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Identification
NameCoagulation factor VIIa Recombinant Human
Accession NumberDB00036  (BTD00006, BIOD00006)
TypeBiotech
GroupsApproved
DescriptionRecombinant human coagulation Factor VIIa (rFVIIa), intended for promoting hemostasis by activating the extrinsic pathway of the coagulation cascade. NovoSeven is a vitamin K-dependent glycoprotein consisting of 406 amino acid residues. Cloned and expressed in hamster kidney cells, the protein is catalytically active in a two-chain form.
Protein structureDb00036
Related Articles
Protein chemical formulaC1972H3076N560O597S28
Protein average weight45079.1 Da
Sequences
>DB00036 sequence
ANAFLEELRPGSLERECKEEQCSFEEAREIFKDAERTKLFWISYSDGDQCASSPCQNGGS
CKDQLQSYICFCLPAFEGRNCETHKDDQLICVNENGGCEQYCSDHTGTKRSCRCHEGYSL
LADGVSCTPTVEYPCGKIPILEKRNASKPQGRIVGGKVCPKGECPWQVLLLVNGAQLCGG
TLINTIWVVSAAHCFDKIKNWRNLIAVLGEHDLSEHDGDEQSRRVAQVIIPSTYVPGTTN
HDIALLRLHQPVVLTDHVVPLCLPERTFSERTLAFVRFSLVSGWGQLLDRGATALELMVL
NVPRLMTQDCLQQSRKVGDSPNITEYMFCAGYSDGSKDSCKGDSGGPHATHYRGTWYLTG
IVSWGQGCATVGHFGVYTRVSQYIEWLQKLMRSEPRPGVLLRAPFP
Download FASTA Format
Synonyms
Coagulation factor VIIa
Coagulation factor VIIa (recombinant)
Eptacog alfa
Eptacog alfa (activated)
rFVIIa
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NiastasePowder, for solution2.4 mgIntravenousNovo Nordisk Canada Inc1999-08-052013-07-22Canada
NiastasePowder, for solution4.8 mgIntravenousNovo Nordisk Canada Inc1999-08-052013-07-22Canada
NiastasePowder, for solution1.2 mgIntravenousNovo Nordisk Canada Inc1999-08-052013-07-22Canada
Niastase RTKit; Powder, for solution1 mgIntravenousNovo Nordisk Canada Inc2010-08-25Not applicableCanada
Niastase RTKit; Powder, for solution2 mgIntravenousNovo Nordisk Canada Inc2015-05-05Not applicableCanada
Niastase RTKit; Powder, for solution2 mgIntravenousNovo Nordisk Canada Inc2010-08-05Not applicableCanada
Niastase RTKit; Powder, for solution5 mgIntravenousNovo Nordisk Canada Inc2015-05-05Not applicableCanada
Niastase RTKit; Powder, for solution8 mgIntravenousNovo Nordisk Canada IncNot applicableNot applicableCanada
Niastase RTKit; Powder, for solution5 mgIntravenousNovo Nordisk Canada Inc2010-08-25Not applicableCanada
Niastase RTKit; Powder, for solution8 mgIntravenousNovo Nordisk Canada IncNot applicableNot applicableCanada
Niastase RTKit; Powder, for solution1 mgIntravenousNovo Nordisk Canada Inc2015-05-05Not applicableCanada
NovosevenInjection, powder, for solution250 KIUIntravenousNovo Nordisk A/s1996-02-23Not applicableEu
NovosevenInjection, powder, for solution400 KIUIntravenousNovo Nordisk A/s1996-02-23Not applicableEu
NovosevenInjection, powder, for solution400 KIUIntravenousNovo Nordisk A/s1996-02-23Not applicableEu
NovosevenInjection, powder, for solution50 KIUIntravenousNovo Nordisk A/s1996-02-23Not applicableEu
NovosevenInjection, powder, for solution50 KIUIntravenousNovo Nordisk A/s1996-02-23Not applicableEu
NovosevenInjection, powder, for solution100 KIUIntravenousNovo Nordisk A/s1996-02-23Not applicableEu
NovosevenInjection, powder, for solution100 KIUIntravenousNovo Nordisk A/s1996-02-23Not applicableEu
NovosevenInjection, powder, for solution250 KIUIntravenousNovo Nordisk A/s1996-02-23Not applicableEu
Novoseven RTKitNovo Nordisk2008-04-302015-10-31Us
