tomaralimab   Click here for help

GtoPdb Ligand ID: 9408

Synonyms: OPN-305 | OPN305 | VK5A/H4
Immunopharmacology Ligand
Compound class: Antibody
Comment: Tomaralimab (OPN305) is a first-in-class humanised monoclonal antibody against Toll-like receptor 2 (TLR2) being developed by Opsona Therapeutics. It is being investigated for potential clinical use in certain hematological and immunological conditions. OPN305 and its possible uses are claimed in patent WO2011003925 [4]. The effect of TLR2 antagonism on myocardial ischemia/reperfusion injury in a large animal model (pigs) is reported in [1].
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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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Bioactivity Comments
OPN305 binds human, mouse and monkey TLR2 and suppresses murine TLR2 responses in vitro and in vivo [4]. OPN305-mediated TLR2 antagonism is not dependent upon the antibody binding to the B cell co-receptor CD32.
In murine studies inhibition of TLR2 signalling has been shown to promote renal graft function primarily by reducing ischemia-reperfusion injury in an isograft model of renal transplantation [5]. The protective effect of TLR2 antagonism in reducing ischemia-reperfusion injury is also reported following myocardial infarction in murine experiments [2].
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
TLR2 Mm Antibody Binding 7.9 pKd - 4
⤷ pKd 7.9 (Kd 1.19x10-8 M) [4]
Description: In a BIACORE surface plasmon resonance (SPR) assay.
TLR2 Primary target of this compound Hs Antibody Binding 7.5 pKd - 4
⤷ pKd 7.5 (Kd 2.89x10-8 M) [4]
Description: In a BIACORE surface plasmon resonance (SPR) assay.