Target Information

Target General Infomation
Target ID
T84631
Former ID
TTDS00203
Target Name
Coagulation factor Xa
Gene Name
F10
Synonyms
Activated coagulation factor X; Factor Xa; Fxa; F10
Target Type
Successful
Disease Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Atrial fibrillation [ICD9: 272, 427.31; ICD10: E78, I48]
Acute coronary syndrome [ICD9: 444; ICD10: I74]
Angina pectoris [ICD9: 413; ICD10: I20]
Bleeding [ICD9: 444, 453; ICD10: I74, I80-I82]
Blood coagulation disorders [ICD10: D65-D68]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Coagulation [ICD10: I80-I82]
Deep venous clots [ICD9: 453.4; ICD10: I80.2]
Deep vein thrombosis [ICD9: 437.6, 453, 453.40, 671.5, 671.9; ICD10: I80-I82, I80.2]
Hematology [ICD10: D50-D77]
Hemophilia [ICD9: 286; ICD10: D66-D68]
Haemophilia B; Christmas disease [ICD9:286.1; ICD10: D67]
Prophylaxis of deep vein thrombosis [ICD9: 437.6, 453, 453.40, 671.5, 671.9; ICD10: I80-I82, I80.2]
Renal cancer [ICD9: 140-229, 189; ICD10: C64]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Thromboembolism [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Thromboembolic disorders [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Venous thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Venous thromboembolism [ICD9: 453; ICD10: I80-I82]
Unspecified [ICD code not available]
Function
Factor Xa is avitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
BioChemical Class
Peptidase
Target Validation
T84631
UniProt ID
P00742
EC Number
EC 3.4.21.6
Sequence
MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE
TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN
CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR
KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE
CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE
AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI
VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG
GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE
VITSSPLK
Structure
1C5M; 1EZQ; 1F0R; 1F0S; 1FAX; 1FJS; 1FXY; 1G2L; 1G2M; 1HCG; 1IOE; 1IQE; 1IQF; 1IQG; 1IQH; 1IQI; 1IQJ; 1IQK; 1IQL; 1IQM; 1IQN; 1KSN; 1LPG; 1LPK; 1LPZ; 1LQD; 1MQ5; 1MQ6; 1MSX; 1NFU; 1NFW; 1NFX; 1NFY; 1NL8; 1P0S; 1V3X; 1WU1; 1XKA; 1XKB; 1Z6E; 2BMG; 2BOH; 2BOK; 2BQ6; 2BQ7; 2BQW; 2CJI; 2D1J; 2EI6; 2EI7; 2EI8; 2FZZ; 2G00; 2GD4; 2H9E; 2J2U; 2J34; 2J38; 2J4I; 2J94; 2J95; 2JKH; 2P16; 2P3F; 2P3T; 2P3U; 2P93; 2P94; 2P95; 2PHB; 2PR3; 2Q1J; 2RA0;2UWL; 2UWO; 2UWP; 2VH0; 2VH6; 2VVC; 2VVU; 2VVV; 2VWL; 2VWM; 2VWN; 2VWO; 2W26; 2W3I; 2W3K; 2WYG; 2WYJ; 2XBV; 2XBW; 2XBX; 2XBY; 2XC0; 2XC4; 2XC5; 2Y5F; 2Y5G; 2Y5H; 2Y7X; 2Y7Z; 2Y80; 2Y81; 2Y82; 3CEN; 3CS7; 3ENS; 3FFG; 3HPT; 3IIT; 3K9X; 3KL6; 3KQB; 3KQC; 3KQD; 3KQE; 3LIW; 3M36; 3M37; 3Q3K; 3SW2; 3TK5; 3TK6; 4A7I; 4BTI; 4BTT; 4BTU; 1C5M; 1EZQ; 1F0R; 1F0S; 1FAX; 1FJS; 1FXY; 1G2L; 1G2M; 1HCG; 1IOE; 1IQE; 1IQF; 1IQG; 1IQH; 1IQI; 1IQJ; 1IQK; 1IQL; 1IQM; 1IQN; 1KSN; 1LPG; 1LPK; 1LPZ; 1LQD; 1MQ5; 1MQ6; 1MSX; 1NFU; 1NFW; 1NFX; 1NFY; 1NL8; 1P0S; 1V3X; 1WU1; 1XKA; 1XKB; 1Z6E; 2BMG; 2BOH; 2BOK; 2BQ6; 2BQ7; 2BQW; 2CJI; 2D1J; 2EI6; 2EI7; 2EI8; 2FZZ; 2G00; 2GD4; 2H9E; 2J2U; 2J34; 2J38; 2J4I; 2J94; 2J95; 2JKH; 2P16; 2P3F; 2P3T; 2P3U; 2P93; 2P94; 2P95; 2PHB; 2PR3; 2Q1J; 2RA0; 2UWL; 2UWO; 2UWP; 2VH0; 2VH6; 2VVC; 2VVU; 2VVV; 2VWL; 2VWM; 2VWN; 2VWO; 2W26; 2W3I; 2W3K; 2WYG; 2WYJ; 2XBV; 2XBW; 2XBX; 2XBY; 2XC0; 2XC4; 2XC5; 2Y5F; 2Y5G; 2Y5H; 2Y7X; 2Y7Z; 2Y80; 2Y81; 2Y82; 3CEN; 3CS7; 3ENS; 3FFG; 3HPT; 3IIT; 3K9X; 3KL6; 3KQB; 3KQC; 3KQD; 3KQE; 3LIW; 3M36; 3M37; 3Q3K; 3SW2; 3TK5; 3TK6; 4A7I; 4BTI; 4BTT; 4BTU
