Flotufolastat F-18

Flotufolastat F-18 (F-rhPSMA-7.3) is an F-labeled ligand that targets the prostate-specific membrane antigen (PSMA). In patients with recurrent prostate cancer that require localized treatment, the use of F-labeled ligands for positron emission tomography (PET) offers accurate diagnostic imaging. Unlike Ga-labeled PSMA-targeting ligands, F-labeled compounds targeting this protein have a longer half-life and can be produced in larger batches. Flotufolastat F-18 is a diastereoisomer of F-rhPSMA-7, and compared to the other diastereoisomers of this compound, flotufolastat F-18 has a faster clearance from blood pool, liver, and kidney, and a high level of accumulation in tumors.

In May 2023, the FDA approved the use of flotufolastat F-18 for PET of PSMA-positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy or suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. This is the first FDA-approved, PSMA-targeted imaging agent developed with proprietary radiohybrid (rh) technology. Additional studies have shown that in patients with primary prostate cancer, the use of flotufolastat F-18 shows led to low interreader variation and a good distinction between primary-tumor activity and bladder background activity.