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.
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
Allocation
NA
Purpose
DIAGNOSTIC
Masking
NONE
Enrollment
10
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.
Istituto Nazionale Tumori Fondazione G. Pascale - SC Medicina Nucleare e Terapia Metabolica
Naples, Italia, Italy
RECRUITINGQuantitative 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)
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)
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
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)
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