Folate receptor α (FRα) is selectively overexpressed on the cell surface of many different cancers, such as non-small-cell lung carcinoma, ovarian cancer or triple negative breast cancer. Targeted Radionuclide Therapies against (FRα) could be of significant importance for the treatment of patients diagnosed with these tumors.1
ITM-52 (225Ac-FRαTM*) is an innovative Targeted Radionuclide Therapy candidate under investigation for patients suffering from FRα+ tumors.
ITM-52 consists of two molecular components – firstly, actinium-225, a high-energy alpha-emitting radioisotope, and secondly, FRαTM*, a FRα specific folate variant, which is currently nondisclosed. This novel tumor-specific FRα targeting molecule has been designed for labeling with therapeutic actinium-225 as well as the companion diagnostic PET-radioisotope fluorine-18.
The FRα targeting molecules, which are under development, bind with high affinity to FRα, retaining receptor-binding properties when labeled with 225Ac or 18F. ITM-55 (18F-AzaFol) has demonstrated excellent dosimetric results and imaging in a Phase I study in patients with cancer.2 Merck KGaA, a global leader in active pharmaceutical development, exclusively supplies ITM FRα targeting molecules for radiolabeling and clinical development.
* FRαTM = Folate Receptor α (FRα) Targeting Molecule
1 Cheung et al., 2016, Oncotarget 7(32): 52553–52574
2 Schniering et al., 2019, Frontiers in Immunology 10: 2724
Please note: ITM-52 (225Ac-FRαTM) and ITM-55 (18F-AzaFol) are not authorized for marketing in any country at this time.