Drug intelligence / Profile preview

actinium-225 PSMA

Development stage
Unknown
Lead developer
Affiliated Hospital of Southwest Medical University
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals
Administration
Intravenous
01

Overview

Actinium-225 PSMA (225Ac-PSMA) is a targeted alpha therapy (TAT) radiopharmaceutical platform designed for the treatment of prostate cancer, particularly metastatic castration-resistant prostate cancer (mCRPC). It consists of a prostate-specific membrane antigen (PSMA)-targeting ligand (such as PSMA-617 or PSMA-I&T) conjugated to the alpha-emitting radioisotope actinium-225 (225Ac). Upon administration, the radioligand binds specifically to PSMA-expressing prostate cancer cells, where the actinium-225 decays, emitting high-energy alpha particles over a short range. This localized radiation induces double-stranded DNA breaks, leading to tumor cell death while minimizing damage to surrounding healthy tissues.

Other names
225Ac-PSMA225Ac-PSMA RLT Agentactinium Ac 225 PSMAactinium-225-labeled PSMAactinium225-labeled PSMAactinium 225-labeled PSMAactinium-225-PSMAactinium225-PSMAactinium 225-PSMAactinium-225-PSMA radioligandactinium225-PSMA radioligandactinium 225-PSMA radioligand
02

Targets

DNAPSMA (Prostate-specific membrane antigen)

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