PSMA-targeting is a clinically validated and increasingly commercially successful approach for positron emission tomography (PET) of prostate cancer and for treatment of PSMA-positive metastatic castration-resistant prostate cancer:
- With 2024 sales of US$ 1,058 mln (+24.3% vs 2023), the fluorinated PSMA-targeted PET imaging agent PYLARIFY exceeds US$ 1 billion in net sales and became the first ever blockbuster radiodiagnostic.
- PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) is a radioligand therapeutic agent. Lutetium Lu 177 vipivotide tetraxetan is a PSMA-binding ligand bound to a DOTA chelator radiolabeled with lutetium-177. Pluvicto posted 2024 sales of US$ 1,392 mln (+42% vs 2023).
PSMA mainly serves as a binding target for delivery of a variety of payloads, including, but not limited to, cytotoxic drugs in antibody-drug conjugates, recruitment of cytotoxic T-cells in bispecific antibodies or directly PSMA-targeted chimeric antigen receptor T-cells or natural killer cells.
PSMA is also an important binding target for delivery of radioactive payloads in targeted radioligand therapy, whereby binding molecules can be small molecules, peptides and antibodies. A variety of radioligands are being evaluated or have already been approved, including lutetium 177, actinium 225, lead 212, cupper 67, terbium 161, and astatine 211.

