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elobixibat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| ileal bile acid transporter (IBAT) inhibitors, bile acid reabsorption inhibitors | 5277 | 439087-18-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Elobixibat is an IBAT inhibitor approved in Japan for the treatment of chronic constipation. IBAT is the bile acid/sodium symporter responsible for the reuptake of bile acids in the ileum which is the initial step in the enterohepatic circulation. By inhibiting the uptake of bile acids, elobixibat increases the bile acid concentration in the gut, and this accelerates intestinal passage and softens the stool.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.652 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 89.743 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.114 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 6.295 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.140 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.300 | % | High | 1 |
| herg | hERG pIC50 | 4.752 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 19.275 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 34.435 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.380 | % | High | 1 |
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TEK | 26 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 20.749 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 9.886 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.130 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 49.091 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.230 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 17.258 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 0.610 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.170 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 91.411 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 19, 2018 | PMDA | EA Pharma |
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 |
|---|---|---|---|---|---|---|
| Pleurothotonus | 51.48 | 38.75 | 9 | 378 | 1202 | 42619746 |
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 |
|---|---|---|---|---|---|---|
| Pleurothotonus | 46.32 | 31.59 | 9 | 850 | 2489 | 110585951 |
| Hepatic function abnormal | 41.48 | 31.59 | 18 | 841 | 89277 | 110499163 |
| Interstitial lung disease | 33.85 | 31.59 | 18 | 841 | 139316 | 110449124 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A06AX09 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation |
| CHEBI has role | CHEBI:50503 | laxative |
Related Drugs by ATC class:
A06AX Other drugs for constipation 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic constipation | indication | 236069009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.63 | acidic |
| pKa2 | 12.17 | acidic |
| pKa3 | 5.36 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Ileal sodium/bile acid cotransporter | Transporter | INHIBITOR | IC50 | 9.28 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Bile acid receptor | Nuclear hormone receptor | IC50 | 8.92 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 865UEK4EJC | UNII |
| C3659266 | UMLSCUI |
| CHEBI:755066 | CHEBI |
| CHEMBL3039515 | ChEMBL_ID |
| 9939892 | PUBCHEM_CID |
| DB12486 | DRUGBANK_ID |
| D10795 | KEGG_DRUG |
| 9414 | INN_ID |
| C581303 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9996 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
None