Piflufolastat
/api/v1/drug/piflufolastatMechanism of action
Sourced from openFDAPiflufolastat F 18 binds to cells that express PSMA, including malignant prostate cancer cells, which usually overexpress PSMA. Fluorine-18 (F 18) is a β+ emitting radionuclide that enables positron emission tomography.
Indications
Sourced from openFDA- PYLARIFY 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 dose is 333 MBq (9 mCi) with an acceptable range of 296 MBq to 370 MBq (8 mCi to 10 mCi), administered as a bolus intravenous injection. ( 2.2 ) Initiate imaging approximately 60 minutes after PYLARIFY administration. The patient should void immediately prior to initiation of imaging. Image acquisition should start from mid-thigh and proceed to the skull vertex. ( 2.3 , 2.4 ) See full prescribing information for additional preparation, handling, administration, imaging, and radiation dosimetry information. ( 2 ) 2.1 Radiation Safety – Drug Handling PYLARIFY is a radioactive drug. Only authorized persons qualified by training and experience should receive, use, and administer PYLARIFY. Handle PYLARIFY with appropriate safety measures to minimize radiation exposure during administration [see Warnings and Precautions (5.3) ] . Use waterproof gloves and effective radiation shielding, including syringe shields, when preparing and handling PYLARIFY. 2.2 Recommended Dosage and Administration Instructions Recommended Dose The recommended amount of radioactivity to be administered for PET imaging is 333 MBq (9 mCi) with an acceptable range of 296 MBq to 370 MBq (8 mCi to 10 mCi) administered as a single bolus intravenous injection. Preparation and Administration Use aseptic technique and radiation shielding when preparing and administering PYLARIFY. Visually inspect the radiopharmaceutical solution. Do not use if it contains particulate matter or if it is discolored (PYLARIFY is a clear, colorless solution).
Warnings & precautions
Sourced from openFDARisk of Image Misinterpretation : PYLARIFY uptake can be seen in a variety of tumor types as well as in non-malignant processes and normal tissues. Image interpretation errors can occur with PYLARIFY imaging. ( 5.1 ) Hypersensitivity Reactions : Monitor patients for hypersensitivity reactions, particularly patients with a history of allergy to other drugs and foods. ( 5.2 ) Radiation Risk : Ensure safe drug handling to protect patients and health care workers from unintentional radiation exposure. ( 5.3 ) 5.1 Risk of Image Misinterpretation Imaging interpretation errors can occur with PYLARIFY imaging. 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 PYLARIFY for imaging of patients with biochemical evidence of recurrence of prostate cancer seems to be affected by serum PSA levels [ see Clinical Studies (14) ]. The performance of PYLARIFY for imaging of metastatic pelvic lymph nodes prior to initial definitive therapy seems to be affected by risk factors such as Gleason score and tumor stage [ see Clinical Studies (14) ]. PYLARIFY uptake is not specific for prostate cancer and may occur with other types of cancer as well as non-malignant processes and in normal tissues. Clinical correlation, which may include histopathological evaluation of the suspected prostate cancer site, is recommended. 5.2 Hypersensitivity Reactions Monitor patients for hypersensitivity reactions, particularly patients with a history of allergy to other drugs and foods.
Adverse reactions
Sourced from openFDAThe most common reported adverse reactions are headache, dysgeusia, and fatigue. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Progenics Pharmaceuticals, Inc. at 1-800-362-2668 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 PYLARIFY was evaluated in 593 patients, each receiving one dose of PYLARIFY. The average injected activity was 340 ± 26 MBq (9.2 ± 0.7 mCi). The adverse reactions reported in >0.5% of patients within the studies are shown in Table 2. In addition, a hypersensitivity reaction was reported in one patient (0.2%) with a history of allergic reaction. Table 2. Adverse Reactions with a Frequency >0.5% in Patients Who Received PYLARIFY (n = 593) Adverse Reaction n (%) Headache 13 (2%) Dysgeusia 10 (2%) Fatigue 7 (1%)
Use in specific populations
Sourced from openFDA8.1 Pregnancy Risk Summary PYLARIFY is not indicated for use in females. There is no information on the risk of adverse developmental outcomes in pregnant women or animals with the use of piflufolastat F 18. All radiopharmaceuticals, including PYLARIFY, 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 PYLARIFY is not indicated for use in females. There is no information on the presence of piflufolastat 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 PYLARIFY in pediatric patients have not been established. 8.5 Geriatric Use Of the 593 patients in completed clinical studies of PYLARIFY, 355 (60%) were ≥65 years old, while 76 (12.8%) were ≥75 years old. The efficacy and safety of PYLARIFY appear similar in adult and geriatric patients with prostate cancer, although the number of patients in the trials was not large enough to allow definitive comparison.
