BOLD-100

BOLD-100

BOLD-100 is an experimental cancer drug currently under development. It is a first-in-class ruthenium-based small molecule that selectively inhibits stress-induced upregulation of GRP78, a protective chaperone protein that is overexpressed in many types of cancer.

Mechanism of Action

BOLD-100's mechanism of action involves the selective inhibition of GRP78, a master regulator of the unfolded protein response (UPR). The UPR is a cellular stress response related to the endoplasmic reticulum (ER). In many types of cancer, the UPR is chronically activated, leading to overexpression of GRP78. By inhibiting GRP78, BOLD-100 disrupts the UPR, leading to cell death in cancer cells.

Clinical Development

BOLD-100 is currently in clinical trials for the treatment of various types of cancer. Early phase trials have shown promising results, with evidence of efficacy and a favorable safety profile. The drug is being developed by Bold Therapeutics, a clinical-stage biopharmaceutical company.

Potential Applications

In addition to its potential as a standalone cancer treatment, BOLD-100 may also have applications in combination therapy. Preclinical studies have shown that it can enhance the efficacy of other cancer drugs, including chemotherapy agents and immunotherapy drugs.

See Also

• GRP78
• Unfolded protein response
• Endoplasmic reticulum
• Clinical trial
• Bold Therapeutics
• Chemotherapy
• Immunotherapy