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.

Study Overview

• Status: Recruiting
• Conditions: Cancer
• Intervention / Treatment: Drug: 68Ga-NOTA-PEG2-RM26

Detailed Description

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.

• Study Type: Interventional
• Enrollment (Estimated): 50
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Antonios Tzortzakakis, MD, PhD; Phone Number: 08-123 70 000; Email: antonios.tzortzakakis@regionstockholm.se
• Study Contact Backup: Name: Annette Fransson-Andreo-Hernandez, PhD; Phone Number: +468 517 753 74; Email: annette.fransson-andreo-hernandez@regionstockholm.se

Study Locations

• Sweden
  • Stockholm, Sweden, 17176
    • Recruiting
    • Karolinska University Hospital
    • Contact: Antonios Tzortzakakis, MD, PhD; Phone Number: 08-123 80 000; Email: antonios.tzortzakakis@regionstockholm.se
    • Sub-Investigator: Rimma Axelsson, MD, PhD
    • Sub-Investigator: Antonios Tzortzakakis, MD, PhD

Participation Criteria

Eligibility Criteria

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

Description

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)

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: 68Ga-NOTA-PEG2-RM26; Participants will be injected with 2 MBq/kg of 68Ga-NOTA-PEG2-RM26 limited to 100-200 MBq and then undergo PET/CT examination.	Drug: 68Ga-NOTA-PEG2-RM26; Single-dose 68Ga-NOTA-PEG2-RM26, a gastrin-releasing peptide receptor antagonist linked with a positron emitting radioisotope intravenously injected into participants before the PET/CT scans.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse events within 2 weeks of injection	Adverse events within 2 weeks of injection and scanning of participants	2 weeks

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Biodistribution of 68Ga-NOTA-PEG2-RM26	The semiquantitative analysis will be performed by the same person for all the cases, uptake in organs with uptake above the blood pool will bes described	During procedure
Dosimetry of 68Ga-NOTA-PEG2-RM26	Mean absorbed radiation doses will be estimated using the source and target organ framework outlined by the Medical Internal Radiation Dose Committee. Absorbed and effective radiation doses will be calculated.	During procedure

Collaborators and Investigators

• Sponsor: Karolinska University Hospital
• Collaborators: Uppsala University; Stockholm South General Hospital
• Investigators: Principal Investigator: Jeffrey Yachnin, MD, PhD, Karolinska University Hospital

Study record dates

Study Major Dates

• Study Start (Actual): June 1, 2022
• Primary Completion (Estimated): December 31, 2023
• Study Completion (Estimated): December 31, 2023

Study Registration Dates

• First Submitted: November 17, 2023
• First Submitted That Met QC Criteria: November 23, 2023
• First Posted (Actual): November 27, 2023

Study Record Updates

• Last Update Posted (Actual): November 27, 2023
• Last Update Submitted That Met QC Criteria: November 23, 2023
• Last Verified: November 1, 2023

More Information

Terms related to this study

• Other Study ID Numbers: EudraCT 2021-004980-28

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: UNDECIDED

Drug and device information, study documents

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