Vildagliptin is a once-daily dipeptidyl peptidase 4 (DPP-4) inhibitor used in the management of type 2 diabetes mellitus.

Brand Names
Galvus, Jalra, Xiliarx
Generic Name
DrugBank Accession Number

Vildagliptin (LAF237) is an orally active antihyperglycemic agent that selectively inhibits the dipeptidyl peptidase-4 (DPP-4) enzyme. It is used to manage type II diabetes mellitus, where GLP-1 secretion and insulinotropic effects are impaired.2 By inhibiting DPP-4, vildagliptin prevents the degradation of glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which are incretin hormones that promote insulin secretion and regulate blood glucose levels. Elevated levels of GLP-1 and GIP consequently results in improved glycemic control.6 In clinical trials, vildagliptin has a relatively low risk of hypoglycemia.2

Oral vildagliptin was approved by the European Medicines Agency in 2008 for the treatment of type II diabetes mellitus in adults as monotherapy or in combination with metformin, a sulfonylurea, or a thiazolidinedione in patients with inadequate glycemic control following monotherapy. It is marketed as Galvus.6 Vildagliptin is also available as Eucreas, a fixed-dose formulation with metformin for adults in who do not adequately glycemic control from monotherapy.8 Vildagliptin is currently under investigation in the US.

Small Molecule
Approved, Investigational
Average: 303.3993
Monoisotopic: 303.194677059
Chemical Formula
  • Vildagliptin
  • Vildagliptina
External IDs
  • LAF 237
  • LAF-237
  • LAF237
  • NVP-LAF 237
  • NVP-LAF-237
  • NVP-LAF237



Vildagliptin is indicated in the treatment of type II diabetes mellitus in adults. As monotherapy, vildagliptin is indicated in adults inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance.6 It is also indicated as dual therapy in combination with metformin, a sulphonylurea, or a thiazolidinedione in adults patients with insufficient glycemic control despite maximal tolerated dose of monotherapy.6

Vildagliptin is also marketed in a combination product with metformin for the treatment of adults with type II diabetes mellitus who inadequately respond to either monotherapy of vildagliptin or metformin. This fixed-dose formulation can be used in combination with a sulphonylurea or insulin (i.e., triple therapy) as an adjunct to diet and exercise in adults who do not achieve adequate glycemic control with monotherapy or dual therapy.8

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used as adjunct in combination to manageType 2 diabetes mellitusCombination Product in combination with: Metformin (DB00331)••••••••••••••••••••••••••• ••••••• •••• •••••• •••••••••• •••••••• •• •••••••••••••••
Used in combination to manageType 2 diabetes mellitusCombination Product in combination with: Metformin (DB00331)••••••••••••••••••••••••••• •••••••• •• •••••••••• •••••••••• ••••••• •••• •••••••••••
Used as adjunct in combination to manageType 2 diabetes mellitusCombination Product in combination with: Metformin (DB00331)••••••••••••••••••••••••••• •••••••• •• •••••••••• •••••••••• •••••••• •• ••••••••••• ••••• •••••••••••••
Used as adjunct in combination to manageType 2 diabetes mellitusCombination Product in combination with: Metformin (DB00331)••••••••••••••••••••••••••• •••••••• •• ••••••••••••• •••••••••• •••••••• •• •••••••••••••••
Used as adjunct in combination to manageType 2 diabetes mellitus••••••••••••••••••••••••••• •••••••• •• ••••••••••• ••••• •••••••• •••••••••• •••••••• •• •••••••••••••••
Contraindications & Blackbox Warnings
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Vildagliptin works to improve glycemic control in type II diabetes mellitus by enhancing the glucose sensitivity of beta-cells (β-cells) in pancreatic islets and promoting glucose-dependent insulin secretion. Increased GLP-1 levels leads to enhanced sensitivity of alpha cells to glucose, promoting glucagon secretion. Vildagliptin causes an increase in the insulin to glucagon ratio by increasing incretin hormone levels: this results in a decrease in fasting and postprandial hepatic glucose production. Vildagliptin does not affect gastric emptying. It also has no effects on insulin secretion or blood glucose levels in individuals with normal glycemic control.6

In clinical trials, treatment with vildagliptin 50-100 mg daily in patients with type 2 diabetes significantly improved markers of beta-cells, proinsulin to insulin ratio, and measures of beta-cell responsiveness from the frequently-sampled meal tolerance test. 6 Vildagliptin has improves glycated hemoglobin (HbA1c) and fasting plasma glucose (FPG) levels.2

