Flotufolastat
/api/v1/drug/flotufolastatMechanism of action
Sourced from openFDAFlotufolastat 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.
Indications
Sourced from openFDA- 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.ICD-10: C61
Contraindications
Sourced from openFDA- None. None.contraindicated
Dosage & administration
Sourced from openFDARecommended 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 )] . Use waterproof gloves, effective radiation shielding, including syringe shields, and other appropriate safety measures when handling and administering POSLUMA. Radiopharmaceuticals should be used by or under the control of physicians who are qualified by specific training and experience in the safe use and handling of radionuclides, and whose experience and training have been approved by the appropriate governmental agency authorized to license the use of radionuclides. 2.2 Recommended Dose and Administration Instructions Recommended Dose The recommended amount of radioactivity to be administered in adults is 296 MBq (8 mCi) as an intravenous bolus injection. Preparation and Administration Instructions Inspect POSLUMA 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 POSLUMA.
Warnings & precautions
Sourced from openFDARisk of Image Misinterpretation: Image interpretation errors can occur with POSLUMA imaging. Interpretation of POSLUMA PET may differ depending on imaging readers in patients with suspected recurrence of prostate cancer. Consider multidisciplinary consultation and histopathological confirmation. ( 5.1 , 14.2 ) Radiation risk: POSLUMA contributes to a patient's long-term cumulative radiation exposure. Ensure safe handling to protect patients and health care workers from unintentional radiation exposure. ( 2.1 , 5.2 ) 5.1 Risk of Image Misinterpretation Image interpretation errors can occur with POSLUMA PET. A negative image does not rule out the presence of prostate cancer and a positive image does not confirm the presence of prostate cancer. The performance of POSLUMA for imaging metastatic pelvic lymph nodes in patients prior to initial definitive therapy seems to be affected by serum PSA levels and risk grouping [See Clinical Studies ( 14.1 )] . The performance of POSLUMA for imaging patients with biochemical evidence of recurrence of prostate cancer seems to be affected by serum PSA levels [See Clinical Studies ( 14.2 )] . Flotufolastat F 18 uptake is not specific for prostate cancer and may occur in other types of cancer, in non-malignant processes, and in normal tissues. Clinical correlation, which may include histopathological evaluation, is recommended.
Adverse reactions
Sourced from openFDAThe 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. The safety of POSLUMA was evaluated in 747 patients with prostate cancer [see Clinical Studies ( 14.1 , 14.2 )] . All patients received a single administration of POSLUMA with an administered radioactivity (mean ± SD) of 307 ± 23 MBq (8.3 ± 0.6 mCi). The mean age of patients was 67 years (range: 43 to 86 years); distribution by race was 78% White, 12% Black or African American, 2% other, and 7% unreported; and distribution by ethnicity was 5% Hispanic/Latino, 87% non-Hispanic/Latino, and 8% unreported. The adverse reactions reported in ≥ 0.4% of patients are shown in Table 2 . Table 2: Adverse Reactions in ≥ 0.4% of Patients with Prostate Cancer Receiving POSLUMA Adverse Reaction POSLUMA N = 747 n (%) Diarrhea 5 (0.7%) Blood pressure increase 4 (0.5%) Injection site pain 3 (0.4%)
Use in specific populations
Sourced from openFDA8.1 Pregnancy Risk Summary POSLUMA is not indicated for use in females. There are no available data on the use of POSLUMA in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Animal reproduction studies have not been conducted with flotufolastat F 18. Radioactive drugs, including POSLUMA, have the potential to cause fetal harm depending on the fetal stage of development and the magnitude of the radiation dose. 8.2 Lactation Risk Summary POSLUMA is not indicated for use in females. There are no data on the presence of flotufolastat F 18 in human milk, the effect on the breastfed infant, or the effect on milk production. 8.4 Pediatric Use The safety and effectiveness of POSLUMA have not been established in pediatric patients. 8.5 Geriatric Use Among the total number of patients receiving POSLUMA in clinical studies of prostate cancer, 463 (62%) were 65 years of age and older, while 118 (16%) were 75 years of age and older [see Clinical Studies ( 14.1 , 14.2 )] . No overall differences in safety or effectiveness were observed between these patients and younger adult patients.
