This study was designed to assess the safety and therapeutic response to 177 Lu-labeled Evans blue-modified prostate-specific membrane antigen (PSMA) 617 (EB-PSMA-617) treatment with escalating doses in patients with metastatic castration-resistant prostate cancer.

Prostate-specific membrane antigen (PSMA) is a promising target for directing new therapies against several types of cancer. PSMA is a 750-amino acid type II transmembrane glycoprotein that is more avidly expressed in primary as well as in metastatic prostate cancer [5].

This first-in-human study demonstrated that ¹⁷⁷Lu-EB-PSMA-617 had higher accumulation in mCRPC and that low imaging dose appears to be effective in treating tumors with high ⁶⁸Ga-PSMA-617 uptakes.

We aimed to investigate the safety and therapeutic efficacy of radioligand therapy (RLT) of 177 Lu-EB-prostate-specific membrane antigen (PSMA) in patients with metastatic castration-resistant prostate cancer.

Lutetium-177 EB-PSMA-617, as a China-developed PSMA-617 analogue enhanced with truncated Evans Blue, represents an incremental evolution in the field of PSMA-targeted RLT.

EUK-based inhibitors have thus far been the base for the most successful PSMA-targeting LMW inhibitors, such as 18 F-DCFPyL or the FDA-approved, 68 Ga-labelled PSMA-11 for PET imaging or the theranostic variants PSMA-617 and PSMA I&T.

Apr 25, 2023 · SPECT imaging of [177 Lu]Lu-LNC1003 demonstrated significantly improved tumor uptake and retention as compared with [177 Lu]Lu-EB-PSMA and [177 Lu]Lu-PSMA-617, making it suitable for prostate cancer therapy.

May 1, 2018 · In this study, we conjugated a truncated Evans Blue (EB) molecule and DOTA chelator onto PSMA-617 (EB-PSMA-617) and labeled it with 177Lu to increase the tumor accumulation and retention for radioligand therapy.

Jun 23, 2021 · Prostate-specific membrane antigen (PSMA) is highly expressed in metastatic castration-resistant prostate cancer. Lutetium-177 (177 Lu)–PSMA-617 is a radioligand therapy that delivers...

Dec 1, 2020 · This study was designed to assess the safety and therapeutic response to 177Lu-labeled Evans blue–modified prostate-specific membrane antigen (PSMA) 617 (EB-PSMA-617) treatment with escalating doses in patients with metastatic castration-resistant prostate cancer.