Investigational Drug Details
| Drug ID: | D338 |
| Drug Name: | Sitagliptin |
| Synonyms: | Sitagliptin |
| Type: | Chemical drug |
| DrugBank ID: | DB01261 |
| DrugBank Description: | Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used in conjunction with diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. The effect of this medication leads to glucose dependent increases in insulin and decreases in glucagon to improve control of blood sugar. Sitagliptin was granted FDA approval on October 16, 2006. |
| PubChem ID: | 4369359 |
| CasNo: | 486460-32-6 |
| Repositioning for NAFLD: | Yes |
| SMILES: | FC(F)(F)c1n2CCN(Cc2nn1)C(=O)C[C@H](N)Cc1c(F)cc(F)c(F)c1 |
| Structure: |
|
| InChiKey: | MFFMDFFZMYYVKS-SECBINFHSA-N |
| Molecular Weight: | 407.318 |
| DrugBank Targets: | Dipeptidyl peptidase 4 inhibitor |
| DrugBank MoA: | Inhibition of DPP-4 by sitagliptin slows DPP-4 mediated inactivation of incretins like GLP-1 and GIP. Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasis. Reduced inhibition of incretins increase insulin synthesis and decrease glucagon release in a manner dependant on glucose concentrations. These effects lead to an overall increase in blood glucose control which is demonstrated by reduced glycosylated hemoglobin (HbA1c). |
| DrugBank Pharmacology: | Sitagliptin inhibits DPP-4 which leads to increased levels of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide(GIP), decreased levels of glucagon, and a stronger insulin response to glucose. |
| DrugBank Indication: | Sitagliptin is indicated for the management of glycemic control in type 2 diabetes mellitus along with diet and exercise. |
| Targets: | DPP4 inhibitor |
| Therapeutic Category: | Antidiabetic drug |
| Clinical Trial Progress: | Phase 4 on-going (NCT05195944) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0015 | NCT01963845 | Phase 2 | Completed | Has Results | January 2014 | October 20, 2016 | Details |
| L0045 | NCT02263677 | Phase 4 | Withdrawn | No Results Available | March 2014 | October 5, 2016 | Details |
| L0049 | NCT02147925 | Phase 4 | Completed | No Results Available | August 2014 | May 18, 2018 | Details |
| L0323 | NCT05195944 | Phase 4 | Not yet recruiting | No Results Available | April 2022 | January 19, 2022 | Details |
| L0340 | NCT01260246 | Not applicable | Terminated | No Results Available | December 2010 | March 14, 2017 | Details |
| L0433 | JPRN-jRCTs031190238 | Not applicable | Recruiting | No Results Available | 03/03/2020 | 18 October 2021 | Details |
| L0630 | ChiCTR-TRC-14004464 | Other | Not Recruiting | No Results Available | 18/03/2014 | 18 April 2017 | Details |
| L0665 | JPRN-UMIN000006197 | Phase 3 | Not Recruiting | No Results Available | 01/09/2011 | 2 April 2019 | Details |
| L0669 | JPRN-UMIN000005349 | Not applicable | Recruiting | No Results Available | 30/03/2011 | 2 April 2019 | Details |
| L0910 | ISRCTN33414972 | Not applicable | Not Recruiting | No Results Available | 16/12/2013 | 27 February 2017 | Details |
| L0926 | JPRN-UMIN000009265 | Phase 3 | Not Recruiting | No Results Available | 10/11/2012 | 2 April 2019 | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00255 | 35163991 | Molecules | Sitagliptin Is More Effective Than Gliclazide in Preventing Pro-Fibrotic and Pro-Inflammatory Changes in a Rodent Model of Diet-Induced Non-Alcoholic Fatty Liver Disease. | Details |
| A01605 | 34681219 | Pharmaceuticals (Basel) | Antiangiogenic Drugs in NASH: Evidence of a Possible New Therapeutic Approach. | Details |
| A01980 | 34543583 | Arch Physiol Biochem | Dipeptedyl peptidase-4 (DPP-4) inhibitor downregulates HMGB1/TLR4/NF-κB signaling pathway in a diabetic rat model of non-alcoholic fatty liver disease. | Details |
| A02751 | 34260003 | Neurochem Res | Resveratrol Protects SH-SY5Y Cells Against Oleic Acid-Induced Glucolipid Metabolic Dysfunction and Cell Injuries Via the Wnt/β-Catenin Signalling Pathway. | Details |
| A03195 | 34094026 | Iran J Basic Med Sci | The therapeutic effects of berberine plus sitagliptin in a rat model of fatty liver disease. | Details |
| A03840 | 33852508 | Eur J Gastroenterol Hepatol | The role of nursing care in the type 2 diabetes treatment associated with chronic liver diseases. | Details |
| A03843 | 33851458 | Hepatology | Hepatic Fibroblast Growth Factor 21 Is Involved in Mediating Functions of Liraglutide in Mice With Dietary Challenge. | Details |
| A04068 | 33771699 | Pharmacol Res | Epigenetics in NAFLD/NASH: Targets and therapy. | Details |
| A05224 | 33333172 | Biochimie | Beneficial and deleterious effects of sitagliptin on a methionine/choline-deficient diet-induced steatohepatitis in rats. | Details |
| A06587 | 32819262 | Curr Drug Saf | Efficacy and Cardiovascular Safety of DPP-4 Inhibitors. | Details |
| A07268 | 32559768 | Horm Metab Res | Effects and Safety of Sitagliptin in Non-Alcoholic Fatty Liver Disease: A Systematic Review and Meta-Analysis. | Details |
| A10082 | 31496048 | Physiol Rep | Dipeptidyl peptidase-4 inhibitors and aerobic exercise synergistically protect against liver injury in ovariectomized rats. | Details |
| A11803 | 30734333 | Hepatology | Letter to Editor: Role of Pharmacotherapy in Patients With Coexisting Nonalcoholic Fatty Liver Disease and Type 2 Diabetes Mellitus. | Details |
| A11810 | 30729549 | Hepatology | Reply. | Details |
| A12334 | 30510994 | Cell Mol Gastroenterol Hepatol | Dipeptidyl Peptidase 4 Inhibitors Reduce Hepatocellular Carcinoma by Activating Lymphocyte Chemotaxis in Mice. | Details |
| A12659 | 30341767 | Hepatology | Liraglutide, Sitagliptin, and Insulin Glargine Added to Metformin: The Effect on Body Weight and Intrahepatic Lipid in Patients With Type 2 Diabetes Mellitus and Nonalcoholic Fatty Liver Disease. | Details |
| A12942 | 30214535 | Exp Ther Med | Sitagliptin reduces insulin resistance and improves rat liver steatosis via the SIRT1/AMPKα pathway. | Details |
| A13075 | 30149145 | Diabetes Metab | SGLT2 inhibitors and incretin agents: Associations with alanine aminotransferase activity in type 2 diabetes. | Details |
| A13100 | 30138985 | Zhonghua Yi Xue Za Zhi | [The expression of chemerin and the influence of sitagliptin on its expression in non-alcoholic fatty liver disease rats complicated with prediabetes]. | Details |
| A13592 | 29890569 | Clin Mol Hepatol | Combined effects of synbiotic and sitagliptin versus sitagliptin alone in patients with nonalcoholic fatty liver disease. | Details |