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 Angina pectoris [ICD9: 413; ICD10: I20]
Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Atrial fibrillation [ICD9: 272, 427.31; ICD10: E78, I48]
Acute coronary syndrome [ICD9: 444; ICD10: I74]
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]
Hemophilia [ICD9: 286; ICD10: D66-D68]
Haemophilia B; Christmas disease [ICD9:286.1; ICD10: D67]
Hematology [ICD10: D50-D77]
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 [1], [2]
BETRIXABAN Drug Info Approved Venous thromboembolism [3]
Certoparin sodium Drug Info Approved Deep vein thrombosis [4]
Coagulation Factor IX Drug Info Approved Haemophilia B; Christmas disease [5], [6]
Dalteparin Sodium Drug Info Approved Hematology [4]
Danaparoid Drug Info Approved Deep venous clots [7], [8]
DU-176b Drug Info Approved Atrial fibrillation [9], [10]
Fondaparinux sodium Drug Info Approved Venous thrombosis [11]
Lmw heparin Drug Info Approved Coagulation [4]
Nadroparin calcium Drug Info Approved Coagulation [4]
Rivaroxaban Drug Info Approved Prophylaxis of deep vein thrombosis [12], [13]
Human coagulation factor X Drug Info BLA submitted Renal cancer [14]
BETRIXABAN Drug Info Phase 3 Cerebrovascular ischaemia [15]
MELAGATRAN Drug Info Phase 3 Discovery agent [16], [17]
PRT4445 Drug Info Phase 3 Bleeding [18]
Semuloparin Drug Info Phase 3 Venous thromboembolism [19], [20]
SSR-126517E Drug Info Phase 3 Thrombosis [21]
SR-123781A Drug Info Phase 2/3 Venous thrombosis [22]
Antistasin Drug Info Phase 2 Attention deficit hyperactivity disorder [23]
EP-217609 Drug Info Phase 2 Thrombosis [24]
GW-813893 Drug Info Phase 2 Thromboembolism [25]
LY-517717 Drug Info Phase 2 Thrombosis [26]
BI-11634 Drug Info Phase 1 Thrombosis [27]
BIBT986 Drug Info Phase 1 Thrombosis [28]
EP-42675 Drug Info Phase 1 Thrombosis [29]
GCC-4401 Drug Info Phase 1 Thrombosis [30]
R-1663 Drug Info Phase 1 Blood coagulation disorders [31]
SSR-128428 Drug Info Phase 1 Thromboembolism [32]
CS-3030 Drug Info Preclinical Thrombosis [33]
Darexaban maleate Drug Info Discontinued in Phase 3 Acute coronary syndrome [34]
Idraparinux Drug Info Discontinued in Phase 3 Thrombosis [35]
Otamixaban Drug Info Discontinued in Phase 3 Angina pectoris [36]
Octopamine Drug Info Discontinued in Phase 2a Thromboembolic disorders [37], [38]
DX-9065 Drug Info Discontinued in Phase 2 Blood coagulation disorders [39], [40]
DX-9065a Drug Info Discontinued in Phase 2 Angina pectoris [40]
PD-348292 Drug Info Discontinued in Phase 2 Thrombosis [41]
TAK-442 Drug Info Discontinued in Phase 2 Thrombosis [42]
AVE-3247 Drug Info Discontinued in Phase 1 Thrombosis [43]
DPC 423 Drug Info Discontinued in Phase 1 Thrombosis [44]
EMD-503982 Drug Info Discontinued in Phase 1 Thrombosis [45]
JTV-803 Drug Info Discontinued in Phase 1 Thrombosis [46]
YM-75466 Drug Info Discontinued in Phase 1 Thrombosis [47]
ZD-4927 Drug Info Discontinued in Phase 1 Thrombosis [48]
Draculin Drug Info Terminated Thrombosis [49]
Hirufaxin Drug Info Terminated Thrombosis [50]
Nematode anticoagulant proteins Drug Info Terminated Angina pectoris [51]
YM60828 Drug Info Terminated Discovery agent [52]
