flotufolastat F18

Action and Spectrum

Actions and Spectrum: 

flotufolastat F 18 is a radiopharmaceutical agent for positron emission tomography (PET) imaging. Its primary action is to selectively target prostate-specific membrane antigen expressed on the surface of prostate cancer cells. The spectrum of flotufolastat F 18 refers to its range of activity and the specific conditions it is designed to visualize.

flotufolastat F 18 is used in PET imaging to detect and evaluate PSMA expression in patients with prostate cancer. PSMA is highly expressed in prostate cancer cells, including primary tumors and metastatic lesions. By binding to PSMA, flotufolastat F 18 allows for the non-invasive visualization and localization of PSMA-expressing lesions during PET imaging. 

The imaging spectrum of flotufolastat F 18 includes the detection and staging of prostate cancer, assessment of disease extent, evaluation of treatment response, and monitoring of disease progression. It provides valuable information for treatment planning, guiding therapeutic strategies, and assessing the effectiveness of prostate cancer interventions. 

Drug Interaction

Adverse Reaction

Frequency defined 

<1% 

Diarrhea (0.7%) 

Enhanced blood pressure (0.5%) 

Pain at the Injection site (0.4%) 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: flotufolastat F 18 should not be used in individuals with known hypersensitivity or allergic reactions to the active substance or its components. Allergic reactions can vary from mild-severe, and caution should be exercised in patients with a history of allergic reactions to similar agents. 
• Pregnancy and Breastfeeding: flotufolastat F 18 during pregnancy condition and breastfeeding is not recommended due to the lack of safety data. Radiation exposure from flotufolastat F 18 may harm the developing fetus or breastfeeding infant.  
• Children: flotufolastat F 18 has not been studied extensively in pediatric populations. The safety and efficacy in children have not been established, and its use in this population is generally not recommended. 
• Uncontrolled Hyperthyroidism: flotufolastat F 18 is excreted through the kidneys, and a small fraction is also eliminated through the thyroid gland. In individuals with uncontrolled hyperthyroidism, there may be an enhanced risk of radiation exposure to the thyroid. Close monitoring and appropriate precautions should be taken in patients with thyroid disorders. 

Caution 

• Radiopharmaceutical Precautions: flotufolastat F 18 is a radiopharmaceutical that emits radiation. Therefore, appropriate radiation safety measures should be followed during handling, administration, and disposal. It should only be used by authorized personnel trained in radiopharmaceutical handling and in compliance with regulatory guidelines. 
• Allergic Reactions: As with any radiopharmaceutical or contrast agent, there is a potential risk of allergic reactions. Patients should be evaluated for any history of allergic reactions to similar agents and monitored closely for any signs of allergic reactions, such as rash, itching, swelling, or difficulty breathing. Prompt medical attention should be sought if any allergic symptoms occur. 
• Renal Impairment: flotufolastat F 18 is primarily excreted through the kidneys. Patients with severe renal impairment may experience slower clearance, leading to prolonged exposure to radiation. Close renal function monitoring and considering alternative imaging options may be necessary for patients with significant renal dysfunction. 
• Pregnancy and Breastfeeding: The safety of flotufolastat F 18 in pregnant or breastfeeding individuals has not been established. It is generally recommended to avoid using radiopharmaceuticals in these populations unless the potential benefits outweigh the risks. Careful consideration should be given to the procedure’s necessity and appropriate radiation safety precautions. 
• Drug Interactions: flotufolastat F 18 is not known to have significant drug interactions. However, it is crucial to inform the healthcare provider about any medications, supplements, or herbal products the patient takes to ensure no potential interactions or contraindications. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

flotufolastat F 18 is a radiopharmaceutical agent used in positron emission tomography (PET) imaging to evaluate prostate-specific membrane antigen (PSMA) expression in patients with prostate cancer. It is a small molecule inhibitor that selectively targets PSMA, an enzyme highly expressed on the surface of prostate cancer cells. flotufolastat F 18 is radiolabeled with fluorine-18, a positron-emitting isotope, allowing for non-invasive imaging of PSMA expression in vivo.

Upon administration, flotufolastat F 18 rapidly binds to PSMA in prostate cancer cells, facilitating the detection and localization of metastatic lesions. Its pharmacological profile includes favorable stability, minimal metabolism, and rapid clearance from non-target tissues, resulting in improved image quality and reduced background signal. flotufolastat F 18 represents a valuable tool in diagnosing, staging, and monitoring prostate cancer patients, aiding in treatment planning and therapeutic response assessment. 

Pharmacodynamics: 

Mechanism of action: The action is closely tied to its ability to target prostate-specific membrane antigen (PSMA) selectively and its role in positron emission tomography (PET) imaging. 

