Trending Topic
Hyponatraemia is primarily a disorder of water balance or distribution, characterized by serum sodium (Nas) levels less than 135 mmol/L.1 Hyponatraemia is the most common electrolyte disorder among elderly patients and is associated with increased mortality rates and longer hospital stays.2–4 The syndrome of inappropriate antidiuretic hormone secretion (SIADH) is a frequent cause of hyponatraemia in […]
The discovery of the incretin hormone glucagon like peptide-1 (GLP-1), and its usefulness in the treatment of type 2 diabetes mellitus
(T2DM) followed by the finding that dipeptidyl peptidase-4 (DPP-4) inhibition prevents GLP-1 inactivation, led to the discovery of
DPP-728. In 1999, studies with DPP-728 established the first proof-of-concept that DPP-4 inhibition improves glycaemic control in
patients with T2DM. Further efforts to improve the binding kinetics of DPP-728 resulted in the discovery of vildagliptin (LAF237). In the last 20
years, a plethora of studies conducted by Novartis in collaboration with external investigators has demonstrated the mechanism of action
of vildagliptin and its efficacy as monotherapy and as an add-on therapy for patients with T2DM. The studies establish that vildagliptin is a
selective DPP-4 inhibitor that blocks GLP-1 and glucose-dependent insulinotropic polypeptide (GIP) inactivation, thereby prolonging their
action, resulting in improved glycaemic control. This review aims to discuss the discovery and development of vildagliptin, with an emphasis
on mechanism of action and clinical efficacy.
Dipeptidyl peptidase-4 (DPP-4) inhibitors,
glucagon-like peptide-1, glucosedependent
insulinotropic polypeptide,
type 2 diabetes mellitus, vildagliptin
James E Foley is an employee
and shareholder of Novartis Pharmaceuticals
Corporation. Bo Ahrén has received speaker
honoraria from Novartis, Merck and Novo Nordisk.
James E Foley,
World Wide Medical Affairs Director, Novartis
Pharmaceuticals Corporation, East Hanover, NJ
07936-1080, US. E: james.foley@novartis.com
The publication of this article was
supported by Novartis Pharma AG.
Open Access: This article is published under the Creative Commons Attribution Noncommercial License, which permits any non-commercial use, distribution, adaptation and reproduction provided the original author(s) and source are given appropriate credit.
Compliance with Ethics: This article reviews
published human and animal studies; two unpublished
animal studies carried out by and reported with
permission from Sandoz/Novartis; these unpublished
animal studies were carried out according to
standards for the ethical treatment for research
animals existing in New Jersey, US in 1995.
2017-05-26T00:00:00
Trending Topic
Diabetes is a chronic disease associated with both acute and chronic complications. Many advances have been introduced throughout history to address these problems. While each clinical breakthrough was welcomed with relief and the expectation that a solution had been discovered, it was followed by the acknowledgement that continued exploration was needed. The scientific trials and […]
Article Highlights Early use of sodium–glucose co-transporter-2 inhibitors following myocardial infarction was associated with the following factors: Lower hospitalization for heart failure (odds ratio [OR]: 0.75; 95% confidence interval [CI]: 0.62–0.90; p=0.002). Similar cardiovascular deaths (OR: 1.04; 95% CI: 0.83–1.30; p=0.76). Similar all-cause mortality (OR: 1.00; 95% ...
Very few trials in the history of medical science have altered the treatment landscape as profoundly as the UK Prospective Diabetes Study (UKPDS). Even 44 years after its inception, the trial and post-study follow-up findings continue to fascinate and enlighten the ...
It is with great pleasure that we present this latest issue of touchREVIEWS in Endocrinology, which brings together a diverse array of high-quality articles focused on the evolving landscape of endocrine disorders. The importance of patient-centred care is exemplified in ...
Dry eye disease (DED) is known as dry eye syndrome (DES) or keratoconjunctivitis sicca. According to the Tear Film and Ocular Surface Society’s Dry Eye Workshop II (TFOS DEWS II), it constitutes a multifactorial disease of the ocular surface, ...
The prevalence of diabetes during pregnancy is rapidly increasing. In the USA alone, an estimated 1–2% of pregnant women have type 1 diabetes (T1D) or type 2 diabetes (T2D), and an additional 6–9% develop gestational diabetes.1 From 2000 to 2010, the prevalence of gestational ...
Dipeptidyl peptidase-4 (DPP-4) is a ubiquitous, multifunctional, 766-amino acid, type 2 transmembrane glycoprotein, which participates in the regulation of metabolic functions, immune and inflammatory responses, cancer growth and cell adhesion.1 It has two forms: the first is a membrane-bound form, which ...
Metformin Metformin has been recommended as the first-line glucose-lowering agent for the management of type 2 diabetes (T2D) for several decades due to its efficacy and safety profile.1–3 In fact, metformin has been widely used as an insulin-sensitizing agent for ...
Welcome to the latest edition of touchREVIEWS in Endocrinology, which features a range of review, case report and original research articles that highlight some key developments in our understanding and management of endocrinological disease. We begin with a commentary from ...
Type 2 diabetes (T2D) continues to pose an ever-greater global health challenge, with 1.31 billion individuals predicted to be living with diabetes globally by 2050; the majority of whom will have T2D.1 Closely linked to T2D is metabolic dysfunction-associated steatotic ...
Gestational diabetes mellitus (GDM) is generally defined as “any degree of glucose tolerance with onset or first recognition during pregnancy”.1 It currently is one of the diseases with the highest morbidity among pregnant women.2 Determining its prevalence has been a ...
Despite the increasing body of knowledge of treatment strategies for diabetes, many patients with type 2 diabetes mellitus (T2DM) are still in a persistent state of poor glycaemia.1,2 In clinical practice, achieving optimal glycaemic targets is challenging; the reasons are ...
Type 2 diabetes (T2D) is one of the most common chronic noncommunicable diseases, its incidence is exponentially increasing and is one of the leading causes of morbidity and mortality worldwide.1 As of 2021, T2D ranked among the top causes of ...
Earn and track your CME credits on the go, save articles for later, and follow the latest congress coverage.
Register for free to hear about the latest expert-led education, peer-reviewed articles, conference highlights, and innovative CME activities.
Or use a Social Account.
Explore the latest in medical education and stay current in your field. Create a free account to track your learning.