Mechanism of action

Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) are incretin hormones that regulate blood glucose levels and maintain glucose homeostasis. It is estimated that the activity of GLP-1 and GIP contribute more than 70% to the insulin response to an oral glucose challenge. They stimulate insulin secretion in a glucose-dependent manner via G-protein-coupled GIP and GLP-1 receptor signalling. In addition to their effects on insulin secretion, GLP-1 is also involved in promoting islet neogenesis and differentiation, as well as attenuating pancreatic beta-cell apoptosis. Incretin hormones also exert extra-pancreatic effects, such as lipogenesis and myocardial function.3 In type II diabetes mellitus, GLP-1 secretion is impaired, and the insulinotropic effect of GIP is significantly diminished.2

Vildagliptin exerts its blood glucose-lowering effects by selectively inhibiting dipeptidyl peptidase-4 (DPP-4), an enzyme that rapidly truncates and inactivates GLP-1 and GIP upon their release from the intestinal cells. DPP-4 cleaves oligopeptides after the second amino acid from the N-terminal end. Inhibition of DPP-4 substantially prolongs the half-life of GLP-1 and GIP, increasing the levels of active circulating incretin hormones.3 The duration of DPP-4 inhibition by vildagliptin is dose-dependent.5 Vildagliptin reduces fasting and prandial glucose and HbA1c. It enhances the glucose sensitivity of alpha- and beta-cells and augments glucose-dependent insulin secretion. Fasting and postprandial glucose levels are decreased, and postprandial lipid and lipoprotein metabolism are also improved.2,4

ADipeptidyl peptidase 4

In a fasting state, vildagliptin is rapidly absorbed following oral administration. Peak plasma concentrations are observed at 1.7 hours following administration.6 Plasma concentrations of vildagliptin increase in an approximately dose-proportional manner.2

Food delays Tmax to 2.5 hours and decreases Cmax by 19%, but has no effects on the overall exposure to the drug (AUC). Absolute bioavailability of vildagliptin is 85%.6

Volume of distribution

The mean volume of distribution of vildagliptin at steady-state after intravenous administration is 71 L, suggesting extravascular distribution.6

Protein binding

The plasma protein binding of vildagliptin is 9.3%. Vildagliptin distributes equally between plasma and red blood cells.6


About 69% of orally administered vildagpliptin is eliminated via metabolism not mediated by cytochrome P450 enzymes. Based on the findings of a rat study, DPP-4 contributes partially to the hydrolysis of vildagliptin.6 Vildagliptin is metabolized to pharmacologically inactive cyano (57%) and amide (4%) hydrolysis products in the kidney.2 LAY 151 (M20.7) is a major inactive metabolite and a carboxylic acid that is formed via hydrolysis of the cyano moiety: it accounts for 57% of the dose.6 Other circulating metabolites reported are an N-glucuronide (M20.2), an N-amide hydrolysis product (M15.3), two oxidation products, M21.6 and M20.9.9

Hover over products below to view reaction partners

Route of elimination

Vildagliptin is eliminated via metabolism. Following oral administration, approximately 85% of the radiolabelled vildagliptin dose was excreted in urine and about 15% of the dose was recovered in feces. Of the recovered dose in urine, about 23% accounted for the unchanged parent compound.6


The mean elimination half-life following intravenous administration is approximately two hours. The elimination half-life after oral administration is approximately three hours.6


After intravenous administration to healthy subjects, the total plasma and renal clearance of vildagliptin were 41 and 13 L/h, respectively.6

Adverse Effects
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The oral Lowest published toxic dose (TDLO) is 0.3 mg/kg in rats and 1 mg/kg in mice.7

There is limited information regarding overdose with vildagliptin. In one study, patients experienced muscle pain, mild and transient paresthesia, fever, edema, and a transient increase in lipase levels at a dose of 400 mg. At 600 mg, one subject experienced edema of the feet and hands and increases in creatine phosphokinase (CPK), aspartate aminotransferase (AST), C-reactive protein (CRP) and myoglobin levels. Supportive management is recommended in case of an overdose. There is no known antidote, and vildagliptin and its major metabolite cannot be removed via hemodialysis.6

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.
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.
Food Interactions
  • Take with or without food. Food reduces Cmax and delays Tmax, but not in a clinically significant way.


