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RYZ801/811 is a GPC3-targeted theranostic radiopharmaceutical peptide-drug conjugate (RI-PDC) program developed by RayzeBio (a Bristol Myers Squibb company) in collaboration with PeptiDream and Modulus Discovery. The program consists of two agents: RYZ801, which is labeled with the alpha-emitting radioisotope Actinium-225 (225Ac) for therapeutic purposes, and RYZ811, which is labeled with Gallium-68 (68Ga) for diagnostic PET imaging. Both agents utilize a high-affinity macrocyclic peptide discovered via PeptiDream's PDPS platform to selectively target Glypican-3 (GPC3), a cell-surface oncofetal antigen that is highly overexpressed in hepatocellular carcinoma (HCC) but absent in most healthy adult tissues. By binding to GPC3, RYZ801 delivers potent alpha radiation directly to the tumor site, inducing double-stranded DNA breaks and cell death, while RYZ811 allows for patient selection and treatment monitoring through molecular imaging. The program is currently in Phase 1 clinical development for patients with GPC3-positive advanced hepatocellular carcinoma.
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