Lutetium Lu 177 Vipivotide Tetraxetan: First Approval

Lutetium Lu 177 vipivotide tetraxetan (PLUVICTO™, formerly known as (177)Lu-PSMA-617) is a radioligand therapeutic agent that is being developed by Advanced Accelerator Applications (a subsidiary of Novartis) for the treatment of prostate-specific membrane antigen (PSMA)-expressing metastatic prostate cancer. The active part of the radiopharmaceutical is lutetium-177, which is linked to a ligand that binds to prostate-specific membrane antigen (PSMA), a transmembrane enzyme overexpressed in primary and metastatic prostate cancers. Based on efficacy results from the phase 3 VISION trial, lutetium Lu 177 vipivotide tetraxetan was approved in the USA on 23 March 2022 for the treatment of adult patients with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor (AR) pathway inhibition and taxane-based chemotherapy. Regulatory review in the EU and other countries is underway. This article summarizes the milestones in the development of Lutetium Lu 177 vipivotide tetraxetan leading to this first approval as a therapeutic radioligand for mCRPC. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s40291-022-00594-2.