Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics

Irina Velikyan^1✉, Olof Eriksson²

1. Department of Medicinal Chemistry, Uppsala University, Uppsala, Sweden
2. Science for Life Laboratory, Department of Medicinal Chemistry, Uppsala University, Uppsala, Sweden

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Citation:
Velikyan I, Eriksson O. Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics. Theranostics 2020; 10(1):437-461. doi:10.7150/thno.38366. Available from http://www.thno.org/v10p0437.htm

Abstract

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, insulinoma, GLP-1, diabetes, PET, SPECT