Related Experiment Video
Updated: Jan 18, 2026
Intracranial Implantation with Subsequent 3D In Vivo Bioluminescent Imaging of Murine Gliomas
Published on: November 6, 2011
Novel Urokinase-Type Plasminogen Activator Receptor-Targeting Optical Imaging Agent ICG-Glu-Glu-AE105 for
Jane Skjøth-Rasmussen1,2, Aleena Azam1,3,4, Karina Juhl3,4,5
1Department of Neurosurgery, Neuroscience Center, Copenhagen University Hospital - Rigshospitalet, Copenhagen , Denmark.
Background And Objectives:
Glioblastoma is an aggressive form of brain cancer for which surgery is the keystone in treatment before oncological treatment. Improving surgical resection without jeopardizing the outcome is eminent, and a fluorescent drug to aid surgical outcome is warranted. To evaluate the safety and the efficacy of a novel urokinase-type Plasminogen Activator Receptor-targeting near-infrared optical imaging agent, ICG-Glu-Glu-AE105 (FG001), in patients with malignant glioma (glioblastoma).
Methods:
First-in-human phase I dose escalation and time elaboration study in 35 patients undergoing surgery for glioblastoma. The tumor-to-background ratio (TBR) was measured on near-infrared images as an objective measure of image contrast. Biopsies were taken during surgery from areas with and without fluorescence (FG001) and compared with pathology as reference. Efficacy was evaluated as sensitivity and specificity of FG001 to detect tumor tissue. The study was conducted with close safety monitoring.
Results:
Administration of FG001 at a dose of 36 mg, 12 to 17 hours before surgery, resulted in optimal image contrast between tumor and normal brain tissue, with a mean TBR of 3.6. A high sensitivity (79%) and specificity (100%) for the detection of tumor tissue was found. Safety monitoring during the study identified only a few related adverse events, all of which were of mild grade.
Conclusion:
FG001 was found to be safe and well tolerated in the patients included in the study. The optimal dose of FG001 was selected on the basis of videos taken during the surgery and the measured TBR values. A dose of 36 mg administered 16 hours (mean) before the surgery showed the best contrast (TBR values) and optimal visualization of the tumor delineation. Histology demonstrated good sensitivity of FG001.
Insights
A novel fluorescent drug, FG001, safely enhances glioblastoma surgical resection by improving tumor visualization. The optimal dose of 36 mg, administered 16 hours prior, demonstrated high sensitivity and specificity in detecting cancerous tissue.
Area of Science:
- Oncology
- Medical Imaging
- Pharmacology
Background:
- Glioblastoma is an aggressive brain cancer requiring maximal surgical resection.
- Improving surgical precision is crucial for better patient outcomes.
- A targeted fluorescent agent can aid intraoperative tumor delineation.
Purpose of the Study:
- To evaluate the safety and efficacy of FG001, a novel near-infrared optical imaging agent.
- To assess FG001's ability to target urokinase-type Plasminogen Activator Receptor in malignant glioma.
- To determine the optimal dose and timing for FG001 administration in glioblastoma patients.
Main Methods:
- Phase I, first-in-human dose escalation study in 35 glioblastoma patients.
- Measurement of tumor-to-background ratio (TBR) for image contrast assessment.
- Histopathological analysis of tumor biopsies to determine FG001 sensitivity and specificity.
Main Results:
- Optimal image contrast (mean TBR 3.6) achieved with 36 mg FG001, 12-17 hours pre-surgery.
- High diagnostic accuracy: 79% sensitivity and 100% specificity for tumor detection.
- FG001 was well-tolerated with few mild adverse events.
Conclusions:
- FG001 is safe and well-tolerated for glioblastoma patients.
- A 36 mg dose, given 16 hours before surgery, provides optimal tumor visualization.
- FG001 demonstrates significant potential to improve surgical resection of malignant gliomas.
