Tracer library / [177Lu]Lu-DOTA-PP-F11N

[177Lu]Lu-DOTA-PP-F11N

Also written as [177Lu]Lu-DOTA-PP-F11N; [Lu-177]Lu-DOTA-PP-F11N

Radionuclide: Lu-177 t½ 9585 min
Modality: Therapy
Production route: —
Stage: Clinical research
Syntheses indexed: 2

Thyroid cancer Receptor expression phenotyping Peptide receptor radionuclide therapy

What it is

Compound class: Minigastrin analogue (CCK-2 receptor-targeting peptide) with DOTA chelator
Target / mechanism: Cholecystokinin-2 receptor (CCK2R) PMID 36558917
Clinical application: Targeted radiotherapy/imaging of CCK2R-expressing tumors, such as Medullary Thyroid Carcinoma (MTC) and Small Cell Lung Cancer (SCLC) PMID 32586246
Theranostic pair: —

Published syntheses

Module	Cassette	Purification	Yield %	RCP %	Precursor / supplier	Source
—	—	none	>95%	>95%	DOTA-PP-F11N	36558917 2022 Pharmaceuticals (Basel)
Manual synthesis	—	none	>99%	≥95%	DOTA-PP-F11N	42477299 2026 EJNMMI Radiopharm Chem After radiolabeling at 90 °C for 15 min, 10 µL of 0.1 M sodium L-ascorbate (in PBS) was added. - 177Lu-Labeling afforded the reference compounds [177Lu]Lu-DOTA-PP-F11N ([177Lu]Lu-2) and [177Lu]Lu-DOTA-CCK-66 ([177Lu]Lu-4) in quantitative radiochemical yields (RCY > 99%)

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Quality control Preliminary - inferred from compound class

Ph. Eur. monograph: not verified No Ph. Eur. check is recorded for this entry.
USP monograph: not verified No USP check is recorded for this entry.

AppearancepHRCP HPLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrityOsmolalityMolar activityMetal impuritiesLu-177m

How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); radiometal tracer -> metal impurities (rule); Lu-177 preparation -> Lu-177m content (rule); therapeutic radiopharmaceutical -> osmolality (rule); receptor ligand with a saturable target -> molar activity (rule)

Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived

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Notes

Added from reverse module search (stage 6); 2 article(s) with Lu-177. Compound class inferred from precursor name (not stated outright) -- PMID 36558917: 'DOTA-PP-F11N'. Stage set/updated at stage 39 from PMID 30002107: 'First human data on 177Lu-DOTA-PP-F11N are also reported.'.