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Home > Encyclopedia > Sitagliptin phosphate monohydrate

Sitagliptin phosphate monohydrate

pharmaceutical raw materials
Sitagliptin phosphate monohydrate structure

Sitagliptin phosphate monohydrate 

structure
  • CAS No:

    654671-77-9

  • Formula:

    C16H15F6N5O.H3O4P.H2O

  • Chemical Name:

    Sitagliptin phosphate monohydrate

  • Synonyms:

    1-Butanone,3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-,(3R)-,phosphate,hydrate (1:1:1);1,2,4-Triazolo[4,3-a]pyrazine,7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-,phosphate (1:1),monohydrate;(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)butan-2-amine dihydrogen phosphate monohydrate;Sitagliptin phosphate monohydrate;1253056-03-9

  • Categories:

    Active Pharmaceutical Ingredients  >  Inhibitor Drugs

Description

Sitagliptin phosphate monohydrate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts


Sitagliptin Phosphate is the phosphate salt form of sitagliptin, an orally available, competitive, beta-amino acid-derived inhibitor of dipeptidyl peptidase 4 (DDP-4) with hypoglycemic activity. Sitagliptin may cause an increased risk in the development of pancreatitis.|A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES.

Sitagliptin phosphate monohydrate Basic Attributes

523.3240802

523.105530

1806241-263-5

TS63EW8X6F

C73811

A10BH01|A10BD24

2933990090

Characteristics

156

1.66180

White or almost white crystalline powder

529.9ºC at 760 mmHg

274.3℃

Safety Information

NONH for all modes of transport

28-38-41-48-62-63

24/25-26-28-36/37/39

P264, P280, P305+P351+P338, P33, P313

H319

|Warning|H319 (100%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]|P264, P280, P305+P351+P338, and P337+P313|Aggregated GHS information provided by 41 companies from 3 notifications to the ECHA C&L Inventory.

Drug Information

For adult patients with type-2 diabetes mellitus, Xelevia is indicated to improve glycaemic control:as monotherapy:in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance;as dual oral therapy in combination with:metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control;a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance;a peroxisome proliferator-activated receptor gamma (PPARγ) agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;as triple oral therapy in combination with:a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control;a PPARγ agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.Xelevia is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dose of insulin do not provide adequate glycaemic control.|For patients with type-2 diabetes mellitus, Tesavel is indicated to improve glycaemic control:as monotherapy:in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance;as dual oral therapy in combination with:metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control;a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance;a PPARγ agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;as triple oral therapy in combination witha sulphonylurea and metformin when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control;a peroxisome-proliferator-activated-receptor-gamma (PPARγ) agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control.Tesavel is also indicated as add on to insulin (with or without metformin) when diet and exercise plus stable dosage of insulin do not provide adequate glycaemic control.|For adult patients with type-2 diabetes mellitus, Januvia is indicated to improve glycaemic control:as monotherapy:in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance;as dual oral therapy in combination with:metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control;a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance;a peroxisome-proliferator-activated-receptor-gamma (PPARγ) agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;a PPARγ agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;as triple oral therapy in combination with:a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control;a PPARγ agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.Januvia is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dose of insulin do not provide adequate glycaemic control.|Steglujan is indicated in adults aged 18 years and older with type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycaemic control:when metformin and/or a sulphonylurea (SU) and one of the monocomponents of Steglujan do not provide adequate glycaemic control.in patients already being treated with the combination of ertugliflozin and sitagliptin as separate tablets.|Treatment of type II diabetes mellitus

Compounds that suppress the degradation of INCRETINS by blocking the action of DIPEPTIDYL-PEPTIDASE IV. This helps to correct the defective INSULIN and GLUCAGON secretion characteristic of TYPE 2 DIABETES MELLITUS by stimulating insulin secretion and suppressing glucagon release. (See all compounds classified as Dipeptidyl-Peptidase IV Inhibitors.)|Substances which lower blood glucose levels. (See all compounds classified as Hypoglycemic Agents.)|Peptides which stimulate INSULIN release from the PANCREATIC BETA CELLS following oral nutrient ingestion, or postprandially. (See all compounds classified as Incretins.)

0431, MK

Sitagliptin phosphate monohydrate Use and Manufacturing

Uses

Sitagliptin phosphate is very effective in treating type 2 diabetes. As a new type of anti-diabetic drug, sitagliptin phosphate is blood sugar-dependent, has a moderate hypoglycemic effect, increases insulin secretion without hypoglycemia, effectively reduces hunger and other advantages, and has no nausea, vomiting, edema and increase Side effects such as body weight.

Human drugs -> Xelevia -> EMA Drug Category|Drugs used in diabetes -> Human pharmacotherapeutic group|Human drugs -> Tesavel -> EMA Drug Category|Human drugs -> Januvia -> EMA Drug Category|Human drugs -> Steglujan -> EMA Drug Category|Drugs used in diabetes, Combinations of oral blood glucose lowering drugs -> Human pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:523.32
Hydrogen Bond Donor Count:5
Hydrogen Bond Acceptor Count:15
Rotatable Bond Count:4
Exact Mass:523.10553934
Monoisotopic Mass:523.10553934
Topological Polar Surface Area:156
Heavy Atom Count:34
Complexity:616
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Pharmacological action not specified

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Registered Holders

  • CHROMO LABORATORIES INDIA PRIVATE LTD

    United States United States
    Active
  • MSN LIFE SCIENCES PRIVATE LTD

    United States United States
    Active
  • OPTIMUS DRUGS PRIVATE LTD

    United States United States
    Active

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