Tracers / [18F]LBT999

[18F]LBT999

Also written as [18F]LBT-999; [18F]LBT999; [F-18]LBT-999; [F-18]LBT999

Radionuclide: F-18 t½ 109.77 min
Modality: PET
Production route: —
Stage: Phase III clinical trial
Syntheses indexed: 3

CNS receptor and transporter imaging

What it is

Compound class: 8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester derivative (tropane analogue)
Target / mechanism: dopamine transporter (DAT) PMID 33196944
Clinical application: PET imaging of dopamine transporter in human brain PMID 33196944
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
TRACERlab FX FN GE HealthCare	fixed tubing	HPLC+SPE	35.3 ± 5.1 yes	99.4 ± 0.2	chlorinated precursor 4 Orphachem	33196944 2020 EJNMMI Radiopharm Chem [18F]LBT999 was produced on a TRACERlab FXFN for the Phase I study — the radiochemical yield of [18F]LBT999 was 35.3 ± 5.1% (23.3% activity yield)
AllinOne (AiO) Trasis	vendor cassette	HPLC+SPE	32.7 ± 5.9 yes	98.3 ± 0.5	chlorinated precursor 4 Orphachem	33196944 2020 EJNMMI Radiopharm Chem production was also implemented on an AllinOne (AIO) system requiring a single use cassette — [18F]LBT999 in 32.7% yield (decay-corrected) within 48 min (n = 5)
iMiDEV PMB-Alcen	vendor cassette	HPLC	10 ± 1%	>98%	chloro-precursor (8-((E)-4-chloro-but-2-enyl)-3-beta-p-tolyl-8-aza-bicyclo[3.2.1]octane-2-beta-carboxylicacid methyl ester) ERAS Labo, France	39692929 2024 EJNMMI Radiopharm Chem the iMiDEV™ radiosynthesiser — RCYa–17 ± 6%10 ± 1%11%

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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); 2 article(s) with F-18. Compound class inferred from precursor name (not stated outright) -- PMID 39692929: '8-((E)-4-chloro-but-2-enyl)-3-beta-p-tolyl-8-aza-bicyclo[3.2.1]octane-2-beta-carboxylicacid methyl ester'. Stage set/updated at stage 23 from PMID 33196944: '[18F]LBT999 was produced on a TRACERlab FXFN for the Phase I study but for Phase III and a potent industrial production transfer, production was also implemented on an AllinOne (AIO) system'.