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Find Clinical Drug Pipeline Developments & Deals by Bold Therapeutics
BOLD-100 is a first-in-class ruthenium-based small molecule therapeutic that alters the unfolded protein response (UPR) through selective GRP78 inhibition and induces reactive oxygen species (ROS) which causes DNA damage and cell cycle arrest.
BOLD-100 is a first-in-class ruthenium-based small molecule therapeutic that (1) alters the unfolded protein response (UPR) through selective GRP78 inhibition.
Preclinical experiments have repeatedly shown that BOLD-100 improves outcomes in combination with a wide range of existing anti-cancer therapies, with particular synergy evident in drug-resistant cell lines.
BOLD-100, a first-in-class anti-resistance oncology therapeutic, has demonstrated potent anti-tumor activity in combination with a PD-1 checkpoint inhibitor in a validated I/O in vivo model of colorectal cancer.
BOLD-100-001 is an open-label, multicenter two-stage study designed to evaluate the safety and efficacy of BOLD-100 in combination with FOLFOX chemotherapy in patients with advanced gastric, pancreatic, colorectal and bile duct cancers.
BOLD-100 is a first-in-class ruthenium-based small molecule therapeutic that (1) alters the unfolded protein response (UPR) through selective GRP78 inhibition; and (2) induces reactive oxygen species (ROS) which causes DNA damage and cell cycle arrest.
BOLD-100 consistently reduced viral concentrations in multiple COVID-19 variants, including the highly prevalent B.1.1.7 variant originally identified in the UK.
BOLD-100 is a first-in-class ruthenium-based therapeutic that selectively inhibits stress-induced upregulation of GRP78 and alters the unfolded protein response (UPR), mitigating resistance, survival and proliferation, with additional synergistic direct anti-cancer activity.
Consistent with prior experiments, BOLD-100 showed low nanomolar IC50 values, a magnitude lower (1/10th) than the IC50 values of Gilead’s remdesivir, the only currently approved therapeutic for COVID-19.
Study performed at the Western University 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.