Antithrombin Alfa

Identification

Summary

Antithrombin Alfa is a recombinant antithrombin used to treat peri-operative and peripartum thromboembolic events in hereditary antithrombin deficiency.

Brand Names
Atryn
Generic Name
Antithrombin Alfa
DrugBank Accession Number
DB11166
Background

Antithrombin Alfa is a recombinant antithrombin , an anticoagulant, that is used for the prevention of thromboembolic events in patients that have hereditary deficiency of antithrombin in high risk situations.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Thrombolytic agents
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • Antithrombin (recombinant)
  • Antithrombin Alfa
  • Antithrombin III, recombinant
  • Antithrombin III,recombinant
External IDs
  • KW-3357

Pharmacology

Indication

Antithrombin alfa is a recombinant antithrombin it is indicated for the prevention of peri-operative and peri-partum thromboembolic events in patients with hereditary deficiency of antithrombin.

Pharmacology
Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
Pharmacodynamics

Hereditary antithrombin deficiency causes an increased risk of venous thromboembolism (VTE). In high risk situations, such as surgery or trauma or for pregnant women during the peri-partum period, the risk of development of VTEs is 10-50 times greater than the general population. In hereditary antithrombin deficient patients antithrombin alfa normalizes plasma antthrombin activity levels during peri-operative and peri-partum periods.

Mechanism of action

Antithrombin is the main inhibitor of thrombin and Factor Xa , the serine proteases involved in blood coagulation. Antithrombin neutralizes the activity of thrombin and Factor Xa by forming a complex which is rapidly removed from the circulation.

TargetActionsOrganism
AProthrombin
inhibitor
Humans
ACoagulation factor X
inhibitor
Humans
Absorption

Given IV so not absorbed.

Volume of distribution

Dose of: 50IU/kg: 126.2 ml/kg 100IU/kg: 156.1 ml/kg Vd in hereditary deficient pregnant women in high risk situations had increased Vd of 14.3L.

Protein binding

Binds and inhibits thrombin and factor Xa.

Metabolism

Not metabolized.

Route of elimination

Irreversible complexes formed between antithrombin III and its target protease are rapidly removed by the liver.

Half-life

Dose of: 50IU/kg: 11.6 h 100IU/kg: 17.7 h

Clearance

Dose of: 50IU/kg: 9.6 ml/hr/kg 100IU/kg: 7.2 ml/hr/kg Cl in hereditary deficient pregnant women in high risk situations had increased Cl of 1.38L/h.

Adverse Effects
Adverseeffects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
Toxicity

Highest dose tested was 360mg/kg/day in rats resulted in transient limb swelling.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Antithrombin Alfa.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Antithrombin Alfa.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Antithrombin Alfa is combined with Acemetacin.
AcenocoumarolThe risk or severity of bleeding can be increased when Acenocoumarol is combined with Antithrombin Alfa.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Antithrombin Alfa.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Antithrombin Alfa.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Antithrombin Alfa.
AldesleukinThe risk or severity of bleeding can be increased when Antithrombin Alfa is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Antithrombin Alfa is combined with Alemtuzumab.
AlteplaseThe risk or severity of bleeding can be increased when Alteplase is combined with Antithrombin Alfa.
Interactions
Identify potential medication risks
Easily compare up to 40 drugs with our drug interaction checker.
Get severity rating, description, and management advice.
Learn more
Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Products

Products2
Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ATrynInjection, powder, lyophilized, for solution1750 [iU]/1mLIntravenousrEVO Biologics, Inc.2009-05-06Not applicableUS flag
ATrynInjection, powder, lyophilized, for solution525 [iU]/1mLIntravenousrEVO Biologics, Inc.2009-05-06Not applicableUS flag
AtrynInjection, powder, for solution1750 IUIntravenousLaboratoire Francais Du Fractionnement Et Des Biotechnologies2016-09-082019-07-02EU flag
AtrynInjection, powder, for solution1750 IUIntravenousLaboratoire Francais Du Fractionnement Et Des Biotechnologies2016-09-082019-07-02EU flag
AtrynInjection, powder, lyophilized, for solution1750 [iU]/10mLIntravenousLundbeck Inc.2009-02-06Not applicableUS flag
AtrynInjection, powder, for solution1750 IUIntravenousLaboratoire Francais Du Fractionnement Et Des Biotechnologies2016-09-082019-07-02EU flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
AWV6I5L6H2
CAS number
84720-88-7

References

General References
  1. Patnaik MM, Moll S: Inherited antithrombin deficiency: a review. Haemophilia. 2008 Nov;14(6):1229-39. doi: 10.1111/j.1365-2516.2008.01830.x. [Article]
  2. ATryn monograph [Link]
PubChem Substance
347911141
RxNav
1427179

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4TerminatedTreatmentThrombophilia Due to Acquired Antithrombin III Deficiency1
4WithdrawnTreatmentNeonates on ECMO1
3CompletedPreventionCongenital Antithrombin Deficiency1
3CompletedPreventionHereditary antithrombin III deficiency1
3CompletedTreatmentDisseminated Intravascular Coagulation (DIC)2
3CompletedTreatmentProphylaxis of preeclampsia1
3RecruitingTreatmentProphylaxis of preeclampsia1
3TerminatedTreatmentDisseminated Intravascular Coagulation (DIC)1
2TerminatedTreatmentDisseminated Intravascular Coagulation (DIC)1
1CompletedNot AvailableCongenital Antithrombin Deficiency1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, for solutionIntravenous1750 IU
Injection, powder, lyophilized, for solutionIntravenous1750 [iU]/10mL
Injection, powder, lyophilized, for solutionIntravenous1750 [iU]/1mL
Injection, powder, lyophilized, for solutionIntravenous525 [iU]/1mL
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available

Targets

Drugtargets2
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Thrombospondin receptor activity
Specific Function
Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostas...
Gene Name
F2
Uniprot ID
P00734
Uniprot Name
Prothrombin
Molecular Weight
70036.295 Da
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serine-type endopeptidase activity
Specific Function
Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
Gene Name
F10
Uniprot ID
P00742
Uniprot Name
Coagulation factor X
Molecular Weight
54731.255 Da

Drug created on December 03, 2015 16:51 / Updated on February 21, 2021 18:52