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Synonyms: BGB-324 | BGB324 | R-428 | R428
Compound class: Synthetic organic
Comment: Bemcentinib (BGB324, R428) is a potent, selective and orally active AXL receptor tyrosine kinase inhibitor that was discovered by Rigel as R428  and which is being developed by BergenBio for anti-cancer potential .
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
|Bemcentinib (BGB324) has advanced to clinical evaluations in a variety of solid tumour types and in leukemia . Click here to link to ClinicalTrials.gov's full list of BGB324 studies. A combination therapy of bemcentinib plus an anti-PD-(L)1 agent was granted FDA fast track designation (June 2021) as a potential option for AXL-positive advanced/metastatic non-small cell lung cancer (NSCLC).
Research data indicates that AXL enhances SARS-CoV-2 infection of host cells , and that bemcentinib inhibits cell entry and promotes the anti-viral Type I interferon response. Bemcentinib is being evaluated in COVID-19 patients as part of the UK's Accelerating COVID-19 Research and Development (ACCORD) initiative (June 2020). ACCORD aims to fast-track potential treatments for COVID-19 through early-stage clinical trials . In this setting researchers would aim to determine if the anti-inflammatory action of AXL-inhibition has potential to reduce mortality in patients with severe COVID-19.