Single Microdose Trial- CXCR4 PET Tracer - Pharmacokinetics and Pharmacodynamics of [68Ga]Ga-R54, a Radiopharmaceutical Directed Toward CXCR4 in Patients With Advanced Solid Neoplasia.

May 5, 2026 updated by: National Cancer Institute, Naples
Phase 1, monocentric, open labeled, no profit "Microdose" trial. A single microdose of the new [68Ga]Ga-R54 PET radiopharmaceutical directed against CXCR4 will be injected into patients with advanced solid tumor or multiple myeloma to evaluate the binding.

Study Overview

Status

Recruiting

Conditions

Intervention / Treatment

Detailed Description

The present study aims to evaluate the pharmacokinetic/pharmacodynamic profile and the engagement capacity of a new PET probe that binds the CXCR4 receptor. A Microdose-Trial (Guideline ICH M3(R2) CPMP/ICH/286/95 type 1 approach and EMEA/CHMP/SWP/28367/07 Rev. 1) is proposed in order to evaluate the pharmacokinetics and pharmacodynamics of a single microdose of the radiopharmaceutical [68Ga]Ga-R54 in patients suffering from solid tumors in the advanced stage of the disease or multiple myeloma. At least 5 and no more than 10 consenting patients with advanced solid tumors (breast, lung, colon, ovary, and pancreas) or multiple myeloma will be recruited with at least 1 patient per pathology whose neoplasm expresses CXCR4. Study patients will receive i.v. a single dose of [68Ga]Ga-R54 ≤100 μg. The localization of the target will be carried out with PET/CT method. Pharmacokinetics will be analyzed by blood samples taken at 2, 5, 10, 30 minutes, 1, 2 and 4 hours post infusion. Patients will be enrolled at least 7 days apart to monitor the onset of adverse events.

Study Type

Interventional

Enrollment (Estimated)

10

Phase

  • Early Phase 1

Contacts and Locations

This section provides the contact details for those conducting the study, and information on where this study is being conducted.

Study Contact

Study Locations

  • Italy
    • Italia
      • Naples, Italia, Italy, 80131
        • Recruiting
        • Istituto Nazionale Tumori Fondazione G. Pascale - SC Medicina Nucleare e Terapia Metabolica
        • Contact:
          • Secondo Lastoria

Participation Criteria

Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.

Eligibility Criteria

Ages Eligible for Study

  • Adult
  • Older Adult

Accepts Healthy Volunteers

No

Description

Inclusion Criteria:

  • Patients > 18 years
  • Patients with histological diagnosis of solid neoplasm (breast, lung, colon, ovary, pancreas) in advanced stages or multiple myeloma evaluated by PET/CT with [18F]FDG carried out in the 3 months prior to enrollment. The neoplasm must express the CXCR4 receptor by immunohistochemistry
  • Patients with ECOG performance status 0-2, able to undergo the scheduled diagnostic procedure (PET/CT with [68Ga]Ga-R54).
  • Patients with alkaline phosphatase (AP), alanine aminotransferase (ALT), and aspartate aminotransferase <3 x upper limit of reference range and total bilirubin <2.0 mg/dL
  • Patients with creatinine < 1.5 x upper limit of reference range or 24-hour creatinine clearance > 50 mL/min
  • Negative serum pregnancy test (b-hCG) for women of childbearing age before administration of [68Ga]Ga-R54).
  • Signature of informed consent indicating that the patient (or legal representative) has been informed of all aspects pertinent to the study
  • Willingness and ability to comply with scheduled visits, laboratory tests and other study procedures.

Exclusion Criteria:

  • Presence of active infections (e.g. requiring antibiotic therapy) or other serious concomitant illness, which, in the opinion of the investigator, would place the patient at undue risk or interfere with the study
  • Declared chronic active hepatitis (hepatitis B / C)
  • Declared active autoimmune diseases
  • Recovery from major trauma including surgery within 4 weeks of study enrollment
  • Presence of neurodegenerative diseases
  • Pregnancy and/or breastfeeding
  • Any conditions that in the opinion of the investigator could hinder compliance with the study protocol
  • Patients who have not signed consent to participate in the study

Study Plan

This section provides details of the study plan, including how the study is designed and what the study is measuring.

