Identification

Summary

Coagulation factor X human is a coagulation factor used to treat Factor X deficiency to control bleeding.

Brand Names
Beriplex, Coagadex, Kcentra, Octaplex
Generic Name
Coagulation factor X human
DrugBank Accession Number
DB13148
Background

Coagulation Factor X (Human), is a plasma-derived human blood coagulation factor is used by adults and children (aged 12 years and above) with hereditary Factor X deficiency. However its use is limited in the perioperative setting for the management of bleeding in major surgery in patients with moderate and severe hereditary Factor X deficiency.

Coagulation Factor X is a vitamin K-dependent, liver-produced serine protease that serves as the first enzyme in the coagulation cascade to form fibrin. It is a two-chain glycoprotein with the molecular weight of approximately 59 kDa 2. While Factor X normally circulates in the plasma as inactive molecules, the activation of Factor X is involved in both the intrinsic and extrinsic coagulation pathways. Inherited factor X deficiency is a rare autosomal recessive bleeding disorder that is estimated to occur in 1:1 000 000 individuals up to 1:500 carriers 1. Administration of coagulation Factor X from healthy donor serves to restore and achieve effective hemostasis.

Coagulation Factor X (Human) solution is approved by the FDA for intravenous injection under the market name Coagadex which contains normally 100 IU/mL of coagulation Factor X derived from healthy donors who have passed viral screening tests 4.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Blood factors
Protein Structure
Protein Chemical Formula
Not Available
Protein Average Weight
59000.0 Da
Sequences
Not Available
Synonyms
  • Coagulation factor X
  • Coagulation factor X (human)
  • Factor X
  • Factor X (stuart prower factor)
  • Human coagulation factor X
  • Stuart-prower factor

Pharmacology

Indication

The human coagulation factor X is indicated in adults and children with hereditary Factor X deficiency for routine prophylaxis to reduce the frequency of bleeding episodes, on-demand treatment and control of bleeding episodes, and perioperative management of bleeding in patients with mild and moderate hereditary Factor X deficiency.4

It is also indicated for the urgent reversal of acquired coagulation factor deficiency induced by Vitamin K antagonist (VKA, e.g., warfarin) therapy in adult patients with acute major bleeding.5

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Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

Clinical human coagulation Factor X solution increases plasma levels of Factor X and can temporarily correct the coagulation defect in these patients, as reflected by decrease in the activated Partial Thromboplastin Time (aPTT) and prothrombin time (PT) 4.

Mechanism of action

Factor X is an inactive zymogen that is synthesized in the liver, which can be activated by Factor IXa (via the intrinsic pathway) or by Factor VIIa (via the extrinsic pathway). It is composed of a light chain which contains the Gla (glutamic acid) domain and two epidermal growth factor domains, and a heavy chain that contains the catalytic serine protease domain 1. The conversion of inactive Factor X into the active form Factor Xa requires the cleavage of a 52-residue peptide from the heavy chain 4 and the release of 52-residue activation peptide that contains the His236, Asp228 and Ser379 catalytic site. This activation step can occur through the extrinsic or intrinsic pathway and is considered to be the first step in the common pathway to fibrin formation 1.

Factor Xa plays a critical initiation step of the coagulation pathway by cleaving and activating prothrombin to thrombin in complex with FVa, Ca2+ and phospholipids. This complex is also known as the prothrombinase complex. Thrombin then acts upon soluble fibrinogen and Factor XIII to generate a cross-linked fibrin clot 3,4.

Absorption

Following a single intravenous dose of 25 IU/kg, the mean peak plasma concentration (CV%) was 0.504 (17.2) IU/mL 4.

Volume of distribution

Following a single intravenous dose of 25 IU/kg, the mean volume of distribution at steady state (CV%) was 56.3 (24.0) mL/kg 4.