Inhibitor 1,2,3,4,6-penta-O-galloyl-beta-D-glucose Drug Info [53]
3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate Drug Info [54]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Drug Info [55]
5-desgalloylstachyurin Drug Info [53]
Antistasin Drug Info [56]
Apixaban Drug Info [57], [58]
AVE-3247 Drug Info [19], [20]
Azaphenylalanine derivative Drug Info [59]
Beta-Hydroxy Aspartic Acid Drug Info [60]
BI-11634 Drug Info [19], [20]
BIBT986 Drug Info [61]
BMS-269223 Drug Info [62]
BMS-344577 Drug Info [62]
BMS-740808 Drug Info [63]
CASUARIIN Drug Info [53]
Chloroaniline 1 Drug Info [64]
CS-3030 Drug Info [19], [20]
D-Pro-Phe-Arg chloromethyl ketone Drug Info [65]
Danaparoid Drug Info [66]
Darexaban maleate Drug Info [67]
DPC 423 Drug Info [68]
DX-9065 Drug Info [19], [20]
DX-9065a Drug Info [69]
EMD-503982 Drug Info [19], [20]
Fondaparinux sodium Drug Info [70], [71]
Gamma-Carboxy-Glutamic Acid Drug Info [72]
GC-2107 Drug Info [19], [20]
GCC-4401 Drug Info [19], [20]
GW-813893 Drug Info [19], [20]
Hirufaxin Drug Info [19], [20]
Idraparinux Drug Info [73]
JTV-803 Drug Info [19], [20]
Lefaxin Drug Info [56]
LY-517717 Drug Info [19], [20]
M55113 Drug Info [74]
M55551 Drug Info [75]
MELAGATRAN Drug Info [76]
Molecule 11 Drug Info [77]
Octopamine Drug Info [78], [79]
Otamixaban Drug Info [73]
PD-348292 Drug Info [58], [80]
PEDUNCULAGIN Drug Info [53]
PhSO2-Gly-(Me-Gly)-Arg-(2-thiazole) Drug Info [81]
PRT-064445 Drug Info [19], [20]
R-1663 Drug Info [19], [20]
RAZAXABAN Drug Info [63]
SC-83157 Drug Info [82]
Semuloparin Drug Info [19], [20]
SF303 Drug Info [68]
SK509 Drug Info [68]
SK549 Drug Info [83]
SK554 Drug Info [56]
SN429 Drug Info [82]
SSR-126517E Drug Info [19], [20]
T01312 Drug Info [84]
TAK-442 Drug Info [85]
Tellimagrandin II Drug Info [53]
Tick anticoagulant peptide Drug Info [86], [56]
Tick anticoagulant peptide (TAP) Drug Info [56]
YM-75466 Drug Info [19], [20]
YM-96765 Drug Info [87]
YM60828 Drug Info [56]
ZD-4927 Drug Info [19], [20]
ZK-810388 Drug Info [88]
ZK-814048 Drug Info [88]
Modulator BETRIXABAN Drug Info
Certoparin sodium Drug Info [89], [90], [11]
CI-1031 Drug Info
Dalteparin Sodium Drug Info [91]
Draculin Drug Info [92]
DU-176b Drug Info [93]
EP-217609 Drug Info
EP-42675 Drug Info [94]
Human coagulation factor X Drug Info [19], [20]
Lmw heparin Drug Info [11]
Nadroparin calcium Drug Info [95], [11]
Nematode anticoagulant proteins Drug Info
PRT4445 Drug Info [19], [20]
Recombinant coagulation factors Drug Info [19], [20]
Recombinant Factor X Drug Info [19], [20]
Rivaroxaban Drug Info [4]
SR-123781A Drug Info [96]
SSR-128428 Drug Info
ZK-813039 Drug Info [88]
Activator Coagulation Factor IX Drug Info [97]
Antagonist DT-831j Drug Info [19], [20]
EP-37 Drug Info [19], [20]
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
REF 1Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
REF 2(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 3Drugs@FDA (Edaravone)
REF 4Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 52014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
REF 6Drug information of Coagulation Factor IX, 2008. eduDrugs.
