Active Ingredient History

  • Now
Sitagliptin (MK-0431), chemically (2R)-4-Oxo-4-[3- (trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifl uorophenyl)butan-2-amine has a very high selectivity towards DPP-4, with an IC(50) of 18 nM. There is no affinity towards other DDP enzymes (DPP- 8 and DPP-9). It has been approved for the treatment of type 2 diabetes in the USA and Europe and is registered by the name Januvia (Merck Pharmaceuticals, Whitehouse Station, NJ, USA). In healthy volunteers and in patients with type 2 diabetes of different ethnic background, the tolerability of different doses given once or twice daily is good. The drug works to competitively inhibit a protein/enzyme, dipeptidyl peptidase 4 (DPP-4), that results in an increased amount of active incretins (GLP-1 and GIP), reduced amount of release of glucagon (diminishes its release) and increased release of insulin. Sitagliptin is an incretin enhancer and the first marketed medication belonging to the gliptin class. In fact, no published literature exists regarding incidence or severity of hypoglycemia when sitagliptin is used off-label in combined with insulin therapy. However, is recommended to use methods to avoid hypoglycemia when using this off-label combination. Approximately 79% of sitagliptin is excreted unchanged in the urine with metabolism being a minor pathway of elimination. Elimination of sitagliptin occurs primarily via renal excretion and involves active tubular secretion. Sitagliptin is a substrate for human organic anion transporter-3 (hOAT-3), which may be involved in the renal elimination of sitagliptin   NCATS

  • SMILES: N[C@@H](CC(=O)N1CCn2c(C1)nnc2C(F)(F)F)Cc3cc(F)c(F)cc3F
  • Mol. Mass: 407.32
  • ALogP: 2.02
  • ChEMBL Molecules:
More Chemistry
  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$10.2859 - $15.8910
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Combination drugs

( metformin (glucophage), sitagliptin (januvia) - other name: janumet xr )
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1,1-dimethylbiguanide | 2,4-thiazolidinedione, 5-004-02-((((methyl-2-pyridinylamino)ethoxy)phenyl)methyl)- | (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 | 5-((4-(2-methyl-2-(pyridinylamino)ethoxy)phenyl)methyl)-2,4-thiazolidinedione-2-butenedioate | (±)-5-[p-[2-(methyl-2-pyridylamino)ethoxy]benzyl]-2,4-thiazolidinedione | dimethylbiguanid | dimethyldiguanide | ertugliflozin l-pyroglutamic acid / sitagliptin phosphate monohydrate | glaxosmithkline brand of rosiglitazone maleate | glaxo wellcome brand of rosiglitazone maleate | januvia | mk0431 | mk 0431 | mk-0431 | n,n-dimethylguanylguanidine | ono-5435 | ristaben | (rs)-5-{4-[2-(methyl-2-pyridylamino)ethoxy]benzyl}-2,4-thiazolidinedion | sitagliptan | sitagliptin | sitagliptina | sitagliptine | sitagliptin / metformin hydrochloride | sitagliptin monophosphate monohydrate | sitagliptin phosphate | sitagliptin phosphate anhydrous | sitagliptin phosphate hydrate | sitagliptin phosphate monohydrate | sitagliptinum | smithkline beecham brand of rosiglitazone maleate


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