Fluoroestradiol F-18 is a radiolabeled analog of estradiol used as a contrast agent in the PET imaging of 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...
- Mechanism
- Curator reviewed · 2 references
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 Bmax of 1901 ± 89 fmol/mg, and a IC50 = 0.085 nM.
- Primary indication
- 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...Curator reviewed · 2 structured indications
- Formula / weight
- C18H23FO2 · 289.381 g/mol (avg)
- First approval
- United States, 2020
- Also known as
- 16 alpha-fluroestradiol-17 beta · F-18 Fes · Fes F-18 · Fluorine-18 16 alpha-fluoroestradiol
Resolves to
KDLLNMRYZGUVMA-ZYMZXAKXSA-NSMILES[H][C@@]12C[C@@H]([18F])[C@H](O)[C@@]1(C)CC[C@]1([H])C3=C(CC[C@@]21[H])C=C(O)C=C3What you can answer from here — as of August 11, 2025
Which drugs share a target with Fluoroestradiol F-18, and which of those have an active Phase 3 trial?
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