Florbetapir (18F) is a radiopharmaceutical compound containing the radionuclide fluorine-18 bound to the compound florbetapir, a molecule that binds with high affinity to beta amyloid plaque, a peptide that plays a key role in Alzheimer's Disease pathogenesis. Marketed as the product Amyvid, florbetapir 18F 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) and other causes of cognitive decline.
The radionucleide fluorine-18 was chosen as it has a half life of 110 minutes allowing it to accumulate sufficiently in the brain before undergoing positon emission decay.
|External IDs||(18F)AV-45 / 18F-AV-45 / 18FAV-45 / 18FAV45 / AV-45 F-18|
|Product Ingredients||Not Available|
|Approved Prescription Products|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|International Brands||Not Available|
|Brand mixtures||Not Available|
|Weight||Average: 359.432 |
Florbetapir 18F 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) and other causes of cognitive decline.
Following intravenous injection, florbetapir F 18 diffuses across the human blood-brain barrier and produces a radioactivity signal detectable throughout the brain. Subsequently, cerebral perfusion decreases the brain florbetapir F 18 content, with differential retention of the drug in areas that contain β-amyloid aggregates compared to areas that lack the aggregates.
|Mechanism of action|
Florbetapir (18F) is a radiopharmaceutical compound containing the radionuclide fluorine-18 bound to the compound florbetapir, a molecule that binds with high affinity to beta amyloid plaque, a peptide that plays a key role in Alzheimer's Disease pathogenesis. The radionucleide fluorine-18 was chosen as it has a half life of 110 minutes allowing it to accumulate sufficiently in the brain before undergoing positon emission decay.
The time-activity curves for florbetapir F 18 in the brain of subjects with positive scans show continual signal increases from time zero through 30 minutes post-administration, with stable values thereafter up to at least 90 minutes post-injection. Following the intravenous administration of 370 MBq (10 mCi) of florbetapir F 18 to healthy volunteers, the drug was distributed throughout the body with less than 5% of the injected F 18 radioactivity present in the blood by 20 minutes following administration, and less than 2% present by 45 minutes after administration.
|Volume of distribution||Not Available|
|Protein binding||Not Available|
The residual F 18 in circulation during the 30-90 minute imaging window was principally in the form of polar F 18 metabolites. Essentially all radioactivity collected in the urine was present as polar metabolites of florbetapir F 18. Three metabolites have been discovered and identified as [18F]AV-160 (desmethyl-[18F]AV-45), [18F]AV-267 (N-acetyl–[18F]AV-160), and an [18F]-Polar species, the identity of which has not been confirmed. Additionally, although metabolites may make some contribution to signal detection, particularly to the nontarget activity, it is concluded that there will be minimal interference from these radiolabeled metabolites to the amyloid target binding in the [18F]AV-45 brain PET image (Wong et al, 2010).
|Route of elimination|
Whole body scanning following the intravenous injection showed accumulation of radioactivity in the liver within four minutes post-injection, followed by elimination of the radioactivity predominantly through the biliary/gastrointestinal tract with much lower radioactivity detected in the bladder. Essentially all radioactivity collected in the urine was present as polar metabolites of florbetapir F 18.
|Half life||Not Available|
The most common reported adverse reaction was headache, occurring in 2% of patients, followed by musculoskeletal pain, blood pressure increased, fatigue, nausea, and injection site reaction, all occurring in <1% of patients.
|Affected organisms||Not Available|
|Pharmacogenomic Effects/ADRs||Not Available|
|Drug Interactions||Not Available|
|Food Interactions||Not Available|
|ATC Codes||V09AX05 — Florbetapir (18f)|
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||Download (4.31 MB)|
|Experimental Properties||Not Available|
|Predicted ADMET features||Not Available|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of organic compounds known as styrenes. These are organic compounds containing an ethenylbenzene moiety.|
|Class||Benzene and substituted derivatives|
|Alternative Parents||Phenylalkylamines / Secondary alkylarylamines / Alkyl aryl ethers / Pyridines and derivatives / Heteroaromatic compounds / Dialkyl ethers / Azacyclic compounds / Organofluorides / Hydrocarbon derivatives / Alkyl fluorides|
|Substituents||Styrene / Phenylalkylamine / Alkyl aryl ether / Secondary aliphatic/aromatic amine / Pyridine / Heteroaromatic compound / Organoheterocyclic compound / Azacycle / Secondary amine / Dialkyl ether|
|Molecular Framework||Aromatic heteromonocyclic compounds|
|External Descriptors||organofluorine compound, aromatic ether, substituted aniline, pyridines, fluorine-18 radiopharmaceutical (CHEBI:66880 )|
- 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
- Choi SR, Golding G, Zhuang Z, Zhang W, Lim N, Hefti F, Benedum TE, Kilbourn MR, Skovronsky D, Kung HF: Preclinical properties of 18F-AV-45: a PET agent for Abeta plaques in the brain. J Nucl Med. 2009 Nov;50(11):1887-94. doi: 10.2967/jnumed.109.065284. Epub 2009 Oct 16. [PubMed:19837759 ]