RAYZ-6114

RAYZ-6114 is a first-in-class radiopharmaceutical therapy (RPT) candidate developed by RayzeBio in collaboration with PeptiDream. It is composed of a high-affinity macrocyclic peptide binder specific to the Ephrin type-A receptor 2 (EphA2), conjugated via a linker to a DOTA chelator. This design allows for complexation with various radiometals, including the alpha-emitter Actinium-225 (225Ac) and the beta-emitter Lutetium-177 (177Lu). EphA2 is a tumor-associated antigen overexpressed in a wide range of solid malignancies—such as lung, pancreatic, colorectal, and bladder cancers—while showing minimal expression in healthy adult tissues. Preclinical data indicate that RAYZ-6114 undergoes rapid target-mediated internalization and exhibits potent anti-tumor activity, with 225Ac-labeled formulations achieving durable tumor regression in animal models.