First clinical PET study measuring the receptor occupancy of a dual GLP1/glucagon receptor agonist is now published

Through a collaboration between Antaros Medical and Sanofi, a first-in-class positron emission tomography (PET) tracer for the Glucagon (GCG) receptor was developed. The tracer was used in a clinical trial in combination with a Glucagon like peptide-1 (GLP-1) receptor tracer to assess the receptor occupancy of the dual GLP1/GCG receptor agonist SAR425899. Receptor occupancy is an important target engagement biomarker for the therapeutic effect for dual acting agonists.

Olof Eriksson, Director PET imaging at Antaros and Associate Professor at Uppsala University comments: “We are very proud of this collaboration between Antaros Medical and Sanofi. These unique PET tools can be used to better understand the drug pharmacology at the GLP-1 and glucagon receptor in human. In addition, we are developing similar tools for the GIP receptor.”

Dual agonists for the incretin hormone GLP-1 and the GCG receptor are emerging as a potential new class of therapeutics for Type 2 Diabetes, a disease affecting over 400 million people worldwide (WHO 2019). Due to somewhat overlapping pharmacological effects of receptor agonism, the ability to distinguish the individual receptor’s contribution has been limited. Understanding the relative occupancy of the receptors is of importance to allow for optimal efficacy of the drug. Measuring receptor occupancy using PET tracers allows quantification of the target engagement providing valuable information for the development of drugs in this class.

For full paper in Scientific Reports:  

Receptor occupancy of dual glucagon-like peptide 1/glucagon receptor agonist SAR425899 in individuals with type 2 diabetes

To read more on the PET tracer development collaboration, please see

Automated GMP-Compliant Production of [ 68 Ga]Ga-DO3A-Tuna-2 for PET Microdosing Studies of the Glucagon Receptor in Humans

EASD 2020: In vivo PET imaging of the gastric inhibitory polypeptide receptor in pancreas

Pressify Share on Linkedin Share on Twitter