Antithrombin III human

Identification

Summary

Antithrombin III human is an alpha-2-glycoprotein used to prevent thromboembolisms in patients with hereditary antithrombin III deficiency.

Brand Names
Thrombate III
Generic Name
Antithrombin III human
DrugBank Accession Number
DB11598
Background

A plasma alpha 2 glycoprotein that accounts for the major antithrombin activity of normal plasma and also inhibits several other enzymes. It is a member of the serpin superfamily.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Thrombolytic agents
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • Antithrombin III
  • Antithrombin III (human)
  • Antithrombin III human
  • Antithrombin III human plasma-derived
  • Antithrombin III, human
  • Antithrombin III,human
  • Antitrombina III
  • AT-III
  • Heparin cofactor B
External IDs
  • ORG 10849

Pharmacology

Indication

Antithrombin III human is a human antithrombin (AT) indicated in patients with hereditary antithrombin deficiency for the treatment and prevention of thromboembolism and prevention of peri-operative and peri-partum thromboembolism

Pharmacology
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Drug Discovery
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Hereditary AT deficiency causes an increased risk of venous thromboembolism (VTE). During high-risk situations such as surgery or trauma or for pregnant women, during the peri-partum period, the risk of development of VTEs as compared to the normal population in these situations is increased by a factor 10 to 50. In hereditary antithrombin deficient patients ATryn restores (normalize) plasma AT activity levels during peri-operative and peri-partum periods.

Mechanism of action

Antithrombin, an alpha2-glycoprotein of molecular weight 58,000, is normally present in human plasma at a concentration of approximately 12.5 mg/dL and is the major plasma inhibitor of thrombin. Inactivation of thrombin by AT occurs by formation of a covalent bond resulting in an inactive 1:1 stoichiometric complex between the two, involving an interaction of the active serine of thrombin and an arginine reactive site on AT. AT is also capable of inactivating other components of the coagulation cascade including factors IXa, Xa, XIa, and XIIa, as well as plasmin. The neutralization rate of serine proteases by AT proceeds slowly in the absence of heparin, but is greatly accelerated in the presence of heparin. As the therapeutic antithrombotic effect of heparin is mediated by AT, heparin in vivo is ineffective in the absence or near absence of AT. After administration, Antithrombin III human temporarily replaces the missing AT in patients with hereditary antithrombin deficiency.

TargetActionsOrganism
UAntithrombin-III
agonist
Humans
Absorption

Therapeutic target plasma concentrations in patients with congenital antithrombin III deficiency range from 80–120% of values in healthy adults. At plasma concentrations ≤70% of normal, increased thrombin generation. Supraphysiologic plasma concentrations (e.g., 150–200% of normal) have increased bleeding risk in patients with sepsis and disseminated intravascular coagulation, not known whether supraphysiologic concentrations increase bleeding risk in patients with congenital antithrombin III deficiency.

Volume of distribution

Distributed into plasma (39%), extravascular space (49%), and vascular endothelial cells (11%).

Protein binding

Not Available

Metabolism

<5% metabolized to low molecular weight breakdown products.

Route of elimination

Complexes of antithrombin III with thrombin or other proteinases cleared principally by liver and excreted in urine.

Half-life

2.5 - 3.8 hs

Clearance

Not Available

Adverse Effects
Medicalerrors
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Toxicity

