225ac-psma-cy313

225Ac-PSMA-CY313 is an investigational targeted alpha therapy radiopharmaceutical for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It consists of the alpha-emitting radionuclide actinium-225 (225Ac) conjugated to a prostate-specific membrane antigen (PSMA)-targeting ligand. The drug selectively delivers high-energy alpha radiation to PSMA-expressing tumor cells, inducing lethal DNA damage while minimizing exposure to healthy tissues due to the short range of alpha particles. Early clinical data from 13 patients with heavily pretreated mCRPC showed all patients achieved reductions in prostate-specific antigen (PSA) levels, with 81.8% achieving a PSA50 response (≥50% decline), and an objective response rate of 60%. The safety profile appears manageable, with the most common adverse event being xerostomia (dry mouth), reported in 84.6% of patients, mostly grade 1–2, and no severe adverse events or grade ≥3 toxicities observed in the initial cohort. Dosimetry studies using SPECT/CT demonstrated high tumor absorbed doses, particularly in soft tissue lesions, while maintaining safe exposure limits in critical organs such as the kidneys and liver[1].

Other names

225Ac-PSMA-CY313