Accession Number
Small Molecule
Approved, Investigational

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. Vidagliptin subsequently acts by inhibiting the inactivation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) by DPP-4. This inhibitory activity ultimately results in a two-fold action where GLP-1 and GIP are present to potentiate the secretion of insulin by beta cells and suppress glucagon secretion by alpha cells in 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
  • Vildagliptina
External IDs
LAF 237 / LAF-237 / LAF237 / NVP-LAF 237 / NVP-LAF-237 / NVP-LAF237
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
GalvusTablet50 mgOralNovartis Europharm Limited2007-09-26Not applicableEu
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands
CAS number
Average: 303.3993
Monoisotopic: 303.194677059
Chemical Formula
InChI Key



Used to reduce hyperglycemia in type 2 diabetes mellitus.

Associated Conditions

Vildagliptin belongs to a class of orally active antidiabetic drugs (DPP-IV inhibitors) that appear to have multiple functional benefits beyond simple blood-glucose control. One of these is a potential protective effect on pancreatic beta cells, which deteriorate in diabetes. Vildagliptin appears to be safe, very well tolerated, and efficacious. Following a meal, gut incretin hormones are released. The most important incretin hormones are GLP-1 and glucose-dependent insulinotropic polypeptide (GIP). These hormones, secreted in the human small intestine, are responsible for insulin release due to increased glucose levels. In contrast to agents that promote insulin secretion via glucose-independent mechanisms, GLP-1's dependence on glucose concentration is considered beneficial due to a lower risk of hypoglycemia. GLP-1 also inhibits glucagon secretion and increases beta cell mass by stimulating proliferation and neogenesis. However, the clinical utility of GLP-1 is limited by its short half-life (2 minutes). GLP-1 is rapidly degraded by the proteolytic enzyme DPP-IV. To enhance GLP-1 activity, inhibition of the DPP-IV enzyme is emerging as a novel therapeutic approach in the treatment of diabetes. Administration of vildagliptin enhances GLP-1's ability to produce insulin in response to elevated concentrations of blood glucose, inhibit the release of glucagon following meals, slow the rate of nutrient absorption into the bloodstream, slow the rate of gastric emptying, and reduce food intake.

Mechanism of action

Vildagliptin inhibits dipeptidyl peptidase-4 (DPP-4). This in turn inhibits the inactivation of GLP-1 by DPP-4, allowing GLP-1 to potentiate the secretion of insulin in the beta cells. Dipeptidyl peptidase-4's role in blood glucose regulation is thought to be through degradation of GIP and the degradation of GLP-1.

ADipeptidyl peptidase 4
Additional Data Available
Adverse Effects

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Additional Data Available

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Blackbox Warnings

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Rapidly absorbed following oral administration with an oral bioavailability of greater than 90%.

Volume of distribution
Not Available
Protein binding


Not Available
Route of elimination
Not Available
Half life

The elimination half-life is approximately 90 minutes.

Not Available
Not Available
Affected organisms
  • Humans and other mammals
Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Vildagliptin is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Vildagliptin can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Vildagliptin.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Vildagliptin.
AcebutololThe therapeutic efficacy of Vildagliptin can be increased when used in combination with Acebutolol.
AcetazolamideThe therapeutic efficacy of Vildagliptin can be increased when used in combination with Acetazolamide.
AcetohexamideVildagliptin may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Vildagliptin can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Vildagliptin.
AgmatineThe risk or severity of hypoglycemia can be increased when Agmatine is combined with Vildagliptin.
Additional Data Available
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    Extended Description

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Food Interactions
  • Take with or without food.


Synthesis Reference

Stephen Winter, Jordi Bosch, Jordi Puig Serrano, Jose Javier Soto, "PROCESS FOR PREPARING VILDAGLIPTIN." U.S. Patent US20080167479, issued July 10, 2008.

