Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H25FN2O3 |
Molecular Weight | 359.425 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC1=CC=C(\C=C\C2=CC=C(OCCOCCOCC[18F])N=C2)C=C1
InChI
InChIKey=YNDIAUKFXKEXSV-CRYLGTRXSA-N
InChI=1S/C20H25FN2O3/c1-22-19-7-4-17(5-8-19)2-3-18-6-9-20(23-16-18)26-15-14-25-13-12-24-11-10-21/h2-9,16,22H,10-15H2,1H3/b3-2+/i21-1
Molecular Formula | C20H25FN2O3 |
Molecular Weight | 359.425 |
Charge | 0 |
Count |
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Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including,
https://investor.lilly.com/releasedetail2.cfm?ReleaseID=662647
Curator's Comment: description was created based on several sources, including,
https://investor.lilly.com/releasedetail2.cfm?ReleaseID=662647
Florbetapir (18F) (trade name AMYViD; also known as florbetapir-fluorine-18 or 18F-AV-45) is a PET scanning radiopharmaceutical compound containing the radionuclide fluorine-18, recently FDA approved as a diagnostic tool for Alzheimer's disease. Florbetapir, like Pittsburgh compound B (PiB), binds to beta-amyloid, however fluorine-18 has a half-life of 110 minutes, in contrast to PiB's radioactive half life of 20 minutes. Wong et al. found that the longer life allowed the tracer to accumulate significantly more in the brains of people with AD, particularly in the regions known to be associated with beta-amyloid deposits. A negative Amyvid scan indicates sparse to no neuritic plaques, and is inconsistent with a neuropathological diagnosis of AD at the time of image acquisition; a negative scan result reduces the likelihood that a patient’s cognitive impairment is due to AD. A positive Amyvid scan indicates moderate to frequent amyloid neuritic plaques; neuropathological examination has shown this amount of amyloid neuritic plaque is present in patients with AD, but may also be present in patients with other types of neurologic conditions as well as older people with normal cognition. Amyvidis an adjunct to other diagnostic evaluations
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: beta-amyloid plaques |
3.7 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Diagnostic | Amyvid Approved UseUsed as a radioactive diagnostic agent for Positron Emission Tomography (PET) imaging of the brain to estimate β-amyloid neuritic plaque density in adult patients with cognitive impairment who are being evaluated for Alzheimer’s Disease (AD) and other causes of cognitive decline. Launch Date2012 |
PubMed
Title | Date | PubMed |
---|---|---|
¹⁸F-labeled 2-phenylquinoxaline derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques. | 2012 Nov |
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¹⁸F-labeled 2-phenylquinoxaline derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques. | 2012 Nov |
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Florbetapir (18F) for brain amyloid positron emission tomography: highlights on the European marketing approval. | 2014 Oct |
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Florbetapir (18F) for brain amyloid positron emission tomography: highlights on the European marketing approval. | 2014 Oct |
Substance Class |
Chemical
Created
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Record UNII |
6W15Z5R0RU
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Validated (UNII)
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WHO-ATC |
V09AX05
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NDF-RT |
N0000177914
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EMA ASSESSMENT REPORTS |
AMYVID (AUTHORIZED: RADIONUCLIDE IMAGING)
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NDF-RT |
N0000175871
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WHO-VATC |
QV09AX05
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9193
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N0000175869
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4285
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Florbetapir F 18
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SUB33779
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DB09149
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6W15Z5R0RU
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66880
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C171884
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C545186
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Florbetapir_(18F)
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CHEMBL1908919
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m5410
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956103-76-7
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1427224
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PRIMARY | RxNorm |
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TARGET->RADIOLIGAND |
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METABOLITE -> PARENT |
The metabolites have shown lower uptake in the brain and lower affinity for binding to beta amyloid thus, it is concluded that there will be minimal interference from the metabolites to the PET image from 18F-AV-45 in the brain.
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METABOLITE INACTIVE -> PARENT |
IN-VIVO
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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