betrixaban Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
blood coagulation factor XA inhibitors, antithrombotics 5241 330942-05-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • betrixaban
  • PRT054021
  • betrixaban maleate
  • bevyxxa
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.
  • Molecular weight: 451.91
  • Formula: C23H22ClN5O3
  • CLOGP: 3.61
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 3
  • TPSA: 107.41
  • ALOGS: -4.44
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 23, 2017 FDA PORTOLA PHARMA INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AF04 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Direct factor Xa inhibitors
FDA EPC N0000175637 Factor Xa Inhibitor
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
CHEBI has role CHEBI:50249 anticoagulant

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
At risk of venous thromboembolus indication 427631000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 6376515 Sept. 15, 2020 PREVENTING CONDITION CHARACTERIZED BY UNDESIRED THROMBOSIS
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 6376515 Sept. 15, 2020 PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT)
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 6376515 Sept. 15, 2020 PROPHYLAXIS OF PULMONARY EMBOLISM
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 6376515 Sept. 15, 2020 PROPHYLAXIS OF VENOUS THROMBOSIS
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8691847 Sept. 15, 2020 PREVENTING CONDITION CHARACTERIZED BY UNDESIRED THROMBOSIS
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8691847 Sept. 15, 2020 PROPHYLAXIS OF VENOUS THROMBOEMBOLISM
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9629831 Sept. 15, 2020 PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT)
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9629831 Sept. 15, 2020 PROPHYLAXIS OF PULMONARY EMBOLISM
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9629831 Sept. 15, 2020 PROPHYLAXIS OF VENOUS THROMBOEMBOLISM
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9629831 Sept. 15, 2020 PROPHYLAXIS OF VENOUS THROMBOSIS
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 6376515 Sept. 15, 2020 PREVENTING CONDITION CHARACTERIZED BY UNDESIRED THROMBOSIS
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 6376515 Sept. 15, 2020 PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT)
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 6376515 Sept. 15, 2020 PROPHYLAXIS OF PULMONARY EMBOLISM
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 6376515 Sept. 15, 2020 PROPHYLAXIS OF VENOUS THROMBOSIS
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8691847 Sept. 15, 2020 PREVENTING CONDITION CHARACTERIZED BY UNDESIRED THROMBOSIS
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8691847 Sept. 15, 2020 PROPHYLAXIS OF VENOUS THROMBOEMBOLISM
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9629831 Sept. 15, 2020 PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT)
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9629831 Sept. 15, 2020 PROPHYLAXIS OF PULMONARY EMBOLISM
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9629831 Sept. 15, 2020 PROPHYLAXIS OF VENOUS THROMBOEMBOLISM
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9629831 Sept. 15, 2020 PROPHYLAXIS OF VENOUS THROMBOSIS
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9555023 Nov. 7, 2026 PROPHYLAXIS OF PULMONARY EMBOLISM
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 9555023 Nov. 7, 2026 PROPHYLAXIS OF PULMONARY EMBOLISM
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8557852 Sept. 8, 2028 PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT)
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8557852 Sept. 8, 2028 PROPHYLAXIS OF VENOUS THROMBOSIS
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8557852 Sept. 8, 2028 PROPHYLAXIS OF DEEP VEIN THROMBOSIS (DVT)
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8557852 Sept. 8, 2028 PROPHYLAXIS OF VENOUS THROMBOSIS
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8404724 March 29, 2031 INHIBITING COAGULATION
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL 8404724 March 29, 2031 INHIBITING COAGULATION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
40MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL June 23, 2022 NEW CHEMICAL ENTITY
80MG BEVYXXA PORTOLA PHARMS INC N208383 June 23, 2017 RX CAPSULE ORAL June 23, 2022 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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

External reference:

IDSource
28Z3021TMU UNII
936539-80-9 SECONDARY_CAS_RN
8950 INN_ID
763702003 SNOMEDCT_US
1927851 RXNORM
32842 MMSL
d08605 MMSL
017262 NDDF
4036878 VANDF
735227003 SNOMEDCT_US
CHEMBL512351 ChEMBL_ID
D08873 KEGG_DRUG
CHEBI:140421 CHEBI
9602 IUPHAR_LIGAND_ID
DB12364 DRUGBANK_ID
10275777 PUBCHEM_CID
C543086 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BEVYXXA HUMAN PRESCRIPTION DRUG LABEL 1 69853-0201 CAPSULE, GELATIN COATED 80 mg ORAL NDA 19 sections
BEVYXXA HUMAN PRESCRIPTION DRUG LABEL 1 69853-0202 CAPSULE, GELATIN COATED 40 mg ORAL NDA 19 sections