Xelevia - sitagliptin

What is Xelevia?

Xelevia is a medicine that contains the active substance sitagliptin. It is available in the form of round tablets (pink: 25 mg; beige: 50 and 100 mg).

What is Xelevia used for?

Xelevia is used in patients with type 2 diabetes to improve the control of blood glucose (sugar) levels. It is used as follows, in addition to diet and exercise:

• on its own, in patients who are not satisfactorily controlled with diet and exercise and for whom metformin (an antidiabetic medicine) is not suitable;
• in combination with metformin or a PPAR gamma agonist (a type of antidiabetic medicine), such as a thiazolidinedione, in patients who are not satisfactorily controlled on metformin or the PPAR gamma agonist used alone;
• in combination with a sulphonylurea (another type of diabetes medicine) in patients who are not satisfactorily controlled on sulphonylurea alone and for whom metformin is not suitable;
• in combination with both metformin and a sulphonylurea or PPAR-gamma agonist, in patients who are not satisfactorily controlled on these two medicines;
• in combination with insulin, with or without metformin, in patients who are not satisfactorily controlled on stable insulin doses.

The medicine can only be obtained with a prescription.

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How is Xelevia used?

Xelevia is taken at a dose of 100 mg once a day, with or without food. If Xelevia is to be taken in combination with a sulphonylurea or insulin, the dose of the sulphonylurea or insulin may need to be lowered to reduce the risk of hypoglycaemia (low blood sugar levels).

How does Xelevia work?

Type 2 diabetes is a disease in which the pancreas does not make enough insulin to control the level of glucose in the blood or where the body is unable to use insulin effectively. The active substance in Xelevia, sitagliptin, is a dipeptidyl peptidase-4 (DPP-4) inhibitor. It works by inhibiting the breakdown of "incretin" hormones in the body. These hormones, released after a meal, stimulate the pancreas to produce insulin. By increasing the level of incretins in the blood, sitagliptin stimulates the pancreas to produce more insulin when the blood sugar level. it is high, while it is ineffective when the blood glucose concentration is low. Sitagliptin also reduces the amount of glucose produced by the liver by increasing insulin levels and decreasing the levels of the hormone glucagon. Together, these processes reduce the rate of glucose in the blood and contribute to the control of type 2 diabetes.

How has Xelevia been studied?

Xelevia has been studied in nine studies involving nearly 6,000 type 2 diabetes patients whose blood glucose levels were not adequately controlled:

• in four of these studies Xelevia was compared with placebo (a dummy treatment): Xelevia or placebo were used alone in two studies involving 1,262 patients, as an add-on to metformin in a study involving 701 patients and as an add-on to pioglitazone (a PPAR gamma agonist) in a study of 353 patients;
• in two studies, Xelevia was compared with other antidiabetic medicines. In the first study, Xelevia was compared with glipizide (a sulphonylurea) when they were used as an add-on to metformin in 1,172 patients. In the second study, Xelevia was compared with metformin, used alone, in 1,058 patients;
• in three further studies Xelevia was compared with placebo when added to other antidiabetic medicines: to glimepiride (an "other sulphonylurea), with or without metformin, in 441 patients; to the combination of metformin and rosiglitazone (a PPAR gamma agonist ) in 278 patients; and stable insulin dosing, with or without metformin, in 641 patients.

In all of the studies, the main measure of effectiveness was the change in the concentration in the blood of a substance called glycosylated hemoglobin (HbA1c), which gives an indication of the effectiveness of blood glucose control.

What benefit has Xelevia shown during the studies?

Xelevia was more effective than placebo both as monotherapy and in combination with other antidiabetic medicines. In patients taking Xelevia alone, HbA1c levels decreased by 0.48% (from approximately 8.0% at the start of the studies) after 18 weeks and by 0.61% after 24 weeks. Conversely, they increased by 0.12% and 0.18%, respectively, in patients taking placebo. Adding Xelevia to metformin reduced HbA1c levels by 0.67% after 24 weeks, compared with a 0.02% reduction in patients with added placebo. Adding Xelevia to pioglitazone reduced HbA1c levels by 0.85% after 24 weeks, compared with a reduction of 0.15% in patients with added placebo.
In studies where Xelevia was compared with other medicines, the effectiveness of adding Xelevia to metformin was similar to that of adding glipizide. When taken alone, Xelevia and metformin achieved similar reductions in HbA1c levels. but the efficacy of Xelevia appeared to be slightly lower than that of metformin. In the other studies, when Xelevia was added to glimepiride (with or without metformin), HbA1c levels decreased by 0.45% after 24 weeks, compared with an increase of 0.28% in patients with added placebo. HbA1c levels decreased by 1.03% after 18 weeks in patients adding Xelevia to metformin and rosiglitazone, compared with a decrease of 0.31% in those adding placebo; finally, they decreased by 0.59% in patients who added Xelevia (with or without metformin) to insulin, compared with a 0.03% decrease in those who added placebo.

What is the risk associated with Xelevia?

The most common side effects seen with Xelevia (generally seen in more than 5% of patients) are upper respiratory tract infections (colds) and nasopharyngitis (inflammation of the nose and throat). For the full list of side effects reported with Xelevia, see the Package Leaflet.
Xelevia should not be used in people who may be hypersensitive (allergic) to sitagliptin or any of the other ingredients.

Why has Xelevia been approved?

The Committee for Medicinal Products for Human Use (CHMP) decided that Xelevia's benefits are greater than its risks and recommended that it be given marketing authorization.

Other information about Xelevia:

On 21 March 2007, the European Commission released to Merck Sharp & Dohme Ltd.
a "Marketing Authorization" for Xelevia, valid throughout the European Union.
The marketing authorization is valid for five years and can be renewed after this period.
For the full version of the Xelevia EPAR click here.

Last update of this summary: 10-2009


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