Fluoroestradiol F-18 API Manufacturers

General Description:

Fluoroestradiol F-18, identified by CAS number 94153-53-4, is a notable compound with significant therapeutic applications. Fluoroestradiol F-18 is an imaging agent used with positron emission tomography (PET) to detect estrogen receptor-positive breast cancer lesions. The ability to image ER-positive tumors _in vivo_ is advantageous in that, while helping to visualize tumor progression/regression, it may also be used to assess for heterogeneity in ER expression across metastases (i.e. to identify sites that no longer express ER) without the need for multiple biopsies. Fluoroestradiol F-18 was first granted FDA approval in May 2020, and will be developed by PETNET Solutions, Inc. and Zionexa USA under the brand name Cerianna. It is expected to be available in late 2020/early 2021.

Indications:

This drug is primarily indicated for: Fluoroestradiol F-18 is a radioactive diagnostic agent indicated for use with positron emission tomography (PET) imaging for the detection of estrogen receptor-positive lesions as an adjunct to biopsy in patients with recurrent or metastatic breast cancer. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Fluoroestradiol F-18 undergoes metabolic processing primarily in: Fluoroestradiol F-18 is highly extracted and metabolized by the liver - at 2 hours post-administration, only 10% of the total activity is attributable to unmetabolized parent drug. The majority of generated metabolites are products of glucuronide or sulfate conjugation. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Protein Binding:

Fluoroestradiol F-18 exhibits a strong affinity for binding with plasma proteins: Following intravenous administration, approximately 95% of fluoroestradiol F-18 is protein-bound to both albumin and sex hormone-binding globulin. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Fluoroestradiol F-18 from the body primarily occurs through: Elimination is primarily via urinary and biliary excretion. Unbound metabolites comprising mainly glucuronide and sulfate conjugates are secreted in the bile, reabsorbed via enterohepatic circulation, and then renally excreted. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Fluoroestradiol F-18 is distributed throughout the body with a volume of distribution of: As fluoroestradiol and its metabolites undergo enterohepatic circulation, it is found primarily distributed within the hepatobiliary system. It also distributes to the intestines, heart wall, blood, kidney, uterus, and bladder. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Fluoroestradiol F-18 is a critical factor in determining its safe and effective dosage: Fluoroestradiol F-18 is rapidly cleared from the blood by the liver. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Fluoroestradiol F-18 exerts its therapeutic effects through: Fluoroestradiol F-18 is an analog of estradiol that emits small amounts of radioactivity, allowing it to be detected using PET. Following intravenous administration, it accumulates in cancerous tissues expressing estrogen receptors, thus allowing for visualization of these lesions. Fluoroestradiol has a relatively short duration of action - at 2 hours post-injection circulating levels are <5% those at peak concentration. The uptake of fluoroestradiol F-18 is not specific to breast cancer cells and make occur in any tumor cell expressing estrogen receptors, including those arising from the uterus or ovaries. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Fluoroestradiol F-18 functions by: Estrogen receptor (ER)-positive breast cancers are a subset of breast cancers in which the cancerous tissue expresses estrogen receptors - these receptors provide a useful target for imaging and treatment agents. Fluoroestradiol F-18 is a fluorinated analog of estradiol that binds to estrogen receptors, allowing for PET imaging of lesions. Following exposure in an ER-positive breast cancer cell line (MCF-7), it was found that fluoroestradiol F-18 bound with a Kd of 0.13 ± 0.02 nM, a B_max of 1901 ± 89 fmol/mg, and a IC50 = 0.085 nM. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Categories:

Fluoroestradiol F-18 is categorized under the following therapeutic classes: Estradiol Congeners, Estranes, Estrogens, Estrogens, agonists, Fluorine Radioisotopes, Fused-Ring Compounds, Gonadal Hormones, Gonadal Steroid Hormones, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Positron Emitting Activity, Radioactive Diagnostic Agent, Steroids. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.