Tracers / [18F]PARPi

[18F]PARPi

Also written as [18F]PARPi; [F-18]PARPi

Radionuclide: F-18 t½ 109.77 min
Modality: PET
Production route: —
Stage: clinical trials
Syntheses indexed: 2

What it is

Compound class: PARP inhibitor-based small molecule (phthalazinone/niraparib-type PARP1 inhibitor)
Target / mechanism: —
Clinical application: —
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
AllinOne (AiO) Trasis	vendor cassette	HPLC+SPE	20.5 ± 3.4% no	≥97%	PARPi precursor Theragnostics Ltd.	35890164 2022 Pharmaceuticals (Basel) the synthesis was automated on a Trasis AllinOne platform equipped with a Knauer pump — obtaining an RCY of 20.5 ± 3.4% n.d.c. (calculated on the final, reformulated product)
Manual synthesis	—	HPLC	9.6% no	—	tert-butyl 4-(4-fluoro-3-(4-(4-nitrobenzoyl)piperazine-1-carbonyl)benzyl)-1-oxophthala-zine-2(1H)-carboxylate	32391930 2020 J Labelled Comp Radiopharm the yield of the manual synthesis, in our hands, has shown to be highly sensitive to precursor purity — yielding [18F]PARPi in 9.6% (non-decay corrected)

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Quality control Preliminary — inferred from compound class

Ph. Eur. monograph: —
USP monograph: —

AppearancepHRCP HPLCRCP TLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrity

How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); organic-phase radiosynthesis assumed from isotope/compound class, no synthesis data confirming it -> GC residual solvents (preliminary); conventional nucleophilic 18F-fluorination assumed from isotope/compound class, no synthesis data confirming K222 use -> Kryptofix test (preliminary)

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); 7 article(s) with F-18. Compound class inferred from precursor name (not stated outright) -- PMID 32391930: 'tert-butyl 4-(4-fluoro-3-(4-(4-nitrobenzoyl) piperazine-1-carbonyl) benzyl)-1-oxophthala-zine-2(1H)-carboxylate in 300 μL of dry DMSO was added'. Stage set/updated at stage 23 from PMID 35890164: '[18F]PARPi is currently undergoing clinical trials as a PET tracer for many applications.'.