BPRDP056

BPRDP056 is an experimental, phosphatidylserine (PS)-targeting prodrug of SN38, the active metabolite of the topoisomerase I inhibitor irinotecan. Developed by the National Health Research Institutes (NHRI) in Taiwan, BPRDP056 is designed to selectively deliver the cytotoxic SN38 payload to the tumor microenvironment. It exploits the externalization of phosphatidylserine on the surface of cancer cells and tumor vascular endothelial cells—a phenomenon typically absent in healthy cells where PS is restricted to the inner leaflet of the plasma membrane. Upon binding to PS, the prodrug is localized to the tumor, where SN38 is released to inhibit DNA topoisomerase I, causing DNA double-strand breaks and cell death. Preclinical studies in head and neck cancer models suggest that BPRDP056 works synergistically with TLR9 agonists, which further increase PS exposure on cancer cells, creating a positive feedback loop for drug targeting.

Other names

Phosphatidylserine-targeting prodrug of SN38