Fluoroestradiol F 18
FDA Drug Information • Also known as: Cerianna
- Brand Names
- Cerianna
- Drug Class
- Radioactive Diagnostic Agent [EPC]
- Route
- INTRAVENOUS
- Dosage Form
- INJECTION
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION 11.1 Chemical Characteristics CERIANNA contains fluoroestradiol fluorine 18 (F 18), a synthetic estrogen analog. Chemically, fluoroestradiol F 18 is [18F]16α-fluoro-3,17β-diol-estratriene-1,3,5(10). The molecular weight is 289.37, and the structural formula is: CERIANNA is a sterile, clear, colorless solution for intravenous injection, with an osmolarity of 340 mOsm. Its pH ranges between 5.5 to 8.0. The composition of the final product in 40 mL solution is fluoroestradiol no more than 5 mcg, fluoroestradiol F 18 148 MBq/mL to 3,700 MBq/mL (4 mCi/mL to 100 mCi/mL), sodium ascorbate 0.44% w/v in sodium chloride 0.9% w/v, and ethanol no more than 3.2% w/v. Chemical Structure 11.2 Physical Characteristics CERIANNA is radiolabeled with F 18, a cyclotron produced radionuclide that decays by positron emission to stable oxygen 18 with a half-life of 109.8 minutes. The principal photons useful for diagnostic imaging are the coincident pair of 511 keV gamma photons, resulting from the interaction of the emitted positron with an electron (Table 2). Table 2. Principal Radiation Produced From Decay of Fluorine 18 Radiation Radiation Energy Level (keV) % Abundance Positron 249.8 96.9 Gamma 511 193.5 11.3 External Radiation The point source air-kerma coefficient for F 18 is 3.75 × 10 -17 Gy m 2 / (Bq s). The first half-value thickness of lead (Pb) for F 18 gamma rays is approximately 6 mm. The relative reduction of radiation emitted by F 18 that results from various thicknesses of lead shielding is shown in Table 3. The use of 8 cm Pb decreases the radiation transmission (i.e., exposure) by a factor of about 10,000. Table 3. Radiation Attenuation of 511 keV Gamma Rays by Lead Shielding Shield Thickness cm of Lead (Pb) Coefficient of Attenuation 0.6 0.5 2 0.1 4 0.01 6 0.001 8 0.0001
What Is Fluoroestradiol F 18 Used For?
1 INDICATIONS AND USAGE CERIANNA is indicated for use with positron emission tomography (PET) imaging for the detection of estrogen receptor (ER)-positive lesions as an adjunct to biopsy in patients with recurrent or metastatic breast cancer. CERIANNA is a radioactive diagnostic agent indicated for use with positron emission tomography (PET) imaging for the detection of estrogen receptor (ER)-positive lesions as an adjunct to biopsy in patients with recurrent or metastatic breast cancer. ( 1 ) Limitations of Use Tissue biopsy should be used to confirm recurrence of breast cancer and to verify ER status by pathology. CERIANNA is not useful for imaging other receptors, such as human epidermal growth factor receptor 2 (HER2) and the progesterone receptor (PR). ( 1 , 5.1 ) Limitations of Use Tissue biopsy should be used to confirm recurrence of breast cancer and to verify ER status by pathology. CERIANNA is not useful for imaging other receptors, such as human epidermal growth factor receptor 2 (HER2) and the progesterone receptor (PR).
