Antithrombin Alfa

Identification

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Name
Antithrombin Alfa
Accession Number
DB11166
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Thrombolytic agents
Description

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.

Protein chemical formula
Not Available
Protein average weight
Not Available
Sequences
Not Available
Synonyms
  • Antithrombin (recombinant)
  • Antithrombin III, recombinant
  • Antithrombin III,recombinant
External IDs
KW-3357
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AtrynInjection, powder, for solution1750 IUIntravenousLaboratoire Francais Du Fractionnement Et Des Biotechnologies2006-07-28Not applicableEu
ATrynInjection, powder, lyophilized, for solution1750 [iU]/1IntravenousGtc Biotherapeutics, Inc.2009-05-06Not applicableUs
AtrynInjection, powder, lyophilized, for solution1750 [iU]/10mLIntravenousLundbeck Inc.2009-02-06Not applicableUs
AtrynInjection, powder, for solution1750 IUIntravenousLaboratoire Francais Du Fractionnement Et Des Biotechnologies2006-07-28Not applicableEu
AtrynInjection, powder, for solution1750 IUIntravenousLaboratoire Francais Du Fractionnement Et Des Biotechnologies2006-07-28Not applicableEu
ATrynInjection, powder, lyophilized, for solution525 [iU]/1mLIntravenousrEVO Bioloigics, Inc.2009-05-06Not applicableUs
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

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Categories
UNII
AWV6I5L6H2
CAS number
84720-88-7

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.

Associated Conditions
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
Additional Data Available
Adverse Effects

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Additional Data Available
Contraindications

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Blackbox Warnings

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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.

Toxicity

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

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(1,2,6,7-3H)TestosteroneThe therapeutic efficacy of Antithrombin Alfa can be increased when used in combination with (1,2,6,7-3H)Testosterone.
(R)-warfarinThe risk or severity of bleeding can be increased when (R)-warfarin is combined with Antithrombin Alfa.
(S)-WarfarinThe risk or severity of bleeding can be increased when (S)-Warfarin is combined with Antithrombin Alfa.
1-TestosteroneThe therapeutic efficacy of Antithrombin Alfa can be increased when used in combination with 1-Testosterone.
18-methyl-19-nortestosteroneThe therapeutic efficacy of Antithrombin Alfa can be increased when used in combination with 18-methyl-19-nortestosterone.
3,5-diiodothyropropionic acid3,5-diiodothyropropionic acid may increase the anticoagulant activities of Antithrombin Alfa.
4-hydroxycoumarinThe risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Antithrombin Alfa.
4-HydroxytestosteroneThe therapeutic efficacy of Antithrombin Alfa can be increased when used in combination with 4-Hydroxytestosterone.
5beta-dihydrotestosteroneThe therapeutic efficacy of Antithrombin Alfa can be increased when used in combination with 5beta-dihydrotestosterone.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Antithrombin Alfa.
Additional Data Available
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Food Interactions
Not Available

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. [PubMed:19141163]
  2. ATryn monograph [Link]
External Links
PubChem Substance
347911141

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableCongenital Antithrombin Deficiency1
1CompletedBasic ScienceAltered Heparin Response / Cardiopulmonary Bypass1
1TerminatedPreventionPostoperative Hemorrhages1
2TerminatedTreatmentDisseminated Intravascular Coagulation (DIC)1
3CompletedPreventionAntithrombin Deficiency, Congenital1
3CompletedTreatmentDisseminated Intravascular Coagulation (DIC)2
3CompletedTreatmentPreeclampsia1
3TerminatedTreatmentDisseminated Intravascular Coagulation (DIC)1
4TerminatedTreatmentThrombophilia Due to Acquired Antithrombin III Deficiency1
4WithdrawnTreatmentNeonates on ECMO1

Pharmacoeconomics

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

Properties

State
Not Available
Experimental Properties
Not Available

Taxonomy

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

Targets

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 09:51 / Updated on June 04, 2019 07:17