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Synonyms: PLX 5622 | PLX-5622
Compound class: Synthetic organic
Comment: PLX5622 is an orally available and highly selective kinase inhibitor targeting CSF1R (FMS) kinase and other Type III receptor tyrosine kinases. It is being investigated for its anti-inflammatory effects in autoimmune diseases, in the first instance rheumatoid arthritis (RA).
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|
|A Phase 1b study of PLX5622 in RA patients receiving methotrexate therapy has been completed- see NCT01329991.|
|Mechanism Of Action and Pharmacodynamic Effects|
|An increasing number of diseases are now recognized as being driven by inflammatory processes, and consequently involve various cells of the immune system. These cells include macrophages, microglial cells, T-cells, B-cells, monocytes and mast cells. CSF1R inhibitors are expected to target pro-inflammatory macrophages in inflamed joints of RA patients as well as reducing bone erosion and pain through inhibition of osteoclasts.
Alzheimer's disease (neuroinflammation): PLX5622 has been shown to eliminate microglia from the brain, which can be sustained in wild-type and the Alzheimer's disease model mice (3xTg-AD model). In the AD model PLX5622 prevents microglial association with amyloid β plaques and improves cognition .
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT01329991||Phase 1b Study of PLX5622 in Rheumatoid Arthritis Patients Who Are Receiving Methotrexate||Phase 1 Interventional||Plexxikon|