Clinical Evaluation of [177Lu]Lu-BQ7876 for Targeting of Prostate-Specific Membrane Antigen

Clinical Evaluation of Lutetium-177 Labeled BQ7876 for Targeting of Prostate-Specific Membrane Antigen

The study should evaluate the biological distribution of [177Lu]Lu-BQ7876 in patients with prostate cancer.

The objective are:

1. To evaluate the content of [177Lu]Lu-BQ7876 in the blood of patients with prostate cancer at different time points after a single intravenous administration.
2. To assess the distribution of [177Lu]Lu-BQ7876 in normal tissues and tumors at different time points.
3. To evaluate dosimetry of [177Lu]Lu-BQ7876.
4. To study the safety and tolerability of the drug [177Lu]Lu-BQ7876 after a single injection.

Study Overview

• Status: Completed
• Conditions: Prostate Cancers
• Intervention / Treatment: Drug: One single intravenous injection of [177Lu]Lu-BQ7876

Detailed Description

The overall goal is to study the effectiveness of prostate-specific membrane antigen targeting using Lutetium-177 - labeled BQ7876.

Phase I of the study:

Biodistribution, dosimetry, safety and tolerability of [177Lu]Lu-BQ7876 in patients with prostate cancer.

The main objectives of the study:

1. To evaluate the content of [177Lu]Lu-BQ7876 in the blood of patients with prostate cancer at different time points after a single intravenous administration.
2. To evaluate the distribution of [177Lu]Lu-BQ7876 in normal tissues and tumors in patients with prostate cancer at different time points after a single intravenous administration.
3. To evaluate dosimetry of [177Lu]Lu-BQ7876 based on the pharmacokinetic parameters of the drug after a single intravenous administration.
4. To study the safety of use and tolerability of the drug [177Lu]Lu-BQ7876 after a single intravenous administration in a diagnostic dosage.

Methodology:

Open-label, exploratory, single centre study. The subjects will receive a single injection of the labeled tracer.

• Study Type: Interventional
• Enrollment (Actual): 7
• Phase: Phase 1

Contacts and Locations

Study Locations

• Russian Federation
  • Tomsk, Russian Federation, 634050
    • TomskNRMC

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: No

Description

Inclusion Criteria:

• Subject is > 18 years of age
• Clinical and radiological diagnosis of prostate cancer with histological verification.
• White blood cell count: > 2.0 x 10^9/L
• Haemoglobin: > 80 g/L
• Platelets: > 50.0 x 10^9/L
• Bilirubin =< 2.0 times Upper Limit of Normal
• Serum creatinine: Within Normal Limits
• Blood glucose level not more than 5.9 mmol/L
• Subject is capable to undergo the diagnostic investigations to be performed in the study
• Informed consent

Exclusion Criteria:

• Active current autoimmune disease or history of autoimmune disease
• Active infection or history of severe infection within the previous 3 months (if clinically relevant at screening)
• Known HIV positive or chronically active hepatitis B or C
• Administration of other investigational medicinal product within 30 days of screening
• Ongoing toxicity > grade 2 from previous standard or investigational therapies, according to US National Cancer Institute's

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Prostate cancer; One single intravenous injection of [177Lu]Lu-BQ7876	Drug: One single intravenous injection of [177Lu]Lu-BQ7876; One single intravenous injection of 600-800 MBq [177Lu]Lu-BQ7876 in prostate cancer patients.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
[177Lu]Lu-BQ7876 blood сlearance	Measurement of [177Lu]Lu-BQ7876 activity in patient blood samples at various time points: after 5, 10, 20, 40, 60 and 90 minutes, 2, 3, 24, 48 hours.	48 hours
Gamma camera-based whole-body [177Lu]Lu-BQ7876	Whole-body [177Lu]Lu-BQ7876 uptake coinciding with normal organs and tissues will be assessed using gamma camera and calculated as percentage (%) of the injected dose of the radiopharmaceutical at 1, 4, 24, 48, 72, 120 hours after single injection.	120 hours
SPECT/CT-based [177Lu]Lu-BQ7876 uptake in tumor lesions (SUVmean)	[177Lu]Lu-BQ7876 uptake (SUVmean) with tumor lesions will be assessed using single-photon emission computed tomography and measured in SUVmean after 4, 48, 72 and 120 hours after single injection of radiopharmaceutical.	120 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Percent of cases with abnormal findings relative to baseline [Safety and Tolerability]	The safety attributable to [177Lu]Lu-BQ7876 injections will be evaluated based on the assessments of physical examination, vital signs, and ECG (percent of cases with abnormal findings relative to baseline)	48 hours
Percent of participants with abnormal laboratory values that are related to [177Lu]Lu-BQ7876 injection [Safety and Tolerability]	The safety attributable to [177Lu]Lu-BQ7876 injections will be evaluated based on the blood and urine laboratory tests (percent of cases with abnormal findings relative to baseline)	48 hours
Percent of participants with adverse events that are related to [177Lu]Lu-BQ7876 injection [Safety and Tolerability]	The safety attributable to [177Lu]Lu-BQ7876 injections will be evaluated based on the rate of adverse events(percent of cases with abnormal findings relative to baseline)	48 hours
Percent of participants requiring administration of medication due to side effects that are related to [177Lu]Lu-BQ7876 injection [Safety and Tolerability]	The safety attributable to [177Lu]Lu-BQ7876 injections will be evaluated based on the rate of administration of concomitant medication (percent of cases with abnormal findings relative to baseline)	48 hours

Collaborators and Investigators

• Sponsor: Tomsk National Research Medical Center of the Russian Academy of Sciences
• Investigators: Principal Investigator: Vladimir I Chernov, MD, Prof, Tomsk NRMC

Study record dates

Study Major Dates

• Study Start (Actual): October 1, 2024
• Primary Completion (Actual): December 1, 2024
• Study Completion (Actual): February 28, 2025

Study Registration Dates

• First Submitted: October 11, 2024
• First Submitted That Met QC Criteria: October 11, 2024
• First Posted (Actual): October 15, 2024

Study Record Updates

• Last Update Posted (Actual): April 9, 2025
• Last Update Submitted That Met QC Criteria: April 7, 2025
• Last Verified: April 1, 2025

More Information

Terms related to this study

• Keywords: Radioligand Therapy; Prostate-Specific Membrane Antigen; Prostate Cancers; [177Lu]Lu-BQ7876
• Additional Relevant MeSH Terms: Urogenital Diseases; Genital Diseases; Genital Neoplasms, Male; Urogenital Neoplasms; Neoplasms by Site; Neoplasms; Genital Diseases, Male; Prostatic Diseases; Male Urogenital Diseases; Prostatic Neoplasms
• Other Study ID Numbers: [177Lu]Lu-BQ7876

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: YES
• IPD Plan Description: Deidentified individual participant data (text, tables, figures, and appendices), underlying the results of the trial, will be shared with researchers to achieve the aims in the approved proposal
• IPD Sharing Time Frame: Proposals may be submitted up to 36 months following publication of the results of the trial. After 36 months, the data will be available in the Center's data ware house but without investigator support other than deposited metadata.
• IPD Sharing Access Criteria: Information regarding submitting proposals and accessing data may be requested from the principal investigator by e-mail.
• IPD Sharing Supporting Information Type: STUDY_PROTOCOL; SAP; ICF

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No