lutetium (177Lu) zadavotide guraxetan

Lutetium (177Lu) zadavotide guraxetan (also known as 177Lu-PSMA-I&T or PNT2002) is an investigational targeted radioligand therapy (RLT). It consists of a peptide-based ligand, zadavotide guraxetan, which targets prostate-specific membrane antigen (PSMA), conjugated to the beta-emitting radioisotope lutetium-177. PSMA is a transmembrane glycoprotein highly overexpressed in prostate cancer and other solid tumors, including salivary gland cancers such as adenoid cystic carcinoma (AdCC) and salivary duct carcinoma (SDC). Upon binding to PSMA, the radiopharmaceutical is internalized, delivering localized cytotoxic beta radiation that induces DNA damage and cell death in tumor cells while minimizing exposure to surrounding healthy tissues. Originally developed by Scintomics, the therapy is being evaluated in Phase 3 clinical trials (such as the ECLIPSE trial by Curium and the SPLASH trial by Point Biopharma/Eli Lilly) for metastatic castration-resistant prostate cancer (mCRPC), and has been investigated in Phase 2 trials by Radboud University Medical Center for advanced salivary gland cancers.

Other names

177Lu-PSMA-I&T[177Lu]Lu-PSMA-I&Tlutetium Lu 177 zadavotide guraxetanlutetium-177 PSMA-I&Tlutetium (177Lu) PSMA