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The vildagliptin experience - 25 years since the initiation of the novartis glucagon-like peptide-1 based therapy programme and 10 years since the first vildagliptin registration

Foley, James E and Ahrén, Bo LU (2017) In European Endocrinology 13(2). p.56-61
Abstract

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... (More)

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.

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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Dipeptidyl peptidase-4 (DPP-4) inhibitors, Glucagon-like peptide-1, Glucosedependent insulinotropic polypeptide, Type 2 diabetes mellitus, Vildagliptin
in
European Endocrinology
volume
13
issue
2
pages
6 pages
publisher
Touch Digital Media
external identifiers
  • scopus:85029805675
ISSN
1758-3772
DOI
10.17925/EE.2017.13.02.56
language
English
LU publication?
yes
id
5c1e991e-2949-43d1-93e8-264cac4cddf1
date added to LUP
2017-10-09 10:47:08
date last changed
2018-10-16 02:42:35
@article{5c1e991e-2949-43d1-93e8-264cac4cddf1,
  abstract     = {<p>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.</p>},
  author       = {Foley, James E and Ahrén, Bo},
  issn         = {1758-3772},
  keyword      = {Dipeptidyl peptidase-4 (DPP-4) inhibitors,Glucagon-like peptide-1,Glucosedependent insulinotropic polypeptide,Type 2 diabetes mellitus,Vildagliptin},
  language     = {eng},
  number       = {2},
  pages        = {56--61},
  publisher    = {Touch Digital Media},
  series       = {European Endocrinology},
  title        = {The vildagliptin experience - 25 years since the initiation of the novartis glucagon-like peptide-1 based therapy programme and 10 years since the first vildagliptin registration},
  url          = {http://dx.doi.org/10.17925/EE.2017.13.02.56},
  volume       = {13},
  year         = {2017},
}