Advances in GLP-1 Receptor Targeting Radiolabeled Agent Development and Prospective of Theranostics

Theranostics. 2020 Jan 1;10(1):437-461. doi: 10.7150/thno.38366. eCollection 2020.


In the light of theranostics/radiotheranostics and prospective of personalized medicine in diabetes and oncology, this review presents prior and current advances in the development of radiolabeled imaging and radiotherapeutic exendin-based agents targeting glucagon-like peptide-1 receptor. The review covers chemistry, preclinical, and clinical evaluation. Such critical aspects as structure-activity-relationship, stability, physiological potency, kidney uptake, and dosimetry are discussed.

Keywords: Exendin-4; GLP-1; PET; SPECT; diabetes; insulinoma.

Publication types

  • Review