sitagliptin phosphate


Summary: 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.

Top Publications

  1. Nomiyama T, Akehi Y, Takenoshita H, Nagaishi R, Terawaki Y, Nagasako H, et al. Contributing factors related to efficacy of the dipeptidyl peptidase-4 inhibitor sitagliptin in Japanese patients with type 2 diabetes. Diabetes Res Clin Pract. 2012;95:e27-8 pubmed publisher
  2. Murohara T. Dipeptidyl peptidase-4 inhibitor: another player for cardiovascular protection. J Am Coll Cardiol. 2012;59:277-9 pubmed publisher
  3. Gosmanov A, Fontenot E. Sitagliptin-associated angioedema. Diabetes Care. 2012;35:e60 pubmed publisher
  4. Nakamura K, Oe H, Kihara H, Shimada K, Fukuda S, Watanabe K, et al. DPP-4 inhibitor and alpha-glucosidase inhibitor equally improve endothelial function in patients with type 2 diabetes: EDGE study. Cardiovasc Diabetol. 2014;13:110 pubmed publisher
    ..Sitagliptin had protective effects on endothelial function without adverse events. registered at under UMIN000003951. ..
  5. Kaneko M, Narukawa M. Assessment of the Risk of Hospitalization for Heart Failure With Dipeptidyl Peptidase-4 Inhibitors, Saxagliptin, Alogliptin, and Sitagliptin in Patients With Type 2 Diabetes, Using an Alternative Measure to the Hazard Ratio. Ann Pharmacother. 2017;51:570-576 pubmed publisher
    ..There are no substantial clinically relevant differences in the risk of cardiovascular events, including hospitalization for heart failure, between 3 of the DPP-4 inhibitors and placebo. ..
  6. Toh S, Hampp C, Reichman M, Graham D, Balakrishnan S, Pucino F, et al. Risk for Hospitalized Heart Failure Among New Users of Saxagliptin, Sitagliptin, and Other Antihyperglycemic Drugs: A Retrospective Cohort Study. Ann Intern Med. 2016;164:705-14 pubmed publisher
    ..In this large cohort study, a higher risk for hHF was not observed in users of saxagliptin or sitagliptin compared with other selected antihyperglycemic agents. U.S. Food and Drug Administration. ..
  7. Nomoto H, Kimachi K, Miyoshi H, Kameda H, Cho K, Nakamura A, et al. Effects of 50 mg vildagliptin twice daily vs. 50 mg sitagliptin once daily on blood glucose fluctuations evaluated by long-term self-monitoring of blood glucose. Endocr J. 2017;64:417-424 pubmed publisher
    ..There were no significant differences in other metabolic parameters evaluated. Reduction of daily blood glucose profile fluctuations by vildagliptin was superior to that of sitagliptin in Japanese patients with type 2 diabetes. ..
  8. Pagidipati N, Navar A, Pieper K, Green J, Bethel M, Armstrong P, et al. Secondary Prevention of Cardiovascular Disease in Patients With Type 2 Diabetes Mellitus: International Insights From the TECOS Trial (Trial Evaluating Cardiovascular Outcomes With Sitagliptin). Circulation. 2017;136:1193-1203 pubmed publisher
    ..URL: Unique identifier: NCT00790205. ..
  9. Navar A, Gallup D, Lokhnygina Y, Green J, McGuire D, Armstrong P, et al. Hypertension Control in Adults With Diabetes Mellitus and Recurrent Cardiovascular Events: Global Results From the Trial Evaluating Cardiovascular Outcomes With Sitagliptin. Hypertension. 2017;70:907-914 pubmed publisher
    ..Lower SBP was not associated with higher risks of fractures or worsening kidney function. ..

More Information


  1. Li M, Yang Y, Jiang D, Ying M, Wang Y, Zhao R. Efficacy and safety of liraglutide versus sitagliptin both in combination with metformin in patients with type 2 diabetes: A systematic review and meta-analysis. Medicine (Baltimore). 2017;96:e8161 pubmed publisher
    ..Meanwhile, the adverse reactions such as gastrointestinal problems were common in the liraglutide treatment group. Thus, this will provide an important reference for the treatment of patients with type 2 diabetes. ..
  2. Skalli S, Wion Barbot N, Baudrant M, Lablanche S, Benhamou P, Halimi S. Angio-oedema induced by dual dipeptidyl peptidase inhibitor and angiotensin II receptor blocker: a first case report. Diabet Med. 2010;27:486-7 pubmed publisher
  3. Oyama J, Ishizu T, Sato Y, Kodama K, Bando Y, Murohara T, et al. Rationale and design of a study to evaluate the effects of sitagliptin on atherosclerosis in patients with diabetes mellitus: PROLOGUE study. Int J Cardiol. 2014;174:383-4 pubmed publisher
  4. Tuesta L, Chen Z, Duncan A, Fowler C, Ishikawa M, Lee B, et al. GLP-1 acts on habenular avoidance circuits to control nicotine intake. Nat Neurosci. 2017;20:708-716 pubmed publisher
    ..GLP-1 neurons may therefore serve as 'satiety sensors' for nicotine that stimulate habenular systems to promote nicotine avoidance before its aversive effects are encountered. ..
  5. Чопей І, Івачевська В, Чубірко К, Гряділь Т, Гечко М. [Pathogenetic substantiation of complex treatment of nonalcoholic steatohepatitis and steatosis in patients with pre-diabetes and type 2 diabetes]. Wiad Lek. 2017;70:169-173 pubmed
    ..Differentiated treatment schemes of nonalcoholic steatosis and steatohepatitis in patients with pre-diabetes and type 2 diabetes have been approved for use. ..
  6. Lee J, Wang T, Liu C, Chien M, Chen M, Hsu Y, et al. Dipeptidyl Peptidase IV as a Prognostic Marker and Therapeutic Target in Papillary Thyroid Carcinoma. J Clin Endocrinol Metab. 2017;102:2930-2940 pubmed publisher
    ..Increased DPP4 expression is associated with cellular invasion and more aggressive disease in papillary thyroid cancer. Targeting DPP4 may be a therapeutic strategy for DPP4-expressing thyroid cancer. ..