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Following a single intravenous dose of 25 IU/kg, the mean plasma half-life (CV%) was 30.3 (22.8) hr.4

Clearance

Following a single intravenous dose of 25 IU/kg, the mean total body clearance was 1.35 (21.7) mL/kg/hr.4

Adverse Effects
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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
AbciximabThe therapeutic efficacy of Coagulation factor X human can be decreased when used in combination with Abciximab.
AcenocoumarolThe therapeutic efficacy of Coagulation factor X human can be decreased when used in combination with Acenocoumarol.
Alpha-1-proteinase inhibitorAlpha-1-proteinase inhibitor may increase the thrombogenic activities of Coagulation factor X human.
AlteplaseThe therapeutic efficacy of Coagulation factor X human 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 Coagulation factor X human.
AncrodThe therapeutic efficacy of Coagulation factor X human can be decreased when used in combination with Ancrod.
AnistreplaseThe therapeutic efficacy of Coagulation factor X human can be decreased when used in combination with Anistreplase.
Antithrombin AlfaThe therapeutic efficacy of Coagulation factor X human can be decreased when used in combination with Antithrombin Alfa.
Antithrombin III humanThe therapeutic efficacy of Coagulation factor X human can be decreased when used in combination with Antithrombin III human.
ApixabanThe therapeutic efficacy of Coagulation factor X human can be decreased when used in combination with Apixaban.
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Food Interactions
No interactions found.

Products

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dosage, form, labeller, route of administration, and marketing period.
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CoagadexKit100 [iU]/1mLIntravenousBio Products Laboratory Limited2015-10-21Not applicableUS flag
CoagadexInjection, powder, for solution250 IUIntravenousBpl Bioproducts Laboratory Gmb H2020-12-21Not applicableEU flag
CoagadexKit100 [iU]/1mLIntravenousBio Products Laboratory Limited2015-10-21Not applicableUS flag
CoagadexInjection, powder, for solution500 IUIntravenousBpl Bioproducts Laboratory Gmb H2020-12-21Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Beriplex P/n 1000Coagulation factor X human (2040 unit) + Coagulation Factor IX Human (1240 unit) + Coagulation factor VII human (1000 unit) + Protein C (1640 unit) + Protein S human (1360 unit) + Prothrombin (1600 unit)Powder, for solutionIntravenousCsl Behring2013-11-21Not applicableCanada flag
Beriplex P/N 1000 I.E. Pulver und Lösungsmittel zur Herstellung einer InjektionslösungCoagulation factor X human (1640 IE) + Coagulation Factor IX Human (1020 IE) + Coagulation factor VII human (700 IE) + Protein C (1200 I.E.) + Protein S human (1000 IE) + Prothrombin (1360 IE)Injection, powder, for solutionParenteralCsl Behring2013-04-16Not applicableAustria flag
Beriplex P/N 250 I.E. Pulver und Lösungsmittel zur Herstellung einer InjektionslösungCoagulation factor X human (410 IE) + Coagulation Factor IX Human (255 IE) + Coagulation factor VII human (175 IE) + Protein C (300 IE) + Protein S human (250 IE) + Prothrombin (340 I.E.)Injection, powder, for solutionParenteralCsl Behring2008-02-27Not applicableAustria flag
Beriplex P/n 500Coagulation factor X human (1020 unit) + Coagulation Factor IX Human (620 unit) + Coagulation factor VII human (500 unit) + Protein C (820 unit) + Protein S human (680 unit) + Prothrombin (800 unit)Powder, for solutionIntravenousCsl Behring2011-07-28Not applicableCanada flag
Beriplex P/N 500 I.E. Pulver und Lösungsmittel zur Herstellung einer InjektionslösungCoagulation factor X human (820 IE) + Coagulation Factor IX Human (510 IE) + Coagulation factor VII human (350 IE) + Protein C (600 I.E.) + Protein S human (500 IE) + Prothrombin (680 IE)Injection, powder, for solutionParenteralCsl Behring2008-02-27Not applicableAustria flag
Cofact 250 I.E. Prothrombinkomplex vom Menschen, 250 I.E. Faktor IX pro Durchstechflasche Pulver und Lösungsmittel zur Herstellung einer InjektionslösungCoagulation factor X human (245 IE) + Coagulation Factor IX Human (250 IE) + Coagulation factor VII human (135 IE) + Prothrombin (245 IE)Injection, powder, for solutionParenteralProthya Biosolutions Netherlands b.v.2007-05-18Not applicableAustria flag
COFACT 250 IU/10 ML IV ENJEKSIYON IÇIN TOZ IÇEREN FLAKON, 1 ADETCoagulation factor X human (245 IU) + Coagulation Factor IX Human (250 IU) + Coagulation factor VII human (135 IU) + Protein C (250 IU) + Protein S human (45 IU) + Prothrombin (245 IU)InjectionIntravenousCENTURION İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
Cofact 500 I.E. Prothrombinkomplex vom Menschen, 500 I.E. Faktor IX pro Durchstechflasche Pulver und Lösungsmittel zur Herstellung einer InjektionslösungCoagulation factor X human (490 IE) + Coagulation Factor IX Human (500 IE) + Coagulation factor VII human (270 IE) + Prothrombin (490 IE)Injection, powder, for solutionParenteralProthya Biosolutions Netherlands b.v.2007-05-18Not applicableAustria flag
COFACT 500 IU/20 ML IV ENJEKSIYON IÇIN TOZ IÇEREN FLAKON, 1 ADETCoagulation factor X human (490 IU) + Coagulation Factor IX Human (500 IU) + Coagulation factor VII human (270 IU) + Protein C (500 IU) + Protein S human (90 IU) + Prothrombin (490 IU)InjectionIntravenousCENTURION İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
Feiba Vh Immuno Anti InhibitorCoagulation factor X human + Antihemophilic factor human (4 unit) + Coagulation factor VII human + Factor IX Complex (Human) + ProthrombinPowder, for solutionIntravenousOsterreichisches Institut Fur Haemoderivate Ges M.B.H.1986-12-311998-08-13Canada flag

