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Synonyms: Januvia® | MK-0431 | Zituvio®
sitagliptin is an approved drug (FDA (2006), EMA (2007))
Compound class: Synthetic organic
Comment: Sitagliptin is a dipeptidyl peptidase 4 (DPP4) inhibitor. Marketed formulations may contain sitagliptin phosphate monohydrate (PubChem CID 11591741).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: sitagliptin
|No information available.
|Summary of Clinical Use
|Used in the treatment of type 2 diabetes, usually as a second-line drug and in combination with other drugs, following the failure of metformin plus diet/exercise to control blood glucose levels.
A small-scale feasibility trial (with EU Clinical Trials Register no. 2016-001120-54) has been performed to assess the ability of sitagliptin (via increasing the bioavailability of the potent chemoattractant stromal cell-derived factor-1α) to elevate recruitment and differentiation of bone marrow-derived cells to endometrial mesenchymal stem-like progenitor cells in the endometrium as a mechanism to increase successful implantation in patients with recurrent pregnancy loss . Positive results suggest that more extensive investigation of the effects of preconception sitagliptin treatment is warranted.
|Mechanism Of Action and Pharmacodynamic Effects
|'Gliptin' class inhibitors improve glucose homoeostasis by blocking DPP4-mediated degradation of the incretin hormones glucagon-like peptide-1 and glucose-dependant insulinotropic polypeptide , thereby increasing insulin production and decreasing glucagon production by the pancreas.
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)