Novoseven RTKitNovo Nordisk2012-10-29Not applicableUs
Novoseven RTKitNovo Nordisk2012-10-29Not applicableUs
Novoseven RTKitNovo Nordisk2012-10-29Not applicableUs
Novoseven RTKitNovo Nordisk2012-10-29Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
NovoSevenNovo Nordisk
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIAC71R787OV
CAS number102786-61-8
Pharmacology
IndicationFor treatment of hemorrhagic complications in hemophilia A and B
Structured Indications
PharmacodynamicsUsed in the treatment of bleeding episodes in hemophilia A or B. NovoSeven is recombinant Factor VIIa and, when complexed with tissue factor can activate coagulation Factor X to Factor Xa, as well as coagulation Factor IX to Factor IXa. Factor Xa, in complex with other factors, then converts prothrombin to thrombin, which leads to the formation of a hemostatic plug by converting fibrinogen to fibrin and thereby inducing local clotting.
Mechanism of actionNovoSeven activates the coagulation or clotting cascade by cleaving Factor IX and Factor X, which activates them and then leads to activation of thrombin and fibrin.
TargetKindPharmacological actionActionsOrganismUniProt ID
Coagulation factor XProteinunknownNot AvailableHumanP00742 details
Tissue factorProteinunknownNot AvailableHumanP13726 details
Serine protease hepsinProteinunknownNot AvailableHumanP05981 details
Tissue factor pathway inhibitorProteinunknownNot AvailableHumanP10646 details
Vitamin K-dependent gamma-carboxylaseProteinunknownNot AvailableHumanP38435 details
Coagulation factor VIIProteinunknownNot AvailableHumanP08709 details
Related Articles
AbsorptionNot Available
Volume of distribution
  • 121 ± 30 mL/kg [adults]
  • 153 ± 29 mL/kg [children]
  • 280 to 290 mL/kg [congenital Factor VII deficiency]
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
Clearance
  • 33 – 37 mL/h x kg [healthy]
  • 1375 +/- 396 mL/hr [severe hemophilia A male children]
  • 57.3 +/- 9.5 mL/hr/kg [severe hemophilia A male children]
  • 2767 +/- 385 mL/hr [severe hemophilia A men]
  • 37.6 +/- 13.1 mL/hr/kg [severe hemophilia A men]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Blackshear PJ, Holloway PA, Alberti KG: Factors regulating amino acid release from extrasplanchnic tissues in the rat. Interactions of alanine and glutamine. Biochem J. 1975 Sep;150(3):379-87. [PubMed:2155 ]
  2. Roberts HR, Monroe DM, White GC: The use of recombinant factor VIIa in the treatment of bleeding disorders. Blood. 2004 Dec 15;104(13):3858-64. Epub 2004 Aug 24. [PubMed:15328151 ]
  3. Kenet G, Walden R, Eldad A, Martinowitz U: Treatment of traumatic bleeding with recombinant factor VIIa. Lancet. 1999 Nov 27;354(9193):1879. [PubMed:10584732 ]
  4. O'Connell KA, Wood JJ, Wise RP, Lozier JN, Braun MM: Thromboembolic adverse events after use of recombinant human coagulation factor VIIa. JAMA. 2006 Jan 18;295(3):293-8. [PubMed:16418464 ]
  5. Mayer SA, Brun NC, Begtrup K, Broderick J, Davis S, Diringer MN, Skolnick BE, Steiner T: Recombinant activated factor VII for acute intracerebral hemorrhage. N Engl J Med. 2005 Feb 24;352(8):777-85. [PubMed:15728810 ]
External Links
ATC CodesB02BD08
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous1.2 mg