Drugs and Mode of Action
Drug(s) Apixaban Drug Info Approved Thrombosis [532210], [541527]
BETRIXABAN Drug Info Approved Venous thromboembolism [889446]
Certoparin sodium Drug Info Approved Deep vein thrombosis [551871]
Coagulation Factor IX Drug Info Approved Haemophilia B; Christmas disease [533123], [550670]
Dalteparin Sodium Drug Info Approved Hematology [551871]
Danaparoid Drug Info Approved Deep venous clots [535201], [541886]
DU-176b Drug Info Approved Atrial fibrillation [524299], [542568]
Fondaparinux sodium Drug Info Approved Venous thrombosis [536361]
Lmw heparin Drug Info Approved Coagulation [551871]
Nadroparin calcium Drug Info Approved Coagulation [551871]
Rivaroxaban Drug Info Approved Prophylaxis of deep vein thrombosis [531783], [541524]
Human coagulation factor X Drug Info BLA submitted Renal cancer [550389]
BETRIXABAN Drug Info Phase 3 Cerebrovascular ischaemia [523883]
MELAGATRAN Drug Info Phase 3 Discovery agent [521709], [541520]
PRT4445 Drug Info Phase 3 Bleeding [549059]
Semuloparin Drug Info Phase 3 Venous thromboembolism [531405], [531982]
SSR-126517E Drug Info Phase 3 Thrombosis [521848]
SR-123781A Drug Info Phase 2/3 Venous thrombosis [521845]
Antistasin Drug Info Phase 2 Attention deficit hyperactivity disorder [531305]
EP-217609 Drug Info Phase 2 Thrombosis [549210]
GW-813893 Drug Info Phase 2 Thromboembolism [522136]
LY-517717 Drug Info Phase 2 Thrombosis [521582]
BI-11634 Drug Info Phase 1 Thrombosis [549573]
BIBT986 Drug Info Phase 1 Thrombosis [548355]
EP-42675 Drug Info Phase 1 Thrombosis [548235]
GCC-4401 Drug Info Phase 1 Thrombosis [524453]
R-1663 Drug Info Phase 1 Blood coagulation disorders [548346]
SSR-128428 Drug Info Phase 1 Thromboembolism [547951]
CS-3030 Drug Info Preclinical Thrombosis [548159]
Darexaban maleate Drug Info Discontinued in Phase 3 Acute coronary syndrome [547958]
Idraparinux Drug Info Discontinued in Phase 3 Thrombosis [546816]
Otamixaban Drug Info Discontinued in Phase 3 Angina pectoris [547363]
Octopamine Drug Info Discontinued in Phase 2a Thromboembolic disorders [525357], [539364]
DX-9065 Drug Info Discontinued in Phase 2 Blood coagulation disorders [526864], [545649]
DX-9065a Drug Info Discontinued in Phase 2 Angina pectoris [545649]
PD-348292 Drug Info Discontinued in Phase 2 Thrombosis [548310]
TAK-442 Drug Info Discontinued in Phase 2 Thrombosis [548667]
AVE-3247 Drug Info Discontinued in Phase 1 Thrombosis [547052]
DPC 423 Drug Info Discontinued in Phase 1 Thrombosis [547044]
EMD-503982 Drug Info Discontinued in Phase 1 Thrombosis [548116]
JTV-803 Drug Info Discontinued in Phase 1 Thrombosis [547277]
YM-75466 Drug Info Discontinued in Phase 1 Thrombosis [546826]
ZD-4927 Drug Info Discontinued in Phase 1 Thrombosis [546656]
Draculin Drug Info Terminated Thrombosis [545778]
Hirufaxin Drug Info Terminated Thrombosis [547022]
Nematode anticoagulant proteins Drug Info Terminated Angina pectoris [546177]
YM60828 Drug Info Terminated Discovery agent [546601]
Inhibitor 1,2,3,4,6-penta-O-galloyl-beta-D-glucose Drug Info [534762]
3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate Drug Info [527883]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Drug Info [527397]
5-desgalloylstachyurin Drug Info [534762]
Antistasin Drug Info [535352]
Apixaban Drug Info [549835], [549974]
AVE-3247 Drug Info [531405], [531982]
Azaphenylalanine derivative Drug Info [526986]
Beta-Hydroxy Aspartic Acid Drug Info [551374]
BI-11634 Drug Info [531405], [531982]
