Folate Receptor Alpha ⁺ Tumors

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

Please note: n.c.a. ¹⁷⁷Lu-FRαTM and ¹⁸F-AzaFol are not authorized for marketing in any country at this time.