General References
  1. Balas B, Baig MR, Watson C, Dunning BE, Ligueros-Saylan M, Wang Y, He YL, Darland C, Holst JJ, Deacon CF, Cusi K, Mari A, Foley JE, DeFronzo RA: The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab. 2007 Apr;92(4):1249-55. Epub 2007 Jan 23. [PubMed:17244786]
External Links
Human Metabolome Database
PubChem Compound
PubChem Substance
ATC Codes
A10BH02 — VildagliptinA10BD08 — Metformin and vildagliptin

Clinical Trials

Clinical Trials
1CompletedNot AvailableHealthy Volunteers1
1CompletedDiagnosticType 2 Diabetes Mellitus1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentType 2 Diabetes Mellitus4
1, 2CompletedTreatmentDiabetes / Impaired kidney function1
1, 2TerminatedBasic ScienceType 2 Diabetes Mellitus1
2CompletedBasic ScienceDiabetes Mellitus1
2CompletedTreatmentDiabetes Mellitus1
2CompletedTreatmentImpaired Glucose Tolerance / Transplantation, Kidney1
2CompletedTreatmentType 2 Diabetes Mellitus2
2RecruitingTreatmentType 1 Diabetes Mellitus1
2Unknown StatusTreatmentInsulin-dependent Gestational Diabetes1
2, 3CompletedTreatmentType 2 Diabetes Mellitus2
2, 3Unknown StatusBasic ScienceSDF-1 is an Important Cytokine for Neovascularization. Cleavage of SDF-1 is Reduced by DPPIV Inhibitors1
3CompletedPreventionEndothelial Dysfunction / Type 2 Diabetes Mellitus1
3CompletedPreventionInsulin Resistance / Microvascular Disease1
3CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent / Type 2 Diabetes Mellitus1
3CompletedTreatmentHealthy Volunteers / Type 2 Diabetes Mellitus1
3CompletedTreatmentPrediabetic State1
3CompletedTreatmentType 2 Diabetes Mellitus63
3CompletedTreatmentImpaired kidney function / Type 2 Diabetes Mellitus2
3RecruitingPreventionDiabetes / Disorder Related to Renal Transplantation1
3RecruitingTreatmentDiabetes, Autoimmune / Insulin Dependent Diabetes / Juvenile Onset Diabetes Mellitus / Type 1 Diabetes Mellitus1
4CompletedBasic ScienceDiabetes1
4CompletedBasic ScienceDiabetes / Hypoglycemia1
4CompletedBasic ScienceType 2 Diabetes Mellitus3
4CompletedTreatment1- Microvascular Function / 2-oxidative Stress / 3-inflammation1
4CompletedTreatmentChronic Foot Ulcers1
4CompletedTreatmentCongestive Heart Failure / Type 2 Diabetes Mellitus1
4CompletedTreatmentCoronary Artery Disease / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent / Type 2 Diabetes Mellitus1
4CompletedTreatmentElderly / Type 2 Diabetes Mellitus1
4CompletedTreatmentEndothelial Dysfunction / High Blood Pressure (Hypertension) / Type 2 Diabetes Mellitus1
4CompletedTreatmentHaemodialyzed, Type 2 Diabetes1
4CompletedTreatmentHypoglycemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentIschemic Heart Disease / Type 2 Diabetes Mellitus2
4CompletedTreatmentMenopause / Osteopenia / Osteoporosis / Type 2 Diabetes Mellitus1
4CompletedTreatmentMild Cognitive Impairment (MCI)1
4CompletedTreatmentReducing the Elevated Blood Pressure for Diabetic Hypertensive Patients1
4CompletedTreatmentType 2 Diabetes Mellitus21
4RecruitingTreatmentBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus2
4TerminatedTreatmentType 2 Diabetes Mellitus2
4Unknown StatusTreatmentDiabetes Mellitus / Oxidative Stress1
4Unknown StatusTreatmentDiabetic Blood Glucose Monitoring / Exercise / Hypoglycemic Agents / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentType 2 Diabetes Mellitus2
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus3
Not AvailableCompletedOtherHealthy Volunteers1
Not AvailableNot Yet RecruitingNot AvailableType 2 Diabetes Mellitus1
Not AvailableRecruitingPreventionIncretinomimetics / Pancreas / Type 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentType 2 Diabetes Mellitus1
Not AvailableUnknown StatusBasic ScienceTransplantation, Liver1
Not AvailableUnknown StatusBasic ScienceVagotomy, Truncal1
Not AvailableUnknown StatusTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD)1
Not AvailableWithdrawnNot AvailableType 2 Diabetes Mellitus1


