sitaxentan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| endothelin receptor antagonists | 3548 | 210421-74-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
endothelin A receptor antagonist
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.40 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 10, 2006 | EMA | Pfizer Ltd |
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 | C02KX03 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES OTHER ANTIHYPERTENSIVES Antihypertensives for pulmonary arterial hypertension |
| MeSH PA | D065128 | Endothelin Receptor Antagonists |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pulmonary arterial hypertension | indication | 11399002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.66 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Endothelin-1 receptor | GPCR | ANTAGONIST | Ki | 9.37 | CHEMBL | IUPHAR | |||
| Endothelin B receptor | GPCR | ANTAGONIST | IC50 | 5.01 | CHEMBL | ||||
| Endothelin-1 receptor | GPCR | ANTAGONIST | Ki | 9.37 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D07171 | KEGG_DRUG |
| CHEBI:135736 | CHEBI |
| CHEMBL282724 | ChEMBL_ID |
| CHEMBL2105740 | ChEMBL_ID |
| C106276 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7952 | INN_ID |
| DB06268 | DRUGBANK_ID |
| J9QH779MEM | UNII |
| 012019 | NDDF |
| 012042 | NDDF |
| 428709002 | SNOMEDCT_US |
| 428712004 | SNOMEDCT_US |
| 428790008 | SNOMEDCT_US |
| C1704271 | UMLSCUI |
| 216235 | PUBCHEM_CID |
| 184036-34-8 | SECONDARY_CAS_RN |
| 3950 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
None