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lobeglitazone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| peroxisome proliferator activating receptor-gamma (PPAR-gamma) agonists, thiazolidinedione derivatives | 5078 | 607723-33-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
putative antidiabetic agent for type 2 diabetes
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.50 | mg | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.269 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.892 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 54.954 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 6.730 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.430 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 1.020 | % | High | 1 |
| herg | hERG pIC50 | 4.814 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 20.045 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 82.035 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.270 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CDK9,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MAP3K21,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PIK3CG,PRKDC | 18 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.246 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 36.728 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.420 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 17.620 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.820 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 45.082 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 13.930 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.210 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 1.875 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 4, 2013 | Korean Food and Drug Administration (KFDA) | Chong Kun Dang |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BD26 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs |
| ATC | A10BG04 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Thiazolidinediones |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Related Drugs by ATC class:
A10BD Combinations of oral blood glucose lowering drugs 19 drugs
A10BG Thiazolidinediones 3 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 | 6.33 | acidic |
| pKa2 | 5.62 | Basic |
| pKa3 | 1.02 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor gamma | Nuclear hormone receptor | AGONIST | EC50 | 7.75 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Peroxisome proliferator-activated receptor alpha | Nuclear hormone receptor | AGONIST | EC50 | 7.70 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| CHEBI:136052 | CHEBI |
| 8LX | PDB_CHEM_ID |
| CHEMBL3585580 | ChEMBL_ID |
| C546215 | MESH_SUPPLEMENTAL_RECORD_UI |
| DB09198 | DRUGBANK_ID |
| C2744790 | UMLSCUI |
| CHEMBL3780740 | ChEMBL_ID |
| 8729 | INN_ID |
| 763108-62-9 | SECONDARY_CAS_RN |
| 9826451 | PUBCHEM_CID |
| MY89F08K5D | UNII |
Pharmaceutical products:
None