LiPyDau

LiPyDau is a pegylated liposomal nanoformulation of 2-pyrrolino-daunorubicin (PyDau), an ultra-potent derivative of the anthracycline daunorubicin. PyDau exhibits cytotoxicity up to 1000-fold greater than daunorubicin or doxorubicin but possesses an extremely narrow therapeutic window that prevents its use as a free drug. Encapsulation within pegylated liposomes (LiPyDau) significantly reduces systemic toxicity while facilitating preferential accumulation in tumor tissues via the enhanced permeability and retention (EPR) effect. The drug exerts its anticancer effect through a unique mechanism involving DNA intercalation and the formation of stable covalent interstrand crosslinks via its reactive pyrrolino-group, leading to catastrophic replication stress and double-strand breaks. LiPyDau has shown curative potential in aggressive preclinical models, including BRCA1-deficient triple-negative breast cancer and patient-derived lung adenocarcinoma, and is notably effective against tumors with P-glycoprotein-mediated multidrug resistance.

Other names

liposomal 2-pyrrolino-daunorubicinliposomal2-pyrrolino-daunorubicinliposomal-2-pyrrolino-daunorubicinliposomal PyDau