What is Rybelsus used for and how does it work?

• Rybelsus may be used to treat type 2 diabetes alongside diet, exercise, and, if needed, other medications.
• Rybelsus works by mimicking the effects of GLP-1, a naturally occurring incretin hormone that is usually released following a meal.
• Rybelsus stimulates the secretion of insulin following food, reduces the amount of glucose produced by the liver, and helps to make you feel full after food.
• Rybelsus is taken orally every day, at least 30 minutes before food.

Rybelsus (semaglutide) is an oral medicine that is used to improve blood sugar control in adults over the age of 18 with type 2 diabetes. It may be prescribed as first-line therapy in addition to diet and exercise or in addition to other medications typically used for type 2 diabetes.

Rybelsus is best taken on an empty stomach when you first wake up, at least 30 minutes before food, and with a small amount of water (no more than 4 oz). This ensures Rybelsus is absorbed properly. After 30 minutes of taking the Rybelsus tablet you may eat, drink or take other oral medicines.

Rybelsus is not used to treat type 1 diabetes.

R1 and R2 formulations

There are two formulations of Rybelsus: R1 and R2.

• Both contain semaglutide, but they are not interchangeable because they differ in their inactive ingredients, which influence how the drug is absorbed. They also differ in their strengths.
• Formulation R1: 3 mg, 7 mg, and 14 mg.
• Formulation R2 (new): 1.5 mg, 4 mg, and 9 mg.

Formulation R2 has enhanced drug absorption that allows for lower doses to achieve the same results as the first formulation (R1). You can switch between formulations but medical guidance is needed to ensure a smooth transition.

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How does Rybelsus work?

Rybelsus belongs to a class of medicines called GLP-1 receptor agonists. It may also be called an incretin mimetic.

Rybelsus works by mimicking the functions of natural incretin hormones in the body that help keep blood sugar levels under control, especially immediately following a meal. Incretin hormones are gut peptides that are secreted from the stomach when food is eaten. They also stimulate the secretion of insulin in response to high blood glucose levels. Two incretin hormones are known as GIP (glucose-dependent insulinotropic polypeptide) and GLP-1 (glucagon-like peptide-1).

In people with type 2 diabetes, natural incretin release is diminished or no longer present. However, it can be stimulated with pharmacological agents, such as Rybelsus.

Rybelsus shares 94% of the same structure as human GLP-1 but is man-made. It acts like GLP-1 and binds to GLP-1 receptors, stimulating insulin release from the pancreas, reducing the amount of glucagon secreted by the liver, and makes a person feel full by slowing gastric emptying.

The reason Rybelsus only needs to be taken once a day and not after every meal is that it binds to albumin which decreases how fast it is excreted through the kidneys and also protects it from being metabolized (broken down) by an enzyme naturally present in the blood, called dipeptidyl peptidase-4 or DPP-4.