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pranlukast 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| leukotriene receptor antagonists | 2237 | 103177-37-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
SRS-A antagonist; leukotriene D4 receptor antagonist
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 18 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.326 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 316.957 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 3.126 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 9.226 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.080 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.190 | % | High | 1 |
| herg | hERG pIC50 | 4.762 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 180.302 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 201.837 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.340 | % | High | 1 |
| kinase-safety-class | ACVR2B,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FGFR1,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPKAPK2,MARK4,MELK,MET,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 49 | |||
| kinase-selectivity-class | AXL,BRAF,CAMK2D,DYRK1B,EIF2AK3,GRK2,MAPK7,PDK1,PDK4,STK33,TTK | 11 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 18.836 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 58.345 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 32.810 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.180 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 12.303 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.150 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.032 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 86.896 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 3.350 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.170 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 16.032 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 15, 2007 | PMDA |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Hepatic function abnormal | 35.55 | 34.60 | 18 | 792 | 51549 | 42568976 |
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 |
|---|---|---|---|---|---|---|
| Hepatic function abnormal | 58.43 | 29.51 | 28 | 1646 | 89267 | 110498358 |
| Concomitant disease aggravated | 34.85 | 29.51 | 12 | 1662 | 16352 | 110571273 |
| Upper respiratory tract inflammation | 30.45 | 29.51 | 8 | 1666 | 4363 | 110583262 |
| Pyrexia | 30.44 | 29.51 | 51 | 1623 | 898214 | 109689411 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R03DC02 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES Leukotriene receptor antagonists |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D018927 | Anti-Asthmatic Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| MeSH PA | D020024 | Leukotriene Antagonists |
Related Drugs by ATC class:
R03DC Leukotriene receptor antagonists 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Allergic rhinitis | indication | 61582004 | |
| Asthma | indication | 195967001 | DOID:2841 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.55 | acidic |
| pKa2 | 10.08 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Cysteinyl leukotriene receptor 1 | GPCR | ANTAGONIST | IC50 | 10 | IUPHAR | SCIENTIFIC LITERATURE | |||
| Cysteinyl leukotriene receptor 2 | GPCR | ANTAGONIST | IC50 | 5.44 | IUPHAR | ||||
| Bile acid receptor | Nuclear hormone receptor | EC50 | 4.82 | CHEMBL | |||||
| Uracil nucleotide/cysteinyl leukotriene receptor | GPCR | Ki | 5.39 | CHEMBL | |||||
| Cysteinyl leukotriene receptor 1 | GPCR | Ki | 9.10 | CHEMBL | |||||
| Replicase polyprotein 1ab | Enzyme | Kd | 4.85 | CHEMBL | |||||
| Cruzipain | Enzyme | IC50 | 5.15 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D02732 | KEGG_DRUG |
| C0526058 | UMLSCUI |
| CHEBI:94810 | CHEBI |
| KNT | PDB_CHEM_ID |
| CHEMBL21333 | ChEMBL_ID |
| CHEMBL11350 | ChEMBL_ID |
| DB01411 | DRUGBANK_ID |
| C047681 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3634 | IUPHAR_LIGAND_ID |
| 6943 | INN_ID |
| TB8Z891092 | UNII |
| 4887 | PUBCHEM_CID |
| 713438006 | SNOMEDCT_US |
| TB8Z891092 | INXIGHT DRUGS |
Pharmaceutical products:
None