Amyvid ® (florbetapir F18 injection)

500-1900 MBq/mL

This information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling. See Prescribing Information above, if applicable.

How does Amyvid® (florbetapir F 18) work?

Amyvid (florbetapir F 18) binds to β-amyloid plaques and the F 18 isotope produces a positron signal that is detected by a PET scanner.

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Florbetapir F 18 Mechanism of Action

Florbetapir F 18 is a fluoropegylated stilbene derivative that reversibly binds to β-amyloid plaques. The positron signal produced by the F 18 isotope is detected by a positron emission tomography (PET) scan.1,2

In in vitro binding studies using postmortem human brain homogenates containing β-amyloid plaques, the

  • dissociation constant, Kd, for florbetapir was 3.7±0.3 nM,2 and
  • inhibition constant, Ki, was 2.87±0.17 nM.1

Correlation of Florbetapir F 18 Binding With Aβ Aggregation and β-Amyloid Plaque Deposition in Postmortem Brain Tissue

High-affinity (Ki1=1.0 nM) and low-affinity (Ki2=65 nM) binding sites have been identified for florbetapir in brain tissue from the frontal cortices of patients with Alzheimer's disease (AD).3

Although the exact binding site of florbetapir F 18 on β-amyloid plaques is unknown, the binding of florbetapir F 18 to amyloid beta (Aβ) aggregates was demonstrated in postmortem human brain sections using

  • autoradiographic methods, thioflavin S, and traditional silver staining correlation studies, and
  • monoclonal antibody Aβ-specific correlation studies.2,4

Florbetapir F 18 autoradiography (ARG) was performed on sections of postmortem human brain tissue from 40 older subjects with or without AD or other age-related pathologies.4

The intensity of ligand signal was found to correlate with

Florbetapir F 18 binding to tau protein and a battery of neuroreceptors was not detected in in vitro studies.2

Correlation Coefficients and P Values for Measures of Florbetapir F 18 Binding and Scores of Plaques or Neurofibrillary Tangles in 16 Brain Tissue Samples4

Comparisona

r

P Value

Florbetapir (F 18) ARG OD vs plaque score

0.95

<.0001

Florbetapir (F 18) binding Bmax vs plaque score

0.88

<.0001

Florbetapir (F 18) ARG OD vs Bmax

0.95

<.0001

Florbetapir (F 18) ARG OD vs tangle score

0.33

.21

Florbetapir (F 18) binding Bmax vs tangle score

0.20

.45

Abbreviations: ARG = autoradiography; Bmax = amount of florbetapir F 18 required to saturate binding sites; OD = optical density; r = correlation coefficient.

aTissue samples obtained from Banner Sun Health Research Institute.

Correlation Coefficients and P Values of Aβ Density Evaluated by Bielschowsky Silver Staining, Aβ IHC, Thioflavin S Fluorescence Microscopy, and Florbetapir F 18 ARG Signal Intensity in 22 Brain Tissue Samples4

Comparisona

r

P Value

Florbetapir (F 18) ARG OD vs β-amyloid NP score (silver stain)

0.71

.0013

Florbetapir (F 18) ARG OD vs β-amyloid NP (thioflavin S)

0.81

<.0001

Florbetapir (F 18) ARG OD vs tangles score (silver stain)

0.31

.1404

Florbetapir (F 18) ARG OD vs Aβ by 6F/3D IHC

0.75

<.0001

Florbetapir (F 18) ARG OD vs 4G8 IHC

0.82

<.0001

Florbetapir (F 18) ARG OD vs Aβ by 10D5 IHC

0.88

<.0001

Abbreviations: Aβ = amyloid beta; ARG = autoradiography; IHC = immunohistochemistry; NP = neuritic plaque; OD = optical density; r = correlation coefficient.

aTissue samples obtained from Rush Alzheimer’s Disease Center.

References

The published references below are available by contacting 1-800-LillyRx (1-800-545-5979).

1Choi SR, Golding G, Zhuang Z, et al. Preclinical properties of 18F-AV-45: a PET agent for Aβ plaques in the brain. J Nucl Med. 2009;50(11):1887-1894. http://dx.doi.org/10.2967/jnumed.109.065284

2Amyvid [package insert]. Indianapolis, IN: Eli Lilly and Company; 2019.

3Ni R, Gillberg P, Bergfors A, et al. Amyloid tracers detect multiple binding sites in Alzheimer’s disease brain tissue. Brain. 2013;136(7):2217-2227. http://dx.doi.org/10.1093/brain/awt142

4Choi SR, Schneider JA, Bennett DA, et al. Correlation of amyloid PET ligand florbetapir F 18 binding with Aβ aggregation and neuritic plaque deposition in postmortem brain tissue. Alzheimer Dis Assoc Disord. 2012;26(1):8-16. http://dx.doi.org/10.1097/WAD.0b013e31821300bc

Date of Last Review: November 15, 2021


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