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

Irina Velikyan; Olof Eriksson

doi:10.7150/thno.38366

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.

Authors

Irina Velikyan¹, Olof Eriksson²

Affiliations

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

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; GLP-1; PET; SPECT; diabetes; insulinoma.

Publication types

Review

MeSH terms

Diabetes Mellitus* / diagnostic imaging
Diabetes Mellitus* / therapy
Glucagon-Like Peptide-1 Receptor / antagonists & inhibitors*
Humans
Neoplasms* / diagnostic imaging
Neoplasms* / therapy
Precision Medicine / methods*
Radiopharmaceuticals / therapeutic use*

Substances

GLP1R protein, human
Glucagon-Like Peptide-1 Receptor
Radiopharmaceuticals