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levocabastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihistaminics | 1564 | 79516-68-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.60 | mg | N |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 70 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.07 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 99 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.17 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.43 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.45 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 33 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.00 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 | 1.210 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.279 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 32.359 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.547 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 25.530 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 41.340 | % | High | 1 |
| herg | hERG pIC50 | 4.919 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.396 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 2.761 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 39.840 | % | High | 1 |
| kinase-safety-class | ACVR2B,CDK5,EIF2AK3,GRK2,ITK,PDK1,PDK2,PDK4,TGFBR1 | 9 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,PDK4 | 4 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 4.426 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.550 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 3.133 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 36.470 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 7.482 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 26.770 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.102 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 3.162 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 77.170 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 23.440 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 887.156 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 10, 1993 | FDA | NOVARTIS |
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 |
|---|---|---|---|---|---|---|
| Abdominal wall haematoma | 24.18 | 18.19 | 6 | 1065 | 3346 | 90624030 |
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 | R01AC02 | RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Antiallergic agents, excl. corticosteroids |
| ATC | S01GX02 | SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D039563 | Histamine H1 Antagonists, Non-Sedating |
Related Drugs by ATC class:
R01AC Antiallergic agents, excl. corticosteroids 7 drugs
S01GX Other antiallergics 12 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.47 | acidic |
| pKa2 | 8.56 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | Ki | 7.28 | WOMBAT-PK | CHEMBL | |||
| Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
| Neurotensin receptor type 2 | GPCR | AGONIST | Ki | 6.80 | IUPHAR | ||||
| Neurotensin receptor 2 | GPCR | Ki | 7.48 | CHEMBL | |||||
| Neurotensin receptor type 2 | GPCR | AGONIST | IC50 | 8.70 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4020853 | VUID |
| N0000022941 | NUI |
| D01717 | KEGG_DRUG |
| 79547-78-7 | SECONDARY_CAS_RN |
| 4020853 | VANDF |
| 4023908 | VANDF |
| C0064870 | UMLSCUI |
| CHEMBL1615438 | ChEMBL_ID |
| CHEMBL1237102 | ChEMBL_ID |
| DB01106 | DRUGBANK_ID |
| C047340 | MESH_SUPPLEMENTAL_RECORD_UI |
| 54385 | PUBCHEM_CID |
| 1586 | IUPHAR_LIGAND_ID |
| 5393 | INN_ID |
| H68BP06S81 | UNII |
| 1294532 | RXNORM |
| 2017 | MMSL |
| 4969 | MMSL |
| 004416 | NDDF |
| 004417 | NDDF |
| 108863001 | SNOMEDCT_US |
| 108864007 | SNOMEDCT_US |
| 372554006 | SNOMEDCT_US |
| CHEBI:135679 | CHEBI |
| H68BP06S81 | INXIGHT DRUGS |
Pharmaceutical products:
None