Powder, for solutionIntravenous2.4 mg
Powder, for solutionIntravenous4.8 mg
Kit; powder, for solutionIntravenous1 mg
Kit; powder, for solutionIntravenous2 mg
Kit; powder, for solutionIntravenous5 mg
Kit; powder, for solutionIntravenous8 mg
Injection, powder, for solutionIntravenous100 KIU
Injection, powder, for solutionIntravenous250 KIU
Injection, powder, for solutionIntravenous400 KIU
Injection, powder, for solutionIntravenous50 KIU
Kit
Prices
Unit descriptionCostUnit
Novoseven 1200 mcg vial1.64USD vial
Novoseven 2400 mcg vial1.64USD vial
Novoseven 4800 mcg vial1.64USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point58 °CPetersen, L.C. et al., Eur. J. Biochem 261: 124-129 (1999)
hydrophobicity-0.311Not Available
isoelectric point6.09Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
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
Molecular Weight:
54731.255 Da
References
  1. Malinvaud G: [Reflections on the use of PPSB fraction (Prothrombin-proconvertin-Stuart factor-antihemophilic factor B)]. Transfusion (Paris). 1966;9(3):245-54. [PubMed:5969560 ]
  2. BLATRIX C, SOULIER JP: [Preparation of a fraction rich in prothrombin, proconvertin, Stuart factor and antihemophilic factor B (P.P.B. fraction)]. Pathol Biol (Paris). 1959 Dec;7:2477-86. [PubMed:13801371 ]
  3. HERMANSKY F, VITEK J: The role of proconvertin and Stuart factor in the inactivation of tissue thromboplastin by serum. Experientia. 1960 Oct 15;16:455-6. [PubMed:13713641 ]
  4. GAERTNER H, CAEN J: [FUNCTIONAL RELATION BETWEEN ERYTHROPLASTIN (ERYTHROCYTE COAGULANT FACTOR) AND PLASMA FACTORS: PROACCELERIN (V), PROCONVERTIN (VII) AND STUART FACTOR(X)]. Acta Physiol Pol. 1964 Mar-Apr;15:237-43. [PubMed:14227143 ]
  5. DIDISHEIM P, LOEB J, BLATRIX C, SOULIER JP: Preparation of a human plasma fraction rich in prothrombin, proconvertin, Stuart factor, and PTC and a study of its activity and toxicity in rabbits and man. J Lab Clin Med. 1959 Feb;53(2):322-30. [PubMed:13621053 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protease binding
Specific Function:
Initiates blood coagulation by forming a complex with circulating factor VII or VIIa. The [TF:VIIa] complex activates factors IX or X by specific limited protolysis. TF plays a role in normal hemostasis by initiating the cell-surface assembly and propagation of the coagulation protease cascade.
Gene Name:
F3
Uniprot ID:
P13726
Molecular Weight:
33067.3 Da
References
  1. HERMANSKY F, VITEK J: The role of proconvertin and Stuart factor in the inactivation of tissue thromboplastin by serum. Experientia. 1960 Oct 15;16:455-6. [PubMed:13713641 ]
  2. Rogers KS, Barton CL, Benson PA, Green RA: Effects of single-dose L-asparaginase on coagulation values in healthy dogs and dogs with lymphoma. Am J Vet Res. 1992 Apr;53(4):580-4. [PubMed:1586032 ]
  3. Christensen NJ: Measurements of some blood clotting factors using a centrifugal analyser (Multistat III). Scand J Clin Lab Invest. 1983 Oct;43(6):521-6. [PubMed:6658368 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type peptidase activity
Specific Function:
Plays an essential role in cell growth and maintenance of cell morphology. May mediate the activating cleavage of HGF and MST1/HGFL. Plays a role in the proteolytic processing of ACE2.
