NAV

Protein S human

Identification

Summary

Protein S human is a medication used for emergency reversal of coagulation factor deficiency in vitamin K antagonist therapy.

Brand Names
Balfaxar, Beriplex, Kcentra, Octaplex
Generic Name
Protein S human
DrugBank Accession Number
DB13149
Background

Protein S human is a vitamin K-dependent plasma glycoprotein which has antcoagulant properties 1. It serves as a negative feedback mechanism in the coagulation cascade.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Blood factors
Protein Structure
Protein Chemical Formula
Not Available
Protein Average Weight
75123.0 Da
Sequences
>sp|P07225|PROS_HUMAN Vitamin K-dependent protein S OS=Homo sapiens GN=PROS1 PE=1 SV=1
MRVLGGRCGALLACLLLVLPVSEANFLSKQQASQVLVRKRRANSLLEETKQGNLERECIE
ELCNKEEAREVFENDPETDYFYPKYLVCLRSFQTGLFTAARQSTNAYPDLRSCVNAIPDQ
CSPLPCNEDGYMSCKDGKASFTCTCKPGWQGEKCEFDINECKDPSNINGGCSQICDNTPG
SYHCSCKNGFVMLSNKKDCKDVDECSLKPSICGTAVCKNIPGDFECECPEGYRYNLKSKS
CEDIDECSENMCAQLCVNYPGGYTCYCDGKKGFKLAQDQKSCEVVSVCLPLNLDTKYELL
YLAEQFAGVVLYLKFRLPEISRFSAEFDFRTYDSEGVILYAESIDHSAWLLIALRGGKIE
VQLKNEHTSKITTGGDVINNGLWNMVSVEELEHSISIKIAKEAVMDINKPGPLFKPENGL
LETKVYFAGFPRKVESELIKPINPRLDGCIRSWNLMKQGASGIKEIIQEKQNKHCLVTVE
KGSYYPGSGIAQFHIDYNNVSSAEGWHVNVTLNIRPSTGTGVMLALVSGNNTVPFAVSLV
DSTSEKSQDILLSVENTVIYRIQALSLCSDQQSHLEFRVNRNNLELSTPLKIETISHEDL
QRQLAVLDKAMKAKVATYLGGLPDVPFSATPVNAFYNGCMEVNINGVQLDLDEAISKHND
IRAHSCPSVWKKTKNS
Download FASTA Format
Synonyms
  • Protein S
  • Protein S (human)
  • Vitamin K-dependent protein S

Pharmacology

Indication

For use in the emergency reversal of coagulation factor deficiency in patients recieving vitamin K antagonist therapy Label. Protein S is administered as part of a cocktail containing several other coagulation factors.

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Protein S acts as an anticoagulant serves as a negative feedback mechanism in the coagulation cascade 1.

Mechanism of action

Thrombin converts protein C to activated protein C (APC) 1. Protein S functions as a cofactor for APC and together they proteolytically cleave factor Va and VIIIa 1 2. This inhibits the activities of the prothrombinase and tenase complexes respectively and leads to a reduction in thrombin generation. The reduction in thrombin generation suppresses the coagulation cascade preventing additional clotting from occuring. Protein S is suggested to inhibit factors Va and Xa through protein-protein interactions 4 1. Protein S is also suggested to inhibit production of factor Xa by the tenase complex by competing for binding to phospholipids via its gamma-carboxyglutamic acid domain.

Protein S is thought to exert an anti-inflammatory effect in addition to its anticoagulant properties. The protein S-C4b-binding protein complex is believed to bind to phosphotidylserines on the cell membranes of apoptotic cells and interact with macrophages, signalling them to phagocytose the cell before it can rupture 3.

TargetActionsOrganism
ACoagulation factor V
antagonist
Humans
ACoagulation factor X
antagonist
Humans
AVitamin K-dependent protein C
cofactor
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Approximately 60% of protein S is bound to C4b-binding protein in systemic circulation 1.

