actinium-225 dotatate

Actinium-225 DOTATATE is a targeted radiopharmaceutical therapy composed of the somatostatin analog tyrosine^3-octreotate (TATE), conjugated via the chelator DOTA to the alpha-emitting radioisotope actinium‑225. It specifically binds to somatostatin receptor type 2 (SSTR2), which are highly expressed on neuroendocrine tumor cells. Upon binding, the drug is internalized and delivers a cytotoxic dose of alpha radiation directly to SSTR-expressing tumor cells, causing lethal double-strand DNA breaks and cell death. This mechanism allows for potent and localized antitumor activity with reduced damage to surrounding healthy tissue. Actinium‑225 DOTATATE is being developed primarily for patients with gastroenteropancreatic neuroendocrine tumors (GEP-NETs), especially those refractory to prior beta-emitting peptide receptor radionuclide therapies such as lutetium‑177 DOTATATE. The drug is currently under clinical investigation in Phase 3 trials by RayzeBio[1][2][4][5][7].

Brand names

RYZ101RYZ-101RYZ 101

Other names

actinium oxodotreotide ac-225actinium (ac 225) oxodotreotide