SITAGLIPTIN PHOSPHATE

PRODUCT IDENTIFICATION
CAS NO. 654671-78-0
654671-77-9 (hydrate)

SITAGLIPTIN

EINECS NO.  
FORMULA C16H15F6N5O.H3·PO4
MOL WT. 505.31

H.S. CODE

  

TOXICITY

 
SYNONYMS Januvia;
4-Oxo-4-(3-(trifluoromethyl)-5,6-dihydro(1,2,4)triazolo(4,3-a)pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl) butan-2-amine phosphate; (3R)-3-amino-1-(3-(trifluoromethyl)-6,8-dihydro-5H-(1,2,4) triazolo(4, 3-a)pyrazin-7-yl)- 4-(2,4,5-trifluorophenyl)butan-1-one phosphoric acid;
DERIVATION  

CLASSIFICATION

 antidiabetic

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE white to off-white crystalline powder
MELTING POINT 198 - 202 C
BOILING POINT

 

SPECIFIC GRAVITY  
SOLUBILITY IN WATER  
pH  
VAPOR DENSITY

 

AUTOIGNITION

 

NFPA RATINGS

  

REFRACTIVE INDEX

  
FLASH POINT

 

STABILITY

Stable under ordinary conditions.

EXTERNAL LINKS & GENERAL DESCRIPTION

Sitagliptin is the first in a new class of once daily, oral anti-hyperglycaemic agents. When added to ongoing metformin or pioglitazone therapy, it significantly improved HbA1c in type-2 diabetic patients who failed to achieve adequate glycaemic control with these agents as monotherapy, and it was found to be non-inferior to glipizide when added to metformin. Sitagliptin treatment was not associated with significantly increased incidences of hypoglycaemia or gastrointestinal adverse events. Sitagliptin as add-on therapy to metformin or a glitazone may be considered as an option for patients who fail to achieve glycaemic control despite an adequate trial of established first and second-line regimens. Comparative and long-term safety and efficacy data are lacking. (http://www.nyrdtc.nhs.uk/)

Sitagliptin (Januvia), the first in a new class of antihyperglycemic agents, was approved in October 2006. It inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), which causes the degradation of glucagon-like peptide-1 (GLP-1). The only other agent on the market that affects levels of GLP-1 is exen­ atide (Byetta). Exenatide is an injectable GLP-1 agonist, which mimics the action of naturally occurring GLP-1. Indications for sitagliptin include use in type 2 diabetes as monotherapy or in combination with metformin or thiazolidinediones . DPP-4 inhibitors have actions similar to those of the GLP-1 agonist, such as stimulation of insulin secretion, inhibition of glucagon secretion, and preservation of beta-cell function. In contrast, DPP-4 inhibitors do not slow gastric emptying or cause weight loss, possibly due to lower concentrations of GLP-1 postprandially compared to the GLP-1 agonist. DPP-4 inhibitors raise incretin levels to normal or slightly above normal levels. The advantage of DPP-4 inhibitors is oral administration; the GLP-1 receptor agonist is injectable. (http://www.uspharmacist.com/)

Dipeptidyl peptidase-IV (DPP-IV) inhibitors are a promising new class of drugs that may potentially play an important role in the management of type 2 diabetes mellitus. These agents improve glycemic control by preventing the rapid inactivation of the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), leading to stimulation of insulin release from the pancreas, inhibition of glucagon secretion, and potentially an improvement in pancreatic beta-cell function. (http://www.modernmedicine.com/)

Dipeptidyl peptidase-4 inhibitors

Product

CAS RN.

Alogliptin

 850649-61-5

Alogliptin benzoate

850649-62-6

Gemigliptin

911637-19-9

Linagliptin

 668270-12-0

Saxagliptin

361442-04-8

Saxagliptin hydrate

 945667-22-1

Sitagliptin

 486460-32-6

Vildagliptin

 274901-16-5
SALES SPECIFICATION

APPEARANCE

 white to off-white crystalline powder

PURITY

 98.0% min
RELATED SUBSTANCES 1.0% max (total impurity), 0.5% max (individual impurity)

ISOMER

1.0% max

MELTING POINT

198 - 202 C

LOSS ON DRYING

5.0% max
HEAVY METALS 20ppm max
TRANSPORTATION
PACKING
 
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UN NO.  
PRICE INFORMATION