Bismuth-213 labeled CHX-A''-DTPA-functionalized liposome (213Bi-CHX-A''-DTPA-liposome)

Bismuth-213 bound to CHX-A''-DTPA on a liposome surface is a radiotherapeutic agent designed for targeted alpha therapy (TAT). Bismuth-213 is a potent alpha-emitting radioisotope with a short half-life of approximately 46 minutes, making it suitable for treating rapidly accessible tumors or micrometastases (Kim & Brechbiel, 2012). The CHX-A''-DTPA (cyclohexyl-diethylenetriaminepentaacetic acid) moiety serves as a highly stable bifunctional chelator that prevents the premature release of the radionuclide from the delivery vehicle (Milenic et al., 2004). Liposomes are utilized as the carrier system to improve the pharmacokinetic profile and facilitate the delivery of a high payload of radiation directly to the tumor microenvironment (Sofou, 2008). This approach leverages the high linear energy transfer (LET) of alpha particles to induce localized cell death through irreparable DNA damage while sparing distant healthy organs (Sgouros et al., 2010). It is primarily investigated for hematological malignancies and solid tumor micrometastases (Jurcic, 2020).

Other names

213Bi-CHX-A''-DTPA-liposomesBismuth-213 liposomal complexAlpha-emitting liposomal radiopharmaceutical

Targeted alpha therapy (TAT) involving the delivery of alpha-emitting Bismuth-213 to tumor cells via liposomal carriers, resulting in high-LET radiation-induced DNA double-strand breaks and subsequent apoptosis.