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[edit | edit source]
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[edit | edit source]
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[edit | edit source]
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[edit | edit source]
- GRP78
- Unfolded protein response
- Endoplasmic reticulum
- Clinical trial
- Bold Therapeutics
- Chemotherapy
- Immunotherapy
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Contributors: Prab R. Tumpati, MD
