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.

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.

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