Fluciclovine (18F) API Manufacturers

General Description:

Fluciclovine (18F), identified by CAS number 222727-39-1, is a notable compound with significant therapeutic applications. Fluciclovine is a -tagged synthetic analog of the amino acid L-leucine. It presents excellent diagnostic properties to be used in positron emission tomography (PET) imaging. The structure of fluciclovine allows it to be uptaken by the tumoral cells by its amino acid transporter without incorporating in the metabolism within the body. Fluciclovine was developed by Blue Earth Diagnostics, Ltd. and FDA approved in May 27, 2016.

Indications:

This drug is primarily indicated for: Fluciclovine is indicated as a detection agent for positron emission tomography (PET) in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment. The overexpression of L-type amino acid transporters such as LAT1 and LAT3 that mediate the uptake of essential amino acids has been extensively reported as a tumoral mechanism of cell growth. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Fluciclovine (18F) undergoes metabolic processing primarily in: Fluciclovine is not metabolized and it is not incorporated into newly synthesized proteins. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Fluciclovine (18F) are crucial for its therapeutic efficacy: After intravenous administration of fluciclovine, the major distribution happens in liver (14%), red bone marrow (12%), lung (7%), myocardium (4%) and pancreas (3%). With increasing time, the dose gets distributed into skeletal muscle. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Fluciclovine (18F) is an important consideration for its dosing schedule: Fluciclovine is a cyclotron produced radionuclide that decays by positron emission (ß+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen 18 with a physical half-life of 109.7 minutes. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Fluciclovine (18F) exhibits a strong affinity for binding with plasma proteins: Pre clinical studies showed that fluciclovine does not bind 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 Fluciclovine (18F) from the body primarily occurs through: In the first four hours post-injection, 3% of administered dose is excreted in the urine which increases to 5% after 24 hours post-injection. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Fluciclovine (18F) is distributed throughout the body with a volume of distribution of: The compartmental volume of distribution of fluciclovine is in prostate 0.97 L, vesicle 0.79 L, red bone marrow 0.98 L, gluteus muscle 2.13 L and obturator muscle 2.23 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Fluciclovine (18F) is a critical factor in determining its safe and effective dosage: Fluciclovine renal clearance and excretion is minimal. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Fluciclovine (18F) exerts its therapeutic effects through: Following intravenous administration, the tumor-to-normal tissue contrast is highest between 2 and 10 minutes after injection, with a 63% reduction in mean tumor uptake at 90 minutes after injection. The scanning time point should be evaluated carefully as an early scanning can present an increased blood pool and a late scanning will translate into an increased muscle uptake. These variations should always be considered in the image interpretation. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Fluciclovine (18F) functions by: Fluciclovine is transported into the prostate cancer cells via ASCT2 and LAT1 transporters. The activity of LAT1 gets increased in acidic pH, condition that is developed intra-tumorally at certain size. The uptake of fluciclovine presents an androgen-dependent dynamic in hormone sensitive cells. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Fluciclovine (18F) belongs to the class of organic compounds known as l-alpha-amino acids. These are alpha amino acids which have the L-configuration of the alpha-carbon atom, classified under the direct parent group L-alpha-amino acids. This compound is a part of the Organic compounds, falling under the Organic acids and derivatives superclass, and categorized within the Carboxylic acids and derivatives class, specifically within the Amino acids, peptides, and analogues subclass.

Categories:

Fluciclovine (18F) is categorized under the following therapeutic classes: Cycloparaffins, Diagnostic Radiopharmaceuticals, Positron Emitting Activity, Radioactive Diagnostic Agent, Tumour Detection. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Fluciclovine (18F) include:

• Water Solubility: Soluble
• Melting Point: 0ºC
• Boiling Point: 100ºC
• Radioactivity: 10