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BOLD-100 + folinic acid + fluorouracil + oxaliplatin
- Development stage
- Unknown
- Lead developer
- Bold Therapeutics
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
BOLD-100 + folinic acid + fluorouracil + oxaliplatin is an investigational combination therapy being developed by Bold Therapeutics for the treatment of advanced gastrointestinal malignancies, including colorectal, pancreatic, gastric, and biliary tract cancers. The regimen combines BOLD-100, a first-in-class ruthenium-based small molecule metallotherapeutic, with the standard-of-care FOLFOX chemotherapy (folinic acid, fluorouracil, and oxaliplatin). BOLD-100 acts by targeting 78 kDa glucose-regulated protein (GRP78), a key chaperone protein in the endoplasmic reticulum, thereby modulating the unfolded protein response (UPR) and inducing endoplasmic reticulum stress. Additionally, it generates reactive oxygen species (ROS) that lead to DNA damage and cell cycle arrest. This multimodal mechanism is designed to overcome resistance to conventional chemotherapies like oxaliplatin. As of 2024, the combination is in Phase 1b/2a clinical trials.
- Brand names
- Eloxatin
- Other names
- BOLD-100 + FOLFOX
02
Targets
Ribosomal protein (Ribosomal protein family)TS (Thymidylate synthase)HSPA5 (Heat shock protein family A member 5)DNA
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