Glucagon-like peptide-1 (GLP-1), traditionally administered through injections, drugs enhance insulin secretion, suppress appetite, and slow gastric emptying, which helps regulate blood sugar levels and reduce weight. But can these beneficial drugs be taken orally? Let’s delve into the advancements in GLP-1 therapy that are opening up new possibilities for patients.
The Challenge of Oral GLP-1 Administration
Most GLP-1 receptor agonists are peptides, which means they are proteins that can easily be broken down by enzymes in the stomach and intestines before they can exert their effects. Additionally, their large molecular size makes it difficult for them to pass through the lining of the gut into the bloodstream. Developing an oral formulation that survives the environment of the gastrointestinal tract presents significant challenges.
Despite these hurdles, the demand for a non-injectable form of GLP-1 therapy has driven significant research and innovation, leading to the development of the first oral GLP-1 receptor agonist.
The Breakthrough: Oral Semaglutide
The introduction of oral semaglutide (brand name Rybelsus) marked a milestone in diabetes treatment. Approved by the FDA in 2019, Rybelsus is the first and only oral GLP-1 receptor agonist available on the market. It offers the same benefits as its injectable counterparts but in a convenient pill form, making it a more attractive option for those averse to injections.
How Does Oral Semaglutide Work?
Oral semaglutide utilizes a novel absorption-enhancing technology. The tablet contains semaglutide along with an absorption enhancer called SNAC (sodium N-[8-(2-hydroxybenzoyl) amino] caprylate), which temporarily increases the pH level around the tablet. This protects the semaglutide from being degraded by stomach acid and enhances its absorption across the stomach lining.
Patients taking oral semaglutide must follow specific guidelines to maximize absorption:
- It should be taken on an empty stomach with a sip of water (no more than 4 ounces).
- Patients must wait at least 30 minutes before eating, drinking, or taking other medications. This regimen is crucial to ensure that the medication is absorbed effectively. This is similar to thyroid medication.
Efficacy and Safety
Clinical trials have shown that oral semaglutide is as effective as its injectable counterparts in lowering blood sugar levels and aiding in weight loss. However, like all medications, it comes with potential side effects. The most common include gastrointestinal issues such as nausea, vomiting, diarrhea, and constipation, which are typical for GLP-1 receptor agonists. Even the injection form of semaglutide causes the side side effects, however, research is still necessary to determine if these side effects are more pronounced with the oral version.
Oral semaglutide is suitable for adults with type 2 diabetes to improve blood sugar control along with diet and exercise. However, it is not recommended for treating type 1 diabetes or diabetic ketoacidosis, nor is it advised for patients with a personal or family history of medullary thyroid carcinoma or patients.
The development of oral semaglutide is a significant advancement in GLP-1 therapy, offering patients who dislike needles a much-needed alternative. As research continues, we may see more innovations in oral peptide drug delivery, potentially expanding the range of medications available in oral form and improving quality of life for patients with chronic conditions. For now, oral semaglutide stands as a testament to the progress in diabetes treatment, providing effective management through an easier, more patient-friendly approach.
