Flutemetamol (18F) is a PET scanning radiopharmaceutical containing the radionuclide fluorine-18. It is indicated 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) or other causes of cognitive decline.
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|Weight||Average: 273.32 |
Flutemetamol F18 is indicated 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) or other causes of cognitive decline.
Following intravenous injection, flutemetamol F 18 diffuses across the human blood-brain barrier and produces a radioactivity signal detectable throughout the brain. Subsequently, cerebral perfusion decreases the brain flutemetamol F 18 content, with differential retention of the drug in cortical areas that contain β-amyloid aggregates compared to areas that lack the aggregates.
|Mechanism of action|
Fluorine-18 (F 18) is a cyclotron-produced radionuclide that decays by positron emission (β+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen-18 with a physical half-life of 109.8 minutes. The positron can undergo annihilation with an electron to produce two gamma rays; the energy of each gamma ray is 511 keV. After flumetamol F18 is given intravenously, it accumulates in beta amyloid plaques in the brain, and thus becomes visible via positron emission tomography (PET).
The time-activity curves for flutemetamol F 18 in the brain of subjects with positive scans shows continual signal increases from time zero through 30 minutes post administration, with stable values thereafter up to at least 120 minutes post-injection. Following intravenous injection of 185 MBq (5 mCi) of Vizamyl in humans, flutemetamol F 18 plasma concentrations declined by approximately 75% in the first 20 minutes post-injection, and by approximately 90% in the first 180 minutes.
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The F 18 in circulation during the 30-120 minutes imaging window in plasma was principally associated with flutemetamol metabolites.
|Route of elimination|
Excretion was found to be approximately 37% renal and 52% hepatobiliary.
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Most commonly reported adverse reactions were flushing (2%), headache (1%), increased blood pressure (2%), nausea (1%), and dizziness (1%).
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|ATC Codes||V09AX04 — Flutemetamol (18f)|
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|FDA label||Download (4.64 MB)|
|Experimental Properties||Not Available|
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|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of organic compounds known as benzothiazoles. These are organic compounds containing a benzene fused to a thiazole ring (a five-membered ring with four carbon atoms, one nitrogen atom and one sulfur atom).|
|Super Class||Organoheterocyclic compounds|
|Sub Class||Not Available|
|Alternative Parents||Phenylalkylamines / Secondary alkylarylamines / Fluorobenzenes / 1-hydroxy-2-unsubstituted benzenoids / Aryl fluorides / Thiazoles / Heteroaromatic compounds / Azacyclic compounds / Organooxygen compounds / Organofluorides / Hydrocarbon derivatives|
|Substituents||1,3-benzothiazole / Phenylalkylamine / 1-hydroxy-2-unsubstituted benzenoid / Fluorobenzene / Halobenzene / Phenol / Secondary aliphatic/aromatic amine / Aryl fluoride / Aryl halide / Monocyclic benzene moiety/ Benzenoid / Heteroaromatic compound / Azole / Thiazole / Azacycle / Secondary amine / Organofluoride / Organohalogen compound / Hydrocarbon derivative / Amine / Organic nitrogen compound / Organic oxygen compound / Organonitrogen compound / Organooxygen compound / Aromatic heteropolycyclic compound|
|Molecular Framework||Aromatic heteropolycyclic compounds|
|External Descriptors||benzothiazoles, secondary amino compound, aromatic amine, ring assembly, fluorine-18 radiopharmaceutical (CHEBI:76611 )|
- Pharmacological action
- General Function:
- Transition metal ion binding
- Specific Function:
- Functions as a cell surface receptor and performs physiological functions on the surface of neurons relevant to neurite growth, neuronal adhesion and axonogenesis. Involved in cell mobility and transcription regulation through protein-protein interactions. Can promote transcription activation through binding to APBB1-KAT5 and inhibits Notch signaling through interaction with Numb. Couples to ap...
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- Amyloid beta A4 protein
- Molecular Weight:
- 86942.715 Da
- Beach TG, Thal DR, Zanette M, Smith A, Buckley C: Detection of Striatal Amyloid Plaques with [18F]flutemetamol: Validation with Postmortem Histopathology. J Alzheimers Dis. 2016 Mar 31;52(3):863-73. doi: 10.3233/JAD-150732. [PubMed:27031469 ]