Fes F-18
Fes F-18 Uses, Dosage, Side Effects, Food Interaction and all others data.
Fes 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.
Fes 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.
Fes 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.
| Trade Name | Fes F-18 |
| Generic | Fluoroestradiol F-18 |
| Fluoroestradiol F-18 Other Names | F-18 Fes, Fes F-18 |
| Type | |
| Formula | C18H23FO2 |
| Weight | Average: 289.381 Monoisotopic: 289.170742648 |
| Protein binding | Following intravenous administration, approximately 95% of fluoroestradiol F-18 is protein-bound to both albumin and sex hormone-binding globulin. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Fes F-18 is a radiolabeled analog of estradiol used as a contrast agent in the PET imaging of estrogen receptor-positive breast cancer lesions.
Fes 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.
Fes F-18 is also used to associated treatment for these conditions: Metastatic Estrogen Receptor Positive Breast Cancer, Recurrent Estrogen Receptor Positive Breast Cancer
How Fes F-18 works
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. Fes 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 Bmax of 1901 ± 89 fmol/mg, and a IC50 = 0.085 nM.
Food Interaction
No interactions found.Volume of Distribution
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.
Clearance
Fes F-18 is rapidly cleared from the blood by the liver.
Elimination Route
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.
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