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What is Rybelsus used for and how does it work?

Medically reviewed by Carmen Pope, BPharm. Last updated on March 21, 2025.

Official Answer by Drugs.com

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.

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.

Related questions

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.

References

Read next

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Although Ozempic is not FDA-approved for weight loss, over 86% of people lose at least 5% of their body weight in trials that have studied semaglutide, the active ingredient of Ozempic. But the same clinical trials also show that just under 14% don’t lose weight, and some may even gain weight. Continue reading

How much does semaglutide cost?

Semaglutide (Wegovy) injection for weight loss treatment costs about $1418 per month if you are paying cash without insurance or manufacturer's copay cards. Semaglutide for treatment of type 2 diabetes costs $1051 per month for either the Ozempic pen injection or 30 oral tablets of Rybelsus. Continue reading

Does Ozempic cause muscle loss and how to prevent it?

Clinical trials have shown GLP-1 agonist drugs like semaglutide (Ozempic) can lead to a 13.9% loss of lean muscle mass (equal to a 6.9 kg or 15 lb) during treatment. Strategies to help prevent muscle loss include regular strength (resistance) training, aerobic exercise and adequate dietary protein, fluid and nutrient intake. Continue reading

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