By Fiona Chin N.D. 
Contents
GLP-1 (Glucagon-Like Peptide-1) and GLP-2 (Glucagon-Like Peptide-2) are naturally occurring hormones classified as incretins produced in the gut in response to food intake. They are vital in regulating glucose metabolism, appetite, and various digestive processes. Both peptides have become targets for therapeutic interventions due to their beneficial effects on metabolic health, weight management, and digestive disorders.
GLP-1 is primarily involved in glucose metabolism. Upon release, it enhances insulin secretion in response to elevated blood sugar levels, slows gastric emptying, and promotes a feeling of fullness (satiety). It also inhibits glucagon release, preventing excessive glucose production in the liver. These effects make GLP-1 a powerful tool in managing type 2 diabetes and obesity.
Key Medications:
GLP-1 receptor agonists (GLP-1 RAs) are widely used to:
Their physiological and pharmacological properties vary depending on which receptors these medications activate. Earlier drugs like liraglutide, liraglutide, and tirzepatide target these receptors differently. For example, tirzepatide is sometimes called a “triple GLP” because it hits three receptors. Each drug has different effects—some people respond better to one drug, while others may experience side effects like bloating or nausea, depending on their genetic makeup and receptor density.
These medications not only target the pancreas but also affect bile production, motility, and many other systems in the body. They even influence intestinal cell junctions.
Mounjaro is a medication developed by Eli Lilly. Its active ingredient is Tirzepatide, a novel peptide that targets two key incretin receptors in the body: GLP-1 (Glucagon-Like Peptide-1) and GIP (Glucose-Dependent Insulinotropic Polypeptide). This dual-action mechanism makes Mounjaro a groundbreaking treatment for both type 2 diabetes and obesity.
Tirzepatide is unique because it mimics the effects of both GLP-1 and GIP (Gastric inhibitory polypeptide). These two incretin hormones are naturally released after eating to regulate blood sugar and fat metabolism. By activating both receptors, tirzepatide enhances insulin release, decreases glucagon production, slows gastric emptying, and increases satiety (the feeling of fullness), making it highly effective for:
While both tirzepatide (Mounjaro) and other GLP-1 receptor agonists like semaglutide (Ozempic, Wegovy) target the GLP-1 receptor, tirzepatide offers additional benefits by also targeting the GIP receptor. This dual action enhances its efficacy, particularly in terms of weight loss and glycemic control.
In trials, tirzepatide has shown to be more effective than GLP-1-only medications in both lowering blood sugar and promoting weight loss. It is often referred to as a “triple incretin” because it impacts insulin, glucagon, and the body’s fat metabolism in a highly integrated manner.
https://jamanetwork.com/journals/jamainternalmedicine/fullarticle/2821080
Common side effects of tirzepatide include:
Some patients may also experience a condition called “Ozempic face” or “Mounjaro face,” where rapid weight loss results in a loss of facial fat, giving a gaunt appearance. This can be managed through careful dose adjustments and adjunct therapies, including exercise, a proper diet and co use of other peptides and things like collagen.
While currently approved for type 2 diabetes and weight management, tirzepatide is being studied for its potential in treating a wide range of metabolic and inflammatory conditions. Its ability to modulate both GLP-1 and GIP receptors opens the door to possible applications in non-alcoholic steatohepatitis (NASH), chronic kidney disease (CKD), and even neurodegenerative diseases due to its impact on metabolic pathways and inflammation.
Chronic Kidney Disease (CKD) is a progressive condition characterized by the gradual loss of kidney function, often due to diabetes, hypertension, or other metabolic disorders. As the kidneys lose their ability to filter waste from the blood, patients face complications like proteinuria, fluid imbalances, and, ultimately, kidney failure. In recent years, GLP-1 receptor agonists have emerged as promising treatments to help slow the progression of CKD, especially in patients with type 2 diabetes.
These medications have shown promise in managing chronic kidney disease (CKD). While reducing glucose levels and body weight helps, they also improve kidney health by directly affecting receptors in the kidneys. They lessen the tension that leads to fibrosis and improve endothelial permeability, which is essential for kidney filtration. They also reduce sympathetic overstimulation, a factor that exacerbates kidney disease.
Moreover, they reduce inflammation in the kidneys by modulating immune responses, particularly in conditions like interstitial nephritis. These medications also affect fibrosis, reducing the likelihood of tissue sclerosis, which is crucial for preventing CKD from progressing to later stages.
