bismuth-213-DOTATATE

Bismuth-213-DOTATATE (213Bi-DOTATATE) is an investigational radiopharmaceutical designed for targeted alpha therapy (TAT) of neuroendocrine tumors. It consists of the alpha-emitting radionuclide bismuth-213, which has a half-life of approximately 45.6 minutes, conjugated to the somatostatin analogue peptide DOTATATE via a DOTA chelator. The drug specifically targets somatostatin receptors, particularly somatostatin receptor type 2 (SSTR2), which are highly expressed on the surface of neuroendocrine tumor cells. Once bound and internalized, the bismuth-213 isotope delivers high linear energy transfer (LET) alpha radiation, causing localized cytotoxic damage through double-strand DNA breaks while minimizing exposure to surrounding healthy tissues. It is primarily being investigated for patients with gastroenteropancreatic neuroendocrine tumors (GEP-NETs) who are refractory to conventional beta-emitting peptide receptor radionuclide therapies (PRRT) like 177Lu-DOTATATE.

Other names

Bismuth-213-DOTA-Tyr3-octreotateBismuth213-DOTA-Tyr3-octreotateBismuth 213-DOTA-Tyr3-octreotateBismuth-213-DOTA-octreotateBismuth213-DOTA-octreotateBismuth 213-DOTA-octreotate