TLX400

TLX400 is a next-generation radiopharmaceutical therapeutic and diagnostic (theranostic) agent that targets fibroblast activation protein (FAP), a pan-cancer marker highly expressed in the tumor microenvironment of many epithelial cancers and some sarcomas and mesotheliomas. The drug consists of a FAP inhibitor molecule labeled with the beta-emitting radioisotope lutetium-177, designed to deliver targeted ionizing radiation to tumors while minimizing off-target effects. Its novel structure enables extended tumor retention, potentially overcoming limitations seen with first-generation FAP-targeting compounds. TLX400 has demonstrated encouraging safety and efficacy in aggressive, radioiodine-resistant thyroid cancer, achieving median progression-free survival of 29 months and overall survival of 32 months in clinical studies. It is being developed for multiple solid tumor indications including bladder cancer, breast cancer, and thyroid cancer[1][3][4][6][8].

Other names

177Lu-DOTAGA.Glu.(FAPi)2