Protein C

Identification

Summary

Protein C is a medication used to treat protein C deficiency leading to purpura fulminans or coumarin-induced skin necrosis.

Brand Names
Beriplex, Ceprotin, Kcentra, Octaplex
Generic Name
Protein C
DrugBank Accession Number
DB11312
Background

Protein C is an endogenously occurring plasma protein that plays a key role within the coagulation cascade. Protein C is a zymogen, or enzyme precursor, of a vitamin K-dependent anticoagulant glycoprotein (serine protease) that is synthesized in the liver. It is converted by the thrombin/thrombomodulin-complex on the endothelial cell surface to Activated Protein C (APC). Once in its activated form, APC functions as a serine protease with potent anticoagulant effects, especially in the presence of its cofactor protein S. APC exerts its effect by inactivating essential components of the coagulation cascade (specifically factors V and VIII), which leads to a decrease in thrombin formation, and therefore a reduction in clot formation.

The Protein C pathway provides a natural mechanism for control of the coagulation system and prevention of excessive procoagulant responses to activating stimuli. A lack of protein C in the body would lead to unchecked coagulation activation, resulting in thrombin generation and intravascular clot formation.

Protein C is available in concentrated form as the product Ceprotin, which is indicated for use in pediatric and adult patients with severe congenital protein C deficiency for the prevention and treatment of venous thrombosis and purpura fulminans.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Blood factors
Protein Structure
Db11312
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • autoprothrombin IIA
  • blood coagulation factor XIV
  • Human protein C
  • Protein C (coagulation inhibitor)
  • Protein C concentrate
  • Protein C concentrate (human)
  • Protein C concentrate human
  • Protein C human

Pharmacology

Indication

Protein C concentrate is indicated for pediatric and adult patients with severe congenital protein C deficiency for the prevention and treatment of venous thrombosis and purpura fulminans.2 It is also found as a component of some prothrombin complex concentrate (i.e. Factor IX Complex (Human)) formulations, such as Kcentra.3

Pharmacology
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Drug Discovery
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

In clinical studies, the intravenous administration of Protein C Concentrate demonstrated a temporary increase, within approximately half an hour of administration, in plasma levels of APC. Replacement of protein C in protein C-deficient patients is expected to control or, if given prophylactically, to prevent thrombotic complications.2

Mechanism of action

Protein C is an endogenously occurring plasma protein that plays a key role within the coagulation cascade. Also known as blood coagulation factor XIV, Protein C is a zymogen, or enzyme precursor, of a vitamin K-dependent anticoagulant glycoprotein (serine protease) that is synthesized in the liver. It is converted by the thrombin/thrombomodulin-complex on the endothelial cell surface to Activated Protein C (APC). Once in its activated form, APC functions as a serine protease with potent anticoagulant effects, especially in the presence of its cofactor protein S. APC exerts its effect by inactivating essential components of the coagulation cascade (specifically factors V and VIII), which leads to a decrease in thrombin formation, and therefore a reduction in clot formation.

TargetActionsOrganism
ACoagulation factor V
inactivator
Humans
ACoagulation factor VIII
inactivator
Humans
Absorption

Cmax = 110 IU/dL Tmax = 0.50 hr

Volume of distribution

Volume of distribution at steady state = 0.74 dL/kg

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Initial half life = 7.8 hr Terminal half life = 9.9 hr

