Target Information

Target General Infomation
Target ID
T83369
Former ID
TTDC00078
Target Name
Coagulation factor IX
Gene Name
F9
Synonyms
Christmas factor; Factor IX; PTC; Plasma thromboplastin component; F9
Target Type
Successful
Disease Blood forming organ disorders [ICD10: D75.9]
Factor IX deficiency [ICD10: D67]
Factor IX deficiency; Haemophilia B [ICD9:286.1; ICD10: D67]
Hemophilia A [ICD9: 286; ICD10: D66]
Hemophilia [ICD9: 286; ICD10: D66-D68]
Sepsis [ICD9: 995.91; ICD10: A40, A41]
Thrombosis; Coronary artery disease; Vascular diseases [ICD9: 325, 410-414, 429.2, 430-459, 437.6, 453, 671.5, 671.9; ICD10: G45-G46, I20-I25, I60-I95, I80-I82]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Unspecified [ICD code not available]
Function
Factor IX is a vitamin K-dependent plasma protein that participates in the intrinsic pathway of blood coagulation by converting factor X to its active form in the presence of Ca(2+) ions, phospholipids, and factor VIIIa.
BioChemical Class
Peptidase
Target Validation
T83369
UniProt ID
P00740
EC Number
EC 3.4.21.22
Sequence
MQRVNMIMAESPGLITICLLGYLLSAECTVFLDHENANKILNRPKRYNSGKLEEFVQGNL
ERECMEEKCSFEEAREVFENTERTTEFWKQYVDGDQCESNPCLNGGSCKDDINSYECWCP
FGFEGKNCELDVTCNIKNGRCEQFCKNSADNKVVCSCTEGYRLAENQKSCEPAVPFPCGR
VSVSQTSKLTRAETVFPDVDYVNSTEAETILDNITQSTQSFNDFTRVVGGEDAKPGQFPW
QVVLNGKVDAFCGGSIVNEKWIVTAAHCVETGVKITVVAGEHNIEETEHTEQKRNVIRII
PHHNYNAAINKYNHDIALLELDEPLVLNSYVTPICIADKEYTNIFLKFGSGYVSGWGRVF
HKGRSALVLQYLRVPLVDRATCLRSTKFTIYNNMFCAGFHEGGRDSCQGDSGGPHVTEVE
GTSFLTGIISWGEECAMKGKYGIYTKVSRYVNWIKEKTKLT
Drugs and Mode of Action
Drug(s) CSL-654 Drug Info Phase 3 Factor IX deficiency [524630]
TTP889 Drug Info Phase 2 Blood forming organ disorders [536572]
AMT-060 Drug Info Phase 1/2 Factor IX deficiency [548603]
RG6013 Drug Info Phase 1/2 Hemophilia A [549416]
AAV2-hFIX16 Drug Info Phase 1 Factor IX deficiency [522086]
N9-GP Drug Info Phase 1 Factor IX deficiency; Haemophilia B [523545]
RB-006 Drug Info Discontinued in Phase 3 Thrombosis; Coronary artery disease; Vascular diseases [547853]
Trenonacog alfa Drug Info Discontinued in Phase 3 Unspecified [1559854]
SB 249417 Drug Info Discontinued in Phase 1 Sepsis [546894]
Draculin Drug Info Terminated Thrombosis [545778]
Recombinant Factor IX Drug Info Terminated Factor IX deficiency [549852]
Inhibitor 2-amidino-4-iodobenzothiophene Drug Info [530682]
4-Benzyloxybenzo[b]thiophene-2-carboxamidine Drug Info [530682]
4-Phenyl-benzo[b]thiophene-2-carboxamidine Drug Info [530682]
5-Benzyloxy-benzo[b]thiophene-2-carboxamidine Drug Info [530682]
6-Benzyloxybenzo[b]thiophene-2-carboxamidine Drug Info [530682]
compound 57 Drug Info [530681]
Gamma-Carboxy-Glutamic Acid Drug Info [551393]
RAZAXABAN Drug Info [527987]
RB-006 Drug Info [537273]
TTP889 Drug Info [536262], [536572]
Modulator AAV2-hFIX16 Drug Info [544166]
AMT-060 Drug Info [550344]
BNP-FIX Drug Info [543608]
CSL-654 Drug Info [544258]
Draculin Drug Info [534730]
F-9TG Drug Info [543608]
Factor IX-XTEN Drug Info [543608]
MG-1104 Drug Info [543608]
MOD-3012 Drug Info [543608]
N9-GP Drug Info [531467]
Recombinant Factor IX Drug Info [532997]
Trenonacog alfa Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Complement and coagulation cascades
PANTHER Pathway Blood coagulation
PathWhiz Pathway Coagulation
Reactome Extrinsic Pathway of Fibrin Clot Formation
Intrinsic 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)
References
Ref 522086ClinicalTrials.gov (NCT00515710) LTFU for Gene Transfer Subjects With Hemophilia B. U.S. National Institutes of Health.
