Tracers / [177Lu]Lu-AMTG

[177Lu]Lu-AMTG

Also written as [Lu-177]Lu-AMTG; Lu-177-AMTG
Radionuclide
Lu-177 t½ 9584.6 min
Modality
Therapy
Production route
Stage
first-in-human
Syntheses indexed
5

What it is

Compound class
GRPR-targeting radiolabeled peptide (α-Me-Trp8-RM2 antagonist analog, DOTA-conjugated)
Target / mechanism
Gastrin-releasing peptide receptor (GRPR) antagonist PMID 38124121
Clinical application
GRPR-targeted radiopharmaceutical therapy of GRPR-expressing malignancies, including metastatic castration-resistant prostate cancer PMID 40306971
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
nonequantitativemore than 95%AMTG (α-Me-Trp8]RM2)40890559
2025 EJNMMI Res
Manual synthesis>98%>98%AMTG precursor40306971
2025 J Nucl Med
177Lu-labeling was performed manually using 25 μg/GBq of AMTG precursor — resulted in radiochemical yields and purities exceeding 98%
AMTG38124121
2024 J Nucl Med
Manual synthesisnonequantitative>98%AMTG (α-Me-l-Trp8-RM2)35027371
2022 J Nucl Med
177Lu labeling of all compounds was performed manually — 177Lu labeling of all compounds was performed manually, each resulting in quantitative radiochemical yields
AMTG42429818
2026 Eur J Nucl Med Mol Imaging
161Tb- and 177Lu-Labeling was completed at 90 °C within 10 min (1.0 M sodium acetate buffer, pH = 5.5, molar activity of ~ 50 MBq/nmol)

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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) -- 4 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 40890559: '[α-Me-Trp8]RM2 (= AMTG)'. Stage set/updated at stage 23 from PMID 40306971: 'First-in-Human Serum Stability Studies of [177Lu]Lu-AMTG: A Step Toward Improved GRPR-Targeted Radiopharmaceutical Therapy.'.