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
N.c.a. 177Lu-FRαTM* is an innovative Targeted Radionuclide Therapy candidate under investigation for patients suffering from FRα+ tumors.
N.c.a. 177Lu-FRαTM* consists of two molecular components – firstly, n.c.a. Lutetium-177 (EndolucinBeta®), a synthetic, low-energy beta-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 beta-emitting n.c.a. Lutetium-177 (EndolucinBeta®) 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 n.c.a. 177Lu or 18F. 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