Fluciclovine F-18
FDA Drug Information • Also known as: Axumin
- Brand Names
- Axumin
- Drug Class
- Radioactive Diagnostic Agent [EPC]
- Route
- INTRAVENOUS
- Dosage Form
- INJECTION, SOLUTION
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION 11.1 Chemical Characteristics Axumin contains the fluorine 18 (F 18) labeled synthetic amino acid analog fluciclovine. Fluciclovine F 18 is a radioactive diagnostic agent used with PET imaging. Chemically, fluciclovine F 18 is (1r, 3r)-1-amino-3[ 18 F]fluorocyclobutane-1-carboxylic acid. The molecular weight is 132.1 and the structural formula is: Axumin is a sterile, non-pyrogenic, clear, colorless, hyperosmolal (approximately 500 mOsm/kg to 540 mOsm/kg) injection for intravenous use. Each milliliter contains up to 2 micrograms of fluciclovine, 335 MBq to 8,200 MBq (9 mCi to 221 mCi) fluciclovine F 18 at calibration time and date, and 20 mg trisodium citrate in water for injection. The solution also contains hydrochloric acid, sodium hydroxide and has a pH between 4 and 6. Structural Formula 11.2 Physical Characteristics Fluorine 18 (F 18) is a cyclotron produced radionuclide that decays by positron emission (ß+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen 18 with a physical half-life of 109.7 minutes. The positron can undergo annihilation with an electron to produce two gamma rays; the energy of each gamma ray is 511 keV ( Table 2 ). Table 2: Principal Radiation Produced from Decay of Fluorine 18 Radiation Energy (keV) Abundance (%) Positron 249.8 96.7 Gamma 511.0 193.5 11.3 External Radiation The point source air-kerma coefficient for F 18 is 3.75 x 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 of Pb will decrease 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 Fluciclovine F-18 Used For?
1 INDICATIONS AND USAGE Axumin is indicated for positron emission tomography (PET) in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment. Axumin is a radioactive diagnostic agent indicated for positron emission tomography (PET) imaging in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment ( 1 ).
Dosage and Administration
2 DOSAGE AND ADMINISTRATION Use appropriate radiation safety handling measures ( 2.1 ). Aseptically withdraw Axumin from its container and administer 370 MBq (10 mCi) as a bolus intravenous injection. ( 2.2 ). Initiate imaging 3 minutes to 5 minutes after administration. Scanning should start from mid-thigh and proceed to base of skull, with a total scan time of approximately 20 minutes to 30 minutes ( 2.4 ). The (radiation absorbed) effective dose associated with 370 MBq (10 mCi) of injected activity of Axumin is approximately 8 mSv (0.8 rem) in an adult ( 2.6 ). 2.1 Radiation Safety - Drug Handling Axumin is a radioactive drug and should be handled with appropriate safety measures to minimize radiation exposure during administration [see Warnings and Precautions ( 5.3 ) ]. Use waterproof gloves and effective shielding, including syringe shields, when handling and administering Axumin. 2.2 Recommended Dose and Administration Instructions The recommended dose is 370 MBq (10 mCi) administered as an intravenous bolus injection. Inspect Axumin visually for particulate matter and discoloration before administration. Do not use the drug if the solution contains particulate matter or is discolored. Use aseptic technique and radiation shielding when withdrawing and administering Axumin. Calculate the necessary volume to administer based on calibration time and date, using a suitably calibrated instrument. The recommended maximum volume of injection of undiluted Axumin is 5mL. Axumin may be diluted with 0.9% Sodium Chloride Injection, USP. After the Axumin injection, administer an intravenous flush of sterile 0.9% Sodium Chloride Injection, USP to ensure full delivery of the dose. Dispose of any unused drug in a safe manner in compliance with applicable regulations. 2.3 Patient Preparation Prior to PET Imaging Advise the patient to avoid any significant exercise for at least one day prior to PET imaging. Advise patients not to eat or drink for at least 4 hours (other than sips of water for taking medications) prior to administration of Axumin. Advise patients to void approximately 30 minutes to 60 minutes prior to administration of Axumin and then refrain from voiding until after the scan has been completed 2.4 Image Acquisition Guidelines Position the patient supine with arms above the head. Begin PET scanning 3 minutes to 5 minutes after completion of the Axumin injection. It is recommended that image acquisition should start from mid-thigh and proceed to the base of the skull. Typical total scan time is between 20 minutes to 30 minutes. 2.5 Image Display and Interpretation Localization of prostate cancer recurrence in sites typical for prostate cancer recurrence is based on fluciclovine F 18 uptake in comparison with tissue background. For small lesions (less than 1cm in diameter) focal uptake greater than blood pool should be considered suspicious for prostate cancer recurrence. For larger lesions, uptake equal to or greater than bone marrow is...
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS Most commonly reported adverse reactions are injection site pain, erythema, and dysgeusia ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Blue Earth Diagnostics, Ltd at 1-855-AXUMIN1 (1-855-298-6461) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 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 clinical trial database for Axumin includes data from 877 subjects including 797 males diagnosed with prostate cancer. Most patients received a single administration of Axumin, a small number of subjects (n = 50) received up to five administrations of the drug. The mean administered activity was 370 MBq (range, 163 MBq to 485 MBq). Adverse reactions were reported in ≤1% of subjects during clinical studies with Axumin. The most common adverse reactions were injection site pain, injection site erythema and dysgeusia.
Contraindications
4 CONTRAINDICATIONS None None ( 4 )
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary Axumin is not indicated for use in females and there is no information on the risk of adverse development outcomes in pregnant women or animals with the use of fluciclovine F 18.
Overdosage
10 OVERDOSAGE In case of overdose of Axumin, encourage patients to maintain hydration and to void frequently to minimize radiation exposure.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING 16.1 How Supplied Axumin is supplied as a clear, colorless injection in a 30 mL or 50 mL multiple-dose glass vial containing approximately 26 mL solution of 335 MBq/mL to 8,200 MBq/mL (9 mCi/mL to 221 mCi/mL) fluciclovine F 18 at calibration time and date. 30 mL sterile multiple-dose vial: NDC 69932-001-30 50 mL sterile multiple-dose vial: NDC 69932-001-50 16.2 Storage and Handling Store Axumin at controlled room temperature (USP) 20°C to 25°C (68°F to 77°F). Axumin does not contain a preservative. Store Axumin within the original container in radiation shielding. Do not use Axumin more than 10 hours after end of synthesis and dispose of in accordance with institutional guidelines. 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.