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Drug intelligence / Profile preview
[64Cu]Cu-Alpha-PET-FAPI
- Development stage
- Preclinical
- Lead developer
- Mayo Clinic
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Positron Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
[64Cu]Cu-Alpha-PET-FAPI is a novel, small-molecule radiotheranostic probe designed to target fibroblast activation protein (FAP), which is highly expressed on cancer-associated fibroblasts in the tumor stroma of over 90% of solid tumors. Developed by researchers at the Mayo Clinic, this 1776 Da molecule features two distinct chelators that allow for selective radiolabeling with both diagnostic and therapeutic radioisotopes without altering its chemical structure. It is primarily intended for diagnostic positron emission tomography (PET) imaging, therapeutic monitoring, and accurate dosimetry estimation. In preclinical models of glioblastoma and pancreatic cancer, [64Cu]Cu-Alpha-PET-FAPI demonstrated high and specific tumor uptake with prolonged retention up to 72 hours post-injection and relatively low kidney retention, highlighting its potential for clinical translation.
- Other names
- 64Cu-Alpha-PET-FAPI[64Cu]Cu-Alpha-PET-FAPI
02
Targets
FAP (Fibroblast activation protein alpha)
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