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International/Other Brands
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
GalvusTablet50 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
GalvusTablet50 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
GalvusTablet50 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
GalvusTablet50 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
GalvusTablet50 mgOralNovartis Europharm Limited2016-09-08Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
EUCREASVildagliptin (50 MG) + Metformin hydrochloride (1000 MG)Tablet, film coatedOralNovartis Europharm Limited2014-07-08Not applicableItaly flag
EucreasVildagliptin (50 mg) + Metformin hydrochloride (660 mg)Tablet, film coatedOralNovartis Europharm Limited2016-09-08Not applicableEU flag
EucreasVildagliptin (50 mg) + Metformin hydrochloride (660 mg)Tablet, film coatedOralNovartis Europharm Limited2020-12-16Not applicableEU flag
EucreasVildagliptin (50 mg) + Metformin hydrochloride (660 mg)Tablet, film coatedOralNovartis Europharm Limited2016-09-08Not applicableEU flag
EUCREASVildagliptin (50 MG) + Metformin hydrochloride (850 MG)Tablet, film coatedOralNovartis Europharm Limited2014-07-08Not applicableItaly flag


ATC Codes
A10BH02 — VildagliptinA10BD08 — Metformin and vildagliptin
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Alcohol / Aliphatic heteropolycyclic compound / Alpha-amino acid amide / Amine / Azacycle / Carbonitrile / Carbonyl group / Carboxamide group / Cyclic alcohol / Hydrocarbon derivative
show 14 more
Molecular Framework
Aliphatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number
InChI Key


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. [Article]
  2. Croxtall JD, Keam SJ: Vildagliptin: a review of its use in the management of type 2 diabetes mellitus. Drugs. 2008;68(16):2387-409. doi: 10.2165/0003495-200868160-00009. [Article]
  3. Ahren B: DPP-4 inhibitors. Best Pract Res Clin Endocrinol Metab. 2007 Dec;21(4):517-33. doi: 10.1016/j.beem.2007.07.005. [Article]
  4. Mathieu C, Degrande E: Vildagliptin: a new oral treatment for type 2 diabetes mellitus. Vasc Health Risk Manag. 2008;4(6):1349-60. doi: 10.2147/vhrm.s3005. [Article]
  5. He YL: Clinical pharmacokinetics and pharmacodynamics of vildagliptin. Clin Pharmacokinet. 2012 Mar 1;51(3):147-62. doi: 10.2165/11598080-000000000-00000. [Article]
  6. Summary of Product Characteristics: Galvus (vildagliptin) oral tablets [Link]
  7. Cayman Chemical: Vildagliptin Safety Data Sheet [Link]
  8. Summary of Product Characteristics: Eucreas (vildagliptin and metformin) oral tablets [Link]
  9. Australian Public Assessment Report: Vildagliptin [Link]
Human Metabolome Database
PubChem Compound
PubChem Substance

Clinical Trials

Clinical Trials
4CompletedBasic ScienceDiabetes1
4CompletedBasic ScienceDiabetes / Hypoglycemia1
4CompletedBasic ScienceType 2 Diabetes Mellitus3
4CompletedTreatment1- Microvascular Function / 2-oxidative Stress / 3-inflammation / Microvascular Function1
4CompletedTreatmentCongestive Heart Failure (CHF) / Type 2 Diabetes Mellitus1


Not Available
Not Available
Dosage Forms
TabletOral50 MG
TabletOral50.000 mg
Tablet, film coatedOral50 mg
Tablet, coatedOral
Tablet, film coatedOral
Tablet, film coatedOral
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-MSsplash10-001i-9640000000-8d45705b266a6c8e72b7
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-0002-0049000000-467b8774aceed12b4d58
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
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0udi-0249000000-1f405a3fa3fc40a37a82
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0udi-0009000000-23371cf66547ac2ca0bd
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0ff9-3911000000-3acaa4dd038624fc6903
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0udj-9046000000-314d160c6a92c8dbcf25
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-9400000000-0bf7913ede0bb390fc0f
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-000t-9060000000-297c5b75613b086be08a
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)


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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. [Article]
  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. [Article]
  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. [Article]
  4. Nadkarni P, Chepurny OG, Holz GG: Regulation of glucose homeostasis by GLP-1. Prog Mol Biol Transl Sci. 2014;121:23-65. doi: 10.1016/B978-0-12-800101-1.00002-8. [Article]
  5. Gallwitz B: Novel Therapeutic Approaches in Diabetes. Endocr Dev. 2016;31:43-56. doi: 10.1159/000439372. Epub 2016 Jan 19. [Article]


Pharmacological action
Curator comments
Transport of vildagliptin was decreased in the presence of the P-glycoprotein inhibitors verapamil and terfenadine indicating in vivo vildagliptin efflux due to P-glycoprotein.
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
Uniprot ID
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
  1. Australian Public Assessment Report: Vildagliptin [Link]

Drug created at October 20, 2007 11:50 / Updated at October 01, 2021 23:55