DPP-4 Inhibitors: Uses, most common brand names, and safety information

Medically reviewed by  Jamie Winn, PharmD

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Researchers discovered that the enzyme dipeptidyl peptidase-4 (DPP-4) inhibited the actions of 2 incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) in the 1990s. By blocking DPP-4, it results in an increased level of these hormones which lowers your blood sugar levels through insulin secretion and inhibition of glucagon secretion.

The first clinical study with a dipeptidyl peptidase IV inhibitor (DPP-IV) which eventually entered the market was published in 2004. The DPP-4 inhibitor used was Galvus (vildagliptin), which is currently not approved for use in the U.S. Januvia (sitagliptin) was the first DPP-4 inhibitor approved by the U.S. Food and Drug Administration (FDA) in October 2006 to improve blood glucose levels in adults with type 2 diabetes mellitus (T2DM).

The list below includes the most common DPP-4 inhibitors, combination products containing DPP-4 inhibitors, and their pricing:

List of DPP-4 inhibitors

What are DPP-4 inhibitors?

DPP-4 inhibitors (also called gliptins) are a class of antidiabetic medications that are used along with a reduced calorie diet and exercise to improve blood glucose control in adults with T2DM. They are not indicated in the treatment of type 1 diabetes or diabetic ketoacidosis.

DPP-4 inhibitors can be used as monotherapy or as add-on therapy with other diabetes medications such as metformin, sulfonylurea, or thiazolidinediones. Clinical trials involving DPP-4 inhibitors have shown they lower HbA1c levels between 0.5% to 1.0% with a low incidence of adverse effects. DPP-4 inhibitors are typically taken by mouth, once daily, before or after meals.

How do DPP-4 inhibitors work?

DPP-4 inhibitors act on incretin hormones, mainly GLP-1 and GIP to help lower blood glucose levels in type 2 diabetic patients. DPP-4 inhibition prevents the degradation of GLP-1 and GIP, increasing their levels circulating in your bloodstream. This increase causes the stimulation of insulin secretion from beta-cells in the pancreas, the inhibition of glucagon secretion, and delayed gastric emptying. This results in a lower postprandial and fasting blood glucose level as well as a reduced HbA1C level, without causing weight gain.

What conditions are DPP-4 inhibitors used to treat?

DPP-4 inhibitors are FDA-approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes, which is a risk factor for heart disease, heart failure, stroke, and other cardiovascular complications.

Are DPP-4 inhibitors safe?

When taken as prescribed, DPP-4 inhibitors can be safe and effective. A systematic review and meta-analysis of randomized, placebo-controlled, cardiovascular outcome trials in patients with type 2 diabetes showed that DPP-4 inhibitors did not increase the risk of death from cardiovascular events (myocardial infarction, stroke) when compared to placebo. Onglyza (saxagliptin) does have an association with an increased rate of hospitalization from heart failure.

Before starting a DPP-4 inhibitor, make sure your healthcare provider is aware of your health conditions, including:

• Heart failure
• Kidney disease
• Arthritis
• Pancreatitis
• Gallbladder disease (gallstones)
• High triglyceride level
• Are pregnant or plan on becoming pregnant
• Are breastfeeding or plan on breastfeeding

Your healthcare provider should also be aware of the prescription drugs, over-the-counter medications, and supplements you are taking, including:

• Insulin or other medications used to treat hyperglycemia (high blood sugar)

Can you take DPP-4 inhibitors while you are pregnant or breastfeeding?

DPP-4 inhibitors are considered Pregnancy Category B because safety in pregnant women has not been proven in adequate and controlled trials. Animal studies suggest that there is a low risk of adverse events if used during pregnancy. You should discuss the risks with your healthcare provider to determine if these medications should be included in your diabetes care plan.

There is no information on whether DPP-4 inhibitors are found in breast milk and the effects they might have. These medications should be used with caution during lactation.

What are the common side effects of DPP-4 inhibitors?

Some common side effects of DPP-4 inhibitors include:

• Increased risk of hypoglycemia (low blood sugar), especially if used with a sulfonylurea or insulin
• Common cold symptoms (nasopharyngitis)
• Upper respiratory tract infections
• Headache
• Nausea
• Diarrhea
• Stomach pain
• Urinary tract infections
• Weight loss

DPP-4 inhibitors can sometimes cause severe adverse effects, including:

• Hypersensitivity reactions, including anaphylaxis and angioedema
• Stevens-Johnson syndrome (serious skin and mucous membrane disorder)
• Acute pancreatitis
• Severe and disabling joint pain
• Bone fractures with Onglyza (saxagliptin)

This is not a complete list of side effects and we encourage you to consult with your healthcare professional for medical advice about any possible side effects.

How much do DPP-4 inhibitors cost?

DPP-4 inhibitors are very expensive with an average cost of around $10,000 per year.

You can purchase DPP-4 Inhibitors for $49 per month from NiceRx if eligible for assistance. Prices at the pharmacy vary by location, strength, and quantity, as well as your insurance status.

Related resources for DPP-4 inhibitors

• The mechanism of action of dipeptidyl peptidase 4 (DPP-4) inhibitors. National Library of Medicine, StatPearls
• Information on dipeptidyl peptidase-4 (DPP-4) inhibitors. FDA
• How do DPP-4 inhibitors work? Diatribe
• Managing your diabetes; DPP-4 inhibitors. Diabetes.org.uk
• FDA Drug Safety Communication: FDA warns that DPP-4 inhibitors for type 2 diabetes may cause severe joint pain. FDA
• Clinical use of DPP-4 inhibitors. Frontiers
• Pleiotropic mechanisms for the glucose-lowering action of DPP-4 inhibitors. American Diabetes Association