What Is a GLP-1 Receptor Agonist?
GLP-1 (Glucagon-Like Peptide-1) receptor agonists are among the biggest names in social media and news headlines. Names like Ozempic, Wegovy, Mounjaro, Zepbound, semaglutide, tirzepatide, and the newly arrived Foundayo. But what are they?
A Little Background on the Hormone GLP-1
GLP-1 receptor agonist [GLP-1 RA] is a gastrointestinal hormone, a member of the incretin group. It affects many bodily processes. GLP-1 receptors are found throughout the body and play several roles: appetite control, fullness, insulin secretion, blood sugar control, and gastric emptying. It is a “receptor agonist,” which can be considered a key that opens a receptor “lock,” triggering reactions that create the various effects of that system.
Our bodies naturally release their own GLP-1RA when we eat. Your natural GLP-1 is gone after 1 to 2 minutes from release. Medically created GLP-1 RA’s can last hours to days in your body. This is a markedly different time span of activity in the body, which is what makes these potent hormones able to produce strong side effects yet can give us a fantastic response of removing excessive hunger, problems getting full, and constant food thoughts that plague many people with Obesity.
From Gila Monster to Medicine
In the early 1980s, a researcher studying Gila Monster physiology (a southwestern desert lizard that eats only every few months) discovered a substance that closely resembles human GLP-1 but lasts much longer in the body. This finding sparked years of research aimed at developing medications that could provide sustained blood sugar control for people with diabetes, potentially working alongside insulin or reducing insulin needs.
The first injectable GLP-1 receptor agonist was approved for patients with diabetes in 1993. It needed to be taken three times daily before meals, but it worked extremely well at lowering blood sugar, and patients lost weight as a bonus.
Where We Are Today
Further research led to longer-acting formulations, and scientists found that higher doses produced even greater weight loss. The race to improve these medications has continued ever since.
Researchers have also been exploring other incretin hormones with more appetite- and weight-related effects. Today, we have two major long-acting GLP-1 medications:
• Semaglutide (Ozempic, Wegovy)
• Tirzepatide (Mounjaro, Zepbound)
More promising incretin hormone combinations are currently in research, with some available as early as 2027.
Something New: A GLP-1 Medication That Isn’t a Peptide
Most recently, a brand-new type of GLP-1 receptor agonist has arrived, one that works differently from anything before it. Rather than being a peptide, orforglipron (Foundayo) is a small molecule, which changes how it can be taken and used. I’ll cover this exciting development in my next blog post.
