Tracers / [18F]T807

[18F]T807

Also written as [18F]AV-1451; [18F]AV1451; [18F]Flortaucipir; [18F]T807; [F-18]AV-1451; [F-18]AV1451; [F-18]Flortaucipir
Radionuclide
F-18 t½ 109.77 min
Modality
PET
Production route
Stage
Approved
Syntheses indexed
9

What it is

Compound class
Radiolabelled carbazole/pyridoindole derivative (tau-binding small molecule)
Target / mechanism
Aggregated tau protein (paired helical filaments) FDA label NDA212123
Clinical application
PET imaging of the brain to estimate the density and distribution of aggregated tau neurofibrillary tangles in adults being evaluated for Alzheimer's disease FDA label NDA212123
Theranostic pair

Regulatory status

FDA
2020, Tauvid, Avid Radiopharmaceuticals (Eli Lilly) FDA (Drugs@FDA/openFDA): NDA212123, approved 2020-05-28
EMA (centralised)
2024, Tauvid, Eli Lilly EMA medicines register export (2026-09-09): EMEA/H/C/006064, 'Authorised', authorised 22 Aug 2024
Other approvals
Brand names
Tauvid

Clinical use

Typical injected activity
Uptake time

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
28241163
2017 JAMA Neurol
TRACERlab FX FN
GE HealthCare
fixed tubingHPLC+SPE14%
no
98 ± 1%N-Boc-protected nitro-precursor
Huayi
29503848
2017 EJNMMI Radiopharm Chem
An optimized [18F]AV1451 synthesis using a TRACERLab FXFN module — 202 ± 57 mCi at end-of-synthesis (EOS) (14% based on starting [18F]fluoride)
TRACERlab FX FN
GE HealthCare
HPLC+SPE14 ± 3%
no
>95%tert-butyl 7-(6-nitropyridin-3-yl)-5H-pyrido[4,3-b]indole-5-carboxylate (1b)
Huayi
24339014
2013 J Labelled Comp Radiopharm
GE Tracerlab™ FXFN radiosynthesis module — The uncorrected RCY of [18F]T807 was 14 ± 3% (n = 3)
TRACERlab FX FN
GE HealthCare
HPLC+SPE2.4%
no
7-(6-nitropyridin-3-yl)-5H-pyrido[4,3-b]indole (1a)
Huayi
24339014
2013 J Labelled Comp Radiopharm
GE Tracerlab™ FXFN radiosynthesis module — The uncorrected radiochemical yield was much lower (2.4%; n = 1)
Synthra RNplusHPLC+SPE14.8-16.6%
no
>99.9%AV162234234995
2021 Am J Nucl Med Mol Imaging
an automated radiosynthesis of [18F]Flortaucipir in a RNplus Research module — The final products were obtained in non-decay corrected radiochemical yields of 14.8-16.6% (n = 3) within total synthesis time of 55 min.
27%
no
>99%31083778
2019 J Labelled Comp Radiopharm
synthesized and formulated using an automated radiosynthesis module — nondecay corrected radiochemical yields of 27% and 29% (relative [18 F]F- ), respectively
5-10%
yes
T807P26048805
2015 Bioorg Med Chem Lett
through manual synthesis with 5-10% decay corrected radiochemical yield in two steps — 5-10% decay corrected radiochemical yield in two steps
HPLC+SPE20-30%
yes
t-Boc-protected T807P26048805
2015 Bioorg Med Chem Lett
in a home-built automated [(18)F]radiosynthesis module with 20-30% decay corrected radiochemical yield in one step — 20-30% decay corrected radiochemical yield in one step
HPLC5 ± 1%
no
≥ 99%25248283
2014 Mol Imaging
adapted to suit a commercial microfluidic flow chemistry module. For this proof of concept, the flow system was integrated to a GE Tracerlab FXFN unit for high-performance liquid chromatography purification and formulation. — an overall uncorrected radiochemical yield of 5 ± 1% (n = 3), relative to starting [18F]fluoride (end of bombardment)

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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); 12 article(s) with F-18.