Anti-inhibitor coagulant complex

Identification

Name
Anti-inhibitor coagulant complex
Accession Number
DB13151
Description

Anti-inhibitor coagulant complex, also known as FEIBA (factor eight inhibitor bypassing activity), contains several proteins involved in the prothrombinase complex. It is used to control bleeding in hemophilia A and B patients with inhibitors.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Blood factors
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • Activated prothrombin complex concentrate
  • Antiinhibitor coagulant complex
  • Factor VIII bypassing fraction
  • Factor VIII inhibitor bypassing activity
  • Factor VIII inhibitor bypassing fraction

Pharmacology

Pharmacology
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Indication

For use in the control of bleeding episodes, perioperative management, and routine prophylaxis against bleeding episodes in hemophilia A and B patients with inhibitors Label. It is not indicated in the absence of factor VIII or IX inhibitors.

Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
Contraindications & Blackbox Warnings
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Pharmacodynamics

FEIBA contains several clotting factors which act at various points in the caogulation cascade to promote thrombosis 1.

Mechanism of action

Factor VIIa present in FEIBA forms a complex with tissue factor and calcium which converts endogenous and FEIBA contained factor X to Xa 1 2. Endogenous and FEIBA contained factor Xa act as parrt of the prothrombinase complex to convert endogenous and FEIBA contained prothrombin to thrombin. Endogenous and FEIBA contained thrombin then cleave fibrinogen to insulouble fibrin and activate factor XIII which covalently cross-links fibrin to form a polymer mesh. FEIBA also contains factor IX and IXa which act as part of the tenase complex to convert factor X to Xa. Thrombin activates factor V, VII, and VIII as part of the amplification phase of the clotting cascade. These events promote the formation of blood clots to prevent or stop bleeding.

TargetActionsOrganism
ACoagulation factor X
agonist
Humans
AProthrombin
agonist
Humans
AFibrinogen alpha chain
cleavage
Humans
AFibrinogen beta chain
cleavage
Humans
ACoagulation factor XIII A chain
agonist
Humans
ACoagulation factor V
agonist
Humans
ACoagulation factor VIII
agonist
Humans
ACoagulation factor VII
agonist
Humans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life

Plasma half lives of included clotting factors are as follows 2: Prothrombin - 65h Factor VII - 5h Factor IX - 25h Factor X - 40h

Clearance
Not Available
Adverse Effects
Medicalerrors
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Toxicity

FEIBA is associated with increased risk of thromboembolic events such as stroke, myocardial infarction, and deep vein thrombosis Label.

Affected organisms
  • Humans and other mammals
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 therapeutic efficacy of Anti-inhibitor coagulant complex can be decreased when used in combination with Abciximab.
AcenocoumarolThe therapeutic efficacy of Anti-inhibitor coagulant complex can be decreased when used in combination with Acenocoumarol.
Acetylsalicylic acidThe therapeutic efficacy of Anti-inhibitor coagulant complex can be decreased when used in combination with Acetylsalicylic acid.
Alpha-1-proteinase inhibitorAlpha-1-proteinase inhibitor may increase the thrombogenic activities of Anti-inhibitor coagulant complex.
AlteplaseThe therapeutic efficacy of Anti-inhibitor coagulant complex can be decreased when used in combination with Alteplase.
Aminocaproic acidThe risk or severity of adverse effects can be increased when Aminocaproic acid is combined with Anti-inhibitor coagulant complex.
AncrodThe therapeutic efficacy of Anti-inhibitor coagulant complex can be decreased when used in combination with Ancrod.
AnistreplaseThe therapeutic efficacy of Anti-inhibitor coagulant complex can be decreased when used in combination with Anistreplase.
Antithrombin AlfaThe therapeutic efficacy of Anti-inhibitor coagulant complex can be decreased when used in combination with Antithrombin Alfa.
Antithrombin III humanThe therapeutic efficacy of Anti-inhibitor coagulant complex can be decreased when used in combination with Antithrombin III human.
Interactions
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Food Interactions
Not Available

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Feiba2500 [USP'U]/50mLIntravenousBaxalta Incorporated1986-01-31Not applicableUS flag
FeibaKit500 [USP'U]/20mLIntravenousBaxalta Incorporated1986-01-31Not applicableUS flag
Feiba1000 [USP'U]/20mLIntravenousBaxalta Incorporated1986-01-31Not applicableUS flag
Feiba500 [USP'U]/10mLIntravenousBaxalta Incorporated1986-01-31Not applicableUS flag
Feiba NfKit500 [USP'U]/20mLIntravenousBaxalta Incorporated1986-01-312017-09-30US flag
Feiba NfKit; Powder, for solution650 unitIntravenousTakedaNot applicableNot applicableCanada flag
Feiba NfKit; Powder, for solution1300 unitIntravenousTakeda1997-10-27Not applicableCanada flag
Feiba NfKit2500 [USP'U]/50mLIntravenousBaxalta Incorporated1986-01-312017-11-30US flag
Feiba NfKit; Powder, for solution3250 unitIntravenousTakeda2011-04-04Not applicableCanada flag
Feiba NfKit1000 [USP'U]/20mLIntravenousBaxalta Incorporated1986-01-312017-11-30US flag

Categories

ATC Codes
B02BD03 — Factor viii inhibitor bypassing activity
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