REF 7A comparison of danaparoid and lepirudin in heparin-induced thrombocytopenia. Thromb Haemost. 2001 Jun;85(6):950-7.
REF 8(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 9ClinicalTrials.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 10(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).
REF 11Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
REF 122011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
REF 13(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 14FDA Accepts BPL's Amended BLA Submission for Coagadex (Coagulation Factor X, Human). BPL Bio Products Laboratory USA, Inc.
REF 15ClinicalTrials.gov (NCT01583218) Acute Medically Ill VTE Prevention With Extended Duration Betrixaban Study (The APEX Study). U.S. National Institutes of Health.
REF 16ClinicalTrials.gov (NCT00206089) Melagatran/Ximelagatran Versus Enoxaparin for the Prevention of Venous Thromboembolic Events. U.S. National Institutes of Health.
REF 17(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 18Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031853)
REF 19Venous thromboembolism in the patient with cancer: focus on burden of disease and benefits of thromboprophylaxis. Cancer. 2011 Apr 1;117(7):1334-49.
REF 20Semuloparin for the prevention of venous thromboembolic events in cancer patients. Drugs Today (Barc). 2012 Jul;48(7):451-7.
REF 21ClinicalTrials.gov (NCT00345618) Clinical Study Assessing SSR126517E Injections Once-weekly in Pulmonary Embolism Therapeutic Approach. U.S. National Institutes of Health.
REF 22ClinicalTrials.gov (NCT00338897) Dose Ranging Study in Elective Total Hip Replacement Surgery. U.S. National Institutes of Health.
REF 23The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor. Nat Rev Drug Discov. 2011 Jan;10(1):61-75.
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033781)
REF 25ClinicalTrials.gov (NCT00541320) Phase IIa Venous Thromboembolism (VTE) Prevention Study In Total Knee Replacement (TKR). U.S. National Institutes of Health.
REF 26ClinicalTrials.gov (NCT00074828) New Oral Anticoagulant Therapy for the Prevention of Blood Clots Following Hip or Knee Replacement Surgery. U.S. National Institutes of Health.
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041083)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024917)
REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023539)
REF 30ClinicalTrials.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 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024856)
REF 32Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020651)
REF 33Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022617)
REF 34Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020726)
REF 35Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010432)
REF 36Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015497)
REF 37Juvenile hormone and octopamine in the regulation of division of labor in honey bee colonies. Horm Behav. 2002 Sep;42(2):222-31.
REF 38(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: 2149).
REF 39DX-9065a Daiichi. Curr Opin Investig Drugs. 2003 Sep;4(9):1105-12.
REF 40Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004028)
REF 41Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024432)
REF 42Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027537)
REF 43Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012558)
REF 44Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012496)
REF 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022087)
REF 46Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014748)
REF 47Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010496)
REF 48Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009534)
REF 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004668)
REF 50Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012166)
REF 51Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006763)
REF 52Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009133)
REF 53J 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 54J Med Chem. 2005 Dec 1;48(24):7592-603.3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa.
REF 55Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
REF 56Novel approaches to the treatment of thrombosis. Trends Pharmacol Sci. 2002 Jan;23(1):25-32.
REF 57Effects of the oral, direct factor Xa inhibitor apixaban on routine coagulation assays and anti-FXa assays. J Thromb Haemost. 2014 Sep;12(9):1545-53.
REF 58Pfizer. Product Development Pipeline. March 31 2009.
REF 59Bioorg Med Chem Lett. 2004 Mar 22;14(6):1563-7.Thrombin inhibitors built on an azaphenylalanine scaffold.
REF 60The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 61Pharmacokinetics and pharmacodynamics of BIBT 986, a novel small molecule dual inhibitor of thrombin and factor Xa. J Thromb Haemost. 2006 Jul;4(7):1502-9.
