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FL-091 (also referred to as FL-PSMA) is a next-generation radionuclide drug conjugate (RDC) developed by Full Life Technologies for the treatment of prostate cancer, specifically metastatic castration-resistant prostate cancer (mCRPC). The therapeutic consists of a small-molecule ligand with high affinity for Prostate-Specific Membrane Antigen (PSMA), a cell-surface protein highly overexpressed in prostate cancer cells, conjugated to the alpha-emitting radioisotope Actinium-225 (225Ac). Upon intravenous administration, the conjugate binds to PSMA and is internalized into the tumor cells. The alpha particles emitted by 225Ac deliver high-linear energy transfer (LET) radiation over a very short range (a few cell diameters), causing complex, lethal DNA double-strand breaks. This mechanism allows for potent targeted cytotoxicity while minimizing radiation exposure to surrounding healthy tissues. FL-091 is designed to optimize the pharmacokinetic profile to enhance tumor uptake and retention while reducing accumulation in off-target organs such as the salivary glands and kidneys.
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