Dosing & Uses
Dosage Forms & Strengths
injection, solution
- 296-5,846 MBq/mL (8-158 mCi/mL) in ~25 mL multidose vials at calibration time and date
Prostate Cancer Imaging
Indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer
- with suspected metastasis who are candidates for initial definitive therapy
- with suspected recurrence based on elevated serum prostate-specific antigen (PSA) level
Recommended dose: 296 MBq (8 mCi) IV bolus (see Administration)
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (6)
- abiraterone
abiraterone, flotufolastat F 18. Other (see comment). Use Caution/Monitor. Comment: Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway (eg, androgen receptor antagonists) can result in changes in uptake of flotufolastat F 18 in prostate cancer. Effects of these therapies on performance of flotufolastat F 18 PET has not been established.
- bicalutamide
bicalutamide, flotufolastat F 18. Other (see comment). Use Caution/Monitor. Comment: Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway (eg, androgen receptor antagonists) can result in changes in uptake of flotufolastat F 18 in prostate cancer. Effects of these therapies on performance of flotufolastat F 18 PET has not been established.
- degarelix
degarelix, flotufolastat F 18. Other (see comment). Use Caution/Monitor. Comment: Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway (eg, androgen receptor antagonists) can result in changes in uptake of flotufolastat F 18 in prostate cancer. Effects of these therapies on performance of flotufolastat F 18 PET has not been established.
- enzalutamide
enzalutamide, flotufolastat F 18. Other (see comment). Use Caution/Monitor. Comment: Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway (eg, androgen receptor antagonists) can result in changes in uptake of flotufolastat F 18 in prostate cancer. Effects of these therapies on performance of flotufolastat F 18 PET has not been established.
- flutamide
flutamide, flotufolastat F 18. Other (see comment). Use Caution/Monitor. Comment: Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway (eg, androgen receptor antagonists) can result in changes in uptake of flotufolastat F 18 in prostate cancer. Effects of these therapies on performance of flotufolastat F 18 PET has not been established.
- nilutamide
nilutamide, flotufolastat F 18. Other (see comment). Use Caution/Monitor. Comment: Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway (eg, androgen receptor antagonists) can result in changes in uptake of flotufolastat F 18 in prostate cancer. Effects of these therapies on performance of flotufolastat F 18 PET has not been established.
Minor (0)
Adverse Effects
<1%
Diarrhea (0.7%)
Increased blood pressure (0.5%)
Injection site pain (0.4%)
Warnings
Contraindications
None
Cautions
Misinterpretation
- Image interpretation errors can occur with flotufolastat F 18 PET imaging
- A negative image does not rule out presence of recurrent prostate cancer, and a positive image does not confirm presence of recurrent prostate cancer
- Performance of flotufolastat F 18 for imaging metastatic pelvic lymph nodes in patients prior to initial definitive therapy seems to be affected by PSA levels and risk grouping
- Not specific for prostate cancer and may occur with other types of cancer, in nonmalignant processes, and in normal tissue
- Clinical correlation, which may include histopathological evaluation of the suspected recurrence site, is recommended
- Interpretation may differ depending on imaging readers, particularly in prostate/prostate bed region
- Because of associated risk of false positive interpretation, consider multidisciplinary consultation and histopathological confirmation when clinical decision-making hinges on flotufolastat F 18 uptake only in the prostate/prostate bed region or only on uptake interpreted as borderline
Radiation Risk
- Use contributes to a patient’s overall long-term cumulative radiation exposure
- Long-term cumulative radiation exposure associated with increased risk for cancer
- Ensure safe handling to minimize radiation exposure to patient and clinicians
Drug interaction overview
-
Therapies targeting androgen pathway
- Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway (eg, androgen receptor antagonists) can result in changes in uptake of flotufolastat F 18 in prostate cancer
- Effects of these therapies on performance of flotufolastat F 18 PET has not been established
Pharmacology
Mechanism of Action
Binds to PSMA (IC50 = 4.4 nM) expressed on cells, including prostate cancer cells, and is internalized
Prostate cancer cells usually overexpress PSMA
Fluorine-18 is a beta-positive–emitting radionuclide that can be detected using positron emission tomography
Distribution
Liver: 15.8%
Heart blood pool: 7.4%
Kidneys: 3.2%
Metabolism
Does not undergo metabolism up to 50 minutes post injection
Elimination
First 2 hr post injection: ~7% excreted in urine
First 4.5 hr post injection: ~15% excreted in urine
Administration
Patient Preparation
Instruct to drink water before administration to ensure adequate hydration
Continue drinking and voiding frequently for first few hours after administration to reduce radiation exposure
IV Preparation
Handle radioactive drug with appropriate safety measures to minimize radiation exposure during administration
Use waterproof gloves and effective shielding, including syringe shields, when handling and administering
Inspect solution visually for particulate matter and discoloration before administration; discard if solution contains particulate matter or is discolored
Use aseptic technique and radiation shielding when withdrawing and administering
Calculate necessary volume to administer based on calibration time and date; assay dose using a suitably calibrated instrument
Recommended maximum volume of injection of undiluted drug is 5 mL; may be diluted with NaCl 0.9%
IV Administration
After IV bolus injection, administer IV flush of sterile NaCl 0.9% to ensure full delivery of the dose
Dispose of any unused drug in a safe manner in compliance with applicable regulations
Image acquisition guidelines
- Have patient void immediately before imaging
- Position patient supine with arms above head
- Begin PET scanning ~60 minutes after injection
- Image acquisition should start from mid-thigh and proceed to base of skull
- Scan duration ~20 minutes depending on number of bed positions and acquisition time per bed position (typically 3 minutes)
- Adapt imaging technique according to equipment used and patient characteristics to obtain the best image quality possible
Image Display and Interpretation
Localization of prostate cancer recurrence in sites typical for prostate cancer recurrence is based on flotufolastat F 18 uptake in comparison with tissue background
Lesions should be considered suspicious if uptake is greater than physiologic uptake in that tissue or greater than adjacent background if no physiologic uptake is expected; tumors that do not express PSMA will not be visualized; increased uptake in tumors is not specific for prostate cancer
Radiation dosimetry: See prescribing information
Storage
Store at controlled room temperature of 20-25°C (68-77°F)
Does not contain a preservative
Store in original container with radiation shielding
Expiration date and time are provided on container label
Use within 10 hr from end of synthesis
Dispose of any unused drug in a safe manner in compliance with applicable regulations
Approved for use by persons under license by the Nuclear Regulatory Commission or the relevant regulatory authority of an Agreement State
Images
Formulary
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