Fluciclovine

Fluciclovine F 18 is a synthetic amino acid transported across mammalian cell membranes by amino acid transporters, such as LAT-1 and ASCT2, which are upregulated in prostate cancer cells. Fluciclovine F 18 is taken up to a greater extent in prostate cancer cells compared with surrounding normal tissues.

• 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 ).ICD-10: C61

• None None ( 4 )contraindicated

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.

Image interpretation errors can occur with Axumin imaging ( 5.1 ). Radiation risk: Axumin 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 , 5.3 ). 5.1 Risk for Image Misinterpretation Image interpretation errors can occur with Axumin PET imaging. A negative image does not rule out the presence of recurrent prostate cancer and a positive image does not confirm the presence of recurrent prostate cancer. The performance of Axumin seems to be affected by PSA levels [See Clinical Studies ( 14 )] . Fluciclovine F 18 uptake is not specific for prostate cancer and may occur with other types of cancer and benign prostatic hypertrophy in primary prostate cancer. Clinical correlation, which may include histopathological evaluation of the suspected recurrence site, is recommended. 5.2 Hypersensitivity Reactions Hypersensitivity reactions including anaphylaxis may occur in patients who receive Axumin. Emergency resuscitation equipment and personnel should be immediately available. 5.3 Radiation Risks Axumin use contributes to a patient's overall long-term cumulative radiation exposure. Long-term cumulative radiation exposure is associated with an increased risk for cancer. Ensure safe handling to minimize radiation exposure to the patient and health care providers [see Dosage and Administration ( 2.1 )] .

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.

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. 8.2 Lactation Risk Summary Axumin is not indicated for use in females and there is no information of the presence of fluciclovine F 18 in human milk. 8.3 Pediatric Use Safety and effectiveness have not been established in pediatric patients. 8.4 Geriatric Use Of the total number of patients in clinical studies of Axumin, the average age was 66 years with a range of 21 to 90 years. No overall differences in safety or effectiveness were observed between older subjects and younger subjects.

Metabolism

Distribution Following intravenous administration, fluciclovine F 18 distributes to the liver (14% of administered activity), pancreas (3%), lung (7%), red bone marrow (12%) and myocardium (4%). With increasing time, fluciclovine F 18 distributes to skeletal muscle.

In case of overdose of Axumin, encourage patients to maintain hydration and to void frequently to minimize radiation exposure.

• May 27, 2016NDANDA208054Blue Earth

1. 1Positron Emission Tomogram Abnormal2222%
2. 2No Adverse Event1818%
3. 3Therapeutic Response Unexpected1818%
4. 4Scan Abnormal1111%
5. 5False Negative Investigation Result77.1%
6. 6Drug Ineffective66.1%
7. 7Injection Site Extravasation55.1%
8. 8Off Label Use55.1%
9. 9False Positive Investigation Result44.0%
10. 10Therapeutic Product Effect Decreased44.0%
11. 11Diarrhoea33.0%
12. 12Extravasation22.0%
13. 13Malaise22.0%
14. 14Manufacturing Product Shipping Issue22.0%
15. 15Product Dose Omission22.0%

The 10 most recently updated of 79 ClinicalTrials.gov registrations naming Fluciclovine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study Using Nivolumab, in Combination With Chemotherapy Drugs to Treat Nasopharyngeal Carcinoma (NPC)
  Recruiting · Phase 2 · Interventional · 50 enrolled · National Cancer Institute (NCI)
  NCT06064097updated 2026-06-12
• Impact of Fluciclovine (18F) PET (Positron Emission Tomography) on the Management of Prostate Cancer Following Negative or Equivocal PSMA (Prostate-Specific Membrane Antigen) PET Imaging at the Time of Biochemical Recurrence
  Not yet recruiting · Phase 4 · Interventional · 142 enrolled · Blue Earth Diagnostics
  NCT07569926updated 2026-06-02
• A Pilot Study to Assess the Clinical Utility of 18F-Fluciclovine (Axumin) PET-CT for Detecting True-versus Pseudo-Progression of Brain Metastases on Immunotherapy
  Active not recruiting · Interventional · 3 enrolled · M.D. Anderson Cancer Center
  NCT06015295updated 2026-06-02
• 18F-Fluciclovine PET/CT in Multiple Myeloma
  Recruiting · Phase 2 · Interventional · 60 enrolled · National Cancer Institute (NCI)
  NCT06103838updated 2026-05-29
• 18F-Fluciclovine PET Amino Acid Evaluation of Brain Metastasis Treated With Stereotactic Radiosurgery
  Recruiting · Phase 1 · Interventional · 46 enrolled · Baptist Health South Florida
  NCT06048094updated 2026-05-20
• Identifying Findings on Brain Scans That Could Help Make Better Predictions About Brain Cancer Progression, The GABLE Trial
  Recruiting · Phase 2 · Interventional · 100 enrolled · ECOG-ACRIN Cancer Research Group
  NCT06319027updated 2026-05-15
• Treating Prostate Cancer That Has Come Back After Surgery With Apalutamide and Targeted Radiation Based on PET Imaging
  Recruiting · Phase 3 · Interventional · 804 enrolled · ECOG-ACRIN Cancer Research Group
  NCT04423211updated 2026-05-15
• Testing the Addition of the Drug Relugolix to the Usual Radiation Therapy for Advanced-Stage Prostate Cancer, The NRG Promethean Study
  Active not recruiting · Phase 2 · Interventional · 194 enrolled · NRG Oncology
  NCT05053152updated 2026-05-04
• Evaluation of 18F-Fluciclovine Positron Emission Tomography - Magnetic Resonance Imaging (PET-MRI) in LGG
  Recruiting · Early phase 1 · Interventional · 30 enrolled · Children's Hospital of Philadelphia
  NCT05555550updated 2026-04-29
• Assess Use of 18F-Fluciclovine for Patients With Large Brain Metastases Treated With Staged Stereotactic Radiosurgery
  Recruiting · Phase 1 · Interventional · 20 enrolled · Baptist Health South Florida
  NCT04689048updated 2026-04-22

Frequently asked questions

How does Fluciclovine work?

Fluciclovine F 18 is a synthetic amino acid transported across mammalian cell membranes by amino acid transporters, such as LAT-1 and ASCT2, which are upregulated in prostate cancer cells. Fluciclovine F 18 is taken up to a greater extent in prostate cancer cells compared with surrounding normal tissues.

What is Fluciclovine used for?

According to FDA labeling, Fluciclovine carries indications including: 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 ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Fluciclovine?

Fluciclovine is classified as Positron Emitting Activity.

What are the contraindications for Fluciclovine?

Fluciclovine labeling lists contraindications including: None None ( 4 ). Always consult the full prescribing information and a clinician.