Gene Name:
HPN
Uniprot ID:
P05981
Molecular Weight:
45011.01 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type endopeptidase inhibitor activity
Specific Function:
Inhibits factor X (X(a)) directly and, in a Xa-dependent way, inhibits VIIa/tissue factor activity, presumably by forming a quaternary Xa/LACI/VIIa/TF complex. It possesses an antithrombotic action and also the ability to associate with lipoproteins in plasma.
Gene Name:
TFPI
Uniprot ID:
P10646
Molecular Weight:
35014.835 Da
References
  1. Mine S, Yamazaki T, Miyata T, Hara S, Kato H: Structural mechanism for heparin-binding of the third Kunitz domain of human tissue factor pathway inhibitor. Biochemistry. 2002 Jan 8;41(1):78-85. [PubMed:11772005 ]
  2. Narita M, Bu G, Olins GM, Higuchi DA, Herz J, Broze GJ Jr, Schwartz AL: Two receptor systems are involved in the plasma clearance of tissue factor pathway inhibitor in vivo. J Biol Chem. 1995 Oct 20;270(42):24800-4. [PubMed:7559599 ]
  3. Stassens P, Bergum PW, Gansemans Y, Jespers L, Laroche Y, Huang S, Maki S, Messens J, Lauwereys M, Cappello M, Hotez PJ, Lasters I, Vlasuk GP: Anticoagulant repertoire of the hookworm Ancylostoma caninum. Proc Natl Acad Sci U S A. 1996 Mar 5;93(5):2149-54. [PubMed:8700900 ]
  4. Lee AY, Vlasuk GP: Recombinant nematode anticoagulant protein c2 and other inhibitors targeting blood coagulation factor VIIa/tissue factor. J Intern Med. 2003 Oct;254(4):313-21. [PubMed:12974870 ]
  5. Hansen CB, Pyke C, Petersen LC, Rao LV: Tissue factor-mediated endocytosis, recycling, and degradation of factor VIIa by a clathrin-independent mechanism not requiring the cytoplasmic domain of tissue factor. Blood. 2001 Mar 15;97(6):1712-20. [PubMed:11238112 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Gamma-glutamyl carboxylase activity
Specific Function:
Mediates the vitamin K-dependent carboxylation of glutamate residues to calcium-binding gamma-carboxyglutamate (Gla) residues with the concomitant conversion of the reduced hydroquinone form of vitamin K to vitamin K epoxide.
Gene Name:
GGCX
Uniprot ID:
P38435
Molecular Weight:
87560.065 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Bouwman CA, Van Dam E, Fase KM, Koppe JG, Seinen W, Thijssen HH, Vermeer C, Van den Berg M: Effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin or 2,2',4,4',5,5'-hexachlorobiphenyl on vitamin K-dependent blood coagulation in male and female WAG/Rij-rats. Chemosphere. 1999 Feb;38(3):489-505. [PubMed:10901669 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type peptidase activity
Specific 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 f...
Gene Name:
F7
Uniprot ID:
P08709
Molecular Weight:
51593.465 Da
References
  1. Perera L, Darden TA, Pedersen LG: Probing the structural changes in the light chain of human coagulation factor VIIa due to tissue factor association. Biophys J. 1999 Jul;77(1):99-113. [PubMed:10388743 ]
  2. Shapiro A: Inhibitor treatment: state of the art. Semin Hematol. 2001 Oct;38(4 Suppl 12):26-34. [PubMed:11735107 ]
  3. Shapiro A: Inhibitor treatment: state of the art. Dis Mon. 2003 Jan;49(1):22-38. [PubMed:12525826 ]
  4. Siddiqui MA, Scott LJ: Recombinant factor VIIa (Eptacog Alfa): a review of its use in congenital or acquired haemophilia and other congenital bleeding disorders. Drugs. 2005;65(8):1161-77. [PubMed:15907148 ]
  5. Rizoli SB, Chughtai T: The emerging role of recombinant activated Factor VII (rFVIIa) in the treatment of blunt traumatic haemorrhage. Expert Opin Biol Ther. 2006 Jan;6(1):73-81. [PubMed:16370916 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23