Chemical Identifiers

UNII
CS849DUN3M
CAS number
Not Available

References

General References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
  2. Palta S, Saroa R, Palta A: Overview of the coagulation system. Indian J Anaesth. 2014 Sep;58(5):515-23. doi: 10.4103/0019-5049.144643. [PubMed:25535411]
PubChem Substance
347911435
RxNav
314504
AHFS Codes
  • 20:28.16 — Hemostatics
FDA label
Download (1.22 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentCongenital Hematological Disorder / Haemophilia A With Inhibitors / Haemophilia B With Inhibitors1
4CompletedTreatmentHemophilia A1
4CompletedTreatmentHereditary Factor VIII Deficiency Disease With Inhibitor1
4RecruitingTreatmentHemophilia A With Inhibitors1
3CompletedTreatmentHemophilia A1
3CompletedTreatmentHemophilia A / Hemophilia A or B With Inhibitors / Hemophilia B1
3Not Yet RecruitingTreatmentHemophilia A1
3RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19) / Hemophilia A or B With Inhibitors1
2, 3CompletedPreventionHemophilia A With Inhibitors1
1CompletedTreatmentCardiovascular Disease (CVD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, for solutionIntravenous50 U/mL
Injection, powder, for solutionIntravenous25 U/mL
Injection, powder, lyophilized, for solutionIntravenous1000 U
Injection, powder, for solutionParenteral25 E./ml
Injection, powder, for solutionParenteral50 E./ml
KitIntravenous1000 [USP'U]/20mL
KitIntravenous2500 [USP'U]/50mL
KitIntravenous500 [USP'U]/20mL
Kit; powder, for solutionIntravenous1300 unit
Kit; powder, for solutionIntravenous3250 unit
Kit; powder, for solutionIntravenous650 unit
Injection, powder, for solutionIntravenous
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Cleavage
General Function
Structural molecule activity
Specific Function
Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function ...
Gene Name
FGA
Uniprot ID
P02671
Uniprot Name
Fibrinogen alpha chain
Molecular Weight
94972.455 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Cleavage
General Function
Structural molecule activity
Specific Function
Cleaved by the protease thrombin to yield monomers which, together with fibrinogen alpha (FGA) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function...
Gene Name
FGB
Uniprot ID
P02675
Uniprot Name
Fibrinogen beta chain
Molecular Weight
55927.9 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Protein-glutamine gamma-glutamyltransferase activity
Specific Function
Factor XIII is activated by thrombin and calcium ion to a transglutaminase that catalyzes the formation of gamma-glutamyl-epsilon-lysine cross-links between fibrin chains, thus stabilizing the fibr...
Gene Name
F13A1
Uniprot ID
P00488
Uniprot Name
Coagulation factor XIII A chain
Molecular Weight
83266.805 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Copper ion binding
Specific Function
Central regulator of hemostasis. It serves as a critical cofactor for the prothrombinase activity of factor Xa that results in the activation of prothrombin to thrombin.
Gene Name
F5
Uniprot ID
P12259
Uniprot Name
Coagulation factor V
Molecular Weight
251701.245 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Oxidoreductase activity
Specific Function
Factor VIII, along with calcium and phospholipid, acts as a cofactor for factor IXa when it converts factor X to the activated form, factor Xa.
Gene Name
F8
Uniprot ID
P00451
Uniprot Name
Coagulation factor VIII
Molecular Weight
267007.42 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Serine-type peptidase activity
Specific Function
Initiates the extrinsic pathway of blood coagulation. Serine protease that circulates in the blood in a zymogen form. Factor VII is converted to factor VIIa by factor Xa, factor XIIa, factor IXa, o...
Gene Name
F7
Uniprot ID
P08709
Uniprot Name
Coagulation factor VII
Molecular Weight
51593.465 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Substrate
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
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Substrate
General Function
Serine-type peptidase activity
Specific Function
Initiates the extrinsic pathway of blood coagulation. Serine protease that circulates in the blood in a zymogen form. Factor VII is converted to factor VIIa by factor Xa, factor XIIa, factor IXa, o...
Gene Name
F7
Uniprot ID
P08709
Uniprot Name
Coagulation factor VII
Molecular Weight
51593.465 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Substrate
General Function
Oxidoreductase activity
Specific Function
Factor VIII, along with calcium and phospholipid, acts as a cofactor for factor IXa when it converts factor X to the activated form, factor Xa.
Gene Name
F8
Uniprot ID
P00451
Uniprot Name
Coagulation factor VIII
Molecular Weight
267007.42 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Substrate
General Function
Serine-type endopeptidase activity
Specific Function
Factor IX is a vitamin K-dependent plasma protein that participates in the intrinsic pathway of blood coagulation by converting factor X to its active form in the presence of Ca(2+) ions, phospholi...
Gene Name
F9
Uniprot ID
P00740
Uniprot Name
Coagulation factor IX
Molecular Weight
51778.11 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Substrate
General Function
Copper ion binding
Specific Function
Central regulator of hemostasis. It serves as a critical cofactor for the prothrombinase activity of factor Xa that results in the activation of prothrombin to thrombin.
Gene Name
F5
Uniprot ID
P12259
Uniprot Name
Coagulation factor V
Molecular Weight
251701.245 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [PubMed:15385040]

Drug created on November 18, 2016 21:27 / Updated on February 24, 2021 19:34