177Lu-LNC1011 in Patients with Metastatic Castration-resistant Prostate Cancer

A Dosimetry Study and Dose-escalation and of [177Lu]Lu-LNC1011 in Metastatic Castration-Resistant Prostate Cancer Patients

This study employed an open-label, non-randomized design, representing the first human trial of its kind. It utilized a standard 3+3 dose-escalation approach, focusing on patients with metastatic castration-resistant prostate cancer, initiating treatment at a dose of 1.85 GBq over a 6-week period. Subsequent cohorts underwent sequential 50% dose escalations until the observation of dose-limiting toxicity (DLT).

[177Lu]Lu-LNC1011 is a novel long-circulating PSMA therapeutic probe. This study represents the first human investigation, aiming to explore its maximum tolerated dose (MTD), safety, dosimetry, and initial treatment efficacy in patients with metastatic castration-resistant prostate cancer (mCRPC).This study employed an open-label, non-randomized design, representing the first human trial of its kind. It utilized a standard 3+3 dose-escalation approach, focusing on patients with metastatic castration-resistant prostate cancer, initiating treatment at a dose of 1.85 GBq over a 6-week period. Subsequent cohorts received a dose escalation of 0.925 GBq from the previous cohort.

Inclusion Criteria:

• progressive metastatic castration-resistant prostate cancer
• tumors with high PSMA expression confirmed on 68Ga-PSMA PET/CT PSMA expression confirmed on 68Ga-PSMA PET/CT

Exclusion Criteria:

• a serum creatinine level of more than 150 μmol per liter
• a hemoglobin level of less than 10.0 g/dl
• a white-cell count of less than 4.0× 109/L
• a platelet count of less than 100 × 109/L
• a total bilirubin level of more than 3 times the upper limit of the normal range
• a serum albumin level of more than 3.0 g per deciliter
• cardiac insufficiency