- Advanced search
- Immuno Portal
- Malaria Portal
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.✖
1. French KJ, Zhuang Y, Maines LW, Gao P, Wang W, Beljanski V, Upson JJ, Green CL, Keller SN, Smith CD. (2010)
Pharmacology and antitumor activity of ABC294640, a selective inhibitor of sphingosine kinase-2.
J Pharmacol Exp Ther, 333 (1): 129-39. [PMID:20061445]
2. Kurd R, Ben-Chetrit E, Karameh H, Bar-Meir M. (2020)
Compassionate Use of Opaganib For Patients with Severe COVID-19.
medRxiv, Preprint. DOI: 10.1101/2020.06.20.20099010
3. Lewis CS, Voelkel-Johnson C, Smith CD. (2018)
Targeting Sphingosine Kinases for the Treatment of Cancer.
Adv Cancer Res, 140: 295-325. [PMID:30060814]