How is the study designed?

Design Details

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

Arms and Interventions

Participant Group / Arm
Intervention / Treatment
Experimental: [68Ga]Ga-R54 PET/CT scan
Eligible patients with advanced or metastatic breast, pancreatic, colorectal, ovarian, lung cancer or multiple myeloma undergo screening with [18F]-FDG PET/CT and tumor CXCR4 immunohistochemical analysis on available cyto-histological material. Patients with CXCR4-positive tumors and confirmed eligibility are scheduled to undergo [68Ga]Ga-R54 PET/CT imaging within 8 days after a positive [18F]-FDG PET/CT scan. If immunohistochemical assessment is delayed beyond 8 days, a repeat [18F]-FDG PET/CT may be required to confirm eligibility before proceeding. The [68Ga]Ga-R54 PET/CT is performed according to protocol and does not interfere with planned therapeutic management. CXCR4-negative patients are considered screening failures and do not undergo investigational imaging.
Drug: [68Ga]Ga-R54 PET/CT
A single intravenous microdose (≤100 μg) of the CXCR4-targeting radiopharmaceutical [68Ga]Ga-R54 is administered, followed by whole-body PET/CT imaging. Serial blood samples are collected up to 4 hours post-injection to assess pharmacokinetics. Imaging is performed according to institutional standards to evaluate in vivo CXCR4 expression in tumor lesions.

What is the study measuring?

Primary Outcome Measures

Outcome Measure
Time Frame
Quantitative analysis of the uptake (pharmacodynamics) of [68Ga]Ga-R54 in the neoplastic lesion by measuring the "maximum standardized uptake value" (SUVmax).
Time Frame: Single time point at PET/CT imaging (Day 1)
Single time point at PET/CT imaging (Day 1)
Pharmacokinetics of the PET radiopharmaceutical [68Ga]Ga-R54 through measurement of radioactivity in blood at the gamma counter (%ID/g).
Time Frame: Peri-procedural (at time of PET/CT imaging, Day 1)
Peri-procedural (at time of PET/CT imaging, Day 1)

Secondary Outcome Measures

Outcome Measure
Time Frame
Evaluation of the dosimetric parameters for the tumor and for healthy organs by determining the absorbed dose per unit of activity administered (mGy/MBq).
Time Frame: From time of [68Ga]Ga-R54 administration up to 4 hours post-injection
From time of [68Ga]Ga-R54 administration up to 4 hours post-injection
SUVmax correlation of the radiopharmaceutical [68Ga]Ga-R54 and CXCR4 expression assessed by immunohistochemistry in the tumor and microenvironment.
Time Frame: Single time point at PET/CT imaging (Day 1)
Single time point at PET/CT imaging (Day 1)

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Sponsor

National Cancer Institute, Naples

Investigators

  • Study Director: Stefania Scala, M.D., Istituto Nazionale Tumori IRCCS - Fondazione G. Pascale
  • Principal Investigator: Secondo Lastoria, M.D., Istituto Nazionale Tumori IRCCS - Fondazione G. Pascale

Study record dates

These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.

Study Major Dates

Study Start (Actual)

January 24, 2025

Primary Completion (Estimated)

January 1, 2027

Study Completion (Estimated)

January 1, 2027

Study Registration Dates

First Submitted

April 22, 2026

First Submitted That Met QC Criteria

May 5, 2026

First Posted (Actual)

May 11, 2026

Study Record Updates

Last Update Posted (Actual)

May 11, 2026

Last Update Submitted That Met QC Criteria

May 5, 2026

Last Verified

April 1, 2026

More Information

Terms related to this study

Keywords

Additional Relevant MeSH Terms

Other Study ID Numbers

  • R4 FOUR-PET
  • 2024-513303-14-00 (Ctis)

Drug and device information, study documents

Studies a U.S. FDA-regulated drug product

No

Studies a U.S. FDA-regulated device product

No

This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.

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