Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus
Open accessAbstract
Aims/hypothesis The aim of this study was to assess the efficacy and safety of sitagliptin (MK-0431) as monotherapy in patients with type 2 diabetes mellitus and inadequate glycaemic control (HbA(1c) > or =7% and < or =10%) on exercise and diet.Methods A total of 521 patients aged 27-76 years with a mean baseline HbA(1c) of 8.1% were randomised in a 1:2:2 ratio to treatment with placebo, sitagliptin 100 mg once daily, or sitagliptin 200 mg once daily, for 18 weeks. The efficacy analysis was based on an all-patients-treated population using an analysis of covariance, excluding data obtained after glycaemic rescue.Results After 18 weeks, HbA(1c) was significantly reduced with sitagliptin 100 mg and 200 mg compared with placebo (placebo-subtracted HbA(1c) reduction: -0.60% and -0.48%, respectively). Sitagliptin also significantly decreased fasting plasma glucose relative to placebo. Patients with higher baseline HbA(1c) (> or =9%) experienced greater placebo-subtracted HbA(1c) reductions with sitagliptin (-1.20% for 100 mg and -1.04% for 200 mg) than those with HbA(1c) <8% (-0.44% and -0.33%, respectively) or > or =8% to 8.9% (-0.61% and -0.39%, respectively). Homeostasis model assessment beta cell function index and fasting proinsulin:insulin ratio, markers of insulin secretion and beta cell function, were significantly improved with sitagliptin. The incidence of hypoglycaemia and gastrointestinal adverse experiences was not significantly different between sitagliptin and placebo. Sitagliptin had a neutral effect on body weight.Conclusions/interpretation Sitagliptin significantly improved glycaemic control and was well tolerated in patients with type 2 diabetes mellitus who had inadequate glycaemic control on exercise and diet.
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DPP-4 inhibitors lower A1C levels by 0.6-0.9 percentage points and are weight neutral and relatively well tolerated.
“In clinical trials performed to date, DPP-4 inhibitors lower A1Clevels by 0.6–0.9 percentage points and are weight neutral and relatively well tolerated (83,84).”
From Medical Management of Hyperglycemia in Type 2 Diabetes: A Consensus Algorithm for the Initiation and Adjustment of Therapy (2009) · cites this paper as [83]
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- Authors
- Raz, I., Hanefeld, M., Xu, L., Caria, C., Williams-Herman, D., Khatami, H., & Sitagliptin Study 023 Group
- Affiliations
- Hadassah Medical Center (IL)
- Merck & Co., Inc., Rahway, NJ, USA (United States) (US)
- Corresponding author
- Khatami, H.
- Venue
- Diabetologia
- Published
- 2006-09-26
- Volume
- 49
- Issue
- 11
- Pages
- 2564-2571
- ISSN
- 0012-186X (ISSN-L)
- 1432-0428
- OpenAlex
- W2051462052
- Cited by
- 614
- References
- 17
- Citations by year
- 2026: 3 · 2025: 6 · 2024: 8 · 2023: 8 · 2022: 9 · 2021: 3 · 2020: 17 · 2019: 12 · 2018: 13 · 2017: 15 · 2016: 23 · 2015: 30 · 2014: 44 · 2013: 46 · 2012: 37
- FWCI
- 49.81
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Diabetologia (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Management and Research
- Health Sciences › Medicine › Pharmacology › Pharmacology and Obesity Treatment
- Keywords
- sitagliptin, DPP-4 inhibitors, type 2 diabetes, monotherapy, glycemic control, HbA1c, fasting blood glucose, beta-cell function, insulin secretion, hypoglycemia, gastrointestinal adverse effects, body weight
- MeSH terms
- Sitagliptin Phosphate, Adolescent, Adult, Aged, Diabetes Mellitus, Type 2, Glycoproteins, Humans, Hypoglycemic Agents, Middle Aged, Placebos, Pyrazines, Triazoles, Dipeptidyl Peptidase 4, Dipeptidyl-Peptidase IV Inhibitors, Adenosine Deaminase Inhibitors
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