Theranostic Somatostatin Receptor Ligands

One of the intrinsic properties of neuroendocrine tumors (NETs) is the overexpression of somatostatin receptors (SSTRs) that mediates reduced sensitivity to growth inhibitory factors and thus, provides the basis for imaging and therapy using radiolabeled SST analogs. Here an innovation is described following the successful radiohybrid concept: The compounds offer both diagnostic and therapeutic solutions for neuroendocrine neoplasms.
Life Sciences
Reference
b83143
IP right year
2025
IP status
PCT application filed in
Applicant
Technical University of Munich
Contact
Katharina Stoiber

Challenge and innovation

The currently used theranostic pairs such as [68Ga]Ga-DOTA-TATE and [177Lu]Lu DOTA-TATE have different chemical and pharmacological properties due to the different metals incorporated, which has increased the interest in "true theranostic compounds" where one compound can be labeled with a diagnostic and therapeutic radionuclide with the same pharmacological properties. In addition, a shift from Ga-68- to F-18-labeled compounds has occurred in recent years.

With the development of the new SiFA building block (SiFA)SeFe, a silicon-based fluoride acceptor is now available for the first time that provides sufficient hydrophilicity directly to the aromatic through the use of a carboxylate group in one meta-position and an amide group in the other meta-position to the Si function. The innovative radiohybrids that can be labeled with fluorine-18 (F-18) for precise diagnostic purposes and lutetium-177 (Lu-177) for effective therapeutic applications.

Talk to an expert

Interested in learning more about this technology offer, exploring potential applications or discussing a possible collaboration? Get in touch to learn more.

Katharina Stoiber