Another candidate against COVID-19

BOLD-100 demonstrates nanomolar range inhibition of live COVID-19 in vitro

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VANCOUVER, British Columbia—Bold Therapeutics, a clinical-stage biopharmaceutical company, recently announced in-vitro data showing that its lead clinical-stage therapeutic, BOLD-100, successfully inhibits live SARS-CoV-2 (the cause of the disease COVID-19) within a therapeutic range. The company says that this data is further supported by recent literature from independent researchers suggesting that GRP78, the primary target for BOLD-100, is “an increasingly attractive antiviral target.”   
Dr. Stephen Barr, an associate professor in the Department of Microbiology and Immunology at Western University and a member of Bold Therapeutics’ COVID-19 Consortium, recently generated and subsequently confirmed in-vitro data showing nanomolar half maximal inhibitory concentration (IC50) values for BOLD-100 in a cytopathic effect assay using a Wuhan strain of SARS-CoV-2. Barr runs a BSL-3 lab that allow his team to study the most dangerous pathogens such as HIV, Ebola-like virus, West Nile virus and, most recently, SARS-CoV-2.
“We are encouraged by this preliminary data demonstrating potent antiviral activity of BOLD-100 against SARS-CoV-2,” explained Barr. “This data is a critical step toward using BOLD-100 to support patients with COVID-19, and we look forward to generating additional data in other antiviral models to both confirm and expand on these results.”
Data generated concurrently from other Bold Therapeutics’ COVID-19 Consortium researchers shows that BOLD-100 is also effective against other viruses, suggesting potential utility against future viral pandemics.
BOLD-100 is a first-in-class anti-resistance ruthenium-based small-molecule drug which selectively inhibits stress-induced upregulation of GRP78, an important resistance, survival and proliferation pathway common across cancers. Recent evidence also suggests that GRP78 plays a critical role in host recognition, viral entry and viral replication. This is articulated in the recent review by Lee, a GRP78 expert at the University of Southern California, entitled “The stress-inducible molecular chaperone GRP78 as potential therapeutic target for Coronavirus infection.”
In June, Bold Therapeutics announced its COVID-19 Consortium, which so far includes note only Barr but also Drs. François Jean and Ted Steiner of the University of British Columbia, Dr. Marc-André Langlois of the University of Ottawa, and Dr. Len Seymour of the University of Oxford.
“We have assembled an enviable team to explore BOLD-100’s efficacy in treating SARS-CoV-2 and the mechanisms underlying this efficacy,” stated E. Russell McAllister, CEO of Bold Therapeutics. “Amidst surging coronavirus cases and uncertainty around the timing and effectiveness of vaccines, novel therapeutics are desperately needed—not just for the current crisis, but inevitable future pandemics. Our data and supporting literature—more than 150 academic articles—suggest that BOLD-100 could substantially reduce severity of infection, shortening hospital stays and reducing morbidities and mortalities.
“With an entirely novel mechanism of action, BOLD-100 could be combined synergistically with other antiviral therapies. With established safety and tolerability from a Phase 1 study in advanced cancer, an open IND with the FDA, and a commercially scalable manufacturing process, we are optimally positioned to address this urgent unmet need in a relevant timeframe. We expect additional confirmatory data from our COVID-19 Consortium and are prepared to initiate human clinical trials expeditiously once we secure the necessary funding and/or partnerships.”

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