Fludeoxyglucose (18F) API Manufacturers

General Description:

Fludeoxyglucose (18F), identified by CAS number 63503-12-8, is a notable compound with significant therapeutic applications. Fludeoxyglucose F 18 Injection is a positron emitting radiopharmaceutical containing no-carrier added radioactive 2-deoxy-2-fluoro-D-g1ucose, which is used for diagnostic purposes in conjunction with Positron Emission Tomography (PET). It is administered by intravenous injection.

Indications:

This drug is primarily indicated for: The uptake of 18F-FDG by tissues is a marker for the tissue uptake of glucose, which in turn is closely correlated with certain types of tissue metabolism. Fludeoxyglucose F 18 Injection is indicated in positron emission tomography (PET) imaging for assessment of abnormal glucose metabolism to assist in the evaluation of malignancy in patients with known or suspected abnormalities found by other testing modalities, or in patients with an existing diagnoses of cancer. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Fludeoxyglucose (18F) undergoes metabolic processing primarily in: Fludeoxyglucose F 18 is transported into cells and phosphorylated to -FDG-6-phosphate at a rate proportional to the rate of glucose utilization within that tissue. -FDG-6-phosphate presumably is metabolized to 2-deoxy-2- fluoro-6-phospho-Dmannose (FDM-6-phosphate). Fludeoxyglucose F 18 Injection may contain several impurities (e.g, 2-deoxy-2-chloro-D-glucose (ClDG)). Biodistribution and metabolism of C1DG are presumed to be similar to Fludeoxyglucose F 18 and would be expected to result in intracellular formation of 2-deoxy-2-chloro-6-phospho-D-glucose (C1DG-6-phosphate) and 2-deoxy-2-chloro-6-phospho-D-mannose (ClDM-6-phosphate). The phosphorylated deoxyglucose compounds are dephosphorylated and the resulting compounds (FDG, FDM, C1DG, and ClDM) presumably leave cells by passive diffusion. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Fludeoxyglucose (18F) are crucial for its therapeutic efficacy: Fludeoxyglucose F 18 Injection is rapidly distributed to all organs of the body after intravenous administration. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Fludeoxyglucose (18F) is an important consideration for its dosing schedule: 10-13 minutes. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Fludeoxyglucose (18F) exhibits a strong affinity for binding with plasma proteins: The extent of binding of Fludeoxyglucose F 18 to plasma proteins is not known. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Fludeoxyglucose (18F) from the body primarily occurs through: Fludeoxyglucose F 18 is cleared from most tissues within 24 hours and can be eliminated from the body unchanged in the urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Fludeoxyglucose (18F) is distributed throughout the body with a volume of distribution of: Fludeoxyglucose F 18 Injection is rapidly distributed to all organs of the body after intravenous administration. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Fludeoxyglucose (18F) is a critical factor in determining its safe and effective dosage: Fludeoxyglucose F 18 and related compounds are cleared from non-cardiac tissues within 3 to 24 hours after administration. Clearance from the cardiac tissue may require more than 96 hours. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Fludeoxyglucose (18F) exerts its therapeutic effects through: Fludeoxyglucose F 18 Injection is rapidly distributed to all organs of the body after intravenous administration. After background clearance of Fludeoxyglucose F 18 Injection, optimal PET imaging is generally achieved between 30 to 40 minutes after administration. In cancer, the cells are generally characterized by enhanced glucose metabolism partially due to (1) an increase in the activity of glucose transporters, (2) an increased rate of phosphorylation activity, (3) a reduction of phosphatase activity or, (4) a dynamic alteration in the balance among all these processes. However, glucose metabolism of cancer as reflected by Fludeoxyglucose F 18 accumulation shows considerable variability. Depending on tumor type, stage, and location, Fludeoxyglucose F 18 accumulation may be increased, normal, or decreased. Also, inflammatory cells can have the same variability of uptake of Fludeoxyglucose F 18. In the heart, under normal aerobic conditions, the myocardium meets the bulk of its energy requirements by oxidizing free fatty acids. Most of the exogenous glucose taken up by the myocyte is converted into glycogen. However, under ischemic conditions, the oxidation of free fatty acids decreases, exogenous glucose becomes the preferred myocardial substrate, glycolysis is stimulated, and glucose taken up by the myocyte is metabolized immediately instead of being converted into glycogen. Under these conditions, phosphorylated Fludeoxyglucose F 18 accumulates in the myocyte and can be detected with PET imaging. Normally, the brain relies on anaerobic metabolism. In epilepsy, the glucose metabolism varies. Generally, during a seizure glucose metabolism increases. Interictally, the seizure focus tends to be hypometabolic. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Fludeoxyglucose (18F) functions by: Fludeoxyglucose F 18 is a glucose analog that concentrates in cells that rely upon glucose as an energy source, or in cells whose dependence on glucose increases under pathophysiological conditions. Fludeoxyglucose F 18 is transported through the cell membrane by facilitative glucose transporter proteins and is phosphorylated within the cell to FDG-6- phosphate by the enzyme hexokinase. Once phosphorylated it cannot exit until it is dephosphorylated by glucose-6-phosphatase. Therefore, within a given tissue or pathophysiological process, the retention and clearance of Fludeoxyglucose F 18 reflect a balance involving glucose transporter, hexokinase and glucose-6- phosphatase activities. When allowance is made for the kinetic differences between glucose and Fludeoxyglucose F 18 transport and phosphorylation (expressed as the “lumped constant” ratio), Fludeoxyglucose F 18 is used to assess glucose metabolism. In comparison to background activity of the specific organ or tissue type, regions of decreased or absent uptake of Fludeoxyglucose F 18 reflect the decrease or absence of glucose metabolism. Regions of increased uptake of Fludeoxyglucose F 18 reflect greater than normal rates of glucose metabolism. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Fludeoxyglucose (18F) belongs to the class of organic compounds known as beta-hydroxy aldehydes. These are organic compounds containing an aldehyde substituted with a hydroxy group on the second carbon atom, classified under the direct parent group Beta-hydroxy aldehydes. This compound is a part of the Organic compounds, falling under the Organic oxygen compounds superclass, and categorized within the Organooxygen compounds class, specifically within the Carbonyl compounds subclass.

Categories:

Fludeoxyglucose (18F) is categorized under the following therapeutic classes: Carbohydrates, Compounds used in a research, industrial, or household setting, Deoxy Sugars, Deoxyglucose, Diagnostic Radiopharmaceuticals, Diagnostic Uses of Chemicals, Drugs that are Mainly Renally Excreted, Indicators and Reagents, Laboratory Chemicals, Radioactive Diagnostic Agent, Radiopharmaceutical Activity, Radiopharmaceuticals, Tumour Detection. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.