Tracers / [68Ga]Ga-DO3A-VS-Cys40-Tuna-2

[68Ga]Ga-DO3A-VS-Cys40-Tuna-2

Also written as [68Ga]Ga-DO3A-Tuna-2; [68Ga]Ga-DO3A-VS-Cys40-S01-GCG; [68Ga]Ga-DO3A-VS-Cys40-Tuna-2; [Ga-68]Ga-DO3A-VS-Cys40-Tuna-2

Radionuclide: Ga-68 t½ 67.71 min
Modality: PET
Production route: —
Stage: —
Syntheses indexed: 1

Metabolic drug-receptor occupancy imaging (GLP-1R, GIPR)

What it is

Compound class: DO3A-conjugated peptide analogue (glucagon receptor-binding peptide, DO3A-VS-Cys40-Tuna-2)
Target / mechanism: Glucagon receptor (GCGR) binding PMID 32752075
Clinical application: PET microdosing study for quantification of GCGR occupancy by an anti-diabetic drug in humans PMID 32752075
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
Modular-Lab PharmTracer Eckert & Ziegler	vendor cassette	SPE	45.2 ± 2.5% no	98.9 ± 0.6%	DO3A-VS-Cys40-Tuna-2 Sanofi	32752075 2020 Pharmaceuticals (Basel) Modular-Lab PharmTrace (Eckert & Ziegler, Eurotope, Germany) — The non-decay-corrected radiochemical yield was 45.2 ± 2.5% (n = 3, process validation)

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Quality control Preliminary — inferred from compound class

Ph. Eur. monograph: —
USP monograph: —

AppearancepHRCP HPLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrityMolar activityMetal impuritiesGe-68 breakthrough

How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); radiometal tracer -> metal impurities (rule); Ga-68, generator production assumed (no synthesis data found) -> Ge-68 breakthrough (preliminary); 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); 1 article(s) with Ga-68. Compound class inferred from precursor name (not stated outright) -- PMID 32752075: 'The active pharmaceutical ingredient starting material DO3A-VS-Cys40-Tuna-2 (GMP-grade) was provided by Sanofi Aventis.'. | Stage 28: added indication(s) end-receptor-occupancy from consolidated missing-rubric review.