Ref 523545ClinicalTrials.gov (NCT01395810) Safety and Efficacy of NNC-0156-0000-0009 After Long-Term Exposure in Patients With Haemophilia B: An Extension to Trials NN7999-3747 and NN7999-3773. U.S. National Institutes of Health.
Ref 524630ClinicalTrials.gov (NCT02053792) A Safety and Efficacy Extension Study of a Recombinant Fusion Protein Linking Coagulation Factor IX With Albumin (rIX-FP) in Patients With Hemophilia B. U.S. NationalInstitutes of Health.
Ref 536572Partial factor IXa inhibition with TTP889 for prevention of venous thromboembolism: an exploratory study. J Thromb Haemost. 2008 Mar;6(3):457-63. Epub 2007 Dec 12.
Ref 545778Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004668)
Ref 546894Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010912)
Ref 547853Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019932)
Ref 548603Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026919)
Ref 549416Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036852)
Ref 549852Clinical pipeline report, company report or official report of Baxter 1nternational.
Ref 1559854Pharmacokinetic properties of IB1001, an investigational recombinant factor IX, in patients with haemophilia B: repeat pharmacokinetic evaluation and sialylation analysis.Haemophilia.2012 Nov;18(6):881-7.
Ref 526314Pharmacokinetic and pharmacodynamic modeling of humanized anti-factor IX antibody (SB 249417) in humans. Clin Pharmacol Ther. 2002 Apr;71(4):235-45.
Ref 527987Bioorg Med Chem Lett. 2006 Apr 1;16(7):1795-8. Epub 2006 Jan 24.Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
Ref 530681Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors. J Med Chem. 2010 Feb 25;53(4):1473-82.
Ref 530682J Med Chem. 2010 Feb 25;53(4):1465-72.Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.
Ref 531467Enhanced pharmacokinetic properties of a glycoPEGylated recombinant factor IX: a first human dose trial in patients with hemophilia B. Blood. 2011 Sep 8;118(10):2695-701.
Ref 532739Anti-factor IXa/X bispecific antibody (ACE910): hemostatic potency against ongoing bleeds in a hemophilia A model and the possibility of routine supplementation. J Thromb Haemost. 2014 Feb;12(2):206-13.
Ref 532997BAX326 (RIXUBIS): a novel recombinant factor IX for the control and prevention of bleeding episodes in adults and children with hemophilia B. Ther Adv Hematol. 2014 Oct;5(5):168-80.
Ref 534730Expression of biological activity of draculin, the anticoagulant factor from vampire bat saliva, is strictly dependent on the appropriate glycosylation of the native molecule. Biochim Biophys Acta. 1998 Oct 23;1425(2):291-9.
Ref 536262Oral anticoagulants in development: focus on thromboprophylaxis in patients undergoing orthopaedic surgery. Drugs. 2006;66(11):1411-29.
Ref 536572Partial factor IXa inhibition with TTP889 for prevention of venous thromboembolism: an exploratory study. J Thromb Haemost. 2008 Mar;6(3):457-63. Epub 2007 Dec 12.
Ref 537273In-vitro evaluation of anti-factor IXa aptamer on thrombin generation, clotting time, and viscoelastometry. Thromb Haemost. 2009 May;101(5):827-33.
Ref 543608(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: 2364).
Ref 544166Assessing the potential for AAV vector genotoxicity in a murine model. Correction in: Blood. 2011 June 16; 117(24): 6739.
Ref 544258Safety and pharmacokinetics of a novel recombinant fusion protein linking coagulation factor IX with albumin (rIX-FP) in hemophilia B patients. Blood. 2012 September 20; 120(12): 2405-2411.
Ref 550344Phase I/II clinical trial of AMT-060 for treating hemophilia B. uniQure N.V.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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