PSMA is an enzyme highly expressed on the surface of prostate cancer cells, including primary tumors and metastatic lesions. flotufolastat F 18 is a small molecule inhibitor that binds to PSMA with high affinity and selectivity. The molecule is radiolabeled with fluorine-18, a positron-emitting isotope. 

Upon intravenous administration, flotufolastat F 18 circulates through the bloodstream and reaches areas of PSMA expression, such as prostate cancer cells. The radiotracer binds to PSMA receptors on the cell surface. The fluorine-18 emits positrons, which subsequently collide with electrons, leading to the emission of two gamma photons in opposite directions. 

During a PET scan, detectors capture these gamma photons, allowing for the reconstruction of three-dimensional images that depict the distribution and concentration of flotufolastat F 18 in the body. The resulting images provide valuable information on the presence, location, and extent of PSMA-expressing lesions in patients with prostate cancer. 

Pharmacokinetics: 

Absorption 

flotufolastat F 18 is administered directly into the bloodstream, bypassing the need for absorption from the gastrointestinal tract. Therefore, absorption is not a relevant consideration for this radiopharmaceutical. 

Distribution 

Following intravenous administration, flotufolastat F 18 rapidly distributes throughout the body via the circulatory system. It travels in the bloodstream and reaches various tissues and organs, including prostate cancer cells expressing prostate-specific membrane antigen (PSMA). 

Metabolism 

flotufolastat F 18 is a small molecule inhibitor radiolabeled with fluorine-18. It undergoes minimal metabolism in the body. 

Elimination and Excretion 

As flotufolastat F 18 is not extensively metabolized, the primary route of excretion is through the urinary system. After performing its imaging function, flotufolastat F 18 is eliminated from the body mainly through renal excretion, as the kidneys filter it from the blood into the urine. 

Adminstartion

Administration: 

Intravenous administration 

flotufolastat F 18 is administered intravenously for positron emission tomography (PET) imaging purposes.  

• Qualified Personnel: flotufolastat F 18 should be handled and administered by authorized personnel trained in radiopharmaceutical handling and in compliance with radiation safety guidelines. 
• Intravenous Injection: flotufolastat F 18 is administered as an intravenous injection. The radiotracer is typically supplied as a sterile, ready-to-use solution in a vial or syringe. 
• Dose and Injection Technique: The dose and injection technique of flotufolastat F 18 may vary depending on the specific imaging protocol and patient characteristics. The prescribed healthcare professional should determine the recommended dose and injection method based on factors such as body weight, imaging goals, and individual patient considerations. 
• Radiopharmaceutical Preparation: flotufolastat F 18 does not require any special preparation or mixing before administration. The radiopharmaceutical is ready for use upon receipt from a reliable and authorized supplier. 
• Radiation Safety Precautions: Appropriate radiation safety precautions should be followed during the handling, administration, and disposal of flotufolastat F 18 to minimize radiation exposure to healthcare providers and others in the vicinity. This includes using proper shielding, wearing appropriate personal protective equipment (PPE), and adhering to local regulations and guidelines. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: flotufolastat F 18 

Pronounced: [ floe-too-FOL-a-stat-F-18 GAL-ee-um ] 

Why do we use flotufolastat F 18? 

flotufolastat F 18 (Posluma) is a radiopharmaceutical used in PET imaging to manage prostate cancer. It is indicated to visualize PSMA-positive lesions in men with prostate cancer suspected of metastasis or recurrence. flotufolastat F 18 is an 18F-labeled ligand that targets the prostate-specific membrane antigen (PSMA). It has advantages over other PSMA-targeting ligands, including a longer half-life and the ability to be produced in larger batches.  

• Prostate Cancer Management: flotufolastat F 18 is primarily used to assist in the management of prostate cancer. It is employed in PET imaging to identify PSMA-positive lesions, aiding in evaluating metastasis and recurrence. 
• Diagnostic Accuracy: Clinical trials have shown that flotufolastat F 18 PET imaging provides improved diagnostic accuracy compared to conventional imaging methods. The SPOTLIGHT trial demonstrated an overall detection rate of 83% for assessing suspected recurrence, and the efficacy analysis showed correct detection rates ranging from 45% to 47% in men with negative baseline conventional imaging. The LIGHTHOUSE study highlighted its high specificity for lymph node disease and the ability to detect extrapelvic disease in 10-14% of cases. 
• Patient Care and Decision-Making: The availability of flotufolastat F 18 aims to benefit physicians and patients by providing valuable information for patient care. By accurately detecting PSMA-positive lesions, flotufolastat F 18 PET imaging can help guide treatment decisions and provide essential information for counseling patients.