Drug intelligence / Profile preview

actinium (225Ac) vipivotide tetraxetan

Development stage
Unknown
Lead developer
Advanced Accelerator Applications
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

actinium (225Ac) vipivotide tetraxetan (AAA817, [225Ac]Ac-PSMA-617) is an investigational targeted alpha-particle radioligand therapy developed by Novartis (via its subsidiary Advanced Accelerator Applications) for the treatment of prostate-specific membrane antigen (PSMA)-positive prostate cancer, including metastatic castration-resistant prostate cancer (mCRPC). The drug consists of the PSMA-targeting ligand vipivotide tetraxetan (PSMA-617) conjugated to the alpha-emitting radioisotope actinium-225. It binds specifically to PSMA on the surface of prostate cancer cells, where it is internalized and delivers high-energy alpha radiation over a very short range, causing lethal double-strand DNA breaks in the tumor cells while sparing surrounding healthy tissue. It is currently being evaluated in Phase III clinical trials.

Other names
[225Ac]Ac-PSMA-617[225Ac]Ac-PSMA617225Ac-PSMA-617actinium Ac-225 vipivotide tetraxetanactinium-225 PSMA-617actinium225 PSMA-617actinium 225 PSMA-617actinium-225-PSMA-617actinium225-PSMA-617actinium 225-PSMA-617actinium-225-vipivotide tetraxetanactinium225-vipivotide tetraxetanactinium 225-vipivotide tetraxetan
02

Targets

PSMA (Prostate-specific membrane antigen)

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