andexanet alfa 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
5336 1262449-58-0

Description:

MoleculeDescription

Synonyms:

  • andexanet alfa
  • ondexxya
  • PRT064445
  • PRT-064445
  • PRT-44545
  • PRT-4445
  • AndexXa
  • AnXa
  • IndexXa
  • andexanet alfa (genetical recombination)
Andexanet alfa is a recombinant form of human FXa protein that has been modified to lack FXa enzymatic activity. The active site serine was substituted with alanine, rendering the molecule unable to cleave and activate prothrombin, and the gamma-carboxyglutamic acid (Gla) domain was removed to eliminate the ability of the protein to assemble into the prothrombinase complex, thus removing any anti-coagulant effects. Andexanet alfa is a specific reversal agent for FXa inhibitors. The predominant mechanism of action is the binding and sequestration of the FXa inhibitor, although there may be a minor contribution from the inhibition of tissue factor pathway inhibitor (TFPI) activity through binding to TFPI. The interaction between andexanet alfa and TFPI has not been fully characterized. Andexanet alfa binds direct FXa inhibitors with high affinity, making them unavailable to exert their anticoagulant effects
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
April 26, 2019 EMA Portola Netherlands BV
May 3, 2018 FDA Portola Pharamceuticals US
March 28, 2022 PMDA Alexion Pharma G.K.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cerebral infarction 352.43 105.91 67 404 26529 90601447
Heparin resistance 180.61 105.91 18 453 39 90627937

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cerebral infarction 242.88 80.64 62 594 31107 42589572
Heparin resistance 214.45 80.64 26 630 140 42620539

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cerebral infarction 580.63 80.44 129 1064 51709 110536397
Heparin resistance 370.42 80.44 43 1150 228 110587878
Ischaemic stroke 84.58 80.44 27 1166 41236 110546870

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V03AB38 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Antidotes

Related Drugs by ATC class:

V03AB Antidotes 28 drugs
4-dimethylaminophenolacetylcysteineamyl nitriteatropinecopper sulfatedimercaprolethanolflumazenilfomepizoleglutathionehydroxocobalaminidarucizumab show all 28 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Direct acting anticoagulant adverse reaction indication 293332005




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
BI009E452R UNII
C4079904 UMLSCUI
CHEBI:755267 CHEBI
CHEMBL3301583 ChEMBL_ID
DB14562 DRUGBANK_ID
D11029 KEGG_DRUG
9883 INN_ID
C580915 MESH_SUPPLEMENTAL_RECORD_UI
7576 IUPHAR_LIGAND_ID
783678000 SNOMEDCT_US
783691004 SNOMEDCT_US
281836 MMSL
2045114 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ANDEXXA HUMAN PRESCRIPTION DRUG LABEL 1 0310-3200 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 200 mg INTRAVENOUS BLA 27 sections