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betrixaban 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 |
| BA (Bioavailability) | 47 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.006 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 11.117 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 5.794 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.489 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 28.520 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 60.380 | % | High | 1 |
| herg | hERG pIC50 | 5.975 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 0.951 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.797 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 35.990 | % | High | 1 |
| kinase-safety-class | ACVR2B,ALK,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IRAK1,ITK,JAK1,KIT,MAP3K1,MAP3K21,MAP4K1,MAPK10,MAPK7,MARK4,MELK,NTRK3,PDK1,PDK2,PDK4,PRKCD,PRKDC,SIK2,SIK3,STK33,TTK | 38 | |||
| kinase-selectivity-class | PDK4,TTK | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 19.454 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 4.315 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 13.460 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 35.563 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 55.280 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.462 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 42.290 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 20.080 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 603.949 | uM | High | 1 |
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 | D006401 | Hematologic Agents |
| MeSH PA | D011480 | Protease Inhibitors |
| MeSH PA | D015842 | Serine Proteinase Inhibitors |
| MeSH PA | D065427 | Factor Xa Inhibitors |
| FDA MoA | N0000175635 | Factor Xa Inhibitors |
| FDA EPC | N0000175637 | Factor Xa Inhibitor |
| CHEBI has role | CHEBI:38070 | anti-arrhythmia drug |
| CHEBI has role | CHEBI:50249 | anticoagulant |
| CHEBI has role | CHEBI:68581 | EC 3.4.21.6 (coagulation factor Xa) inhibitor |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Related Drugs by ATC class:
B01AF Direct factor Xa inhibitors 4 drugs
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 |
| C543086 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9602 | IUPHAR_LIGAND_ID |
| 735227003 | SNOMEDCT_US |
| 763702003 | SNOMEDCT_US |
| 258885 | MMSL |
| 32842 | MMSL |
| d08605 | MMSL |
| 017262 | NDDF |
| 017304 | NDDF |
| 1927851 | RXNORM |
| 74RWP7W0J9 | INXIGHT DRUGS |
Pharmaceutical products:
None