Florbetapir (18F) API Manufacturers

General Description:

Florbetapir (18F), identified by CAS number 956103-76-7, is a notable compound with significant therapeutic applications. 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.

Indications:

This drug is primarily indicated for: 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. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Florbetapir (18F) undergoes metabolic processing primarily in: 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 AV-160 (desmethyl-AV-45), AV-267 (N-acetyl–AV-160), and an -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 AV-45 brain PET image (Wong et al, 2010). This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Florbetapir (18F) are crucial for its therapeutic efficacy: 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. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Route of Elimination:

The elimination of Florbetapir (18F) from the body primarily occurs through: 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. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Pharmacodynamics:

Florbetapir (18F) exerts its therapeutic effects through: 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. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Florbetapir (18F) functions by: 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. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Florbetapir (18F) belongs to the class of organic compounds known as styrenes. These are organic compounds containing an ethenylbenzene moiety, classified under the direct parent group Styrenes. This compound is a part of the Organic compounds, falling under the Benzenoids superclass, and categorized within the Benzene and substituted derivatives class, specifically within the Styrenes subclass.

Categories:

Florbetapir (18F) is categorized under the following therapeutic classes: Alcohols, Amines, Central Nervous System, Diagnostic Radiopharmaceuticals, Drugs that are Mainly Renally Excreted, Fluorine Radioisotopes, Glycols, Positron Emitting Activity, Radioactive Diagnostic Agent. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.