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Progressive impairment of insulin secretion in people with type 2 diabetes leads to blood glucose concentrations worsening over time, often resulting in escalation of blood glucose lowering therapy.(1) In 2015/2016, more money was spent on dipeptidyl peptidase-4 (DPP-4) inhibitors ('gliptins') than on any other class of antidiabetic drug except for insulins.(2) In 2008, we reviewed sitagliptin and vildagliptin.(3) Here, we briefly review three other DPP-4 inhibitors, saxagliptin (Onglyza-AstraZeneca), linagliptin (Trajenta-Boehringer Ingelheim) and ▼alogliptin (Vipidia-Takeda), and consider data from recent cardiovascular outcomes studies...
December 2016: Drug and Therapeutics Bulletin
Sohita Dhillon
Saxagliptin (Onglyza(®)) is a highly potent, reversible, competitive dipeptidyl peptidase-4 inhibitor indicated for the treatment of patients with type 2 diabetes. Numerous well-designed clinical studies and their extensions showed that saxagliptin as monotherapy or as dual or triple combination therapy with other antihyperglycaemics improved glycaemic control and was generally well tolerated in patients with type 2 diabetes during ≤2 years' therapy. Saxagliptin was generally weight-neutral and had a low risk of hypoglycaemia (unless coadministered with agents that may be associated with hypoglycaemia, such as sulfonylureas or insulin)...
October 2015: Drugs
Vijay V Upreti, Chi-Fung Keung, David W Boulton, Ming Chang, Li Li, Angela Tang, Bonnie C Hsiang, Donette Quamina-Edghill, Ernst U Frevert, Frank P Lacreta
BACKGROUND: As compared with individual tablets, saxagliptin/metformin immediate release (IR) fixed-dose combination (FDC) tablets offer the potential for increased convenience, compliance, and adherence for patients requiring combination therapy. OBJECTIVES: Two bioequivalence studies assessed the fed-state and the fasted-state bioequivalence of saxagliptin/metformin IR 2.5 mg/500 mg FDC (study 1) and saxagliptin/metformin IR 2.5 mg/1,000 mg FDC (study 2) relative to the same dosage strengths of the individual component tablets [saxagliptin (Onglyza™) and metformin IR (Glucophage(®))] administered concurrently...
May 2013: Clinical Drug Investigation
Xiaohui Sophia Xu, Stephen R Dueker, Lisa J Christopher, Pete N Lohstroh, Chi Fung Anther Keung, Kai Kevin Cao, Samuel J Bonacorsi, Laura Cojocaru, Jim X Shen, W Griffith Humphreys, Bruce Stouffer, Mark E Arnold
BACKGROUND: An absolute bioavailability study that utilized an intravenous [(14)C]microdose was conducted for saxagliptin (Onglyza(®)), a marketed drug product for the treatment of Type 2 diabetes mellitus. Concentrations of [(14)C]saxagliptin were determined by accelerator MS (AMS) after protein precipitation, chromatographic separation by UPLC and analyte fraction collection. A series of investigative experiments were conducted to maximize the release of the drug from high-affinity receptors and nonspecific adsorption, and to determine a suitable quantitation range...
August 2012: Bioanalysis
Xiaohui Sophia Xu, Roger Demers, Huidong Gu, Lisa J Christopher, Hong Su, Laura Cojocaru, David W Boulton, Mark Kirby, Bruce Stouffer, William G Humphreys, Mark E Arnold
A liquid chromatography and tandem mass spectrometry (LC-MS/MS) method was developed and validated to simultaneously determine the concentrations of saxagliptin (Onglyza™, BMS-477118) and its major active metabolite, 5-hydroxy saxagliptin to support pharmacokinetic analyses in clinical studies. The dynamic range of the assay was 0.1-50 ng/mL for saxagliptin and 0.2-100 ng/mL for 5-hydroxy saxagliptin. Protein precipitation (PPT) with acetonitrile was used to extract the analytes from plasma matrix before injecting on an Atlantis(®) dC18 column (50 mm × 2...
March 15, 2012: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Lily P H Yang
Saxagliptin (Onglyza™) is a dipeptidyl peptidase 4 inhibitor widely approved for the treatment of type 2 diabetes mellitus. In the EU, saxagliptin is indicated as combination therapy with metformin, a sulfonylurea, a thiazolidinedione, or insulin (with or without metformin) for the treatment of adult patients with type 2 diabetes, including those with mild to severe renal impairment. This article reviews the clinical efficacy and tolerability of add-on saxagliptin therapy in patients with type 2 diabetes, in line with its approved indications in the EU, and summarizes the drug's pharmacological properties...
January 22, 2012: Drugs
G Scott Jones, Scott A Savage, Sabrina Ivy, Patrick L Benitez, Antonio Ramirez
The dipeptidyl peptidase-IV inhibitor saxagliptin (Onglyza) can undergo a thermodynamically favored cyclization to form the corresponding cyclic amidine. The kinetics and mechanism of this conversion were examined to develop a commercial synthesis that afforded saxagliptin with only trace levels of this key byproduct. Important findings of this work are the identification of a profound solvent effect and the determination of an autocatalytic pathway. Both of these phenomena result from transition structures involving proton transfer...
