¹⁷⁷Lu-PSMA-R2 was developed as patent protected equivalent of ¹⁷⁷Lu-PSMA-617. This is another prostate-specific membrane antigen (PSMA) based molecule developed as a new prostate cancer therapeutic agent. It is a urea-based PSMA antigen targeting carboxypeptidase-II.

A first clinical trial with this drug was initiated in May 2018, the study PROter (96 patients, completion June 2022), in which the patients are selected on the basis of Imaging provided with ⁶⁸Ga-PSMA-R2 (Phase I/II).

Target/Mechanism: PSMA

Carrier/Ligand: PSMA-R2

Radiation Type: beta electrons (β^–)