piflufolastat F18

Action and Spectrum

Actions and spectrum: 

piflufolastat F18 is a radiopharmaceutical used for diagnostic purposes. It is a positron emission tomography (PET) imaging agent that targets prostate-specific membrane antigen (PSMA), which is highly expressed in prostate cancer cells. 

Once administered, piflufolastat F18 binds to PSMA on the surface of prostate cancer cells, allowing for the detection of the cancer cells through PET imaging. PET imaging provides a non-invasive way to determine the extent of the disease and monitor the progression of cancer. 

The spectrum of piflufolastat F18 is limited to the detection of prostate cancer cells expressing PSMA. It is not effective for the diagnosis of other types of cancer or non-cancerous conditions. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Fatigue (1%) 

Dysgeusia (2%) 

Headache (2%)  

<1% 

Hypersensitivity (0.2%) 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

There are no absolute contraindications for piflufolastat F18, but its use should be carefully considered in certain patient populations. Patients with hypersensitivity or allergy to the active ingredient or any of the components of the formulation should not receive piflufolastat F18.

Additionally, pregnant, or breastfeeding women should not receive piflufolastat F18 due to the potential risks of radiation exposure to the developing fetus or infant. In general, the use of radiopharmaceuticals like piflufolastat F18 should be approached with caution in patients with compromised renal or hepatic function, as these organs are involved in the clearance of the radiopharmaceutical from the body.  

Caution: 

piflufolastat F18 should be used with caution in certain patient populations. Patients with a history of hypersensitivity or allergic reactions to other radiopharmaceuticals should be monitored closely for signs of an allergic reaction during the administration of piflufolastat F18. 

piflufolastat F18 is eliminated from the body through the kidneys, so caution should be used in patients with renal impairment. The radiopharmaceutical should be used with caution in patients with moderate to severe renal impairment, as the risk of radiation exposure may be increased in these patients. 

The safety and efficacy of piflufolastat F18 in pediatric patients have not been established, so its use in this population should be carefully considered. Similarly, the safety and efficacy of piflufolastat F18 in pregnant or breastfeeding women have not been established, and the benefits and risks of its use should be carefully weighed in these patients.  

Comorbidities: 

There are no known specific comorbidities associated with piflufolastat F18 use. However, as with any radiopharmaceutical, caution should be exercised in patients with underlying medical conditions that may increase their susceptibility to adverse reactions or radiation exposure. Patients with compromised renal function, liver function, or immune function may be at increased risk of adverse reactions or radiation exposure, and the use of piflufolastat F18 should be carefully considered in these patients. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: Not assigned 

Lactation: It is not known whether piflufolastat F18 is excreted in human milk.  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

piflufolastat F18 is a radiopharmaceutical imaging agent that binds to prostate-specific membrane antigen (PSMA), a protein that is expressed over the surface of prostate cancer cells. It consists of a small molecule inhibitor of PSMA conjugated to a radioactive isotope of fluorine-18 (F18), a positron-emitting radionuclide that allows for PET imaging. 

After intravenous administration, piflufolastat F18 rapidly distributes throughout the body and binds to PSMA on the surface of prostate cancer cells. The radioactive decay of F18 results in the emission of positrons, which can be detected by PET imaging equipment. The resulting PET images can provide information on the location, size, and extent of prostate cancer lesions, which can aid in diagnosis, staging, and treatment planning.  

Pharmacodynamics: 

piflufolastat F18 is a radiopharmaceutical agent used in positron emission tomography (PET) imaging to visualize prostate-specific membrane antigen (PSMA) lesions in patients with prostate cancer. PSMA is expressed in prostate cancer cells, and piflufolastat F18 binds to PSMA with high affinity. Upon binding to PSMA, piflufolastat F18 emits positrons that can be detected by a PET scanner, allowing for the non-invasive detection and localization of PSMA-positive tumors. The pharmacodynamics of piflufolastat F18 is primarily related to its ability to bind to PSMA and emit positrons for imaging purposes.  

Pharmacokinetics: 

Absorption 

piflufolastat F18 is administered intravenously, resulting in immediate and complete absorption. 

Distribution 

piflufolastat F18 rapidly distributes throughout the body and binds to PSMA on the surface of prostate cancer cells. 

Metabolism 

piflufolastat F18 undergoes minimal metabolism in the body. 

Elimination and excretion 

piflufolastat F18 is rapidly cleared from the bloodstream, with the majority of the administered dose eliminated within 2 hours of injection. The radioactive decay of F18 results in the emission of photons with low energy, which can be detected by PET imaging equipment. The effective half-life of piflufolastat F18 is approximately 110 minutes. 

Adminstartion

Administration: 

piflufolastat F18 is administered as an intravenous injection. The usual recommended dose is 370 MBq (10 mCi) in a total volume of 5 mL. The injection should be given over a period of 1-2 minutes. 

Prior to administration, patients should be instructed to drink plenty of fluids to encourage urination, which can help to eliminate the radioactive tracer from the body. Patients should also be advised to empty their bladder immediately prior to imaging to reduce background radiation and improve image quality. 

Imaging should be performed approximately 1 hour after injection using a PET imaging system that is equipped to detect the low-energy photons emitted by F18. The imaging procedure typically takes 15-20 minutes to complete 

Patient Information Leaflet

Patient information leaflet 

Generic Name: piflufolastat F18 

Pronounced: [ pif-loo-FOE-la-stat-F-18]  

Why do we use piflufolastat F18? 

piflufolastat F18 is a radioactive tracer used in positron emission tomography (PET) imaging to help detect and localize prostate-specific membrane antigen (PSMA) positive lesions in patients with suspected or confirmed prostate cancer. PSMA is a cell surface protein that is highly expressed in prostate cancer cells, making it a valuable target for imaging and treatment of the disease. 

PET imaging with piflufolastat F18 can provide information on the location, size, and metabolic activity of prostate cancer lesions, which can help guide treatment decisions and monitor response to therapy. It is particularly useful in detecting early-stage prostate cancer, recurrent or metastatic disease, and in patients with rising prostate-specific antigen (PSA) levels despite previous treatment.