Overview
11 DESCRIPTION 11.1 Chemical Characteristics POSLUMA (flotufolastat F 18) injection is a radioactive diagnostic agent for intravenous use. The active ingredient of POSLUMA is flotufolastat F 18 gallium, of which the molecular structure includes a DOTAGA complex with nonradioactive gallium. Radioactive fluorine-18 is covalently bound to silicon.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of action Flotufolastat F 18 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 ß+ emitting radionuclide that can be detected using positron emission tomography. 12.2 Pharmacodynamics The relationship between flotufolastat F 18 plasma concentrations and image interpretation has not been fully characterized. 12.3 Pharmacokinetics Distribution Following intravenous administration, flotufolastat F 18 distributes to liver (15.8% of administered activity), heart blood pool (7.4%), and kidneys (3.2%) and is cleared from the blood. Elimination Metabolism Flotufolastat F 18 does not undergo metabolism up to 50 minutes post injection.
Indications
- 1 INDICATIONS AND USAGE POSLUMA is 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. POSLUMA is a radioactive diagnostic agent 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...
Common Doses
- 5 mL
Dosage
2 DOSAGE AND ADMINISTRATION Recommended amount of radioactivity of POSLUMA is 296 MBq (8 mCi) administered as an intravenous bolus injection. ( 2.2 ) Initiate imaging approximately 60 minutes after administration. Scanning should start from mid-thigh and proceed to base of skull. ( 2.4 ) See full prescribing information for additional preparation, handling, administration, imaging, and radiation dosimetry information. ( 2.3 , 2.4 ) 2.1 Radiation Safety - Drug Handling Handle POSLUMA with safety measures to minimize radiation exposure [ see Warnings and Precautions ( 5.2 )] .
Contraindications
- 4 CONTRAINDICATIONS None. None. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The most common adverse reactions (≥0.4%) are diarrhea, blood pressure increase, and injection site pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Blue Earth Diagnostics Ltd at 1-844-POSLUMA (1-844-767-5862) 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.
Interactions
- 7 DRUG INTERACTIONS Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway, such as androgen receptor antagonists, can result in changes in uptake of flotufolastat F 18 in prostate cancer. The effect of these therapies on performance of POSLUMA PET has not been established.