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tamibarotene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| arotinoid derivatives | 3580 | 94497-51-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
has retinoid-binding activity
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.089 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.503 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 63.533 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.133 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.980 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 4.060 | % | High | 1 |
| herg | hERG pIC50 | 4.814 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 13.521 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 15.488 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.390 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,CAMK2D,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IKBKB,ITK,JAK1,JAK2,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MARK4,PDK1,PDK2,PDK4,PIK3CB,PRKCD,PRKDC,SIK2,STK33,SYK,TEK,TTK | 40 | |||
| kinase-selectivity-class | BRAF,DDR1,EIF2AK3,EPHB4,GRK2,NTRK3,PDK4,TTK | 8 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 3.516 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 5.916 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 18.793 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.360 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 23.227 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.180 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.041 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 8.110 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 26.550 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.450 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 776.247 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 11, 2005 | PMDA |
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:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50741 | retinoic acid receptor α/β agonist |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute promyelocytic leukemia, FAB M3 | indication | 110004001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.75 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Enzyme | IC50 | 4.97 | CHEMBL | |||||
| Retinoic acid receptor alpha | Nuclear hormone receptor | IC50 | 7.11 | CHEMBL | |||||
| Retinoic acid receptor beta | Nuclear hormone receptor | AGONIST | EC50 | 6.63 | IUPHAR | ||||
| Retinoic acid receptor gamma | Nuclear hormone receptor | AGONIST | EC50 | 6.23 | IUPHAR | ||||
| Flavin reductase (NADPH) | Enzyme | Kd | 5.86 | CHEMBL | |||||
| Cytochrome P450 26A1 | Enzyme | IC50 | 4.88 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01418 | KEGG_DRUG |
| C1567753 | UMLSCUI |
| CHEBI:32181 | CHEBI |
| CHEMBL25202 | ChEMBL_ID |
| DB04942 | DRUGBANK_ID |
| C061133 | MESH_SUPPLEMENTAL_RECORD_UI |
| 108143 | PUBCHEM_CID |
| 2648 | IUPHAR_LIGAND_ID |
| 7349 | INN_ID |
| 08V52GZ3H9 | UNII |
| A80 | PDB_CHEM_ID |
| 08V52GZ3H9 | INXIGHT DRUGS |
Pharmaceutical products:
None