Florbetaben F-18 API Manufacturers

General Description:

Florbetaben F-18, identified by CAS number 902143-01-5, is a notable compound with significant therapeutic applications. Florbetaben is a fluorine-18 (18F)-labeled stilbene derivative used for Positron Emission Tomography (PET) imaging of the brain. It is used for the non-invasive detection of the density of ß-amyloid neuritic plaques in the brain of adult patients with cognitive impairment.

Indications:

This drug is primarily indicated for: Florbetaben is a radioactive diagnostic agent 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:

Florbetaben F-18 undergoes metabolic processing primarily in: In vitro studies show that metabolism of florbetaben is predominantly catalyzed by CYP2J2 and CYP4F2. Almost all F18 radioactivity in urine was excreted as polar metabolites of florbetaben F18 and only trace amounts of florbetaben F18 were detected. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Florbetaben F-18 are crucial for its therapeutic efficacy: Ten minutes after intravenous bolus injection of 300 MBq of Neuraceq in human volunteers, approximately 6% of the injected radioactivity was distributed to the brain. Florbetaben F 18 plasma concentrations declined by approximately 75% at 20 minutes post-injection, and by approximately 90% at 50 minutes. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Florbetaben F-18 is an important consideration for its dosing schedule: 1 hr. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Florbetaben F-18 exhibits a strong affinity for binding with plasma proteins: Florbetaben is 98.5% bound to plasma proteins. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Florbetaben F-18 from the body primarily occurs through: At 12 hours post-administration, approximately 30% of the injected radioactivity had been excreted in urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Pharmacodynamics:

Florbetaben F-18 exerts its therapeutic effects through: Following intravenous administration, Neuraceq crosses the blood brain barrier and shows differential retention in brain regions that contain β-amyloid deposits. Differences in signal intensity between brain regions showing specific and non-specific Neuraceq uptake form the basis for the image interpretation method. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Florbetaben F-18 functions by: Florbetaben F18 is a F18-labeled stilbene derivative, which binds to β-amyloid plaques in the brain. The F 18 isotope produces a positron signal that is detected by a PET scanner. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Florbetaben F-18 belongs to the class of organic compounds known as stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids, classified under the direct parent group Stilbenes. This compound is a part of the Organic compounds, falling under the Phenylpropanoids and polyketides superclass, and categorized within the Stilbenes class, specifically within the None subclass.

Categories:

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