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Dotamtate Pb-212

Development stage
Phase 2
Lead developer
Radiomedix
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

Dotamtate Pb-212 (also known as 212Pb-DOTAMTATE or AlphaMedix) is a targeted radiopharmaceutical therapy designed for the treatment of somatostatin receptor-positive neuroendocrine tumors (NETs). It consists of three main components: the radioisotope Lead-212 (an in vivo generator of alpha-emitting particles), the chelator DOTAM (which stably binds Lead-212), and the somatostatin analogue Dotamtate that targets somatostatin receptors—particularly SSTR2—on tumor cells. Upon intravenous administration, Dotamtate Pb-212 selectively binds to SSTR-expressing tumor cells and delivers potent alpha radiation directly to these malignant cells. The short-range but high-energy alpha emissions induce complex DNA damage in target cells, leading to cell death while minimizing harm to surrounding healthy tissue. This mechanism offers an advantage over beta-emitting therapies by providing more effective cytotoxicity for resistant or advanced NETs. Clinical development has included Phase I and II trials for NETs[1][4][5][6].

Brand names
alphamedix
Other names
lead-212 dotamtatelead212 dotamtatelead 212 dotamtatepb-212-dotamtatepb212-dotamtatepb 212-dotamtate
02

Targets

SSTR (Somatostatin receptors)SSTR2 (Somatostatin receptor type 2)

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