Tracer library / [212Pb]Pb-DOTAM-GRPR1

[212Pb]Pb-DOTAM-GRPR1

Also written as [Pb-212]Pb-DOTAM-GRPR1

Radionuclide: Pb-212 t½ 638.4 min
Modality: Therapy
Production route: —
Stage: Preclinical
Syntheses indexed: 1

Prostate cancer Dosimetry and biodistribution studies Preclinical only, no clinical indication yet Peptide receptor radionuclide therapy

What it is

Compound class: DOTAM-conjugated GRPR-targeting peptide
Target / mechanism: Gastrin-releasing peptide receptor (GRPR)-targeting peptide PMID 39327021
Clinical application: Peptide receptor radionuclide therapy for prostate cancer (preclinical) PMID 39327021
Theranostic pair: —

Published syntheses

Module	Cassette	Purification	Yield %	RCP %	Precursor / supplier	Source
Manual synthesis	—	—	—	>95%	DOTAM-GRPR1 Macrocyclics	39327021 2024 J Nucl Med Chelation was achieved by adding 212Pb in ammonium acetate (Sigma-Aldrich) to DOTAM-GRPR1 alone or in the presence of 5% ethanol (Spectrum Chemical), up to 30 mM ascorbic acid (Honeywell), and 0.02% polysorbate 80 (J.T. Baker). Experiments were conducted for 10 min at either room temperature or 50°C.

Precursor

Common precursor: —
Suppliers seen in the literature: —
Cited suppliers in indexed syntheses: Macrocyclics
Typical final purification: —

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Notes

Added at stage 22: promoted from 'Reported once' (single-article, no diagnostic pair at discovery) because a full-text synthesis with extracted data exists in parsed-therapy.xlsx -- PMID(s): 39327021. 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 39327021: 'DOTAM-GRPR1 (C77H119N23O17, Fig. 1) was manufactured by Macrocyclics using Fmoc solid-phase peptide synthesis.'. Stage set/updated at stage 23 from PMID 39327021: 'Preclinical Investigation of [212Pb]Pb-DOTAM-GRPR1 for Peptide Receptor Radionuclide Therapy in a Prostate Tumor Model.'.