Basic information New antidiabetic drug DPP-4 inhibitors Safety Related Supplier

Sitagliptin phosphate

Basic information New antidiabetic drug DPP-4 inhibitors Safety Related Supplier
Sitagliptin phosphate Basic information
Sitagliptin phosphate Chemical Properties
  • Melting point:202-204°C
  • storage temp. -20°C Freezer
Sitagliptin phosphate Usage And Synthesis
  • New antidiabetic drugSitagliptin phosphate is dipeptidyl peptidase Ⅳ(DDP-4) inhibitor class of drugs developed by the German Merck company and firstly obtained the US Food and Drug Administration approval for the treatment of type 2 diabetes, is a new antidiabetic drug, can improve the body's own ability to reduce high blood glucose levels, and the relatively increase naturally occurring incretin by inhibiting the activity of this enzyme, including the levels of glucagon-like peptide 1 and glucose-dependent insulinotropic peptide, thereby triggering the pancreas to improve insulin production and stop glucose production in liver, and ultimately reduce the clinical effect of blood glucose concentration. Features of this product is to stimulate insulin secretion, at the same time can alleviate hunger, but does not make weight gain, and also cannot happen hypoglycemia and edema, is not suitable for use in diabetic patients with poor glycemic control and often developed hypoglycemia. By verification of clinical 552 cases of mild to moderate type 2 diabetes, taken once a day Sitagliptin phosphate, once time 100 mg, after taking the drug for 12 weeks, can make glycated hemoglobin reduce 0.6%-1.1%. Incidence of adverse reactions is similar to placebo, the most frequently reported adverse reactions (incidence> 5% and greater than placebo) is a stuffy or runny nose, and sore throat, upper respiratory tract infection and headache.
    Clinical studies showed that the Sitagliptin phosphate as monotherapy in patients with type 2 diabetes, can make glycated hemoglobin (HbA1c) levels significantly reduce. When in combination with the metformin or TZDs, has a significant role of adjuvant therapy, can focus on three kinds of major defect in type 2 diabetes: insulin resistance, β-cell dysfunction (reduction of insulin release), and α-cell dysfunction (unsuppressed hepatic glucose generation) plays a role. But the drug should not be used for treatment of patients with type 1 diabetes or diabetic ketoacidosis.
    The above information is edited by the chemicalbook of Liu Yujie.
  • DPP-4 inhibitorsSitagliptin phosphate (trade name Januvia) is the DPP-4 inhibitor first clinically approved for the treatment of type 2 diabetes, developed by Germany company Merck, and was listed in 2006 in Mexico and the United States in 2007, also obtained EU approval for the treatment of type 2 diabetes. China approval was soon, currently Sitagliptin phosphate tablets has become the second largest drug of oral diabetes drugs in US.
    Sitagliptin phosphate can enhance a called incretin system of human physiological system, resulting in physiological hypoglycemic effect. This physiological system itself can affect β cells and α cells of the islet, help to regulate glucose, and insulin reduction only caused by β-cell dysfunction can cause the increase of blood glucose, or because cells α and β-cell dysfunction cause loss of control in hepatic glucose synthesis and thus lead to elevated blood glucose, DPP-4 will produce efficacy.
    Sitagliptin phosphate exists dependent of glucose levels, it will not only know hypoglycemic blindly, not predatorily press islet, exhaust the pancreas function. In contrast, the test proved that it has the prospect of long-term protection of human β cells. In addition, it does not lead to side effects such as weight gain, decreased blood glucose, medication compliance of patient will be greatly enhanced. Therefore, in theory it's effective role in life will greatly exceed the current oral antidiabetic drug, insulin dependent of patients will be greatly delayed.
  • Chemical PropertiesWhite Solid
  • UsesA trizolopyrazine dipeptidyl peptidase IV inhibitor. It has recently been approved for the therapy of type II diabetes.
  • UsesSitagliptin is a trizolopyrazine dipeptidyl peptidase IV inhibitor. Sitagliptin has recently been approved for the therapy of type II diabetes.
  • General DescriptionSitagliptin phosphate is the 1:1 phosphoric acid salt ofsitagliptin free base (i.e., (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)-2-butanamine), and is marketed(Junuvia, 2006) in 25-, 50-, and 100-mg tablets. Acombination product with metformin (Janumet, 2007) intwo strengths (50 mg/500 mg and 50 mg/1,000 mgsitagliptin/metformin) is also available, and sitagliptin mayalso be prescribed with a thiazolidinedione, or possibly a sulfonylurea.The phosphate salt provides very high water solubility.The bioavailability of orally administered sitagliptinis~87%. The drug exhibits relatively low plasma protein binding (~38%), a relatively large volume of distribution(198 L), and a terminal elimination half-life of 12 hours.About 79% of a 100-mg oral dose is excreted unchanged inurine, the balance as trace-level metabolites (CYP3A4, lessercontribution by CYP2C8) in urine or feces: 87% of administeredradioactivity is excreted in urine, and 13% in feces.Active tubular excretion is reported to play a key role in renalclearance of unchanged drug, and may be mediated at least inpart via the organic anion transporter hOAT-3.
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