actinium-225 DOTA-(Tyr3)-octreotide

Actinium-225 DOTA-(Tyr3)-octreotide (also known as actinium-225 DOTATOC or $^{225}\text{Ac-DOTATOC}$) is a clinical-stage targeted alpha-particle therapeutic radiopharmaceutical. It consists of the alpha-emitting radionuclide actinium-225 conjugated via the chelator DOTA to edotreotide (DOTATOC), a synthetic somatostatin analog. The peptide moiety selectively targets somatostatin receptor subtype 2 (SSTR2), which is highly overexpressed on gastroenteropancreatic neuroendocrine tumors (GEP-NETs). Upon binding and internalization, the decay cascade of actinium-225 delivers highly localized, high-energy alpha radiation directly to the tumor cells, causing double-strand DNA breaks and subsequent cell death while minimizing damage to surrounding healthy tissues. The drug is primarily developed through academic collaborations, notably between the European Commission Joint Research Centre (JRC) Karlsruhe, University Hospital Heidelberg, and Zentralklinik Bad Berka, and is being evaluated as a salvage therapy for patients refractory to conventional beta-emitting radioligand therapies.

Other names

225Ac-DOTA-TOC225Ac-DOTATOC225Ac-edotreotideAc-225 DOTA-(Tyr3)-octreotideAc-225 DOTATOCAc225 DOTATOCAc 225 DOTATOCAc-225-DOTA-TOCAc225-DOTA-TOCAc 225-DOTA-TOCAc-225-DOTATOCAc225-DOTATOCAc 225-DOTATOCactinium-225 DOTA-TOCactinium225 DOTA-TOCactinium 225 DOTA-TOCactinium-225 DOTATOCactinium225 DOTATOCactinium 225 DOTATOCactinium-225 edotreotideactinium225 edotreotideactinium 225 edotreotide