Dosage and Administration
2 DOSAGE AND ADMINISTRATION Recommended dose is 222 MBq (6 mCi), with a range of 111 MBq to 222 MBq (3 mCi to 6 mCi), administered as an intravenous injection over 1 to 2 minutes. ( 2.2 ) Recommended imaging start time is 80 minutes (range 20 minutes to 80 minutes) after drug administration. ( 2.4 ) See full prescribing information for additional preparation, administration, imaging, and radiation dosimetry information. ( 2 ) 2.1 Radiation Safety - Drug Handling CERIANNA is a radioactive drug. Only authorized persons qualified by training and experience should receive, use, and administer CERIANNA. Handle CERIANNA with appropriate safety measures to minimize radiation exposure during administration [see Warnings and Precautions (5.2) ] . Use waterproof gloves and effective radiation shielding, including syringe shields, when preparing and handling CERIANNA. 2.2 Recommended Dosage and Administration Instructions Recommended Dosage The recommended amount of radioactivity to be administered for PET imaging is 222 MBq (6 mCi), with a range of 111 MBq to 222 MBq (3 mCi to 6 mCi), administered as a single intravenous injection of 10 mL or less over 1 to 2 minutes. Preparation and Administration For patient preparation instructions, see Dosage and Administration 2.3 . Use aseptic technique and radiation shielding when withdrawing and administering CERIANNA. Visually inspect the radiopharmaceutical solution. Do not use if it contains particulate matter or if it is cloudy or discolored (CERIANNA is a clear, colorless solution). CERIANNA may be diluted with 0.9% Sodium Chloride Injection, USP. Assay the dose in a suitable dose calibrator prior to administration. Post-Administration Instructions Follow the CERIANNA injection with an intravenous flush of 0.9% Sodium Chloride injection, USP. Dispose of any unused CERIANNA in compliance with applicable regulations. 2.3 Patient Preparation Assessment for Drug Interactions Before administering CERIANNA, discontinue drugs that bind to ER (e.g., selective estrogen receptor modulators (SERMs) and selective estrogen receptor down-regulators (SERDs)) [see Drug Interactions (7) ] . Patient Hydration and Voiding Instruct patients to drink water to ensure adequate hydration prior to administration of CERIANNA and to continue drinking and voiding frequently during the first hours following administration to reduce radiation exposure. Pregnancy Status Assessment of pregnancy status is recommended in females of reproductive potential before administering CERIANNA. 2.4 Image Acquisition Position the patient supine with arms above the head, if possible. The recommended start time for image acquisition is 80 minutes after the intravenous administration of CERIANNA. Scan duration adapted from the range of 20 minutes to 30 minutes and imaging start times adapted within the range of 20 minutes to 80 minutes may be customized according to the equipment used and patient and tumor characteristics for optimal image quality. 2.5...
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS Reported adverse reactions include: injection-site pain and dysgeusia ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact GE HealthCare at 1-800-654-0118 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of CERIANNA was evaluated from published clinical studies of 1,207 patients with breast cancer receiving at least one fluoroestradiol F 18 administration. The following adverse reactions occurred at a rate < 1%: General disorders : injection-site pain Neurological and gastrointestinal disorders : dysgeusia
Drug Interactions
7 DRUG INTERACTIONS Drugs that bind to the estrogen receptor (ER) may compete with the binding of fluoroestradiol F 18 and may reduce the detection of ER-positive lesions with CERIANNA. Before administering CERIANNA, discontinue drugs that bind to the ER, such as SERMs and SERDs, for at least 5 biological half-lives (e.g., elacestrant for 11 days, tamoxifen for 8 weeks, and fulvestrant for 28 weeks) [see Dosage and Administration (2.3) ] . Before administering CERIANNA, discontinue drugs that bind to the ER, such as SERMs and SERDs, for at least 5 biological half-lives (e.g., elacestrant for 11 days, tamoxifen for 8 weeks, and fulvestrant for 28 weeks). ( 2.3 , 7 )
Contraindications
4 CONTRAINDICATIONS None . None. ( 4 )
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary All radiopharmaceuticals, including CERIANNA, have the potential to cause fetal harm depending on the fetal stage of development and the magnitude of radiation dose. Advise a pregnant woman of the potential risks of fetal exposure to radiation from administration of CERIANNA. There are no available data on CERIANNA use in pregnant women. No animal reproduction studies using fluoroestradiol F 18 have been conducted to evaluate its effect on female reproduction and embryo-fetal development. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING 16.1 How Supplied CERIANNA is supplied in a 50 mL multiple-dose glass vial (NDC 72874-001-01) containing a clear, colorless injection solution at a strength of 148 MBq/mL to 3,700 MBq/mL (4 mCi/mL to 100 mCi/mL) fluoroestradiol F 18 at the end of synthesis. Each vial contains multiple doses and is enclosed in a shield container to minimize external radiation exposure. 16.2 Storage and Handling Storage Store CERIANNA at controlled room temperature (USP) 20°C to 25°C (68°F to 77°F). Store CERIANNA upright in the original container with radiation shielding. The expiration date and time are provided on the container label. Use CERIANNA within 12 hours from the time of the end of synthesis. Handling This preparation is approved for use by persons under license by the Nuclear Regulatory Commission or the relevant regulatory authority of an Agreement State.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.