Clearance

CL = 0.0533 dL/kg/h

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
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Protein C.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Protein C.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Protein C.
AcenocoumarolThe risk or severity of bleeding can be increased when Acenocoumarol is combined with Protein C.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Protein C.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Protein C.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Protein C.
AldesleukinThe risk or severity of bleeding can be increased when Protein C is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Protein C is combined with Alemtuzumab.
AlteplaseThe risk or severity of bleeding can be increased when Protein C is combined with Alteplase.
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
CeprotinKit1000 [iU]/10mLIntravenousBaxalta US Inc.2010-08-09Not applicableUS flag
CeprotinInjection, powder, for solutionIntravenousTakeda Manufacturing Austria Ag2016-09-08Not applicableEU flag
CeprotinKit500 [iU]/5mLIntravenousBaxalta US Inc.2010-08-09Not applicableUS flag
CeprotinInjection, powder, for solutionIntravenousTakeda Manufacturing Austria Ag2016-09-08Not applicableEU flag
CeprotinKit100 [iU]/1mLIntravenousBaxalta Us Inc2010-08-092018-11-30US flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Beriplex P/n 1000Protein C (1640 unit) + Coagulation Factor IX Human (1240 unit) + Coagulation factor VII human (1000 unit) + Coagulation factor X human (2040 unit) + Protein S human (1360 unit) + Prothrombin (1600 unit)Powder, for solutionIntravenousCsl Behring2013-11-21Not applicableCanada flag
Beriplex P/n 500Protein C (820 unit) + Coagulation Factor IX Human (620 unit) + Coagulation factor VII human (500 unit) + Coagulation factor X human (1020 unit) + Protein S human (680 unit) + Prothrombin (800 unit)Powder, for solutionIntravenousCsl Behring2011-07-28Not applicableCanada flag
COFACT 250 IU/10 ML IV ENJEKSIYON IÇIN TOZ IÇEREN FLAKON, 1 ADETProtein C (250 IU) + Coagulation Factor IX Human (250 IU) + Coagulation factor VII human (135 IU) + Coagulation factor X human (245 IU) + Protein S human (45 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 C (500 IU) + Coagulation Factor IX Human (500 IU) + Coagulation factor VII human (270 IU) + Coagulation factor X human (490 IU) + Protein S human (90 IU) + Prothrombin (490 IU)InjectionIntravenousCENTURION İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
KcentraProtein C (1240 U/40mL) + Coagulation Factor IX Human (1020 U/40mL) + Coagulation factor VII human (700 U/40mL) + Coagulation factor X human (1520 U/40mL) + Protein S human (920 U/40mL) + Prothrombin (1180 U/40mL)KitIntravenousCSL Behring GmbH2013-12-13Not applicableUS flag
KcentraProtein C (620 U/20mL) + Coagulation Factor IX Human (510 U/20mL) + Coagulation factor VII human (350 U/20mL) + Coagulation factor X human (760 U/20mL) + Protein S human (460 U/20mL) + Prothrombin (590 U/20mL)KitIntravenousCSL Behring GmbH2013-04-29Not applicableUS flag
OctaplexProtein C (1240 unit) + Coagulation Factor IX Human (1000 unit) + Coagulation factor VII human (960 unit) + Coagulation factor X human (1200 unit) + Protein S human (1280 unit) + Prothrombin (1520 unit)Kit; Powder, for solutionIntravenousOctapharma Pharmazeutika Produktionsges M B H2015-08-11Not applicableCanada flag
OctaplexProtein C (620 unit) + Coagulation Factor IX Human (500 unit) + Coagulation factor VII human (480 unit) + Coagulation factor X human (600 unit) + Protein S human (640 unit) + Prothrombin (760 unit)Kit; Powder, for solutionIntravenousOctapharma Pharmazeutika Produktionsges M B H2008-07-08Not applicableCanada flag

Categories

ATC Codes
B01AD12 — Protein c
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
Y2RU654EXB
CAS number
Not Available

References

General References
  1. Esmon CT, Vigano-D'Angelo S, D'Angelo A, Comp PC: Anticoagulation proteins C and S. Adv Exp Med Biol. 1987;214:47-54. [Article]
  2. FDA Approved Drug Products: Ceprotin (protein C concentration [human]) powder for solution [Link]
  3. FDA Approved Drug Products: Kcentra (prothrombin complex concentrate [human]) powder for reconsitution [Link]
KEGG Drug
D08796
PubChem Substance
347911185
RxNav
723868
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Protein_C
FDA label
Download (674 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Enrolling by InvitationTreatmentBleeding / Blood Loss,Surgical / Cardiovascular Surgical Procedures / Fresh Frozen Plasma / Prothrombin Complex Concentrates1
4RecruitingTreatmentCoagulation Disorders / Massive Hemorrhage / Traumatic haemorrhage1
4WithdrawnTreatmentPostpartum Haemorrhage (PPH)1
3CompletedTreatmentAcute Major Bleeding / Disorders, Blood Coagulation1
3CompletedTreatmentReversal of Anticoagulant Treatment1
3CompletedTreatmentReversal of Coagulopathy1
3RecruitingTreatmentCongestive Heart Failure (CHF) / Heart Disease End Stage1
3RecruitingTreatmentSignificant Bleeding Risk1
3TerminatedTreatmentSepsis1
2Active Not RecruitingOtherBleeding in Cardiac Surgery1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Powder, for solutionIntravenous
Injection, powder, for solutionParenteral
Injection, powder, for solutionIntravenous
Injection, powder, for solutionIntravenous
Injection, powder, for solutionIntravenous; Subcutaneous
KitIntravenous100 [iU]/1mL
KitIntravenous1000 [iU]/10mL
KitIntravenous500 [iU]/5mL
Injection, solutionIntravenous
InjectionIntravenous
KitIntravenous
Kit; powder, for solutionIntravenous
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
Yes
Actions
Inactivator
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. FDA Approved Drug Products: Ceprotin (protein C concentration [human]) powder for solution [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inactivator
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. FDA Approved Drug Products: Ceprotin (protein C concentration [human]) powder for solution [Link]

Drug created on December 03, 2015 16:52 / Updated on July 11, 2020 03:43