Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C17H25N3O2.ClH |
| Molecular Weight | 339.86 |
| Optical Activity | ( - ) |
| Defined Stereocenters | 1 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.OC12CC3CC(C1)CC(C3)(C2)NCC(=O)N4CCC[C@H]4C#N
InChI
InChIKey=RZUUYWHYKBKAGN-DNSMMRBLSA-N
InChI=1S/C17H25N3O2.ClH/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16;/h12-14,19,22H,1-8,10-11H2;1H/t12?,13?,14-,16?,17?;/m0./s1
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.drugbank.ca/drugs/DB04876
Curator's Comment: Description was created based on several sources, including
https://www.drugbank.ca/drugs/DB04876
Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions. Vildagliptin is marketed under the trade names Galvus, Zomelis.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Gateways to clinical trials. | 2004 Dec |
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| Gateways to clinical trials. | 2004 Nov |
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| Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta-cell function in patients with type 2 diabetes. | 2005 Aug |
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| Gateways to clinical trials. | 2005 Jun |
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| Improved glycaemic control with dipeptidyl peptidase-4 inhibition in patients with type 2 diabetes: vildagliptin (LAF237) dose response. | 2005 Nov |
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| Gateways to clinical trials. | 2006 Apr |
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| Newer therapeutic options for children with diabetes mellitus: theoretical and practical considerations. | 2006 Apr |
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| Therapeutic options in development for management of diabetes: pharmacologic agents and new technologies. | 2006 Jan-Feb |
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| Gateways to clinical trials. | 2006 Jan-Feb |
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| [Dipeptidylpeptidase IV inhibitors and dual action PPAR-agonists]. | 2006 Mar |
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| Dipeptidyl peptidase-4 inhibitors and the management of type 2 diabetes mellitus. | 2007 Apr |
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| [Glucagon-like peptide-1 (GLP-1), new target for the treatment of type 2 diabetes]. | 2007 Apr |
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| Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes. | 2007 Apr |
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| Effects of vildagliptin on glucose control over 24 weeks in patients with type 2 diabetes inadequately controlled with metformin. | 2007 Apr |
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| The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. | 2007 Apr |
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| Does addition of vildagliptin to metformin monotherapy improve glycemic control in patients with type 2 diabetes mellitus? | 2007 Aug |
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| Management of type 2 diabetes in treatment-naive elderly patients: benefits and risks of vildagliptin monotherapy. | 2007 Dec |
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| Vildagliptin does not affect C-peptide clearance in patients with type 2 diabetes. | 2007 Jan |
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| The physiology of incretin hormones and the basis for DPP-4 inhibitors. | 2007 Jan-Feb |
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| A review of the effects of antihyperglycaemic agents on body weight: the potential of incretin targeted therapies. | 2007 Jul |
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| The influence of hepatic impairment on the pharmacokinetics of the dipeptidyl peptidase IV (DPP-4) inhibitor vildagliptin. | 2007 Jul |
|
| Vildagliptin in drug-naïve patients with type 2 diabetes: a 24-week, double-blind, randomized, placebo-controlled, multiple-dose study. | 2007 Mar |
|
| Dipeptidyl peptidase-IV inhibitors: a major new class of oral antidiabetic drug. | 2007 Mar |
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| The role of vildagliptin in the management of type 2 diabetes mellitus. | 2007 May |
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| Dipeptidyl peptidase 8/9-like activity in human leukocytes. | 2007 May |
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| Vildagliptin was noninferior to rosiglitazone for glycemic control in type 2 diabetes but caused less weight gain. | 2007 May-Jun |
|
| DPP-4 inhibition improves glucose tolerance and increases insulin and GLP-1 responses to gastric glucose in association with normalized islet topography in mice with beta-cell-specific overexpression of human islet amyloid polypeptide. | 2007 Oct 4 |
|
| Dose proportionality and the effect of food on vildagliptin, a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers. | 2007 Sep |
|
| Effects of the dipeptidyl peptidase-IV inhibitor vildagliptin on incretin hormones, islet function, and postprandial glycemia in subjects with impaired glucose tolerance. | 2008 Jan |
|
| The effect of age, gender, and body mass index on the pharmacokinetics and pharmacodynamics of vildagliptin in healthy volunteers. | 2008 Mar |
Sample Use Guides
When used as monotherapy, in combination with metformin, in combination with thiazolidinedione, in combination with metformin and a sulphonylurea, or in combination with insulin (with or without
metformin), the recommended daily dose of vildagliptin is 100 mg, administered as one dose of 50 mg in the morning and one dose of 50 mg in the evening. When used in dual combination with a sulphonylurea, the recommended dose of vildagliptin is 50 mg
once daily administered in the morning. In this patient population, vildagliptin 100 mg daily was no more effective than vildagliptin 50 mg once daily.
Route of Administration:
Oral
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924914-75-0
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9KND64V2AA
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PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