BIBT986 Drug Info [528309]
BMS-269223 Drug Info [530503]
BMS-344577 Drug Info [530503]
BMS-740808 Drug Info [529078]
CASUARIIN Drug Info [534762]
Chloroaniline 1 Drug Info [535710]
CS-3030 Drug Info [531405], [531982]
D-Pro-Phe-Arg chloromethyl ketone Drug Info [529454]
Danaparoid Drug Info [535592]
Darexaban maleate Drug Info [531926]
DPC 423 Drug Info [535405]
DX-9065 Drug Info [531405], [531982]
DX-9065a Drug Info [535685]
EMD-503982 Drug Info [531405], [531982]
Fondaparinux sodium Drug Info [535484], [535819]
Gamma-Carboxy-Glutamic Acid Drug Info [551393]
GC-2107 Drug Info [531405], [531982]
GCC-4401 Drug Info [531405], [531982]
GW-813893 Drug Info [531405], [531982]
Hirufaxin Drug Info [531405], [531982]
Idraparinux Drug Info [549823]
JTV-803 Drug Info [531405], [531982]
Lefaxin Drug Info [535352]
LY-517717 Drug Info [531405], [531982]
M55113 Drug Info [535279]
M55551 Drug Info [535566]
MELAGATRAN Drug Info [528066]
Molecule 11 Drug Info [535485]
Octopamine Drug Info [537045], [537289]
Otamixaban Drug Info [549823]
PD-348292 Drug Info [549974], [551665]
PEDUNCULAGIN Drug Info [534762]
PhSO2-Gly-(Me-Gly)-Arg-(2-thiazole) Drug Info [529193]
PRT-064445 Drug Info [531405], [531982]
R-1663 Drug Info [531405], [531982]
RAZAXABAN Drug Info [529078]
SC-83157 Drug Info [535728]
Semuloparin Drug Info [531405], [531982]
SF303 Drug Info [535405]
SK509 Drug Info [535405]
SK549 Drug Info [534887]
SK554 Drug Info [535352]
SN429 Drug Info [535728]
SSR-126517E Drug Info [531405], [531982]
T01312 Drug Info [535782]
TAK-442 Drug Info [551717]
Tellimagrandin II Drug Info [534762]
Tick anticoagulant peptide Drug Info [535302], [535352]
Tick anticoagulant peptide (TAP) Drug Info [535352]
YM-75466 Drug Info [531405], [531982]
YM-96765 Drug Info [535942]
YM60828 Drug Info [535352]
ZD-4927 Drug Info [531405], [531982]
ZK-810388 Drug Info [528872]
ZK-814048 Drug Info [528872]
Modulator BETRIXABAN Drug Info
Certoparin sodium Drug Info [525658], [534676], [536361]
CI-1031 Drug Info
Dalteparin Sodium Drug Info [556264]
Draculin Drug Info [534730]
DU-176b Drug Info [543603]
EP-217609 Drug Info
EP-42675 Drug Info [532552]
Human coagulation factor X Drug Info [531405], [531982]
Lmw heparin Drug Info [536361]
Nadroparin calcium Drug Info [526062], [536361]
Nematode anticoagulant proteins Drug Info
PRT4445 Drug Info [531405], [531982]
Recombinant coagulation factors Drug Info [531405], [531982]
Recombinant Factor X Drug Info [531405], [531982]
Rivaroxaban Drug Info [551871]
SR-123781A Drug Info [535183]
SSR-128428 Drug Info
ZK-813039 Drug Info [528872]
Activator Coagulation Factor IX Drug Info [536124]
Antagonist DT-831j Drug Info [531405], [531982]
EP-37 Drug Info [531405], [531982]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Complement and coagulation cascades
PANTHER Pathway Blood coagulation
Pathway Interaction Database Beta2 integrin cell surface interactions
PathWhiz Pathway Coagulation
Reactome Extrinsic Pathway of Fibrin Clot Formation
Intrinsic Pathway of Fibrin Clot Formation
Common 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
Human Complement System
gamma carboxylation, hypusine formation and arylsulfatase activation
Blood Clotting Cascade
Formation of Fibrin Clot (Clotting Cascade)
References
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Ref 521709ClinicalTrials.gov (NCT00206089) Melagatran/Ximelagatran Versus Enoxaparin for the Prevention of Venous Thromboembolic Events. U.S. National Institutes of Health.
