Vildagliptin
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Also known as EquaGalvusJalraLAF 237LAF-237LAF237NVP-LAF 237NVP-LAF237VildagliptinaVildagliptineVitagliptinXiliarxVidagliptinVILDAGLIPTIN (LAF-237)
Summary
Vildagliptin (CHEMBL142703) is an approved small molecule (ATC A10BH02) targeting DPP4, DPP8, and DPP9; indicated across 8 conditions including diabetes mellitus and type 2 diabetes mellitus.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: A10BH02
- Targets: 4 (DPP4, DPP8, DPP9…)
- Indications: 8 conditions
- Clinical trials: 159
- Chemistry: 303.4 Da · C17H25N3O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL142703 |
| Name | Vildagliptin |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 6918537 |
| ATC | A10BH02 |
| Molecular formula | C17H25N3O2 |
| Molecular weight | 303.4 |
| InChIKey | SYOKIDBDQMKNDQ-XWTIBIIYSA-N |
SMILES: C1C[C@H](N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N
IUPAC name: (2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
Also known as: Equa, Galvus, Jalra, LAF 237, LAF-237, LAF237, NVP-LAF 237, NVP-LAF237, Vildagliptin, Vildagliptina, Vildagliptine, Vitagliptin
Patent coverage: 5,256 distinct patent families (20,312 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| DPP4 | dipeptidyl peptidase 4 | Inhibition | 8 | 0% | P27487 |
| DPP8 | dipeptidyl peptidase 8 | Inhibition | 5.66 | 0.1% | Q6V1X1 |
| DPP9 | dipeptidyl peptidase 9 | Inhibition | 6.64 | 0.2% | Q86TI2 |
| TRPV4 | TRPV4 | Activation | 3 | 0.6% | Q9HBA0 |
Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Dipeptidyl peptidase 4, Dipeptidyl peptidase 4, Dipeptidyl peptidase 8, Prolyl endopeptidase FAP, Dipeptidyl peptidase 9, Prolyl endopeptidase FAP.
Bioactivity
ChEMBL activities: 79 potent at pChembl ≥ 5 of 93 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| DPP9 | 9.92 | IC50 | 0.12 | nM | CHEMBL_ACT_23297177 |
| DPP4 | 9.24 | IC50 | 0.58 | nM | CHEMBL_ACT_6335421 |
| DPP8 | 8.73 | IC50 | 1.85 | nM | CHEMBL_ACT_23297200 |
| DPP4 | 8.62 | Kd | 2.4 | nM | CHEMBL_ACT_19442629 |
| DPP4 | 8.52 | Ki | 3 | nM | CHEMBL_ACT_12044046 |
| DPP4 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_13421612 |
| DPP4 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_2697711 |
| DPP4 | 8.49 | IC50 | 3.2 | nM | CHEMBL_ACT_11014707 |
| DPP4 | 8.46 | IC50 | 3.5 | nM | CHEMBL_ACT_14583367 |
| DPP4 | 8.46 | IC50 | 3.5 | nM | CHEMBL_ACT_1463619 |
| DPP4 | 8.46 | IC50 | 3.5 | nM | CHEMBL_ACT_25636087 |
| DPP4 | 8.46 | IC50 | 3.5 | nM | CHEMBL_ACT_2713701 |
| DPP4 | 8.4 | Ki | 4 | nM | CHEMBL_ACT_1774761 |
| DPP4 | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_3302925 |
| DPP4 | 8 | IC50 | 10 | nM | CHEMBL_ACT_13903928 |
| DPP4 | 8 | IC50 | 10 | nM | CHEMBL_ACT_25642825 |
| DPP4 | 7.97 | Kd | 10.7 | nM | CHEMBL_ACT_19442665 |
| DPP4 | 7.89 | Ki | 13 | nM | CHEMBL_ACT_25636176 |
| DPP4 | 7.82 | IC50 | 15 | nM | CHEMBL_ACT_18896738 |
| DPP4 | 7.8 | IC50 | 16 | nM | CHEMBL_ACT_3313879 |
| DPP4 | 7.78 | IC50 | 16.6 | nM | CHEMBL_ACT_2713691 |
| DPP4 | 7.77 | IC50 | 17 | nM | CHEMBL_ACT_3313864 |
| DPP4 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_13856200 |
| DPP4 | 7.64 | IC50 | 23 | nM | CHEMBL_ACT_15714329 |
| P28843 | 7.58 | IC50 | 26 | nM | CHEMBL_ACT_25636170 |
| DPP4 | 7.47 | IC50 | 34 | nM | CHEMBL_ACT_24967493 |
| DPP4 | 7.47 | IC50 | 34 | nM | CHEMBL_ACT_25636152 |
| DPP4 | 7.47 | IC50 | 34 | nM | CHEMBL_ACT_2605858 |
| DPP4 | 7.47 | IC50 | 34 | nM | CHEMBL_ACT_325933 |
| DPP9 | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_19099073 |
Target pathways
Aggregated over 4 target gene(s): DPP4, DPP8, DPP9, TRPV4.
