¹⁷⁷Lu-TLX250 (177Lu-Lutarex®, ¹⁷⁷Lu-Girentuximab), a Lutetium-177-labeled monoclonal antibody is being developed as a potential RIT for various cancers including renal cell carcinoma (RCC). ¹⁷⁷Lu-cG250’s development became an extension of the development of the Imaging agent ¹²⁴I-Girentuximab (¹²⁴I-Redectane®).

G250 (Girentuximab) is a chimeric murine human monoclonal antibody which targets the Carbonic Anhydrase IX (CA-IX) molecule/G250 antigen, expressed on over 90% of clear cell renal cell carcinomas.

A Phase I/II safety and efficacy trial with ¹⁷⁷Lu-cG250 was initiated in February 2005 in patients with advanced RCC. The Dosimetry was determined using ¹¹¹In-cG250. A Phase II efficacy study was initiated in 2013 in patients with advanced clear cell kidney cancer. The study demonstrated stability in about 75% of the patients.

The development of this molecule is now progressing in a fast way (Phase II) and the diagnostic agent could reach the market by 2023.

Target/Mechanism: CAIX

Carrier/Ligand: Girentuximab

Radiation Type: beta electrons (β^–)