Pharmacokinetics
Sourced from openFDA- Metabolism
- 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.
Overdosage
Sourced from openFDAIn the event of an overdose of POSLUMA, maintain hydration of the patient and frequent voiding to minimize radiation exposure. A diuretic might also be considered. If possible, an estimate of the radiation effective dose administered to the patient should be made.
Approval history
Sourced from openFDA- May 25, 2023NDANDA216023Blue Earth
FAERS reports
- 1Positron Emission Tomogram Abnormal1026%
- 2No Adverse Event924%
- 3Drug Effect Less Than Expected821%
- 4Overdose411%
- 5Incorrect Dose Administered37.9%
- 6Wrong Product Administered37.9%
- 7Drug Ineffective25.3%
- 8Product Dispensing Error25.3%
- 9Accidental Exposure To Product12.6%
- 10Acute Respiratory Failure12.6%
- 11Asthenia12.6%
- 12Chest Pain12.6%
- 13Covid-1912.6%
- 14Death12.6%
- 15Diarrhoea12.6%
Clinical trials
The 10 most recently updated of 23 ClinicalTrials.gov registrations naming Flotufolastat as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.
- Androgen-responsive POSLUMA-guided Intra-prostatic BoostRecruiting · Phase 2 · Interventional · 23 enrolled · Martin T. King, MD, PhDNCT07393867updated 2026-05-29
- Prostate Specific Membrane Antigen (PSMA) Imaging for Detection of Residual and Metastatic Prostate CancerNot yet recruiting · Phase 2 · Interventional · 20 enrolled · Washington University School of MedicineNCT07593079updated 2026-05-18
- Flotufolastat F 18 PET in Men With Very Low PSA RecurrenceRecruiting · Observational · 50 enrolled · Massachusetts General HospitalNCT06862856updated 2026-05-15
- Assessing Efficacy of Neoadjuvant ADT in Localized High-Risk Prostate Cancer Patients Utilizing 18F-Flotufolastat PSMA PET/CTRecruiting · Phase 2 · Interventional · 50 enrolled · Baptist Health South FloridaNCT07455903updated 2026-05-13
- Intrapatient Comparison of Urinary Radioactivity Following Piflufolastat (18F) and Flotufolastat (18F) PET in Men With Low PSA Biochemical Recurrence of Prostate Cancer Following Radical ProstatectomyCompleted · Phase 4 · Interventional · 62 enrolled · Blue Earth DiagnosticsNCT06604442updated 2026-05-12
- Utilization of Flotufolastat 18F PET for Post-Focal Therapy Prostate Cancer EvaluationNot yet recruiting · Phase 2 · Interventional · 60 enrolled · University of California, IrvineNCT07568756updated 2026-05-06
- [18F]-rhPSMA PET-CT Imaging Performance in Patients With Prostate CancerActive not recruiting · Interventional · 20 enrolled · City of Hope Medical CenterNCT06580015updated 2026-04-27
- POSLUMA® (18F-rhPSMA-7.3) PET-CT for PIRADS 2/3 LesionsRecruiting · Phase 2 · Interventional · 30 enrolled · University of FloridaNCT07220720updated 2026-04-13
- Accuracy of 18F-rhPSMA-7.3 PET/ MRI for Prediction of Lymph Node Metastasis in Localized High-Risk Prostate CancerRecruiting · Interventional · 50 enrolled · Mayo ClinicNCT06389786updated 2026-04-06
- Androgen Deprivation Therapy (Relugolix) for the Improvement of Diagnostic Imaging (PSMA PET/CT Scan) in Patients With High Risk or Very High Risk Prostate Cancer, The EnrichPSMA TrialRecruiting · Phase 2 · Interventional · 30 enrolled · Mayo ClinicNCT07025369updated 2026-03-13
Frequently asked questions
- How does Flotufolastat work?
- 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.
- What is Flotufolastat used for?
- According to FDA labeling, Flotufolastat carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
- What class of drug is Flotufolastat?
- Flotufolastat is classified as Positron Emitting Activity.
- What are the contraindications for Flotufolastat?
- Flotufolastat labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
flotufolastat is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.