Ref 521845ClinicalTrials.gov (NCT00338897) Dose Ranging Study in Elective Total Hip Replacement Surgery. U.S. National Institutes of Health.
Ref 521848ClinicalTrials.gov (NCT00345618) Clinical Study Assessing SSR126517E Injections Once-weekly in Pulmonary Embolism Therapeutic Approach. U.S. National Institutes of Health.
Ref 522136ClinicalTrials.gov (NCT00541320) Phase IIa Venous Thromboembolism (VTE) Prevention Study In Total Knee Replacement (TKR). U.S. National Institutes of Health.
Ref 523883ClinicalTrials.gov (NCT01583218) Acute Medically Ill VTE Prevention With Extended Duration Betrixaban Study (The APEX Study). U.S. National Institutes of Health.
Ref 524299ClinicalTrials.gov (NCT01857622) Safety and Pharmacokinetics Study of DU-176b Administered to Non-valvular Atrial Fibrillation With Severe Renal Impairment. U.S. National Institutes of Health.
Ref 524453ClinicalTrials.gov (NCT01954238) A Study to Access Safety, Tolerability, Pharmacokinetics(PK) and Pharmacodynamics(PD) of Orally Administered GCC-4401C in Healthy Volunteers. U.S. National Institutesof Health.
Ref 525357Juvenile hormone and octopamine in the regulation of division of labor in honey bee colonies. Horm Behav. 2002 Sep;42(2):222-31.
Ref 526864DX-9065a Daiichi. Curr Opin Investig Drugs. 2003 Sep;4(9):1105-12.
Ref 531305The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor. Nat Rev Drug Discov. 2011 Jan;10(1):61-75.
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Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
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Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
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Ref 541520(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: 6382).
Ref 541524(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: 6388).
Ref 541527(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: 6390).
Ref 541886(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: 6804).
Ref 542568(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: 7575).
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Ref 528872J Med Chem. 2007 Jun 28;50(13):2967-80. Epub 2007 May 31.Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors.
Ref 529078J Med Chem. 2007 Nov 1;50(22):5339-56. Epub 2007 Oct 3.Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban,BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Ref 529193Bioorg Med Chem. 2008 Feb 15;16(4):1562-95. Epub 2007 Nov 6.Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Ref 529454J Med Chem. 2008 Jun 12;51(11):3077-80. Epub 2008 May 7.Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.
Ref 530503Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
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Ref 531926The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4. Br J Clin Pharmacol. 2013 Feb;75(2):440-9.
Ref 531982Semuloparin for the prevention of venous thromboembolic events in cancer patients. Drugs Today (Barc). 2012 Jul;48(7):451-7.
Ref 532552EP42675, a synthetic parenteral dual-action anticoagulant: pharmacokinetics, pharmacodynamics, and absence of interactions with antiplatelet drugs. J Thromb Haemost. 2014 Jan;12(1):24-33.
Ref 534676Low molecular weight heparins for venous thromboembolism. Drug Ther Bull. 1998 Apr;36(4):25-9.
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 534762J Nat Prod. 1998 Nov;61(11):1356-60.Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.
Ref 534887Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2. J Med Chem. 1999 Jul 29;42(15):2760-73.
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