Top Reactome pathways
4 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| TRP channels | 1 | TRPV4 |
| Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1) | 1 | DPP4 |
| Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP) | 1 | DPP4 |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 1 | TRPV4 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| proteolysis | 3 |
| response to hypoxia | 2 |
| negative regulation of programmed cell death | 2 |
| protein maturation | 2 |
| CARD8 inflammasome complex assembly | 2 |
| pyroptotic cell death | 2 |
| NLRP1 inflammasome complex assembly | 2 |
| behavioral fear response | 1 |
| cell adhesion | 1 |
| positive regulation of cell population proliferation | 1 |
| negative regulation of extracellular matrix disassembly | 1 |
| peptide hormone processing | 1 |
| receptor-mediated endocytosis of virus by host cell | 1 |
| T cell costimulation | 1 |
| regulation of cell-cell adhesion mediated by integrin | 1 |
Indications & clinical
Indications
8 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| diabetes mellitus | 4 | MONDO:0005015 | EFO:0000400 |
| type 2 diabetes mellitus | 4 | MONDO:0005148 | MONDO:0005148 |
| prediabetes syndrome | 3 | MONDO:0006920 | EFO:1001121 |
| type 1 diabetes mellitus | 3 | MONDO:0005147 | MONDO:0005147 |
| glucose intolerance | 2 | MONDO:0001076 | EFO:0002546 |
| gestational diabetes | 2 | MONDO:0005406 | EFO:0004593 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| major depressive disorder | 1 | MONDO:0002009 | MONDO:0002009 |
Clinical trials
Total trials: 159.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 71 |
| PHASE4 | 50 |
| Not specified | 13 |
| PHASE2 | 9 |
| PHASE1 | 9 |
| PHASE2/PHASE3 | 4 |
| PHASE1/PHASE2 | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05366868 | PHASE4 | ACTIVE_NOT_RECRUITING | Durable Effect of Imeglimin on the Glycemic Control in Patients With Type 2 Diabetes Mellitus |
| NCT06851962 | PHASE4 | ACTIVE_NOT_RECRUITING | Impact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes. |
| NCT00894868 | PHASE4 | COMPLETED | Effect of Vildagliptin on Left Ventricular Function in Patients With Type 2 Diabetes and Congestive Heart Failure |
| NCT01099137 | PHASE4 | COMPLETED | Effect of Vildagliptin in Type 2 Diabetes Treated With Sulphonylurea and Metformin |
| NCT01147276 | PHASE4 | COMPLETED | Vildagliptin and the Glucagon Response to Hypoglycemia in Type 1 Diabetes |
| NCT01193296 | PHASE4 | COMPLETED | Glycemic Holter Study (Continuous Glucose Monitoring) - |
| NCT01196546 | PHASE4 | COMPLETED | Efficacy and Safety of Combination Therapy of Vildagliptin/Metformin in Patients in Type 2 Diabetes Mellitus (T2DM) |
| NCT01219400 | PHASE4 | COMPLETED | Vildagliptin and the Glucagon Response to Hypoglycemia in Insulin-Treated Patients With Type 2 Diabetes |
| NCT01238978 | PHASE4 | COMPLETED | Phase 4 Study in the Elderly Patients With T2DM |
| NCT01309698 | PHASE4 | COMPLETED | Drug Interaction of Vildagliptin (LAF237) With Voglibose in Japanese Patients With Type 2 Diabetes |
| NCT01339143 | PHASE4 | UNKNOWN | Compare the Effect of DPP-IV Inhibitor or TZD on Glycemic Variability and Oxidative Stress in Patient With 2 Diabetes |
