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3BP-3940, a highly potent FAP-targeting peptide for theranostics - production, validation and first in human
Lukas Greifenstein1, Annika Gunkel1, Aileen Hoehne2
1CURANOSTICUM Wiesbaden-Frankfurt, Center for Advanced Radiomolecular Precision Oncology, 65191 Wiesbaden, Germany.
Abstract:
Hardly any new tracers attracted more attention in nuclear medicine in the last couple of years than radiolabeled fibroblast activation protein inhibitors (FAPi's). Molecules targeting cancer-associated fibroblasts (CAFs) or disease-associated fibroblasts in benign disorders (DAFs) gave rise to a new class of radiopharmaceuticals widely applicable for imaging and with the desired use as therapeutic compounds. Despite displaying benefits in diagnostic sensitivity over FDG, most FAP-targeting compounds in today's clinical routine continue to lack therapeutic utility due to short tumor retention. In this study, we evaluated 3BP-3940, specifically designed for achieving prolonged tumor retention and remarkably low uptake in healthy tissues. We herein present the automated manufacturing of gallium-68 (Ga-68) and lutetium-177 (Lu-177)-labeled 3BP-3940, their respective in vitro stability, validation of an automated production process, and validation of an analytical HPLC method for quality control. Finally, we give a first insight into the clinical utility of the two compounds.
Insights
New fibroblast activation protein inhibitors (FAPIs) show promise for cancer imaging and therapy. This study introduces 3BP-3940, a novel FAPI designed for enhanced tumor retention and low healthy tissue uptake, with automated production of its Ga-68 and Lu-177 versions.
Area of Science:
- Nuclear Medicine
- Radiopharmaceutical Chemistry
- Oncology
Background:
- Radiolabeled fibroblast activation protein inhibitors (FAPIs) are emerging as crucial tools in nuclear medicine.
- While FAPIs offer superior diagnostic sensitivity over FDG, many lack therapeutic utility due to insufficient tumor retention.
Purpose of the Study:
- To evaluate 3BP-3940, a novel FAPI designed for prolonged tumor retention and minimal healthy tissue uptake.
- To present the automated manufacturing and quality control of gallium-68 (Ga-68) and lutetium-177 (Lu-177) labeled 3BP-3940.
- To provide initial insights into the clinical utility of these FAPI agents.
Main Methods:
- Automated synthesis of Ga-68 and Lu-177 labeled 3BP-3940.
- In vitro stability assessment of the radiolabeled compounds.
- Validation of the automated production process and an analytical HPLC method for quality control.
Main Results:
- Successful automated manufacturing of both Ga-68-3BP-3940 and Lu-177-3BP-3940.
- Demonstrated in vitro stability of the radiopharmaceuticals.
- Validated analytical methods ensuring quality control for clinical application.
Conclusions:
- The automated production of Ga-68 and Lu-177 labeled 3BP-3940 is feasible and validated.
- 3BP-3940 demonstrates potential for improved tumor retention and diagnostic/therapeutic applications in FAPI-based nuclear medicine.
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