BOLD-100 Development Pipeline

Clinical Investigations

BOLD-100 is the most clinically advanced ruthenium-based therapeutic currently in development.

Previously, BOLD-100 successfully completed a Phase 1 monotherapy dose escalation study in advanced cancer patients that showed BOLD-100 was generally safe and well-tolerated with a safety profile suggesting that it could be combined with other anti-cancer therapies.

BOLD-100 has a granted an Orphan Drug Designation (ODD) in pancreatic cancer. An ODD in gastric cancer was recently filed.

BOLD-100 is currently in a Phase 1b clinical trial in combination with FOLFOX for the treatment of advanced gastric, pancreatic, colon and bile duct cancers (NCT04421820).

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Molecular Structure


BOLD-100 is an anticancer agent being developed in combination with standard of care therapies, to improve patient outcomes in difficult to treat cancers. Most current treatment strategies for advanced cancers are either effective in only some patient populations or have high relapse rates - BOLD-100 is designed to be used in combination with these treatments to enhance response rates. BOLD-100 alters the unfolded protein response (UPR) through selective GRP78 inhibition; and induces reactive oxygen species (ROS) which causes DNA damage and cell cycle arrest. Collectively, these effects result in cell death in both sensitive and resistant cancers. BOLD-100 thus has a unique potential to improve patient care in a wide range of solid and liquid tumors when combined with standard therapies.

Molecular Structure


The global fight against COVID-19 (SARS-CoV-2) requires novel therapeutic approaches to improve patient outcomes. BOLD-100 impacts a previously non-targeted pathway that is important for SARS-CoV-2 infection and replication.

  • BOLD-100 was one of four therapeutics selected for funding by the Canadian Government NRC-IRAP program for COVID-19 therapeutic development.
  • Bold Therapeutics has comprehensive preclinical data supporting the use of BOLD-100 against COVID-19.
  • Bold Therapeutics is leading a global consortium of COVID-19 experts.
  • BOLD-100 is initially being developed as a therapeutics for COVID-19, but has potential across a wide range of challenging current and emerging pathogens.
Molecular Structure

Global Development and Collaborations

Bold Therapeutics is working with a leading team of international partners, clinicians and collaborators to develop BOLD-100. We believe collaborations and partnerships are the key to scientific discovery and advancement. Connect with us if you’re interested in collaborating with us to explore the potential of BOLD-100.

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BOLD-100’s clinical scientific and clinical advancements have been presented and published in dozens of peer-reviewed forums.
A full list of publications is available here.
Select papers:

Bakewell S, Conde I, Fallah Y, et al. Inhibition of DNA Repair Pathways and Induction of ROS Are Potential Mechanisms of Action of the Small Molecule Inhibitor BOLD-100 in Breast Cancer. Cancers (Basel). 2020 Sep 16;12(9):2647. View

Neuditschko B, Legin AA, Baier D, et al. Interaction with Ribosomal Proteins Accompanies Stress Induction of the Anticancer Metallodrug BOLD-100/KP1339 in the Endoplasmic Reticulum. Angew Chem Int Ed Engl. 2021 Mar 1;60(10):5063-5068. View

Burris HA, Bakewell S, Bendell JC, et al. Safety and activity of IT-139, a ruthenium-based compound, in patients with advanced solid tumours: a first-in-human, open-label, dose-escalation phase I study with expansion cohort. ESMO Open. 2017;1(6):e000154. Published 2017 Feb 23. View

Bakewell SJ, Rangel DF, Ha DP, et al. Suppression of stress induction of the 78-kilodalton glucose regulated protein (GRP78) in cancer by IT-139, an anti-tumor ruthenium small molecule inhibitor. Oncotarget. 2018;9(51):29698–29714. Published 2018 Jul 3. View

Lizardo MM, Morrow JJ, Miller TE, et al. Upregulation of Glucose-Regulated Protein 78 in Metastatic Cancer Cells Is Necessary for Lung Metastasis Progression. Neoplasia. 2016;18(11):699–710. View

Heffeter P, Atil B, Kryeziu K, et al. The ruthenium compound KP1339 potentiates the anticancer activity of sorafenib in vitro and in vivo. Eur J Cancer. 2013;49(15):3366–3375. View

Gifford JB, Huang W, Zeleniak AE, et al. Expression of GRP78, Master Regulator of the Unfolded Protein Response, Increases Chemoresistance in Pancreatic Ductal Adenocarcinoma. Mol Cancer Ther. 2016;15(5):1043–1052. View

*BOLD-100 is also referred to as KP1339, NKP-1339 and IT-139.