131I-iodofalan

131I-iodofalan (also known as TLX101, 131I-IPA, or ACD-101) is an investigational, systemically administered small molecule radiopharmaceutical therapy being developed by Telix Pharmaceuticals (originally originated by Therapeia) for the treatment of glioblastoma multiforme (GBM) and other high-grade gliomas. The drug consists of L-4-iodophenylalanine labeled with the beta-emitting radioisotope iodine-131 (131I). It selectively crosses the blood-brain barrier and targets L-type amino acid transporters (primarily LAT1/SLC7A5 and LAT2/SLC7A8), which are highly overexpressed in glioma cells. Upon intracellular accumulation, 131I-iodofalan delivers targeted cytotoxic radiation directly to the tumor cells, inducing DNA damage and cell death, while also acting as an intrinsic radiosensitizer to enhance the efficacy of external beam radiation therapy (EBRT). It is currently in Phase III clinical development.

Other names

131I-L-4-iodophenylalanine4-L-[131I]iodophenylalanine4-L-[131I]iodo-phenylalaninecarrier-added 4-L-[131I]iodophenylalanineiodofalan (131I)iodofalan I-131L-phenylalanine, 4-(iodo-131I)-4-(131I)iodo-L-phenylalanine131I-IPA