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
Balfaxar, 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
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

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prevention ofPurpura fulminans•••••••••••••••••• •••••••••• ••••••• • •••••••••••••••••••• ••••••• •••••••••••• ••• ••••••••
Treatment ofPurpura fulminans•••••••••••••••••• •••••••••• ••••••• • •••••••••••••••••••• ••••••• •••••••••••• ••• ••••••••
Prevention ofThrombosis, venous•••••••••••••••••• •••••••••• ••••••• • •••••••••••••••••••• ••••••• •••••••••••• ••• ••••••••
Treatment ofThrombosis, venous•••••••••••••••••• •••••••••• ••••••• • •••••••••••••••••••• ••••••• •••••••••••• ••• ••••••••
Contraindications & Blackbox Warnings
Prevent Adverse Drug Events Today
Tap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events with our Clinical API
Learn more
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
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!
See the data
Improve decision support & research outcomes with our structured adverse effects data.
See a data sample
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 Protein C is combined with Acemetacin.
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.
Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Products

Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CeprotinInjection, powder, for solution1000 IUIntravenousTakeda Manufacturing Austria Ag2016-09-08Not applicableEU flag
CeprotinInjection, powder, lyophilized, for solution; Kit500 [iU]/5mLIntravenousTakeda Pharmaceuticals America, Inc.2010-08-09Not applicableUS flag
CeprotinInjection, powder, for solution500 IUIntravenousTakeda Manufacturing Austria Ag2016-09-08Not applicableEU flag
CeprotinKit100 [iU]/1mLIntravenousBaxalta Us Inc2010-08-092018-11-30US flag
CeprotinInjection, powder, lyophilized, for solution; Kit1000 [iU]/10mLIntravenousTakeda Pharmaceuticals America, Inc.2010-08-09Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
BalfaxarProtein C (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 S human (22 [iU]/1mL) + Prothrombin (26 [iU]/1mL)Powder, for solutionIntravenousOctapharma USA Inc2023-11-30Not applicableUS flag
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 1000 I.E. Pulver und Lösungsmittel zur Herstellung einer InjektionslösungProtein C (1200 I.E.) + Coagulation Factor IX Human (1020 IE) + Coagulation factor VII human (700 IE) + Coagulation factor X human (1640 IE) + 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 InjektionslösungProtein C (300 IE) + Coagulation Factor IX Human (255 IE) + Coagulation factor VII human (175 IE) + Coagulation factor X human (410 IE) + Protein S human (250 IE) + Prothrombin (340 I.E.)Injection, powder, for solutionParenteralCsl Behring2008-02-27Not applicableAustria 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

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)) For Intravenous Use, Lyophilized Powder for Reconstitution [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

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Powder, for solutionIntravenous
Injection, powder, for solutionParenteral
Injection, powder, for solutionIntravenous
Injection, powder, for solutionIntravenous1000 IU
Injection, powder, for solutionIntravenous500 IU
Injection, powder, for solutionIntravenous; Subcutaneous1000 IU
Injection, powder, for solutionIntravenous; Subcutaneous500 IU
Injection, powder, lyophilized, for solution; kitIntravenous1000 [iU]/10mL
Injection, powder, lyophilized, for solution; kitIntravenous500 [iU]/5mL
KitIntravenous100 [iU]/1mL
Injection, solutionIntravenous500 iu
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

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
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 at December 03, 2015 16:52 / Updated at July 11, 2020 03:43