fluoroestradiol F 18 (Rx)

Brand and Other Names:Cerianna
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 148-3,700 MBq/mL (4-100 mCi/mL) per vial at end of synthesis

Breast Cancer PET Imaging

Indicated for use with positron-emission tomography (PET) imaging to detect estrogen receptor positive (ER+) lesions as an adjunct to biopsy in patients with recurrent or metastatic breast cancer

222 MBq (6 mCi), range of 111-222 MBq (3-6 mCi), administered as a single IV injection of ≤10 mL over 1-2 minutes

Dosing Considerations

Before administration

  • Assess for drug interactions (eg, drugs targeting estrogen receptors)
  • Assess pregnancy status in females of reproductive potential

Limitations of use

  • Use tissue biopsy to confirm recurrence of breast cancer and to verify ER status by pathology
  • Fluoroestradiol F 18 is not useful for imaging other receptors (eg, human epidermal growth factor receptor 2 [HER2], progesterone receptor [PR])

Not indicated

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Interactions

Interaction Checker

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                  Minor (0)

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                    Adverse Effects

                    <1%

                    General disorders: Injection-site pain

                    Neurological and gastrointestinal disorders: Dysgeusia

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                    Warnings

                    Contraindications

                    None

                    Cautions

                    Radiation risks

                    • Diagnostic radiopharmaceuticals expose patients to radiation
                    • Radiation exposure is associated with a dose-dependent increased risk of cancer
                    • Ensure safe drug handling and patient preparation procedures to protect patients and healthcare providers from unintentional radiation exposure

                    Misdiagnosis risks

                    • Inadequate tumor characterization and other ER+ pathology
                      • Breast cancer may be heterogeneous within patients and across time
                      • Fluoroestradiol F 18 images ER and is not useful for imaging other receptors (eg, HER2, PR)
                      • Uptake is not specific for breast cancer and may occur in a variety of ER+ tumors that arise outside of the breast, including uterus and ovaries
                      • Do not use in lieu of biopsy when biopsy is indicated in patients with recurrent or metastatic breast cancer
                    • False-negative scan
                      • A negative scan does not rule out ER+ breast cancer
                      • Pathology or clinical characteristics that suggest a patient may benefit from systemic hormone therapy should take precedence over a discordant negative scan

                    Drug interaction overview

                    • Certain classes of systemic endocrine therapies, including ER modulators and ER down-regulators, block ER, reduce the uptake of fluoroestradiol F 18, and may reduce detection of ER+ lesions after administration
                    • Drugs from these classes (eg, tamoxifen, fulvestrant) may block ER for up to 8-28 weeks, respectively
                    • Do not delay indicated therapy in order to administer fluoroestradiol F 18
                    • Administer fluoroestradiol F 18 before starting systemic endocrine therapies that block ER
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                    Pregnancy & Lactation

                    Pregnancy

                    All radiopharmaceuticals have potential to cause fetal harm depending on fetal stage of development and the magnitude of radiation dose

                    Advise pregnant females of the potential risks of fetal exposure to radiation from administration

                    There are no available data on use during pregnancy

                    No animal reproduction studies have been conducted

                    Lactation

                    There are no data on the presence of fluoroestradiol F 18 in human milk, or its effects on breastfed infants or milk production

                    Lactation studies have not been conducted in animals

                    Advise breastfeeding females to avoid breastfeeding for 4 hr after administration

                    Pregnancy Categories

                    A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                    B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                    C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                    D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                    X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                    NA: Information not available.

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                    Pharmacology

                    Mechanism of Action

                    Fluoroestradiol F 18 binds estrogen receptor (ER)

                    The following binding affinity: Kd = 0.13 ± 0.02 nM, Bmax = 1901 ± 89 fmol/mg, and IC50 = 0.085 nM, was determined in an ER+ human breast cancer cell line (MCF7)

                    Distribution

                    Protein bound: 95%

                    Distributes primarily to hepatobiliary system, and also to small and large intestines, heart wall, blood, kidney, uterus, and bladder

                    Metabolism

                    Metabolized in liver; 20 minutes after injection, ~20% of circulating radioactivity in plasma is in the form of nonmetabolized fluoroestradiol F 18; at 2 hr after injection, circulating fluoroestradiol F 18 levels are <5% of peak concentration

                    Elimination

                    Excretion: Biliary and urinary

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                    Administration

                    IV Preparation

                    Use aseptic technique and radiation shielding when withdrawing and administering

                    Visually inspect solution; do not use if it contains particulate matter or is cloudy or discolored (fluoroestradiol F 18 is a clear, colorless solution)

                    May be diluted with 0.9% NaCl

                    Assay dose in a suitable dose calibrator before administration

                    Patient preparation

                    • Instruct patients to drink water to ensure adequate hydration before administration and continue drinking and voiding frequently during the first hours following administration to reduce radiation exposure

                    Image acquisition

                    • Position patient supine with arms above the head, if possible
                    • Recommended start time for image acquisition is 80 minutes after IV administration
                    • Scan duration adapted from range of 20-30 minutes and imaging start times adapted within range of 20-80 minutes may be customized according to equipment used and patient and tumor characteristics for optimal image quality

                    Image interpretation

                    • Uptake of fluoroestradiol F 18 depends on ER density and function in tumors and physiologic tissue, including liver, ovary, and uterus
                    • Base detection of ER+ tumors on comparison with tissue background outside of organs with high physiologic uptake and regions with high activity due to hepatobiliary and urinary excretion
                    • See radiation dosimetry in prescribing information for specific tissues

                    Radiation safety

                    • Fluoroestradiol F 18 is a radioactive drug; only authorized persons qualified by training and experience should receive, use, or administer
                    • Handle with appropriate safety measures to minimize radiation exposure during administration
                    • Use waterproof gloves and effective radiation shielding, including syringe shields, when preparing and handling

                    IV Administration

                    Administer IV over 1-2 minutes

                    Follow injection with IV flush of 0.9% NaCl

                    Dispose of any unused drug in compliance with radiopharmaceutical regulations

                    Storage

                    Store at 20-25ºC (68-77ºF)

                    Store upright in original container with radiation shielding

                    Expiration date and time are provided on the container label

                    Use within 10 hr from the time of the end of synthesis

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                    Images

                    No images available for this drug.
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                    Patient Handout

                    A Patient Handout is not currently available for this monograph.
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                    Formulary

                    FormularyPatient Discounts

                    Adding plans allows you to compare formulary status to other drugs in the same class.

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                    • Compare formulary status to other drugs in the same class.
                    • Access your plan list on any device – mobile or desktop.

                    The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                    Tier Description
                    1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                    2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                    3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                    4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                    NC NOT COVERED – Drugs that are not covered by the plan.
                    Code Definition
                    PA Prior Authorization
                    Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                    QL Quantity Limits
                    Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                    ST Step Therapy
                    Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                    OR Other Restrictions
                    Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                    Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.