| NCT01356381 | PHASE4 | COMPLETED | Study to Assess the Effect of 24 Weeks of Treatment With Vildagliptin in Patients With Type 2 Diabetes |
| NCT01398592 | PHASE4 | COMPLETED | Vildagliptin Versus Sitagliptin - Differences in Fasting Plasma Glucose Lowering Efficacy |
| NCT01426737 | PHASE4 | UNKNOWN | The Swiss Glucose Variability Study |
| NCT01426802 | PHASE4 | COMPLETED | Vildagliptin 50 mg Twice Daily in Patients With Type 2 Diabetes Mellitus Inadequately Controlled With Metformin |
| NCT01472432 | PHASE4 | COMPLETED | DPP IV Inhibition Facilitates Healing of Chronic Foot Ulcers in Type 2 Diabetes |
| NCT01518101 | PHASE4 | COMPLETED | Vildagliptin Versus Liraglutide - Patient Preference After Receiving Both Medications |
| NCT01528254 | PHASE4 | COMPLETED | VERIFY:A Study to Compare Combination Regimen With Vildagliptin & Metformin Versus Metformin in Treatment-naïve Patients With Type 2 Diabetes Mellitus |
| NCT01541956 | PHASE4 | COMPLETED | Efficacy of VIldagliptin aS an Add-on Therapy to Metformin Compared to Metformin Up-TitratION in Chinese Patients With Type 2 Diabetes.(VISION) |
| NCT01565096 | PHASE4 | UNKNOWN | Effect of Adding Vildagliptin on Beta Cell Function and Cardiovascular Risk Markers in Patients With Moderate Metabolic Control During Metformin Monotherapy |
| NCT01582243 | PHASE4 | COMPLETED | Safety and Efficacy of Vildagliptin Plus Metformin (SPC) Treatment in Type 2 Diabetes Mellitus Patients |
| NCT01649466 | PHASE4 | COMPLETED | Safety and Efficacy of Vildagliptin Versus NPH Insulin add-on to Glimepiride in Type 2 Diabetes Mellitus Patients. |
| NCT01679899 | PHASE4 | COMPLETED | Effect of Anti-diabetic Drugs on Bone Metabolism and Glycemic Variability |
| NCT01686932 | PHASE4 | COMPLETED | Vildagliptin vs Sitagliptin add-on to Insulin - Impact on Glycemic Profile and Correlation of Hypoglycemic Episodes and Heart Function |
| NCT01757587 | PHASE4 | COMPLETED | Galvus (Vildagliptin) vs Placebo in Combination With Metformin and Insulin |
| NCT01758380 | PHASE4 | COMPLETED | Vildagliptin Compared to Gliclazide as Dual Therapy With Metformin in Muslim Patients With Type 2 Diabetes Fasting During Ramadan |
| NCT01766778 | PHASE4 | COMPLETED | Early add-on Vildagliptin in Patients With Type 2 Diabetes Inadequately Controlled by Metformin |
| NCT01812122 | PHASE4 | COMPLETED | Effects of Vildagliptine and Glimepiride on Glucose Variability |
| NCT01827280 | PHASE4 | COMPLETED | Acute and Short-term Chronic Effects of Galvus (Vildagliptin) in Diabetes Type 2 Obese Women |
| NCT01862263 | PHASE4 | TERMINATED | Effect of 13-Week Treatment With Vildagliptin as Add-On Therapy to Improve Glucose Variability in Type II Diabetes |
| NCT01882907 | PHASE4 | COMPLETED | Safety and Efficacy Study to Compare Vildagliptin to Pioglitazone as Adding on Metformin in Type 2 Diabetes |
| NCT01910441 | PHASE4 | TERMINATED | Comparison of Vildagliptin vs. Glimepiride on Glucose Variability in Metformin Uncontrolled Type 2 Diabetic Patients |
| NCT02002221 | PHASE4 | COMPLETED | Study of Efficacy and Safety of Vildagliptin as add-on Insulin Therapy in T2DM Patients |
| NCT02007278 | PHASE4 | COMPLETED | Glycemic Excursions in Type 2 Diabetic Patients With Vildagliptin and Metformin Versus Vildagliptin and Glimepiride |
