Synonyms: BBI-608 | BBI608
Compound class:
Synthetic organic
Comment: Napabucasin (BBI608) is a small molecule naphthoquinone that blocks cancer stemness properties [3,6], It does this by targeting the signal transducer and activator of transcription 3 (STAT3) pathway [4]. Napabucasin is orally administered, and is bioactivated by the intracellular antioxidant NAD(P)H:quinone oxidoreductase 1 (NQO1), to produce reactive oxygen species (ROS), principally NO. The high level of NO generation causes cell death, and positively correlates with the compound's anti-proliferative activity in cancer cells [1].
COVID-19: Napabucasin has been proposed as a potential repurposing candidate for the treatment of COVID-19, based on a virtual screening analysis of the interaction of existing approved and experimental compounds with the SARS-CoV-2 main protease (Mpro) [2]. Extensive in vitro and in vivo studies would be required to validate napabucasin's antiviral activity. Ligand Activity Visualisation ChartsThese 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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No information available. |
Summary of Clinical Use |
Napabucasin has been advanced to clinical trials to determine its anti-tumour activity, as monotherapy and in combination with conventional therapeutics, |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT01830621 | BBI608 and Best Supportive Care vs Placebo and Best Supportive Care in Pretreated Advanced Colorectal Carcinoma | Phase 3 Interventional | Canadian Cancer Trials Group | This study was terminated for futility in 2014. It was determined that overall survival did not differ significantly between the napabucasin and placebo groups. | 5 |
NCT02851004 | Special Combination of BBI608 and Pembrolizumab | Phase 1/Phase 2 Interventional | National Cancer Center Hospital East | 5 | |
NCT01325441 | A Study of BBI608 Administered With Paclitaxel in Adult Patients With Advanced Malignancies | Phase 1/Phase 2 Interventional | Sumitomo Dainippon Pharma Oncology, Inc | 5 |