Tracers / [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 study
Syntheses indexed
1
Prostate cancerDosimetry and biodistribution studiesPreclinical only, no clinical indication yetPeptide 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
—

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

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Manual synthesis———more than 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.

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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.'.