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

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
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interactions in your software
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Protein S human.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Protein S human.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Protein S human is combined with Acemetacin.
AcenocoumarolThe therapeutic efficacy of Protein S human can be decreased when used in combination with Acenocoumarol.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Protein S human.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Protein S human.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Protein S human.
AldesleukinThe risk or severity of bleeding can be increased when Protein S human is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Protein S human is combined with Alemtuzumab.
Alpha-1-proteinase inhibitorAlpha-1-proteinase inhibitor may increase the thrombogenic activities of Protein S human.
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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

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
BalfaxarProtein S human (22 [iU]/1mL) + Coagulation Factor IX Human (25.5 [iU]/1mL) + Coagulation factor VII human (16.5 [iU]/1mL) + Coagulation factor X human (24 [iU]/1mL) + Protein C (22 [iU]/1mL) + Prothrombin (26 [iU]/1mL)Powder, for solutionIntravenousOctapharma USA Inc2023-07-21Not applicableUS flag
Beriplex P/n 1000Protein S human (1360 unit) + Coagulation Factor IX Human (1240 unit) + Coagulation factor VII human (1000 unit) + Coagulation factor X human (2040 unit) + Protein C (1640 unit) + Prothrombin (1600 unit)Powder, for solutionIntravenousCsl Behring2013-11-21Not applicableCanada flag
Beriplex P/N 1000 I.E. Pulver und Lösungsmittel zur Herstellung einer InjektionslösungProtein S human (1000 IE) + Coagulation Factor IX Human (1020 IE) + Coagulation factor VII human (700 IE) + Coagulation factor X human (1640 IE) + Protein C (1200 I.E.) + Prothrombin (1360 IE)Injection, powder, for solutionParenteralCsl Behring2013-04-16Not applicableAustria flag
Beriplex P/N 250 I.E. Pulver und Lösungsmittel zur Herstellung einer InjektionslösungProtein S human (250 IE) + Coagulation Factor IX Human (255 IE) + Coagulation factor VII human (175 IE) + Coagulation factor X human (410 IE) + Protein C (300 IE) + Prothrombin (340 I.E.)Injection, powder, for solutionParenteralCsl Behring2008-02-27Not applicableAustria flag
Beriplex P/n 500Protein S human (680 unit) + Coagulation Factor IX Human (620 unit) + Coagulation factor VII human (500 unit) + Coagulation factor X human (1020 unit) + Protein C (820 unit) + Prothrombin (800 unit)Powder, for solutionIntravenousCsl Behring2011-07-28Not applicableCanada flag
Beriplex P/N 500 I.E. Pulver und Lösungsmittel zur Herstellung einer InjektionslösungProtein S human (500 IE) + Coagulation Factor IX Human (510 IE) + Coagulation factor VII human (350 IE) + Coagulation factor X human (820 IE) + Protein C (600 I.E.) + Prothrombin (680 IE)Injection, powder, for solutionParenteralCsl Behring2008-02-27Not applicableAustria flag
COFACT 250 IU/10 ML IV ENJEKSIYON IÇIN TOZ IÇEREN FLAKON, 1 ADETProtein S human (45 IU) + Coagulation Factor IX Human (250 IU) + Coagulation factor VII human (135 IU) + Coagulation factor X human (245 IU) + Protein C (250 IU) + Prothrombin (245 IU)InjectionIntravenousCENTURION İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
COFACT 500 IU/20 ML IV ENJEKSIYON IÇIN TOZ IÇEREN FLAKON, 1 ADETProtein S human (90 IU) + Coagulation Factor IX Human (500 IU) + Coagulation factor VII human (270 IU) + Coagulation factor X human (490 IU) + Protein C (500 IU) + Prothrombin (490 IU)InjectionIntravenousCENTURION İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
KcentraProtein S human (460 U/20mL) + Coagulation Factor IX Human (510 U/20mL) + Coagulation factor VII human (350 U/20mL) + Coagulation factor X human (760 U/20mL) + Protein C (620 U/20mL) + Prothrombin (590 U/20mL)Injection, powder, lyophilized, for solution; KitIntravenousCSL Behring GmbH2013-04-29Not applicableUS flag
KcentraProtein S human (920 U/40mL) + Coagulation Factor IX Human (1020 U/40mL) + Coagulation factor VII human (700 U/40mL) + Coagulation factor X human (1520 U/40mL) + Protein C (1240 U/40mL) + Prothrombin (1180 U/40mL)Injection, powder, lyophilized, for solution; KitIntravenousCSL Behring GmbH2013-12-13Not applicableUS flag