Not Available

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
AbacavirAbacavir may decrease the excretion rate of Antithrombin III human which could result in a higher serum level.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Antithrombin III human.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Antithrombin III human.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Antithrombin III human.
AcenocoumarolThe risk or severity of bleeding can be increased when Acenocoumarol is combined with Antithrombin III human.
AcetaminophenAcetaminophen may decrease the excretion rate of Antithrombin III human which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Antithrombin III human which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Antithrombin III human.
AclidiniumAclidinium may decrease the excretion rate of Antithrombin III human which could result in a higher serum level.
AcrivastineAcrivastine may decrease the excretion rate of Antithrombin III human which could result in a higher serum level.
Interactions
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Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Antithrombin III NFKit; Powder, for solutionIntravenousBaxalta Canada Corporation1999-07-05Not applicableCanada flag
Antithrombin III NFKit; Powder, for solutionIntravenousBaxalta Canada Corporation1999-07-05Not applicableCanada flag
Thrombate IIIPowder, for solution500 unit / vialIntravenousGrifols Therapeutics LlcNot applicableNot applicableCanada flag
Thrombate IIIKit50 [iU]/1mLIntravenousGRIFOLS USA, LLC1991-12-30Not applicableUS flag
Thrombate IIIKit50 [iU]/1mLIntravenousGRIFOLS USA, LLC1991-12-302017-06-22US flag
Thrombate IIIPowder, for solution1000 unit / vialIntravenousGrifols Therapeutics Llc1996-11-11Not applicableCanada flag
Thrombate IIIKit50 [iU]/1mLIntravenousGRIFOLS USA, LLC1991-12-30Not applicableUS flag
Thrombate III Pws IV 1000iu/vialPowder, for solution1000 unit / vialIntravenousMiles Inc. Pharmaceutical Division1995-12-311998-09-25Canada flag
Thrombate III Pws IV 500iu/vialPowder, for solution500 unit / vialIntravenousMiles Inc. Pharmaceutical Division1995-12-311998-09-25Canada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Antithrombin III ImmunoAntithrombin III human (1650 unit / kit) + Water (30 mL / kit)Powder, for solutionIntravenousBaxter Ag1999-07-052011-10-07Canada flag

Categories

ATC Codes
B01AB02 — Antithrombin iii
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
  • Humans and other mammals

Chemical Identifiers

UNII
T0LTO7L82X
CAS number
9000-94-6

References

General References
  1. Cavenagh JD, Colvin BT: Guidelines for the management of thrombophilia. Department of Haematology, The Royal London Hospital, Whitechapel, London, UK. Postgrad Med J. 1996 Feb;72(844):87-94. [Article]
  2. Menache D, Grossman BJ, Jackson CM: Antithrombin III: physiology, deficiency, and replacement therapy. Transfusion. 1992 Jul-Aug;32(6):580-8. [Article]
  3. Aibiki M, Fukuoka N, Nishiyama T, Maekawa S, Shirakawa Y: Differences in antithrombin III activities by administration method in critical patients with disseminated intravascular coagulation: a pharmacokinetic study. Shock. 2007 Aug;28(2):141-7. [Article]
  4. Collen D, Schetz J, de Cock F, Holmer E, Verstraete M: Metabolism of antithrombin III (heparin cofactor) in man: effects of venous thrombosis and of heparin administration. Eur J Clin Invest. 1977 Feb;7(1):27-35. [Article]
  5. FDA label [Link]
PubChem Substance
347911209
RxNav
221062

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Unknown StatusSupportive CareAcute Coronary Syndrome (ACS) / Aortic Valve Insufficiency / Mitral Valve Insufficiency / Mitral Valve Stenosis / Valve Stenoses, Aortic1
4WithdrawnSupportive CareHereditary antithrombin III deficiency1
3CompletedTreatmentCardiopulmonary Bypass1
3Not Yet RecruitingPreventionCongenital Antithrombin Deficiency1
2Active Not RecruitingTreatmentVeno Occlusive Disease, Hepatic1
2CompletedPreventionAcquired Antithrombin III Deficiency / Coronary Artery Bypass Grafting (CABG)1
2CompletedTreatmentATIII Deficiency1
2CompletedTreatmentCardiopulmonary Bypass / Surgery, Cardiac1
2CompletedTreatmentReperfusion Injury1
2RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19) / Hereditary antithrombin III deficiency1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous
Injection, powder, for solutionParenteral
Powder, for solutionIntravenous
Kit; powder, for solutionIntravenous
Powder, for solution
Powder, for solutionParenteral
Injection, powder, lyophilized, for solutionIntravenous1000 IU
Injection, powder, lyophilized, for solutionIntravenous500 IU
Powder, for solutionIntravenous
Injection, powder, for solutionIntravenous
Injection, powder, for solution
KitIntravenous50 [iU]/1mL
Powder, for solutionIntravenous1000 unit / vial
Powder, for solutionIntravenous500 unit / vial
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serine-type endopeptidase inhibitor activity
Specific Function
Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade. AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa. Its inhibitory a...
Gene Name
SERPINC1
Uniprot ID
P01008
Uniprot Name
Antithrombin-III
Molecular Weight
52601.935 Da
References
  1. Menache D, Grossman BJ, Jackson CM: Antithrombin III: physiology, deficiency, and replacement therapy. Transfusion. 1992 Jul-Aug;32(6):580-8. [Article]

Drug created on May 20, 2016 20:36 / Updated on July 24, 2021 14:57