68Ga-NOTA-PEG2-RM26 PET/CT, First in Man Study

68Ga-NOTA-PEG2-RM26 PET/CT: Tracer Biodistribution and Uptake in Different Kinds of Cancer With Gastrin-Releasing Peptide Receptor (GRPR) Overexpression

This is an open-label positron emission tomography/computed tomography (PET/CT) study to investigate the diagnostic performance and evaluation efficacy of 68Ga-NOTA-PEG2-RM26 in prostate cancer patients. A single dose of 2 MBq/kg of 68Ga-NOTA-PEG2-RM26 limited to 100-200 MBq per examination will be given intravenously. Visual and semiquantitative method will be used to assess PET/CT images.

The gastrin-releasing peptide receptor (GRPR), also known as bombesin receptor subtype II (BB2), is a member of the G protein-coupled receptor family of bombesin receptors. GRPR is over-expressed in various types of human tumors. RM26, a GRPR antagonist with high affinity, was discovered by peptide backbone modification of bombesin analogues.

To target gastrin-releasing peptide receptor in human neoplastic cells NOTA-PEG2-RM26 was synthesised and then labeled with 68Ga.

An open-label whole-body PET/ CT study was designed to investigate the safety and dosimetry of 68Ga-NOTA-PEG2-RM26 and to assess its clinical diagnostic value in patients with cancer.

Inclusion Criteria:

• Primary/recurrent or metastatic cancer in: prostate cancer, breast cancer, colorectal cancer, gastrointestinal carcinoid, gastric cancer, or lung cancer
• Histopathological diagnosis
• Age 18 years or more and palliative disease OR age above 50 years
• Adequate bone marrow, hepatic and renal function, Eastern Cooperative Oncology Group Performance Status Scale 0 or 1 and a negative pregnancy test

Exclusion Criteria:

• Age less than 18 years
• Less than 6 months since a clinically significant cardiovascular event such as myocardial infarction, unstable angina, angioplasty, bypass surgery, stroke or transient ischemic attack
• Congestive heart failure New York Heart Association class ≥ II
• Pregnant or breast-feeding women
• Patients with reproductive potential not implementing accepted and effective means of contraception
• Participation in any other clinical trial within the previous 4 weeks
• Unable to comply with study procedures (e.g., claustrophobia, low back pain not allowing the patient to lay down in the examination bed)