Target Information

Target General Infomation
Target ID
T43332
Former ID
TTDR00947
Target Name
Coagulation factor VII
Gene Name
F7
Synonyms
Eptacog alfa; Factor VII; Proconvertin; SPCA; Serum prothrombin conversion accelerator; F7
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Bleeding [ICD9: 444, 453; ICD10: I74, I80-I82]
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Factor VII deficiency [ICD10: D68]
Factor IX deficiency [ICD10: D67]
Hemophilia [ICD9: 286; ICD10: D66-D68]
Function
Initiates the extrinsic pathway of bloodcoagulation. 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 factor IXa in the presence of tissue factor and calcium.
BioChemical Class
Peptidase
Target Validation
T43332
UniProt ID
P08709
EC Number
EC 3.4.21.21
Sequence
MVSQALRLLCLLLGLQGCLAAGGVAKASGGETRDMPWKPGPHRVFVTQEEAHGVLHRRRR
ANAFLEELRPGSLERECKEEQCSFEEAREIFKDAERTKLFWISYSDGDQCASSPCQNGGS
CKDQLQSYICFCLPAFEGRNCETHKDDQLICVNENGGCEQYCSDHTGTKRSCRCHEGYSL
LADGVSCTPTVEYPCGKIPILEKRNASKPQGRIVGGKVCPKGECPWQVLLLVNGAQLCGG
TLINTIWVVSAAHCFDKIKNWRNLIAVLGEHDLSEHDGDEQSRRVAQVIIPSTYVPGTTN
HDIALLRLHQPVVLTDHVVPLCLPERTFSERTLAFVRFSLVSGWGQLLDRGATALELMVL
NVPRLMTQDCLQQSRKVGDSPNITEYMFCAGYSDGSKDSCKGDSGGPHATHYRGTWYLTG
IVSWGQGCATVGHFGVYTRVSQYIEWLQKLMRSEPRPGVLLRAPFP
Drugs and Mode of Action
Drug(s) Factor viia Drug Info Approved Hemophilia [551871]
BAX-817 Drug Info Phase 3 Hemophilia [549120]
Vatreptacog alfa (activated) Drug Info Phase 3 Bleeding [523543]
Activated recombinant FVII-albumin fusion protein Drug Info Phase 2/3 Hemophilia [525247]
Recombinant factor VIIa PEGylated liposomal Drug Info Phase 1/2 Factor VII deficiency [530934]
CB-813 Drug Info Phase 1 Hemophilia [548685]
Eptacog alfa intravenous Drug Info Phase 1 Hemophilia [524674]
F-7TG Drug Info Phase 1 Hemophilia [551675]
compound 1 Drug Info Clinical trial Alzheimer disease [528175], [541676]
BAY 86-6150 Drug Info Discontinued in Phase 2/3 Hemophilia [548091]
RNAPc2 Drug Info Discontinued in Phase 2 Colorectal cancer [546176]
Inhibitor 4-(3,4-Diethoxy-benzylamino)-benzamidine Drug Info [527397]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Drug Info [527397]
BAX-817 Drug Info [549853]
compound 1 Drug Info [528175]
compound 11 Drug Info [527967]
Fucose Drug Info [551393]
Modulator Activated recombinant FVII-albumin fusion protein Drug Info [523809]
BAY 86-6150 Drug Info [551671]
CB-813 Drug Info [550533]
Eptacog alfa intravenous Drug Info [529378]
F-7TG Drug Info [543607]
Factor viia Drug Info [543607]
Factor-VIIa-XTEN Drug Info [543607]
Human recombinant factor VIIa Drug Info [543607]
Long-acting Factor VII conjugate Drug Info [543607]
MOD-5023 Drug Info [543607]
Recombinant factor VIIa PEGylated liposomal Drug Info [543607]
RNAPc2 Drug Info [529895]
Vatreptacog alfa (activated) Drug Info [531867]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Complement and coagulation cascades
PANTHER Pathway Angiogenesis
Blood coagulation
PathWhiz Pathway Coagulation
Reactome CLOCK,NPAS2 activates circadian gene expression
Extrinsic Pathway of Fibrin Clot Formation
Gamma-carboxylation of protein precursors
Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus
Removal of aminoterminal propeptides from gamma-carboxylated proteins
WikiPathways Complement and Coagulation Cascades
gamma carboxylation, hypusine formation and arylsulfatase activation
Blood Clotting Cascade
Formation of Fibrin Clot (Clotting Cascade)
Circadian Clock
Folate Metabolism
Vitamin B12 Metabolism
Selenium Micronutrient Network
References
Ref 523543ClinicalTrials.gov (NCT01392547) Efficacy and Safety of NNC 0078-0000-0007 in Patients With Congenital Haemophilia and Inhibitors. U.S. National Institutes of Health.
Ref 524674ClinicalTrials.gov (NCT02084810) Investigating the Bioequivalence of Eptacog Alfa A 6 mg and NovoSeven in Healthy Male Subjects. U.S. National Institutes of Health.
Ref 525247ClinicalTrials.gov (NCT02484638) Study of Recombinant Factor VIIa Fusion Protein (rVIIa-FP, CSL689) for On-demand Treatment of Bleeding Episodes in Patients With Hemophilia A or B With Inhibitors.
Ref 528175Efforts toward oral bioavailability in factor VIIa inhibitors. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3829-32. Epub 2006 May 2.
Ref 530934Safety, pharmacokinetics and efficacy of factor VIIa formulated with PEGylated liposomes in haemophilia A patients with inhibitors to factor VIII--an open label, exploratory, cross-over, phase I/II study. Haemophilia. 2010 Nov;16(6):910-8.
Ref 541676(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6552).
Ref 546176Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006762)
Ref 548091Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021847)
Ref 548685Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027663)
Ref 549120Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032604)
Ref 551675GTC BIOTHERAPEUTICS REPORTS THIRD QUARTER 2010 FINANCIAL RESULTS. U.S. Securities and Exchange Commission. October 27, 2010.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 523809ClinicalTrials.gov (NCT01542619) A Safety and Pharmacokinetics Study of a Recombinant Fusion Protein Linking Coagulation Factor VIIa With Albumin (rVIIa-FP) in Healthy Male Volunteers. U.S. National Institutes of Health.
Ref 527397Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
Ref 527967Small molecule inhibitors of plasma kallikrein. Bioorg Med Chem Lett. 2006 Apr 1;16(7):2034-6. Epub 2006 Jan 18.
Ref 528175Efforts toward oral bioavailability in factor VIIa inhibitors. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3829-32. Epub 2006 May 2.
Ref 529378Recombinant factor VIIa (eptacog alfa): a review of its use in congenital hemophilia with inhibitors, acquired hemophilia, and other congenital bleeding disorders. BioDrugs. 2008;22(2):121-36.
Ref 529895rNAPc2 inhibits colorectal cancer in mice through tissue factor. Clin Cancer Res. 2009 Jan 1;15(1):208-16.
Ref 531867Recombinant factor VIIa analog (vatreptacog alfa [activated]) for treatment of joint bleeds in hemophilia patients with inhibitors: a randomized controlled trial. J Thromb Haemost. 2012 Jan;10(1):81-9.
Ref 543607(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2363).
Ref 549853Clinical pipeline report, company report or official report of Baxter.
Ref 550533Clinical pipeline report, company report or official report of Catalyst Biosciences.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551671Bayer HealthCare and Maxygen Announce Hematology Agreement. U.S. Securities and Exchange Commission. July 2, 2008.

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