Not Available
Not Available
Dosage forms
TabletOral50 mg
Not Available
Not Available


Experimental Properties
Not Available
Predicted Properties
Water Solubility1.75 mg/mLALOGPS
pKa (Strongest Acidic)14.71ChemAxon
pKa (Strongest Basic)9.03ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area76.36 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity82 m3·mol-1ChemAxon
Polarizability33.17 Å3ChemAxon
Number of Rings4ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Human Intestinal Absorption+0.9313
Blood Brain Barrier+0.7886
Caco-2 permeable-0.6768
P-glycoprotein substrateSubstrate0.6301
P-glycoprotein inhibitor IInhibitor0.5624
P-glycoprotein inhibitor IIInhibitor0.9723
Renal organic cation transporterNon-inhibitor0.6373
CYP450 2C9 substrateNon-substrate0.7472
CYP450 2D6 substrateNon-substrate0.6984
CYP450 3A4 substrateSubstrate0.5965
CYP450 1A2 substrateNon-inhibitor0.8627
CYP450 2C9 inhibitorNon-inhibitor0.6428
CYP450 2D6 inhibitorNon-inhibitor0.7168
CYP450 2C19 inhibitorNon-inhibitor0.6922
CYP450 3A4 inhibitorNon-inhibitor0.866
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5
Ames testNon AMES toxic0.7053
BiodegradationNot ready biodegradable0.9959
Rat acute toxicity2.4274 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.853
hERG inhibition (predictor II)Inhibitor0.6939
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0109000000-f6f13525e0841cb9a0ce
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0902000000-39449b9fce86086b9f42
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0900000000-e42a57f8c41f08f0fe2b
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0900000000-bdf96b3bb5758ccb2ee2
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0ue9-0900000000-813cd0c1f6616a3aac1a
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0309000000-4cc7261ec4a8a5eb3c50
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0901000000-2828160e08a306467998
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-5900000000-797e5126c08d2be98d02
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0f6t-9600000000-55a58d88d2018c5adff8
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0002-9200000000-b511fd9b2243cdaf69cc
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0005-9100000000-5c5cb1119f70d6852572
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-1709000000-d62dc38a0bb019fd4bed


This compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.
Organic compounds
Super Class
Organic acids and derivatives
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Alpha amino acid amides
Alternative Parents
N-acylpyrrolidines / Tertiary carboxylic acid amides / Tertiary alcohols / Cyclic alcohols and derivatives / Nitriles / Dialkylamines / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives
show 1 more
Alpha-amino acid amide / N-acylpyrrolidine / Cyclic alcohol / Pyrrolidine / Tertiary alcohol / Tertiary carboxylic acid amide / Carboxamide group / Secondary aliphatic amine / Carbonitrile / Nitrile
show 14 more
Molecular Framework
Aliphatic heteropolycyclic compounds
External Descriptors
Not Available


1. Dipeptidyl peptidase 4
Pharmacological action
General Function
Virus receptor activity
Specific Function
Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
Gene Name
Uniprot ID
Uniprot Name
Dipeptidyl peptidase 4
Molecular Weight
88277.935 Da
  1. Ahren B, Gomis R, Standl E, Mills D, Schweizer A: Twelve- and 52-week efficacy of the dipeptidyl peptidase IV inhibitor LAF237 in metformin-treated patients with type 2 diabetes. Diabetes Care. 2004 Dec;27(12):2874-80. [PubMed:15562200]
  2. Mentlein R, Gallwitz B, Schmidt WE: Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum. Eur J Biochem. 1993 Jun 15;214(3):829-35. [PubMed:8100523]
  3. Gupta R, Walunj SS, Tokala RK, Parsa KV, Singh SK, Pal M: Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes. Curr Drug Targets. 2009 Jan;10(1):71-87. [PubMed:19149538]

Drug created on October 20, 2007 05:50 / Updated on May 01, 2020 23:13

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