Drug Candidate Significantly Outperforms Gilead’s Remdesivir Head-to-Head in SARS-CoV-2 (COVID-19) Model

In a series of experiments in which a first-in-class ruthenium-based small molecule drug and Gilead Sciences’ (Foster City, CA, USA) remdesivir were tested head-to-head in a cytopathic effect assay against a live Wuhan strain of SARS-CoV-2 in Vero E6 cells, the new drug candidate clearly demonstrated its efficacy as a highly potent antiviral agent.

The new drug candidate, BOLD-100, developed by Bold Therapeutics, Inc. (Vancouver, BC, Canada), showed low nanomolar IC50 values, a magnitude lower (1/10th) than the IC50 values of remdesivir, the only currently approved therapeutic for COVID-19. BOLD-100 selectively inhibits stress-induced upregulation of the chaperone protein GRP78. In cancer, GRP78 plays a critical role in resistance, survival and proliferation, whereas in viral infections, GRP78 plays a critical role in host recognition, viral entry and viral replication. BOLD-100 has the potential to substantially reduce severity of infection, shortening hospital stays and reducing morbidity and mortality. Most importantly, BOLD-100 could be effective against not just the current pandemic, but also future viral pandemics.


Bold Therapeutics has already manufactured more than sufficient drug product to support immediate clinical studies in COVID-19 due to an ongoing Phase 1/2 trial of BOLD-100 in combination with FOLFOX in the treatment of advanced GI cancers, with an open IND with the US FDA and a February 2020 NOL from Health Canada. In an earlier Phase 1 dose-escalation study of 46 patients with advanced cancer, BOLD-100 was safe and well-tolerated, potentially allowing BOLD-100 to move immediately into Phase 2 trials in COVID-19. These factors allow BOLD-100 to be developed and potentially approved as an anti-COVID-19 therapeutic in a relevant timeframe, rather than years from now.

“Bold Therapeutics’ ongoing collaboration with some of the top virologists in Canada continues to produce independent data supporting BOLD-100 as a novel antiviral,” said Dr. Mark Bazett, Bold Therapeutics’ Director of Preclinical Development. “Today’s data is particularly impressive, showing that BOLD-100 is substantially more potent as an antiviral than remdesivir, the only recently Health Canada approved treatment for COVID-19. The collective evidence on BOLD-100 supports further, rapid development of this novel treatment option to support patients with COVID-19.”

Related Links:

Bold Therapeutics, Inc.
Gilead Sciences