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oxatomide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2014 | 60607-34-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
orally active H1-histamine receptor antagonist used to treat chronic urticaria and allergic rhinitis
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 60 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.04 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.93 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 41 | |||
| kinase-selectivity-class | AXL,GRK2,SIK2 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1981 | YEAR INTRODUCED |
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 |
|---|---|---|
| ATC | R06AE06 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Piperazine derivatives |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D018926 | Anti-Allergic Agents |
| MeSH PA | D018927 | Anti-Asthmatic Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| CHEBI has role | CHEBI:37955 | H<small><sub>1</sub></small>-receptor antagonist |
| CHEBI has role | CHEBI:48279 | serotonergic antagonist |
| CHEBI has role | CHEBI:50857 | anti-allergic agent |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
| CHEBI has role | CHEBI:176497 | geroprotector |
Related Drugs by ATC class:
R06AE Piperazine derivatives 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.04 | acidic |
| pKa2 | 7.15 | Basic |
| pKa3 | 3.15 | 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 | 7.70 | WOMBAT-PK | SCIENTIFIC LITERATURE | |||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 8.15 | WOMBAT-PK | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.20 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 8.06 | WOMBAT-PK | |||||
| P2X purinoceptor 7 | Ion channel | IC50 | 6.08 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 6.13 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | IC50 | 8.05 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01773 | KEGG_DRUG |
| C0134337 | UMLSCUI |
| CHEBI:31943 | CHEBI |
| CHEMBL13828 | ChEMBL_ID |
| DB12877 | DRUGBANK_ID |
| C015408 | MESH_SUPPLEMENTAL_RECORD_UI |
| 4615 | PUBCHEM_CID |
| 4329 | INN_ID |
| J31IL9Z2EE | UNII |
| 54236 | RXNORM |
| 004013 | NDDF |
| 320759006 | SNOMEDCT_US |
| 419369005 | SNOMEDCT_US |
| J31IL9Z2EE | INXIGHT DRUGS |
Pharmaceutical products:
None