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laropiprant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| prostaglandin receptors antagonists, non-prostanoids | 4326 | 571170-77-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a potent orally active human prostaglandin D(2) receptor 1 antagonist
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 1 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.21 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 11.80 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 71 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.750 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 4.018 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 73.282 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 15.031 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.690 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 1.740 | % | High | 1 |
| herg | hERG pIC50 | 4.769 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 16.255 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 13.490 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.560 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CG,PRKDC,TGFBR1 | 17 | |||
| kinase-selectivity-class | AXL,GRK2,MAP2K6 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 7.727 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 26.242 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.990 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 27.542 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.660 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 30.269 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 28.520 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.450 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 881.049 | uM | High | 1 |
Approvals:
None
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 |
|---|---|---|
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:35821 | anticholesteremic drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dyslipidemia | indication | 370992007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.04 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin D2 receptor | GPCR | ANTAGONIST | Kd | 10.52 | CHEMBL | SCIENTIFIC LITERATURE | |||
| D(3) dopamine receptor | GPCR | Ki | 5.95 | CHEMBL | |||||
| Prostaglandin E2 receptor EP1 subtype | GPCR | Ki | 5.94 | CHEMBL | |||||
| Prostaglandin D2 receptor 2 | GPCR | Ki | 6.13 | CHEMBL | |||||
| Prostaglandin E2 receptor EP3 subtype | GPCR | Ki | 6.05 | CHEMBL | |||||
| Translocator protein | Transporter | Ki | 6.54 | CHEMBL | |||||
| Thromboxane A2 receptor | GPCR | Ki | 8.53 | CHEMBL | |||||
| Prostaglandin E2 receptor EP2 subtype | GPCR | Ki | 6.87 | CHEMBL | |||||
| Prostaglandin F2-alpha receptor | GPCR | Ki | 5 | CHEMBL | |||||
| Prostacyclin receptor | GPCR | Ki | 5.18 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D08940 | KEGG_DRUG |
| C1956497 | UMLSCUI |
| CHEBI:135942 | CHEBI |
| CHEMBL426559 | ChEMBL_ID |
| DB11629 | DRUGBANK_ID |
| C518174 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3356 | IUPHAR_LIGAND_ID |
| 8855 | INN_ID |
| G7N11T8O78 | UNII |
| 9867642 | PUBCHEM_CID |
| 013266 | NDDF |
| 15859311000001100 | SNOMEDCT_US |
| G7N11T8O78 | INXIGHT DRUGS |
Pharmaceutical products:
None