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lumiracoxib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| selective cyclo-oxygenase inhibitors | 1618 | 220991-20-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A selective non-steroidal anti-inflammatory drug (NSAID) that belongs to the group cyclo-oxygenase 2 (COX-2) inhibitors. It blocks the COX-2 enzyme, resulting in a reduction in the production of prostaglandins, substances that are involved in the inflammation process.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 74 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.151 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.033 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 109.648 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 17.865 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.640 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 1.410 | % | High | 1 |
| herg | hERG pIC50 | 4.542 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 94.842 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 40.365 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.720 | % | High | 1 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.618 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 49.091 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 2.200 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 4.159 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.140 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 154.882 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 53.910 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.850 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 883.080 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 12, 2003 | UK Medicines and Healthcare Products Regulatory Agency (MHRA) | Novartis Pharmaceuticals UK Limited |
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 | M01AH06 | MUSCULO-SKELETAL SYSTEM ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS Coxibs |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D016861 | Cyclooxygenase Inhibitors |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| MeSH PA | D052246 | Cyclooxygenase 2 Inhibitors |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35842 | antirheumatic drug |
| CHEBI has role | CHEBI:50629 | cyclooxygenase 2 inhibitor |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
Related Drugs by ATC class:
M01AH Coxibs 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Osteoarthritis | indication | 396275006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.24 | acidic |
| pKa2 | 0.42 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Enzyme | INHIBITOR | Ki | 6.49 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Prostaglandin G/H synthase 1 | Enzyme | IC50 | 8.15 | CHEMBL | |||||
| Prostaglandin G/H synthase 2 | Enzyme | IC50 | 7.40 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D03714 | KEGG_DRUG |
| C1176415 | UMLSCUI |
| CHEBI:73044 | CHEBI |
| LUR | PDB_CHEM_ID |
| CHEMBL404108 | ChEMBL_ID |
| DB01283 | DRUGBANK_ID |
| C473384 | MESH_SUPPLEMENTAL_RECORD_UI |
| 151166 | PUBCHEM_CID |
| 2897 | IUPHAR_LIGAND_ID |
| 8151 | INN_ID |
| V91T9204HU | UNII |
| 011158 | NDDF |
| 422506000 | SNOMEDCT_US |
| 424967004 | SNOMEDCT_US |
| V91T9204HU | INXIGHT DRUGS |
Pharmaceutical products:
None