Drug information of Saxagliptin


Drug group:

Saxagliptin (rINN) is an orally active hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs.

Mechanism of effect

Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor antidiabetic for the treatment of type 2 diabetes. DPP-4 inhibitors are a class of compounds that
work by affecting the action of natural hormones in the body called incretins. Incretins decrease blood sugar by increasing consumption of sugar by the body, mainly through increasing insulin production in the pancreas, and by reducing production of sugar by the liver. DPP-4 is a membrane associated peptidase which is found in many tissues, lymphocytes and plasma. DPP-4 has two main mechanisms of action, an enzymatic function and another mechanism where DPP-4 binds adenosine deaminase, which conveys intracellular signals via dimerization when activated. Saxagliptin forms a reversible, histidine-assisted covalent bond between its nitrile group and the S630 hydroxyl oxygen on DPP-4. The inhibition of DPP-4 increases levels active of glucagon like peptide 1 (GLP-1), which inhibits glucagon production from pancreatic alpha cells and increases production of insulin from pancreatic beta cells.


Post-administration of saxagliptin, GLP-1 and GIP levels rise up to 2- to 3- fold. Because it is very selective of DPP-4 inhibition, there are fewer systemic side effects. Saxagliptin inhibits DPP-4 enzyme activity for a 24-hour period. It also decreased glucagon concentrations and increased glucose-dependent insulin secretion from pancreatic beta cells. Saxagliptin did not prolong the QTc interval to a clinically significant degree.


Peak plasma time: 2hr (saxagliptin); 4 hr (5-hyroxy saxagliptin)

Vd: Negligible

Metabolism: Hepatic by CYP450 3A4/5 to active metabolite (50% potency of parent compound)

Half-life (elimination): 2.5 hr (saxagliptin); 3.1 hr (5-hydroxy saxagliptin)

Renal clearance: 7.2 L/hr

Excretion: Urine (75%); feces (22%)



Diabetes Mellitus Type 2

2.5-5 mg PO qDay


<18 years: Safety and efficacy not established


Renal impairment

Decrease dose with strong CYP450 3A4/5 inhibitors

Coadministration with thiazolidinediones (eg, rosiglitazone, pioglitazone) increases risk for peripheral edema

Pancreatitis reported with saxagliptin; monitor for signs and symptoms and discontinue if pancreatitis suspected

Serious hypersensitivity reactions with saxagliptin reported (typically within the first 3 months of therapy)

History of angioedema

Coadministration with a sulfonylurea or with insulin may increase hypoglycemia; monitor closely and adjust sulfonylurea and/or insulin dose accordingly

Postmarketing cases of bullous pemphigoid requiring hospitalization reported with DPP-4 inhibitor use; patients typically recovered with topical or systemic immunosuppressive treatment and discontinuation of the DPP-4 inhibitor; inform patients to report development of blisters or erosions while on treatment; if bullous pemphigoid is suspected, discontinue therapy and refer patient to dermatologist for diagnosis and appropriate treatment

Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate

Congestive heart failure (CHF) risks

  • Observe patients for signs and symptoms of heart failure during therapy; inform patients of characteristic symptoms of heart failure and advise patients to immediately report them; if heart failure develops, evaluate and manage according to current standards of care and consider discontinuation of therapy

Points of recommendation

Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take saxagliptin in larger or smaller amounts or for longer than recommended.

You may take this medicine with or without food. Follow your doctor's instructions.

Do not crush, chew, or break a saxagliptin tablet. Swallow it whole.

Low blood sugar (hypoglycemia) can happen to everyone who has diabetes. Symptoms include headache, hunger, sweating, pale skin, irritability, dizziness, feeling shaky, or trouble concentrating. Always keep a source of sugar with you in case you have low blood sugar. Sugar sources include fruit juice, hard candy, crackers, raisins, and non-diet soda. Be sure your family and close friends know how to help you in an emergency.

If you have severe hypoglycemia and cannot eat or drink, use a glucagon injection. Your doctor can prescribe a glucagon emergency injection kit and tell you how to use it.

Check your blood sugar carefully during times of stress, travel, illness, surgery or medical emergency, vigorous exercise, or if you drink alcohol or skip meals. These things can affect your glucose levels and your dose needs may also change. Do not change your medication dose or schedule without your doctor's advice.

Saxagliptin is only part of a complete program of treatment that also includes diet, exercise, weight control, and possibly other medications. It is important to use this medicine regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

Store at room temperature away from moisture and heat

Take the missed dose as soon as you remember (be sure to take the medicine with food if your doctor has instructed you to). Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Related drugs

Linagliptin , Alogliptin , Sitagliptin

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