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

Irina Velikyan1, Olof Eriksson2

  • 1Department of Medicinal Chemistry, Uppsala University, Uppsala, Sweden.

Theranostics
|January 7, 2020
PubMed

Insights

Radiolabeled exendin agents targeting the glucagon-like peptide-1 receptor show promise for personalized diabetes and oncology theranostics. This review covers their development, evaluation, and key properties for clinical use.

Area of Science:

  • Nuclear medicine
  • Endocrinology
  • Oncology
  • Medicinal chemistry

Background:

  • Personalized medicine and theranostics are advancing diabetes and oncology treatments.
  • Glucagon-like peptide-1 receptor (GLP-1R) is a key target in these diseases.
  • Exendin-based agents offer a platform for developing targeted radiopharmaceuticals.

Purpose of the Study:

  • To review advances in radiolabeled exendin-based agents for GLP-1R imaging and therapy.
  • To discuss the chemistry, preclinical, and clinical evaluations of these agents.
  • To highlight critical factors influencing their therapeutic and diagnostic potential.

Main Methods:

  • Literature review of radiolabeled exendin agents.
  • Analysis of structure-activity relationships.
  • Evaluation of preclinical and clinical data including stability, potency, and dosimetry.

Main Results:

  • Development of various radiolabeled exendin analogs for GLP-1R targeting.
  • Demonstrated potential for both diagnostic imaging and therapeutic applications.
  • Identified key challenges such as kidney uptake and need for optimized dosimetry.

Conclusions:

  • Radiolabeled exendin agents represent a promising theranostic approach for GLP-1R-related diseases.
  • Further optimization is needed to improve clinical efficacy and safety.
  • These agents align with the goals of personalized medicine in diabetes and oncology.
Keywords:
Exendin-4GLP-1PETSPECTdiabetesinsulinoma

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