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teneligliptin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| dipeptidyl aminopeptidase-IV inhibitors | 4895 | 760937-92-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A long-acting, orally bioavailable, pyrrolidine-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Teneligliptin may also reduce plasma triglyceride levels through a sustained increase in GLP-1 levels.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,PDK2,PDK4,PRKDC | 12 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 6.668 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| rat-kpuu-brain | Rat brain Kpuu | 0.037 | % | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 29, 2012 | PMDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Pemphigoid | 59.18 | 35.79 | 14 | 752 | 9012 | 90618669 |
| Diabetic ketoacidosis | 41.18 | 35.79 | 13 | 753 | 24394 | 90603287 |
| Glycosylated haemoglobin increased | 37.90 | 35.79 | 11 | 755 | 15551 | 90612130 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Cerebral infarction | 53.63 | 27.58 | 25 | 1527 | 31144 | 42588639 |
| Diabetes mellitus | 43.24 | 27.58 | 27 | 1525 | 60060 | 42559723 |
| Pemphigoid | 42.83 | 27.58 | 16 | 1536 | 11451 | 42608332 |
| Renal impairment | 40.81 | 27.58 | 33 | 1519 | 110195 | 42509588 |
| Cardiac failure | 35.39 | 27.58 | 30 | 1522 | 106826 | 42512957 |
| Interstitial lung disease | 34.45 | 27.58 | 26 | 1526 | 78436 | 42541347 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Cerebral infarction | 88.03 | 26.99 | 36 | 2513 | 51802 | 110534948 |
| Pemphigoid | 79.81 | 26.99 | 26 | 2523 | 19681 | 110567069 |
| Renal impairment | 60.22 | 26.99 | 43 | 2506 | 188402 | 110398348 |
| Diabetes mellitus | 49.61 | 26.99 | 30 | 2519 | 99351 | 110487399 |
| Diabetes mellitus inadequate control | 48.20 | 26.99 | 20 | 2529 | 29755 | 110556995 |
| Cardiac failure | 46.96 | 26.99 | 37 | 2512 | 187589 | 110399161 |
| Interstitial lung disease | 44.94 | 26.99 | 32 | 2517 | 139302 | 110447448 |
| Hypoglycaemia | 40.54 | 26.99 | 28 | 2521 | 116076 | 110470674 |
| Glycosylated haemoglobin increased | 38.68 | 26.99 | 16 | 2533 | 23603 | 110563147 |
| Pneumonia bacterial | 37.05 | 26.99 | 16 | 2533 | 26245 | 110560505 |
| Diabetic ketoacidosis | 35.61 | 26.99 | 18 | 2531 | 42040 | 110544710 |
| Hepatic function abnormal | 34.66 | 26.99 | 23 | 2526 | 89272 | 110497478 |
| Pneumonia aspiration | 31.71 | 26.99 | 21 | 2528 | 81212 | 110505538 |
| Decreased appetite | 31.16 | 26.99 | 46 | 2503 | 475800 | 110110950 |
| Dehydration | 27.49 | 26.99 | 33 | 2516 | 279478 | 110307272 |
| Toxic encephalopathy | 27.28 | 26.99 | 11 | 2538 | 15203 | 110571547 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BD28 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs |
| ATC | A10BH08 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Dipeptidyl peptidase 4 (DPP-4) inhibitors |
Related Drugs by ATC class:
A10BD Combinations of oral blood glucose lowering drugs 19 drugs
A10BH Dipeptidyl peptidase 4 (DPP-4) inhibitors 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.33 | Basic |
| pKa2 | 4.33 | Basic |
| pKa3 | 2.09 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Dipeptidyl peptidase 4 | Enzyme | INHIBITOR | IC50 | 9.43 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Dipeptidyl peptidase 8 | Enzyme | IC50 | 6.59 | SCIENTIFIC LITERATURE | |||||
| Dipeptidyl peptidase 9 | Enzyme | IC50 | 6.27 | SCIENTIFIC LITERATURE | |||||
| Dipeptidyl peptidase 4 | Enzyme | IC50 | 9.54 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 28ZHI4CF9C | UNII |
| D08616 | KEGG_DRUG |
| 2574405-80-2 | SECONDARY_CAS_RN |
| C2981308 | UMLSCUI |
| M51 | PDB_CHEM_ID |
| CHEMBL2147777 | ChEMBL_ID |
| 11949652 | PUBCHEM_CID |
| DB11950 | DRUGBANK_ID |
| 8994 | INN_ID |
| C579035 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9906 | IUPHAR_LIGAND_ID |
| 1172794002 | SNOMEDCT_US |
| 1172797009 | SNOMEDCT_US |
| 1172926000 | SNOMEDCT_US |
| CHEBI:136042 | CHEBI |
| 28ZHI4CF9C | INXIGHT DRUGS |
Pharmaceutical products:
None