lutetium (177lu) psma i&t

Lutetium (177Lu) PSMA I&T is a targeted radioligand therapy (RLT) developed for the treatment of prostate cancer. It consists of the beta-emitting radioisotope lutetium-177 conjugated to the PSMA I&T (Imaging & Therapy) ligand, a urea-based small molecule that binds with high affinity to the extracellular domain of prostate-specific membrane antigen (PSMA). PSMA is a transmembrane protein that is significantly overexpressed in prostate cancer cells, including metastatic and castration-resistant forms. Upon binding, the complex is internalized by the cancer cells, allowing the lutetium-177 to deliver localized ionizing radiation (beta particles) that induces double-stranded DNA breaks, leading to cell death. While functionally similar to the FDA-approved 177Lu-PSMA-617 (Pluvicto), PSMA I&T is chemically distinct, utilizing a DOTAGA chelator instead of DOTA. The drug is being evaluated in late-stage clinical trials (e.g., the SPLASH trial) for metastatic castration-resistant prostate cancer (mCRPC) and in earlier-phase studies for neoadjuvant applications in oligometastatic disease.

Other names

177Lu-PSMA-I&T[177Lu]Lu-PSMA-I&TLutetium-177 PSMA I&TDOTAGA-PSMA-I&T177Lu-PNT2002