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atosiban 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| oxytocin antagonists | 3008 | 90779-69-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Atosiban is a synthetic peptide which is a competitive antagonist of human oxytocin at receptor level. In human pre-term labour, atosiban at the recommended dosage antagonises uterine contractions and induces uterine quiescence.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 165 | mg | P |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.968 | Moderate | 0.66 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 20, 2000 | EMA | Ferring Pharmaceuticals A/S |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Premature delivery | 990.85 | 191.65 | 205 | 1306 | 38557 | 90588379 |
| Normal labour | 877.29 | 191.65 | 106 | 1405 | 511 | 90626425 |
| Delivery | 764.23 | 191.65 | 106 | 1405 | 1687 | 90625249 |
| Maternal exposure during pregnancy | 662.72 | 191.65 | 238 | 1273 | 359825 | 90267111 |
| Product use in unapproved indication | 349.03 | 191.65 | 148 | 1363 | 336088 | 90290848 |
| Premature baby | 259.76 | 191.65 | 64 | 1447 | 25013 | 90601923 |
| Foetal exposure during pregnancy | 203.10 | 191.65 | 59 | 1452 | 42916 | 90584020 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Premature delivery | 215.71 | 123.68 | 42 | 308 | 30590 | 110558359 |
| Maternal exposure during pregnancy | 182.47 | 123.68 | 55 | 295 | 254828 | 110334121 |
| Exposure during pregnancy | 158.37 | 123.68 | 45 | 305 | 167379 | 110421570 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G02CX01 | GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS OTHER GYNECOLOGICALS Other gynecologicals |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D012102 | Reproductive Control Agents |
| MeSH PA | D015149 | Tocolytic Agents |
Related Drugs by ATC class:
G02CX Other gynecologicals 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Prevention of Premature Labor | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.81 | acidic |
| pKa2 | 12.85 | acidic |
| pKa3 | 13.13 | acidic |
| pKa4 | 13.53 | acidic |
| pKa5 | 13.54 | acidic |
| pKa6 | 13.87 | acidic |
| pKa7 | 9.93 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Oxytocin receptor | GPCR | ANTAGONIST | Ki | 7.96 | CHEMBL | DRUG LABEL | |||
| Vasopressin V1a receptor | GPCR | Ki | 9.82 | CHEMBL | |||||
| Vasopressin V1b receptor | GPCR | Ki | 7.36 | CHEMBL | |||||
| Vasopressin V2 receptor | GPCR | Ki | 6.48 | CHEMBL | |||||
| Oxytocin receptor | GPCR | Ki | 7.40 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D03008 | KEGG_DRUG |
| 914453-95-5 | SECONDARY_CAS_RN |
| C0164398 | UMLSCUI |
| CHEBI:135899 | CHEBI |
| CHEMBL382301 | ChEMBL_ID |
| CHEMBL5315050 | ChEMBL_ID |
| DB09059 | DRUGBANK_ID |
| C047046 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2213 | IUPHAR_LIGAND_ID |
| 6392 | INN_ID |
| 081D12SI0Z | UNII |
| 5311010 | PUBCHEM_CID |
| 2680385 | RXNORM |
| 008327 | NDDF |
| 008328 | NDDF |
| 326166008 | SNOMEDCT_US |
| 391792002 | SNOMEDCT_US |
| 427147004 | SNOMEDCT_US |
| 081D12SI0Z | INXIGHT DRUGS |
Pharmaceutical products:
None