lutetium Lu 177 girentuximab tetraxetan

Lutetium Lu 177 girentuximab tetraxetan (also known as 177Lu-DOTA-girentuximab or TLX250-Tx) is a first-in-class, targeted radiopharmaceutical therapy (radioimmunotherapy) consisting of the chimeric monoclonal antibody girentuximab (cG250) conjugated via a tetraxetan (DOTA) chelator to the beta-emitting radioisotope lutetium-177. Girentuximab specifically targets carbonic anhydrase IX (CAIX), a cell-surface protein highly overexpressed in more than 95% of clear cell renal cell carcinoma (ccRCC) cases due to VHL gene mutation-induced hypoxia, with minimal expression in normal tissues. Upon binding to CAIX, the radioimmunoconjugate is internalized, delivering localized cytotoxic beta radiation directly to the tumor cells, which induces DNA double-strand breaks and subsequent cell death. Originally developed by Radboud University Medical Center and WILEX (now Heidelberg Pharma), the drug is being globally developed by Telix Pharmaceuticals. It is currently in Phase 3 clinical development (the LUTEON trial) for the treatment of advanced, relapsed, or recurrent clear cell renal cell carcinoma, and is also being evaluated in Phase 1/2 trials in combination with other agents (such as peposertib, nivolumab, and cabozantinib) for ccRCC and other CAIX-expressing solid tumors.

Brand names

Lutarex

Other names

lutetium Lu 177-DOTA-girentuximablutetium (177Lu) girentuximab tetraxetanlutetium Lu-177 girentuximab tetraxetan177Lu-girentuximab tetraxetan