177Lu-PSMA-617 is a radioligand therapy (RLT) being developed by Novartis (acquired from Endocyte) that utilizes a high affinity targeting ligand to direct potent radiotherapy to prostate cancer cells. The specific targeting of this therapy comes from the “ligand” portion of the RLT, which is a small molecule designed to bind to Prostate Specific Membrane Antigen, or, PSMA, a protein highly expressed on the cell surface of most prostate cancer cells but absent on most normal cells. The PSMA targeting ligand in 177Lu-PSMA-617, is chemically attached to a therapeutic radioactive atom called Lutetium-177 (177Lu), which releases an energetic beta particle to precisely deliver cell killing radiation to the site of disease. Unlike traditional external beam radiotherapy, 177Lu-PSMA-617 is administered as a systemic injection where it can directly target multiple sites of PSMA-positive prostate cancer throughout the body, including the bone and soft tissue, while bypassing the PSMA-negative healthy cells. The expression of PSMA prior to treatment with 177Lu-PSMA-617 can be determined using whole body PSMA-directed imaging, allowing for personalization of treatment so that the best course of therapy might be selected. It is estimated that approximately 80% of men with metastatic castration-resistant prostate cancer (mCRPC) express PSMA on their cancer cells.


Purdue Faculty

Dr. Philip Low

Clinical Trial Information

Phase 3 Trial - Study of 177Lu-PSMA-617 In Metastatic Castrate-Resistant Prostate Cancer (VISION)

Phase 2 Trial - A Trial of 177Lu-PSMA617 Theranostic Versus Cabazitaxel in Progressive Metastatic Castration Resistant Prostate Cancer (TheraP)

Phase 2 Trial - Lutetium-177 (Lu177) Prostate-Specific Antigen (PSMA)-Directed EndoRadiotherapy

Phase 2 Trial - Radiometabolic Therapy (RMT) With 177Lu PSMA 617 in Advanced Castration Resistant Prostate Cancer (CRPC) (LU-PSMA)

Phase 1 Trial - Phase I Dose-escalation Study of Fractionated 177Lu-PSMA-617 for Progressive Metastatic CRPC

Phase 1 Trial - 177Lu-EB-PSMA617 in Patients With Metastatic Castration-resistant Prostate Cancer

Development Partner



Research Articles

External radiation exposure, excretion, and effective half-life in 177Lu-PSMA-targeted therapies

Predictors of overall survival in metastatic castration-resistant prostate cancer patients receiving [177Lu]Lu-PSMA-617 radioligand therapy

177Lu-PSMA-617 radioligand therapy for a patient with lymph node metastatic prostate cancer

Radioligand therapy of metastatic prostate cancer using 177Lu-PSMA-617 after radiation exposure to 223Ra-dichloride

Repeated 177Lu-Labeled PSMA-617 Radioligand Therapy Using Treatment Activities of Up to 9.3 GBq

Combination of 177Lu-PSMA-617 and External Radiotherapy for the Treatment of Cerebral Metastases in Patients With Castration-Resistant Metastatic Prostate Cancer

177Lu-PSMA-617 radioligand therapy and outcome in patients with metastasized castration-resistant prostate cancer

Possible Treatment Approach to an Extravasation of 177Lu-PSMA-617

Overall survival and response pattern of castration-resistant metastatic prostate cancer to multiple cycles of radioligand therapy using [177Lu]Lu-PSMA-617

The impact of repeated cycles of radioligand therapy using [177Lu]Lu-PSMA-617 on renal function in patients with hormone refractory metastatic prostate cancer

44Sc-PSMA-617 for radiotheragnostics in tandem with 177Lu-PSMA-617—preclinical investigations in comparison with 68Ga-PSMA-11 and 68Ga-PSMA-617

German Multicenter Study Investigating 177Lu-PSMA-617 Radioligand Therapy in Advanced Prostate Cancer Patients

Successful Treatment of Hepatic Metastases of Hormone Refractory Prostate Cancer Using Radioligand Therapy With 177Lu-PSMA-617

Predictors of Response to Radioligand Therapy of Metastatic Castrate-Resistant Prostate Cancer with 177Lu-PSMA-617

Cocktail Therapy of 177Lu-PSMA-617 and 177Lu-EDTMP in Patients With mCRPC: A Proof-of-Principle Application

Radioligand Therapy With 177Lu-PSMA-617 as A Novel Therapeutic Option in Patients With Metastatic Castration Resistant Prostate Cancer

Response and Tolerability of a Single Dose of 177Lu-PSMA-617 in Patients with Metastatic Castration-Resistant Prostate Cancer: A Multicenter Retrospective Analysis

Establishing 177Lu-PSMA-617 Radioligand Therapy in a Syngeneic Model of Murine Prostate Cancer

PSMA-Targeted Radionuclide Therapy of Metastatic Castration-Resistant Prostate Cancer with 177Lu-Labeled PSMA-617

Metastatic Prostate Cancer With Restored Hormone-Response After Radioligand Therapy With 177Lu-PSMA-617

Pre-therapeutic dosimetry of normal organs and tissues of 177Lu-PSMA-617 prostate-specific membrane antigen (PSMA) inhibitor in patients with castration-resistant prostate cancer