girentuximab (Telix Pharmaceuticals Limited)

Girentuximab (formerly known as cG250) is a chimeric IgG1 monoclonal antibody that specifically targets carbonic anhydrase IX (CAIX), a cell-surface glycoprotein overexpressed in over 95% of clear cell renal cell carcinomas (ccRCC) and other hypoxic solid tumors, but minimally expressed in normal tissues. Originally developed by Wilex AG (now Heidelberg Pharma) as an unconjugated therapeutic antibody (Rencarex) for the adjuvant treatment of ccRCC, its development as a naked antibody was suspended after a Phase III trial (ARISER) failed to show a disease-free survival benefit. In 2017, Telix Pharmaceuticals in-licensed girentuximab to develop it as a radiopharmaceutical platform. Telix is currently developing several radiolabeled formulations of girentuximab: TLX250-CDx/TLX250-Px (Zircaix; zirconium-89 girentuximab senvedoxam), a PET imaging diagnostic agent for ccRCC that completed the Phase III ZIRCON trial and is undergoing BLA resubmission; TLX250-Tx (lutetium-177 girentuximab tetraxetan), a therapeutic radioligand therapy in Phase III (LUTEON study) for advanced ccRCC; and TLX252-Tx (actinium-225 girentuximab), a targeted alpha therapy in Phase I. Girentuximab is also being evaluated in other CAIX-expressing malignancies, including non-muscle-invasive bladder cancer and triple-negative breast cancer.

Brand names

RedectaneRencarexZircaix

Other names

177Lu-DOTA-girentuximab177Lu-girentuximab89Zr-DFO-girentuximab89Zr-girentuximab89Zr-TLX250chimeric monoclonal antibody cG250girentixumabgirentuximablutetium-177 girentuximab tetraxetanlutetium177 girentuximab tetraxetanlutetium 177 girentuximab tetraxetanmonoclonal antibody G-250zirconium-89 girentuximab senvedoxamzirconium89 girentuximab senvedoxamzirconium 89 girentuximab senvedoxam