177Lu-PSMA-EB-01

177Lu-PSMA-EB-01 is a novel radiopharmaceutical designed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It consists of a prostate-specific membrane antigen (PSMA) ligand modified with Evans Blue (EB), which allows reversible binding to albumin. This modification slows plasma clearance and increases tumor accumulation compared to earlier PSMA-targeted radioligands. The compound is labeled with the beta-emitting radioisotope lutetium‑177 (^177Lu), enabling targeted radioligand therapy (RLT) that delivers cytotoxic radiation directly to PSMA-expressing tumor cells. The primary mechanism involves selective binding to PSMA on prostate cancer cells, followed by internalization and localized radiation-induced cell death. Early clinical studies indicate promising efficacy in reducing PSA levels and controlling disease progression in mCRPC patients[1][3][5][8].

Other names

177Lu-labeled Evans blue-modified PSMA ligand