GLP-1 receptors are found not only in the pancreas but also in the kidneys, cardiovascular system, and other tissues, which enables these drugs to exert protective effects beyond glycemic control.
https://link.springer.com/article/10.1007/s12020-024-03757-9
Several clinical trials have highlighted the benefits of GLP-1 receptor agonists in people with CKD, particularly those with diabetic kidney disease (diabetic nephropathy), which is a leading cause of CKD. The LEADER trial, which evaluated the effects of liraglutide (Victoza) in type 2 diabetes patients, showed that the drug significantly reduced the risk of kidney-related adverse events, including new-onset persistent macroalbuminuria (a marker of kidney damage).
Similarly, the SUSTAIN-6 trial, focusing on semaglutide (Ozempic), demonstrated significant reductions in the progression of kidney disease, especially in reducing albuminuria and slowing the decline in glomerular filtration rate (GFR), which is a key measure of kidney function.
Tirzepatide (Mounjaro) also shows potential for kidney protection, though long-term studies are ongoing. The dual action on both GLP-1 and GIP receptors offers enhanced metabolic benefits, and it’s expected to have more substantial renal protective effects compared to traditional GLP-1 therapies.
https://www.nature.com/articles/s41467-024-50199
https://www.nejm.org/doi/full/10.1056/NEJMoa2403347
https://pubmed.ncbi.nlm.nih.gov/38411162/
https://cardiab.biomedcentral.com/articles/10.1186/s12933-023-01793-9
https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2789684
While GLP-1 receptor agonists have shown great promise in managing CKD, there are still some limitations:
Ongoing studies are expected to provide more data on:
GLP-1 receptor agonists offer a promising avenue for slowing the progression of CKD, particularly in diabetic patients. By addressing key risk factors such as hyperglycemia, hypertension, and inflammation, these drugs not only help preserve kidney function but also reduce the risk of cardiovascular events in CKD patients. As more research unfolds, GLP-1 receptor agonists may become a standard part of CKD management, offering hope for patients with this progressive and often life-threatening condition.
GLP-1 receptor agonists have demonstrated significant cardiovascular benefits in clinical trials, particularly in people with type 2 diabetes. Off-label, these medications are being considered for:
NAFLD and NASH are metabolic liver conditions associated with obesity and insulin resistance. Off-label use of GLP-1 receptor agonists has shown promising results in:
There is growing interest in the potential of GLP-1 receptor agonists as treatments for neurodegenerative diseases such as Alzheimer’s and Parkinson’s. The off-label focus here is on:
PCOS is a common endocrine disorder that often leads to insulin resistance, obesity, and metabolic issues. Off-label use of GLP-1 agonists has shown potential for:
While GLP-1 receptor agonists are approved for weight management in people with type 2 diabetes or obesity, off-label use for general weight loss in non-diabetic individuals is becoming increasingly popular. GLP-1 drugs help by:
Another emerging area for off-label use of GLP-1 receptor agonists is in the treatment of substance abuse disorders, including:
https://www.nature.com/articles/nrendo.2012.140
As research on GLP-1 receptor agonists continues, there are several exciting developments on the horizon that could expand their therapeutic use.
Following the success of tirzepatide (Mounjaro), which targets both GLP-1 and GIP receptors, the next generation of medications will likely include </span>dual and triple agonists that activate additional pathways, such as glucagon receptors, for even greater metabolic benefits. These agonists are designed to:
While current GLP-1 receptor agonists are typically administered via injection, research is underway to develop oral formulations. This would increase accessibility and convenience for patients, especially those who are resistant to injectable treatments. Early studies on oral semaglutide (Rybelsus) show promise for managing diabetes and weight loss.
GLP-1’s role in modulating the immune system is an area of intense interest. Researchers are exploring its potential in treating chronic inflammatory and autoimmune diseases, such as:
The anti-inflammatory effects of GLP-1 agonists may help reduce immune system overactivity and tissue damage in these conditions.
Preliminary studies suggest that GLP-1 receptor agonists may have potential anti-cancer properties by:
There’s emerging research on how GLP-1 receptor agonists may influence the gut microbiome, improving gut health and potentially influencing longevity:
GLP-1 receptor agonists have already proven to be revolutionary for managing type 2 diabetes and obesity, but ongoing research and off-label uses show that their potential goes far beyond these applications. From neurodegenerative diseases to chronic kidney disease, cardiovascular health, and even addiction treatment, GLP-1 receptor agonists are poised to become critical tools in treating a wide array of conditions in the near future. But, they have side effects and, in my opinion, should never be used as a monotherapy (a stand-alone therapy). We always need to ensure that one’s diet and lifestyle are optimised towards kidney health first before we think about adding these types of medications. Also, in speaking to many doctors who are using and prescribing these medications, using them with other peptides to reduce side effects and preserve muscle mass is paramount.
As always, please talk to your healthcare provider before starting any new medications.
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