REF 62Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
REF 63J 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 64Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1023-8.
REF 65J Med Chem. 2008 Jun 12;51(11):3077-80. Epub 2008 May 7.Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.
REF 66Effect of factor X inhibition on coagulation activation and cytokine induction in human systemic inflammation. J Infect Dis. 2002 Nov 1;186(9):1270-6. Epub 2002 Oct 8.
REF 67The 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 68The design and synthesis of noncovalent factor Xa inhibitors. Curr Top Med Chem. 2001 Jun;1(2):137-49.
REF 69DX-9065a inhibition of factor Xa and the prothrombinase complex: mechanism of inhibition and comparison with therapeutic heparins. Thromb Haemost. 2003 Jan;89(1):112-21.
REF 70Fondaparinux, a synthetic pentasaccharide: the first in a new class of antithrombotic agents - the selective factor Xa inhibitors. Cardiovasc Drug Rev. 2002 Winter;20(1):37-52.
REF 71Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb. 2002 Sep-Dec;32(5-6):218-24.
REF 72How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 73Pharma & Vaccines. Product Development Pipeline. April 29 2009.
REF 74Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor. Chem Pharm Bull (Tokyo). 2001 Oct;49(10):1237-44.
REF 75Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as a factor Xa inhibitor II. Substituent effect on biological activities. Chem Pharm Bull (Tokyo). 2002 Sep;50(9):1187-94.
REF 76Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7. Epub 2006 Mar 6.Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.
REF 77Role of tissue factor pathway inhibitor in the regulation of tissue factor-dependent blood coagulation. Cardiovasc Drug Rev. 2002 Winter;20(1):67-80.
REF 78AVE5026, a new hemisynthetic ultra-low-molecular-weight heparin for the prevention of venous thromboembolism in patients after total knee replacement surgery--TREK: a dose-ranging study. J Thromb Haemost. 2009 Apr;7(4):566-72. Epub 2009 Jan 24.
REF 79Description of the chemical and pharmacological characteristics of a new hemisynthetic ultra-low-molecular-weight heparin, AVE5026. J Thromb Haemost. 2009 Jul;7(7):1143-51. Epub 2009 Apr 27.
REF 80Nilotinib: a novel, selective tyrosine kinase inhibitor. Semin Oncol. 2011 Apr;38 Suppl 1:S3-9.
REF 81Bioorg 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 82Pharmacological intervention at disparate sites in the coagulation cascade: comparison of anti-thrombotic efficacy vs bleeding propensity in a rat model of acute arterial thrombosis. J Thromb Thrombolysis. 2002 Oct;14(2):113-21.
REF 83Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2. J Med Chem. 1999 Jul 29;42(15):2760-73.
REF 84Computer-aided design of a factor Xa inhibitor by using MCSS functionality maps and a CAVEAT linker search. J Mol Graph Model. 2003 Nov;22(2):105-14.
REF 85Clinical pipeline report, company report or official report of Takeda (2009).
REF 86Non-hemostatic activity of coagulation factor Xa: potential implications for various diseases. Curr Opin Pharmacol. 2001 Apr;1(2):169-75.
REF 87Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity. Bioorg Med Chem. 2004 May 1;12(9):2179-91.
REF 88J 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 89Low-molecular-weight heparins in pregnancy. Pharmacotherapy. 1999 Sep;19(9):1013-25.
REF 90Low molecular weight heparins for venous thromboembolism. Drug Ther Bull. 1998 Apr;36(4):25-9.
REF 91Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 92Expression 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 93(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: 2359).
REF 94EP42675, 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 95Serum zinc concentrations: contamination from laboratory equipment. JPEN J Parenter Enteral Nutr. 1979 May-Jun;3(3):179-81.
REF 96SR123781A, a synthetic heparin mimetic. Thromb Haemost. 2001 May;85(5):852-60.
REF 97Haemophilia B: Christmas disease. Expert Opin Pharmacother. 2005 Aug;6(9):1517-24.

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