Anti-inhibitor coagulant complex

Identification

Summary

Anti-inhibitor coagulant complex is a medication used to control bleeding episodes and prevent bleeding episodes in hemophilia A and B.

Brand Names
Feiba
Generic Name
Anti-inhibitor coagulant complex
DrugBank Accession Number
DB13151
Background

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

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.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofBleeding caused by hemophilia a••••••••••••
Prophylaxis ofBleeding caused by hemophilia a••••••••••••
Treatment ofBleeding caused by hemophilia b••••••••••••
Prophylaxis ofBleeding caused by hemophilia b••••••••••••
Prophylaxis ofPerioperative bleeding caused by hemophilia a••••••••••••
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
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Toxicity

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

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.
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.
Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FeibaKit; Powder, for solution1000 U/20mLIntravenousTakeda Pharma A/S1986-01-31Not applicableUS flag
FeibaKit; Powder, for solution500 U/10mLIntravenousTakeda Pharma A/S1986-01-31Not applicableUS flag
FeibaKit; Powder, for solution2500 U/50mLIntravenousTakeda Pharma A/S1986-01-31Not applicableUS flag
FeibaKit500 [USP'U]/20mLIntravenousBaxalta US Inc.1986-01-31Not applicableUS flag
Feiba NfKit; Powder, for solution3250 unit / vialIntravenousTakeda Italia S.P.A.2011-04-04Not applicableCanada 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
Affected organisms
  • Humans and other mammals

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. [Article]
  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. [Article]
PubChem Substance
347911435
RxNav
314504
FDA label
Download (1.22 MB)

Clinical Trials

Clinical Trials
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Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package
PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
Not AvailableCompletedNot AvailableCongenital Hematological Disorder / Hemophilia A With Inhibitors / Hemophilia B With Inhibitors1somestatusstop reasonjust information to hide
Not AvailableCompletedNot AvailableHemorrhage1somestatusstop reasonjust information to hide
Not AvailableCompletedTreatmentSevere Hemophilia A With an Inhibitor1somestatusstop reasonjust information to hide
Not AvailableRecruitingNot AvailableHemophilia A1somestatusstop reasonjust information to hide
4Active Not RecruitingTreatmentHemophilia A With Inhibitors1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Kit; powder, for solutionIntravenous1000 U/20mL
Kit; powder, for solutionIntravenous2500 U/50mL
Kit; powder, for solutionIntravenous500 U/10mL
Injection, powder, for solutionParenteral100 E./ml
Injection, powder, for solutionIntravenous50 u/ml
Injection, powder, lyophilized, for solutionIntravenous1000 U
Injection, powder, for solutionParenteral25 E./ml
Injection, powder, for solutionParenteral50 E./ml
Injection, powder, for solutionIntravenous25 u/ml
KitIntravenous1000 [USP'U]/20mL
KitIntravenous2500 [USP'U]/50mL
KitIntravenous500 [USP'U]/20mL
Kit; powder, for solutionIntravenous1300 unit / vial
Kit; powder, for solutionIntravenous3250 unit / vial
Kit; powder, for solutionIntravenous650 unit / vial
Injection, powder, for solutionIntravenous1000 iu/1vial
Injection, powder, for solutionIntravenous500 iu/1vial
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General 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. Factor Xa activates pro-inflammatory signaling pathways in a protease-activated receptor (PAR)-dependent manner (PubMed:24041930, PubMed:30568593, PubMed:34831181). Up-regulates expression of protease-activated receptors (PARs) F2R, F2RL1 and F2RL2 in dermal microvascular endothelial cells (PubMed:35738824). Triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2 and IL6, in cardiac fibroblasts and umbilical vein endothelial cells in PAR-1 (F2R)-dependent manner (PubMed:30568593, PubMed:34831181). Triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2, IL6, TNF-alpha/TNF, IL-1beta/IL1B, IL8/CXCL8 and IL18, in endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824, PubMed:9780208). Induces expression of adhesion molecules, such as ICAM1, VCAM1 and SELE, in endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824, PubMed:9780208). Increases expression of phosphorylated ERK1/2 in dermal microvascular endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824). Triggers activation of the transcription factor NF-kappa-B in dermal microvascular endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824). Up-regulates expression of plasminogen activator inhibitor 1 (SERPINE1) in atrial tissues (PubMed:24041930)
Specific Function
calcium ion binding
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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General 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 homeostasis, inflammation and wound healing. Thrombin triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2 and IL8/CXCL8, in endothelial cells (PubMed:30568593, PubMed:9780208)
Specific Function
calcium ion binding
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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Cleavage
General 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 in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelialization. Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However, subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets via an ITGB3-dependent pathway. Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the immune response via both innate and T-cell mediated pathways
Specific Function
extracellular matrix structural constituent
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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Cleavage
General 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 in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelialization. Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets. Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the antibacterial immune response via both innate and T-cell mediated pathways
Specific Function
extracellular matrix structural constituent
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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General 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 fibrin clot. Also cross-link alpha-2-plasmin inhibitor, or fibronectin, to the alpha chains of fibrin
Specific Function
metal ion binding
Gene Name
F13A1
Uniprot ID
P00488
Uniprot Name
Coagulation factor XIII A chain
Molecular Weight
83267.785 Da
References
  1. Turecek PL, Varadi K, Gritsch H, Schwarz HP: FEIBA: mode of action. Haemophilia. 2004 Sep;10 Suppl 2:3-9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General 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
Specific Function
copper ion binding
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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Factor VIII, along with calcium and phospholipid, acts as a cofactor for F9/factor IXa when it converts F10/factor X to the activated form, factor Xa
Specific Function
copper ion binding
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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General 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, or thrombin by minor proteolysis. In the presence of tissue factor and calcium ions, factor VIIa then converts factor X to factor Xa by limited proteolysis. Factor VIIa will also convert factor IX to factor IXa in the presence of tissue factor and calcium
Specific Function
calcium ion binding
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. [Article]

Drug created at November 18, 2016 21:27 / Updated at June 03, 2022 07:24