Categories

ATC Codes
B02BD13 — Coagulation factor x
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
HYF6HN9XGQ
CAS number
Not Available

References

General References
  1. Brown DL, Kouides PA: Diagnosis and treatment of inherited factor X deficiency. Haemophilia. 2008 Nov;14(6):1176-82. doi: 10.1111/j.1365-2516.2008.01856.x. [Article]
  2. Venkateswarlu D, Perera L, Darden T, Pedersen LG: Structure and dynamics of zymogen human blood coagulation factor X. Biophys J. 2002 Mar;82(3):1190-206. doi: 10.1016/S0006-3495(02)75476-3. [Article]
  3. 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]
  4. FDA Approved Drug Products: COAGADEX (Coagulation Factor X (Human)) Lyophilized Powder for Solution for Intravenous Injection [Link]
  5. FDA Approved Drug Products: KCENTRA (Prothrombin Complex Concentrate (Human)) For Intravenous Use, Lyophilized Powder for Reconstitution [Link]
PubChem Substance
347911432
RxNav
4262

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentBleeding / Blood Loss During Surgery / Cardiovascular Surgical Procedures / Fresh Frozen Plasma / Prothrombin Complex Concentrates1
4RecruitingTreatmentCoagulation Disorder / Massive Hemorrhage / Traumatic haemorrhage1
4WithdrawnTreatmentPostpartum Haemorrhage (PPH)1
3CompletedPreventionFactor X Deficiency1
3CompletedTreatmentAcute Major Bleeding / Coagulation Disorder1
3CompletedTreatmentFactor X Deficiency1
3CompletedTreatmentReversal of Anticoagulant Treatment1
3CompletedTreatmentReversal of Coagulopathy1
3CompletedTreatmentSignificant Bleeding Risk1
3Not Yet RecruitingTreatmentBleeding Cardiac Surgery Patients1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, for solutionIntravenous
Injection, powder, for solutionIntravenous100 UI/ML
Injection, powder, for solutionIntravenous250 IU
Injection, powder, for solutionIntravenous500 IU
KitIntravenous100 [iU]/1mL
InjectionIntravenous
Powder, for solutionIntravenous
KitIntravenous
Powder, for solutionParenteral
Kit; powder, for solutionIntravenous
Injection, powder, for solutionIntravenous drip520 IU/vial
Injection, powder, for solutionParenteral
SolutionIntravenous
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Drug created at November 18, 2016 20:47 / Updated at March 24, 2022 01:23