Tracers / [18F]AV-45

[18F]AV-45

Also written as [18F]AV-45; [18F]florbetapir; [F-18]AV-45; [F-18]florbetapir; AV-45; F-18 AV-45; F-18 Florbetapir
Radionuclide
F-18 t½ 109.77 min
Modality
PET
Production route
Stage
Approved
Syntheses indexed
8

What it is

Compound class
Radiolabelled stilbene derivative (amyloid-binding small molecule)
Target / mechanism
β-amyloid neuritic plaques (Kd approx. 3.7 nM in postmortem brain homogenates) PMID 23527322
Clinical application
PET imaging of the brain to estimate β-amyloid neuritic plaque density in adults with cognitive impairment, for evaluation of Alzheimer's disease and other causes of cognitive decline FDA label NDA202008
Theranostic pair

Regulatory status

FDA
2012, Amyvid, Avid Radiopharmaceuticals (Eli Lilly) FDA (Drugs@FDA/openFDA): NDA202008, approved 2012-04-06
EMA (centralised)
2013, Amyvid, Eli Lilly EMA medicines register export (2026-09-09): EMEA/H/C/002422, 'Authorised', authorised 14 Jan 2013
Other approvals
Brand names
Amyvid

Clinical use

Typical injected activity
370 MBq (10 mCi) as a single IV bolus FDA label NDA202008 (human clinical dosing)
Uptake time
10-minute PET scan performed within 90 minutes after administration FDA label NDA202008

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
TRACERlab FX FN
GE HealthCare
fixed tubingHPLC14.8 ± 2.1%
no
>95%AV-45 precursor (O-tosylated precursor)
Wuxi Jiangyuan Industrial Technology and Trade Corporation
35494660
2022 Front Chem
Radiochemical synthesis and purification of [18F] AV-45 was carried out using a Tracerlab FXF-N Synthesizer — the average non-decay corrected radiochemical yield of [18F]AV-45 was 14.8 ± 2.1% (n = 4)
BNU F-A2custom manifoldSPE33.6 ± 5.2% (no decay corrected); 50.1 ± 7.9% (decay corrected)
yes
> 95%1 (-OTs derivative)21055622
2010 Nucl Med Biol
a radiosynthesis module (BNU F-A2) — the automated synthesis yield was 33.6 ± 5.2% (no decay corrected, n = 4), 50.1 ± 7.9% (decay corrected) in 50 min at a quantity level of 10~100 mCi (370~3700 MBq)
SPE42.7 ± 5.9%
yes
greater than 95%O-tosylated precursor31697847
2020 J Labelled Comp Radiopharm
SPE14.2%>95%37526186
2024 Curr Med Chem
produced in a simple, stable, and repeatable manner on the Tracerlab FXF-N platform — the radiochemical yield was 14.2 % ± 2.7% (n = 6)
31.0%±2.8%
no
>98AV-10538149774
2023 Hell J Nucl Med
can be easily and quickly prepared by the All in One radiochemical synthesis module — the uncorrected synthesis efficiency was about 31.0%±2.8%
31554771
2019 Kaku Igaku
radiopharmaceutical synthesizer NEPTIS plug - 01
25.4±7.7%95.3±2.2%tosylate precursor20638295
2010 Appl Radiat Isot
using a tosylate precursor with Sumitomo modules for radiosynthesis under GMP-compliant conditions — The overall yield was 25.4+/-7.7%
42142951
2026 J Nucl Cardiol

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