| NCT02089438 | PHASE4 | COMPLETED | DPP-4 Inhibition, Incretins and Islet Function |
| NCT02142309 | PHASE4 | UNKNOWN | Glycemic Durability After Metformin Failure |
| NCT02145611 | PHASE4 | COMPLETED | Vildagliptin vs. Glibenclamide in Endothelial Function in Type 2 Diabetes and Hypertension |
| NCT02176681 | PHASE4 | COMPLETED | A Prospective, Multicenter, Randomized, Open-label Study of 12 Week Duration to Evaluate the Effect of VILDagliptin Added to Insulin on Glycaemic Control in haemoDIALyzed Patients With Type 2 Diabetes: Probe Analysis of CGM |
| NCT02475070 | PHASE4 | COMPLETED | Vildagliptin Versus Dapagliflozin on Glucagon |
| NCT02832999 | PHASE4 | COMPLETED | Short Term Effect of Liraglutide Versus Vildagliptine on Insulin Secretion and Insulin Sensitivity in Type 2 Diabetes |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 25 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
33 molecules share ≥1 primary target. Top 33 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ALOGLIPTIN | ChEMBL + PubChem | Phase 4 (approved) | DPP4, DPP8, DPP9 |
| LINAGLIPTIN | ChEMBL + PubChem | Phase 4 (approved) | DPP4, DPP8, DPP9 |
| SAXAGLIPTIN | ChEMBL + PubChem | Phase 4 (approved) | DPP4, DPP8, DPP9 |
| GOSOGLIPTIN | ChEMBL | Phase 4 (approved) | DPP4, DPP8, DPP9 |
| SITAGLIPTIN | ChEMBL | Phase 4 (approved) | DPP4, DPP8, DPP9 |
| TENELIGLIPTIN | ChEMBL | Phase 4 (approved) | DPP4, DPP8, DPP9 |
| DUTOGLIPTIN | ChEMBL | Phase 3 | DPP4, DPP8, DPP9 |
| TALABOSTAT | ChEMBL | Phase 3 | DPP4, DPP8, DPP9 |
| ANAGLIPTIN | ChEMBL | Phase 4 (approved) | DPP4 |
| EVOGLIPTIN | ChEMBL | Phase 4 (approved) | DPP4 |
| GEMIFLOXACIN | ChEMBL | Phase 4 (approved) | DPP4 |
| METFORMIN | ChEMBL | Phase 4 (approved) | DPP4 |
| OMARIGLIPTIN | ChEMBL | Phase 4 (approved) | DPP4 |
| TRELAGLIPTIN | ChEMBL | Phase 4 (approved) | DPP4 |
| VIDARABINE | ChEMBL | Phase 4 (approved) | DPP4 |
| CAFFEIC ACID | ChEMBL | Phase 3 | DPP4 |
| CANNABINOL | ChEMBL | Phase 3 | TRPV4 |
| DBPR-108 | ChEMBL | Phase 3 | DPP4 |
| EPIGALOCATECHIN GALLATE | ChEMBL | Phase 3 | DPP4 |
| QUERCETIN | ChEMBL | Phase 3 | DPP4 |
| RESVERATROL | ChEMBL | Phase 3 | DPP4 |
| RETAGLIPTIN | ChEMBL | Phase 3 | DPP4 |
| CANNABIDIVARIN | ChEMBL | Phase 2 | TRPV4 |
| CANNABIGEROL | ChEMBL | Phase 2 | TRPV4 |
| CARMEGLIPTIN | ChEMBL | Phase 2 | DPP4 |
| COFROGLIPTIN | ChEMBL | Phase 2 | DPP4 |
| FLAVONE | ChEMBL | Phase 2 | DPP4 |
| GALLIC ACID | ChEMBL | Phase 2 | DPP4 |
| GENISTEIN | ChEMBL | Phase 2 | DPP4 |
| GSK2798745 | ChEMBL | Phase 2 | TRPV4 |
| LUTEOLIN | ChEMBL | Phase 2 | DPP4 |
| TETRAHYDROCANNABIVARIN | ChEMBL | Phase 2 | TRPV4 |
| Carfilzomib | PubChem | Approved | DPP4 |
Related Atlas pages
- Genes: DPP4, DPP8, DPP9, TRPV4
- Diseases: diabetes mellitus, type 2 diabetes mellitus, prediabetes syndrome, type 1 diabetes mellitus
- Drugs: Alogliptin, Linagliptin, Saxagliptin, Gosogliptin, Sitagliptin, Teneligliptin, Dutogliptin, Talabostat, Anagliptin, Evogliptin, Gemifloxacin, Metformin, Omarigliptin, Trelagliptin, Vidarabine, Caffeic Acid, Cannabinol, DBPR-108, Epigalocatechin Gallate, Quercetin, Resveratrol, Retagliptin, Carfilzomib