lutetium (177Lu) zadavotide guraxetan (ITM Isotope Technologies Munich)

177Lu-ITG-PSMA-1 (lutetium (177Lu) zadavotide guraxetan, also known as 177Lu-PSMA-I&T) is a prostate-specific membrane antigen (PSMA)-targeted radioligand therapy. It consists of a small-molecule urea-based PSMA inhibitor (zadavotide guraxetan) conjugated to the beta-emitting radioisotope lutetium-177 via a DOTAGA chelator. Originally developed by Scintomics, the radiopharmaceutical is being developed by several entities, including ITM Isotope Technologies Munich (as 177Lu-ITG-PSMA-1), Curium (as 177Lu-PSMA-I&T), and POINT Biopharma/Lantheus/Eli Lilly (as PNT-2002). It selectively binds to PSMA (glutamate carboxypeptidase II), which is highly overexpressed on prostate cancer cells and the neovasculature of various solid tumors. Upon binding, the compound is internalized, and the beta radiation emitted by lutetium-177 induces DNA damage and cell death in the target tumor cells. It is primarily in Phase III clinical development for metastatic castration-resistant prostate cancer (mCRPC) and is also being investigated in early-phase trials for other PSMA-expressing malignancies, such as soft tissue sarcoma.

Other names

177Lu-PSMA I&T177Lu-PSMA-I&TLu-177-PSMA-I&Tlutetium Lu 177 zadavotide guraxetanlutetium Lu-177 zadavotide guraxetanzadavotide guraxetan