betrixaban 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| blood coagulation factor XA inhibitors, antithrombotics | 5241 | 330942-05-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Betrixaban is an oral FXa inhibitor that selectively blocks the active site of FXa and does not require a cofactor (such as Anti-thrombin III) for activity. Betrixaban inhibits free FXa and prothrombinase activity. By directly inhibiting FXa, betrixaban decreases thrombin generation. Betrixaban has no direct effect on platelet aggregation.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 1 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 |
|---|---|---|---|
| June 23, 2017 | FDA | PORTOLA PHARMA INC |
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 | B01AF04 | BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Direct factor Xa inhibitors |
| MeSH PA | D000925 | Anticoagulants |
| MeSH PA | D000991 | Antithrombins |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D065427 | Factor Xa Inhibitors |
| MeSH PA | D006401 | Hematologic Agents |
| MeSH PA | D011480 | Protease Inhibitors |
| MeSH PA | D015842 | Serine Proteinase Inhibitors |
| FDA MoA | N0000175635 | Factor Xa Inhibitors |
| FDA EPC | N0000175637 | Factor Xa Inhibitor |
| CHEBI has role | CHEBI:50249 | anticoagulants |
| CHEBI has role | CHEBI:68581 | factor Xa inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| At risk of venous thromboembolus | indication | 427631000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.67 | acidic |
| pKa2 | 13.8 | acidic |
| pKa3 | 10.18 | Basic |
| pKa4 | 1.61 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 40MG | BEVYXXA | PORTOLA PHARMS INC | N208383 | June 23, 2017 | DISCN | CAPSULE | ORAL | 9555023 | Nov. 7, 2026 | PROPHYLAXIS OF PULMONARY EMBOLISM |
| 80MG | BEVYXXA | PORTOLA PHARMS INC | N208383 | June 23, 2017 | DISCN | CAPSULE | ORAL | 9555023 | Nov. 7, 2026 | PROPHYLAXIS OF PULMONARY EMBOLISM |
| 40MG | BEVYXXA | PORTOLA PHARMS INC | N208383 | June 23, 2017 | DISCN | CAPSULE | ORAL | 8557852 | Sept. 8, 2028 | PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT) |
| 40MG | BEVYXXA | PORTOLA PHARMS INC | N208383 | June 23, 2017 | DISCN | CAPSULE | ORAL | 8557852 | Sept. 8, 2028 | PROPHYLAXIS OF VENOUS THROMBOSIS |
| 80MG | BEVYXXA | PORTOLA PHARMS INC | N208383 | June 23, 2017 | DISCN | CAPSULE | ORAL | 8557852 | Sept. 8, 2028 | PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT) |
| 80MG | BEVYXXA | PORTOLA PHARMS INC | N208383 | June 23, 2017 | DISCN | CAPSULE | ORAL | 8557852 | Sept. 8, 2028 | PROPHYLAXIS OF VENOUS THROMBOSIS |
| 40MG | BEVYXXA | PORTOLA PHARMS INC | N208383 | June 23, 2017 | DISCN | CAPSULE | ORAL | 8404724 | March 29, 2031 | INHIBITING COAGULATION |
| 80MG | BEVYXXA | PORTOLA PHARMS INC | N208383 | June 23, 2017 | DISCN | CAPSULE | ORAL | 8404724 | March 29, 2031 | INHIBITING COAGULATION |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Coagulation factor X | Enzyme | INHIBITOR | IC50 | 8.82 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | Ki | 5.75 | CHEMBL | |||||
| Prothrombin | Enzyme | IC50 | 4.75 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 74RWP7W0J9 | UNII |
| 936539-80-9 | SECONDARY_CAS_RN |
| 4036878 | VANDF |
| C2698385 | UMLSCUI |
| CHEBI:140421 | CHEBI |
| CHEMBL512351 | ChEMBL_ID |
| 10275777 | PUBCHEM_CID |
| DB12364 | DRUGBANK_ID |
| D08873 | KEGG_DRUG |
| 8950 | INN_ID |
| 9602 | IUPHAR_LIGAND_ID |
| 258885 | MMSL |
| 32842 | MMSL |
| d08605 | MMSL |
| 017262 | NDDF |
| 017304 | NDDF |
| 735227003 | SNOMEDCT_US |
| 763702003 | SNOMEDCT_US |
| 1927851 | RXNORM |
| C543086 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
None