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BOLD-100
- Development stage
- Phase 2
- Lead developer
- Bold Therapeutics
- Modality
- Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
BOLD-100 is a first-in-class ruthenium-based small molecule anticancer agent developed for the treatment of solid and liquid tumors, particularly gastrointestinal cancers. Its mechanism of action is multimodal and includes selective inhibition of Glucose-regulated protein 78 leading to alteration of the unfolded protein response (UPR), induction of endoplasmic reticulum stress, production of reactive oxygen species (ROS), DNA damage, cell cycle arrest at G2/M phase, and ultimately apoptosis. BOLD-100 can synergize with cytotoxic chemotherapies and targeted agents to improve cancer cell death. It has shown activity in preclinical models as well as in clinical trials when combined with FOLFOX chemotherapy for advanced gastrointestinal cancers such as colon, gastric, pancreatic, and biliary tract cancers. The drug is administered intravenously as a lyophilized powder for parenteral use[1][2][4][5][6].
- Brand names
- BOLD-100BOLD100BOLD 100
- Other names
- sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)]
02
Targets
HSPA5 (Heat shock protein family A member 5)DNA
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