Categories

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
90J3F6N5FN
CAS number
Not Available

References

General References
  1. Rigby AC, Grant MA: Protein S: a conduit between anticoagulation and inflammation. Crit Care Med. 2004 May;32(5 Suppl):S336-41. [Article]
  2. Somajo S, Koshiar RL, Norstrom E, Dahlback B: Protein S and factor V in regulation of coagulation on platelet microparticles by activated protein C. Thromb Res. 2014 Jul;134(1):144-52. doi: 10.1016/j.thromres.2014.04.031. Epub 2014 May 2. [Article]
  3. Webb JH, Blom AM, Dahlback B: Vitamin K-dependent protein S localizing complement regulator C4b-binding protein to the surface of apoptotic cells. J Immunol. 2002 Sep 1;169(5):2580-6. [Article]
  4. Hackeng TM, van 't Veer C, Meijers JC, Bouma BN: Human protein S inhibits prothrombinase complex activity on endothelial cells and platelets via direct interactions with factors Va and Xa. J Biol Chem. 1994 Aug 19;269(33):21051-8. [Article]
PubChem Substance
347911433
RxNav
34822
FDA label
Download (638 KB)
MSDS
Download (744 KB)

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
3CompletedTreatmentAcute Major Bleeding / Coagulation Disorder1
3CompletedTreatmentHigh Bleeding Risk1
3CompletedTreatmentReversal of Anticoagulant Treatment1
3CompletedTreatmentReversal of Coagulopathy1
3RecruitingTreatmentAcute Major Bleeding1
3RecruitingTreatmentBleeding Cardiac Surgery Patients1
3RecruitingTreatmentCongestive Heart Failure (CHF) / Heart Disease End Stage1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Powder, for solutionIntravenous
Injection, powder, for solutionParenteral
Injection, powder, for solutionIntravenous
InjectionIntravenous
Injection, powder, lyophilized, for solution; kitIntravenous
Kit; powder, for solutionIntravenous
Injection, powder, for solutionIntravenous drip520 IU/vial
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

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Details1. Coagulation factor V
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
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. Hackeng TM, van 't Veer C, Meijers JC, Bouma BN: Human protein S inhibits prothrombinase complex activity on endothelial cells and platelets via direct interactions with factors Va and Xa. J Biol Chem. 1994 Aug 19;269(33):21051-8. [Article]
Details2. Coagulation factor X
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
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. Hackeng TM, van 't Veer C, Meijers JC, Bouma BN: Human protein S inhibits prothrombinase complex activity on endothelial cells and platelets via direct interactions with factors Va and Xa. J Biol Chem. 1994 Aug 19;269(33):21051-8. [Article]
Details3. Vitamin K-dependent protein C
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Cofactor
General Function
Serine-type endopeptidase activity
Specific Function
Protein C is a vitamin K-dependent serine protease that regulates blood coagulation by inactivating factors Va and VIIIa in the presence of calcium ions and phospholipids (PubMed:25618265). Exerts ...
Gene Name
PROC
Uniprot ID
P04070
Uniprot Name
Vitamin K-dependent protein C
Molecular Weight
52070.82 Da
References
  1. Somajo S, Koshiar RL, Norstrom E, Dahlback B: Protein S and factor V in regulation of coagulation on platelet microparticles by activated protein C. Thromb Res. 2014 Jul;134(1):144-52. doi: 10.1016/j.thromres.2014.04.031. Epub 2014 May 2. [Article]

Drug created at November 18, 2016 20:51 / Updated at July 11, 2020 03:43