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Synonyms: ABC 294640 | ABC-294640 | Yeliva®
Compound class: Synthetic organic
Comment: Opaganib (ABC294640) is an orally bioavailable sphingosine kinase 2-selective inhibitor that is being investigated for clinical antiproliferative efficacy in various cancers . The sphingosine kinases (SK1 and SK2) are key enzymes within the sphingolipid metabolism pathway that promote tumour growth and pathologic inflammation. Opaganib is being developed by RedHill Bio. In 2017 the FDA granted this compound orphan designation for the treatment of cholangiocarcinoma.
SARS-CoV-2 and COVID-19: A medRxiv preprint descibes the compassionate use of opaganib in a small cohort of patients with severe COVID-19 , predicated upon the drug's anti-inflammatory and anti-viral properties. The analysis indicated trends in favour of clinical efficacy which led to extended investigation in a Phase 2 randomised placebo-controlled trial.
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|
|ABC294640 has advanced to clinical evaluation in patients with advanced cholangiocarcinoma, advanced hepatocellular carcinoma and refractory/relapsed multiple myeloma (to view ClinicalTrials.gov's list of ABC294640 trials click here).|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT04414618||A Study of Opaganib in Coronavirus Disease 2019 Pneumonia||Phase 2 Interventional||RedHill Biopharma Limited|
|NCT03377179||A Study of ABC294640 (Yeliva ®) Alone and in Combination With Hydroxychloroquine Sulfate in Treatment of Patients With Advanced Cholangiocarcinoma||Phase 2 Interventional||RedHill Biopharma Limited||2|
|NCT04435106||Compassionate Use of Opaganib in Patients With Coronavirus Disease 2019 (COVID-19)||Observational||Shaare Zedek Medical Center||Results analysis indicated trends in favour of clinical efficacy, along with favourable safety, which led to extended investigation in a Phase 2 randomised placebo-controlled trial in patients with COVID-19 pneumonia.||2|