December 16, 2011: Journal of Organic Chemistry
Ola Granström, Klas Bergenheim, Phil McEwan, Karin Sennfält, Martin Henriksson
AIM: The objective of this study was to investigate the cost-effectiveness of saxagliptin (Onglyza(®)), a DPP-4 inhibitor, plus metformin compared with a sulphonylurea (SU) (Glipizide) plus metformin in Swedish patients not well controlled on metformin alone. METHODS: Data from a 52-week clinical trial comparing saxagliptin and glipizide in combination with metformin was used in a simulation model to estimate long term complications in a cohort of type 2 diabetes patients...
July 2012: Primary Care Diabetes
Antonio R Chacra
Saxagliptin (Onglyza™) is a potent, selective, once-daily dipeptidyl peptidase-4 (DPP-4) inhibitor indicated for improving glycemic control in patients with type 2 diabetes (T2D). By blocking DPP-4, saxagliptin increases and prolongs the effects of incretins, a group of peptide hormones released by intestinal cells after meals, which stimulate glucose-dependent insulin secretion to lower blood glucose. In controlled clinical trials, saxagliptin administered as monotherapy or in combination with metformin, glyburide, or a thiazolidinedione improved glycemic control in a clinically significant manner, reflected by significant decreases in glycated hemoglobin (monotherapy, -0...
September 22, 2010: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
David W Boulton, Li Li, Ernst U Frevert, Angela Tang, Lorna Castaneda, Nimish N Vachharajani, David M Kornhauser, Chirag G Patel
BACKGROUND AND OBJECTIVE: Patients with type 2 diabetes mellitus often have impaired renal function or may have impaired hepatic function, which can pose significant safety and tolerability issues for antihyperglycaemic pharmacotherapies. Therefore, the pharmacokinetics and tolerability of saxagliptin and its pharmacologically active metabolite, 5-hydroxy saxagliptin, in nondiabetic subjects with mild, moderate or severe renal or hepatic impairment, or end-stage renal disease (ESRD) were compared with saxagliptin and metabolite pharmacokinetics and tolerability in healthy adult subjects...
April 2011: Clinical Pharmacokinetics
A J Scheen
Saxagliptin (Onglyza) is a specific and reversible inhibitor of dipeptidylpeptidase-4 (DPP-4), which inhibits the activity of the enzyme for at least 24 hours after one single oral administration. It increases the circulating levels of incretin hormones (GLP-1, GIP), which contributes to amplify the insulin secretory response to meals and to reduce postprandial hyperglycaemia and, subsequently, fasting glycaemia. Saxagliptin, 5 mg once daily, has been shown to be effective in patients with type 2 diabetes treated with diet alone, metformin, sulfonylurea or glitazone, with a favourable tolerance profile...
September 2010: Revue Médicale de Liège
Kristen Kulasa, Steven Edelman
INTRODUCTION: The worldwide prevalence of type 2 diabetes mellitus (T2DM) is high, and the chronically poor metabolic control that can result from T2DM is associated with a high risk for microvascular and macrovascular complications. Because of the progressive pathophysiology of T2DM, oral antidiabetic agents often fail to provide sustained glycemic control, indicating the need for new therapies. Saxagliptin (Onglyza™; Bristol-Myers Squibb Company, Princeton, NJ, USA; AstraZeneca Pharmaceuticals LP, Wilmington, DE, USA) is an oral dipeptidyl peptidase-4 inhibitor, recently approved for the treatment of T2DM...
October 21, 2010: Core Evidence
Nancy L Borja-Hart, Karen L Whalen
OBJECTIVE: To review the pharmacology, pharmacokinetics, efficacy, and safety of saxagliptin, a new dipeptidyl peptidase-4 (DPP-4) inhibitor for the treatment of type 2 diabetes. DATA SOURCES: Searches of PubMed (1966-March 2010) and International Pharmacy Abstracts (1970-March 2010) were conducted using the key words saxagliptin, Onglyza, and BMS-477118. A review of bibliographies of retrieved articles was also performed to identify additional references. STUDY SELECTION AND DATA EXTRACTION: All identified studies published in English and involving efficacy and safety of saxagliptin in the treatment of type 2 diabetes were reviewed...
June 2010: Annals of Pharmacotherapy
Suresh Thareja, Saurabh Aggarwal, Priyanka Malla, Diksha Haksar, Tilak Raj Bhardwaj, Manoj Kumar
Saxagliptin (BMS-477118) has been recently FDA approved drug for the management of T2DM developed by Bristol-Myers Squibb and AstraZeneca under the trade name Onglyza. Saxagliptin is a nitrile-containing selective, potent, reversible and durable DPP IV inhibitor developed as an alternative second-line adds on to Metformin in place of a sulphonylurea. Saxagliptin increases and prolongs the action of incretin hormones by inhibiting the DPP IV enzyme that inactivates incretins usually within minutes. Saxagliptin is well absorbed and has low plasma protein binding and displays slow-binding properties to DPP IV...
July 2010: Mini Reviews in Medicinal Chemistry
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November 2, 2009: Medical Letter on Drugs and Therapeutics
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