177Lu-EB-PSMA-617

177Lu-EB-PSMA-617 is a radioligand therapeutic agent designed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It is an analogue of PSMA-targeted radioligands, specifically based on PSMA‑617, but modified by conjugation with a truncated Evans Blue (EB) molecule and DOTA chelator. The addition of the EB moiety allows reversible binding to serum albumin, which prolongs plasma half-life and increases tumor uptake and retention compared to unmodified agents like 177Lu‑PSMA‑617. Mechanistically, after intravenous administration, the compound binds to prostate-specific membrane antigen (PSMA), which is highly overexpressed on prostate cancer cells. Upon internalization into tumor cells, lutetium‑177 emits beta particles that induce DNA double-strand breaks and cell death in targeted malignant tissue while minimizing damage to surrounding healthy tissues due to its short emission range. Clinical studies have shown promising safety and efficacy profiles in mCRPC patients[1][2][3][5][8].

Other names

177Lu-labeled Evans blue–modified PSMA ligandEvans blue–modified PSMA radioligand