Tracers / [212Pb]Pb-DOTAMTATE

[212Pb]Pb-DOTAMTATE

Also written as [Pb-212]Pb-DOTAMTATE; Pb-212-DOTAMTATE

Radionuclide: Pb-212 t½ 638.4 min
Modality: Therapy
Production route: —
Stage: preclinical
Syntheses indexed: 3

What it is

Compound class: DOTAM-chelated somatostatin analogue (octreotate-based peptide, SSTR2-targeting)
Target / mechanism: Somatostatin receptor type 2 (SSTR2)-targeting octreotate analogue PMID 37513897
Clinical application: Peptide receptor radionuclide therapy (targeted alpha therapy) for somatostatin receptor-positive neuroendocrine tumors PMID 37513897
Theranostic pair: —

Regulatory status

FDA: —
EMA (centralised): —
Other approvals: —
Brand names: —

Clinical use

Typical injected activity: —
Uptake time: —

Reported in the literature. Not a dosing recommendation.

Published syntheses

Module	Cassette	Purification	Yield %	RCP %	Precursor / supplier	Source
Manual synthesis	—	—	96.5%	>95%	DOTAMTATE (C65H93N17O16S2) Macrocyclics	39884771 2025 J Nucl Med Chelation was performed by incubating 27.5 nmol of peptide per 444 MBq of 212Pb for 10 min at room temperature in 0.4 M ammonium acetate buffer, with a pH of 6.1. — 10 min at RT96.5% ± 0.7%
Manual synthesis	—	none	≥96%	≥95%	DOTAM-TATE	37513897 2023 Pharmaceuticals (Basel) [203Pb]PbCl2 (40 MBq) in 0.5 M HCl ... was added to a mixture of DOTAM-TATE or eSOMA-(01-03) (1 nmol), ascorbic acid/gentisic acid (10 μL, 50 mM), sodium acetate (30 μL, 2.5 M), and H2O (final volume of 140 μL). The mixture was incubated for 20 min at rt. — All labeled compounds were obtained with a RCY ≥ 96% and a RCP ≥ 95%.
Manual synthesis	—	—	—	>95%	GMP DOTAMTATE Macrocyclics	30926632 2019 Mol Cancer Ther DOTAMTATE was added to purified 212Pb at a ratio of 2.4μCi/ng and incubated at 50°C for 10 minutes with shaking at 300rpm.

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Notes

Added at stage 21 from therapy-discovered.xlsx (bulk PubMed search by isotope/therapy-type/known-agent, not individually researched yet) -- 3 articles found. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Compound class inferred from precursor name (not stated outright) -- PMID 30926632: 'GMP DOTAMTATE (C65H93N17O16S2, Figure 1) was manufactured by Macrocyclics using Fmoc solid phase peptide synthesis.'. Stage set/updated at stage 23 from PMID 30926632: 'Preclinical Investigation of 212Pb-DOTAMTATE for Peptide Receptor Radionuclide Therapy in a Neuroendocrine Tumor Model.'.