Table 1.
Summary of multireceptor agonists currently in preclinical and clinical trials and their effect on metabolic regulation.
| Agonists | Receptors involved | Effect on glycemic control | Effect on appetite suppression | Effect on body weight | Effect on lipid metabolism | Effect on beta-cell proliferation/apoptosis | Other metabolic effects | Side effects |
|---|---|---|---|---|---|---|---|---|
| GLP-1/GcG39-43 | GLP-1R, GcGR |
|
|
|
|
– | Non-alcoholic steatohepatitis | – |
| GLP-1/GIP28,51-59 | GLP-1R, GIPR |
|
|
|
|
– | Neuroprotective effects and memory function | Gastrointestinal side effects |
| GLP-1/CCK31,64 | GLP-1R, CCK-AR |
|
|
|
|
– | – | – |
| GLP-1/gastrin68,69 | GLP-1R, CCK-BR |
|
– |
|
– |
|
– | – |
| GLP-1/xenin or GIP/xenin75,76 | GLP-1R or GIPR, NTSR, muscarinic |
|
– | – |
|
|
GIP potentiation | – |
| GLP-1/amylin84,85 | GLP-1R, amylinR |
|
– |
|
– | – | – | – |
| GLP-1/GIP/Glucagon29,30,87-89 | GLP-1R, GIPR, GcGR |
|
– |
|
|
|
Fibrosis, non-alcoholic steatohepatitis, neuroprotection | – |
| GLP-1/gastrin/xenin90,91 | GLP-1R, CCK-BR, NTSR, muscarinic |
|
– | – |
|
– | GIP potentiation | – |
Abbreviations: CCK, cholecystokinin; GIP, glucose-dependent insulinotropic polypeptide; GLP-1, glucagon-like-peptide-1.