Ngô Minh Toàn, Adrienn Vágner, Gábor Nagy, Gábor Ország, Tamás Nagy, Csaba Csikos, Balázs Váradi, Gergő Zoltán Sajtos, István Kapus, Zoltán Szoboszlai, Dezső Szikra, György Trencsényi, Gyula Tircsó, Ildikó Garai
This study aimed to develop a novel radiotracer using trastuzumab and the long-lived [52 Mn]Mn isotope for HER2-targeted therapy selection and monitoring. A new Mn(II) chelator, BPPA, synthesized from a rigid bispyclen platform possessing a picolinate pendant arm, formed a stable and inert Mn(II) complex with favorable relaxation properties. BPPA was converted into a bifunctional chelator (BFC), conjugated to trastuzumab, and labeled with [52 Mn]Mn isotope. In comparison to DOTA-GA-trastuzumab, the BPPA-trastuzumab conjugate exhibits a labeling efficiency with [52 Mn]Mn approximately 2 orders of magnitude higher...
May 1, 2024: Journal of Medicinal Chemistry