Synonyms: RG-7625 | RG7625 | RO-5459072
Compound class: Synthetic organic
Comment: Petesicatib is the INN for a cathepsin S inhibitor. The structure (and CAS registry number) submitted to the WHO match PubChem CID 59543597, and this ties the INN together with the research code RO5459072 assigned by Hoffman-La Roche to their cathepsin S inhibitor [2-3]. This same chemical structure is claimed in Hoffmann-La Roche patent WO2010121918A1, where it is example 238 .
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.✖
|Petesicatib causes a dose-dependent intracellular accumulation of invariant chain fragment (and cathepsin S substrate) Lip10 in B cells and myeloid dendritic cells in vitro (in human PBMCs ex vivo) and in vivo (in cynomolgus monkeys and in cells from human Phase 1 trial volunteers) , proving target engagement, and supporting Lip10 as a pharmacodynamic biomarker of cathepsin S inhibition.
|Completed Phase 2 evaluation in SS- see NCT02701985.
|Completed Phase 1 evaluation in celiac patients- see NCT02679014.