Pharmacokinetics
Sourced from openFDA- Metabolism
- Distribution Following intravenous administration of piflufolastat F 18, blood levels decline in a biphasic fashion. The distribution half-life is 0.17 ± 0.044 hours and the elimination half-life is 3.47 ± 0.49 hours.
Overdosage
Sourced from openFDAIn the event of an overdose of PYLARIFY, reduce the radiation absorbed dose to the patient where possible by increasing the elimination of the drug from the body using hydration and frequent bladder voiding. 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 26, 2021NDANDA214793Progenics Pharms Inc
FAERS reports
- 1Radioisotope Scan Abnormal7639%
- 2Drug Ineffective5327%
- 3Product Dispensing Error3417%
- 4Product Preparation Error147.1%
- 5Product Dose Omission Issue115.6%
- 6Intercepted Product Dispensing Error94.6%
- 7Dizziness63.0%
- 8Fatigue63.0%
- 9Product Dose Omission In Error63.0%
- 10Wrong Product Administered63.0%
- 11Product Administration Error52.5%
- 12Nausea42.0%
- 13Off Label Use42.0%
- 14Tongue Neoplasm Malignant Stage Unspecified42.0%
- 15False Negative Investigation Result31.5%
Clinical trials
The 10 most recently updated of 18 ClinicalTrials.gov registrations naming Piflufolastat as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.
- An Open-label Study Comparing Lutetium (177Lu) Vipivotide Tetraxetan Versus Observation in PSMA Positive OMPC.Recruiting · Phase 3 · Interventional · 450 enrolled · Novartis PharmaceuticalsNCT05939414updated 2026-06-10
- A Phase 2 Trial of 61Cu-NU101 PET/CT Compared Against Current Standard-of-care 18F-piflufolastat (Pylarify®) PET/CT.Not yet recruiting · Phase 2 · Interventional · 34 enrolled · Hoag Memorial Hospital PresbyterianNCT07635524updated 2026-06-09
- Relugolix and Enzalutamide in Combination With Radiation Therapy for the Treatment of Very High Risk Prostate Cancer, OPTIMAL TrialRecruiting · Phase 2 · Interventional · 50 enrolled · Sean SachdevNCT06499870updated 2026-06-05
- RefleXion PET/CT Imaging Performance in Patients With Prostate CancerActive not recruiting · Interventional · 34 enrolled · City of Hope Medical CenterNCT05470699updated 2026-06-02
- A Phase II Study of AAA617 Alone and AAA617 in Combination With ARPI in Patients With PSMA PET Scan Positive CRPCActive not recruiting · Phase 2 · Interventional · 49 enrolled · Novartis PharmaceuticalsNCT05849298updated 2026-05-27
- 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
- A Pilot Presurgical Trial of REGN5678 (Anti-PSMA x CD28) in Patients With High-risk, Localized Prostate Cancer Followed by Radical ProstatectomyRecruiting · Phase 1 · Phase 2 · Interventional · 42 enrolled · M.D. Anderson Cancer CenterNCT06085664updated 2026-05-05
- A Pilot Study to Assess the Clinical Utility of PYLARIFY PET-CT for Detecting Metastasis in Pancreatic Cancer, Hepatocellular Carcinoma and Breast CancerRecruiting · Phase 1 · Interventional · 36 enrolled · M.D. Anderson Cancer CenterNCT05394259updated 2026-04-15
- Pilot of 18F-DCFPyL-PSMA PET in mCRPC Patients Receiving 117Lu-Vipivotide TetraxetanRecruiting · Phase 4 · Interventional · 30 enrolled · Brigham and Women's HospitalNCT06099093updated 2026-01-29
- Study to Assess [177Lu]Lu-PSMA-R2 (AAA602) and [225Ac]Ac-PSMA-R2 (AAA802) in Participants With PSMA-positive HRLPCWithdrawn · Phase 1 · Phase 2 · Interventional · 0 enrolled · Novartis PharmaceuticalsNCT06881823updated 2025-12-29
Frequently asked questions
- How does Piflufolastat work?
- Piflufolastat F 18 binds to cells that express PSMA, including malignant prostate cancer cells, which usually overexpress PSMA. Fluorine-18 (F 18) is a β+ emitting radionuclide that enables positron emission tomography.
- What is Piflufolastat used for?
- According to FDA labeling, Piflufolastat carries indications including: PYLARIFY 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 Piflufolastat?
- Piflufolastat is classified as Imaging Contrast Activity.
- What are the contraindications for Piflufolastat?
- Piflufolastat labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
piflufolastat 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.