Target General Infomation
Target ID
T84631 (Former ID: TTDS00203)
Target Name
Coagulation factor Xa (F10)
Synonyms
Fxa; Factor Xa; F10; Activated coagulation factor X
Gene Name
F10
Target Type
Successful target
[1]
Disease [+] 8 Target-related Diseases +
1 Blood-forming organ disease [ICD-11: 3C0Z]
2 Christmas disease [ICD-11: 3B11]
3 Coagulation defect [ICD-11: 3B10]
4 Coronary thrombosis [ICD-11: BA43]
5 Deep vein thrombosis [ICD-11: BD71]
6 Supraventricular tachyarrhythmia [ICD-11: BC81]
7 Thrombosis [ICD-11: DB61-GB90]
8 Venous thromboembolism [ICD-11: BD72]
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
UniProt ID
FA10_HUMAN
EC Number
EC 3.4.21.6
Sequence
MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE
TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN
CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR
KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE
CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE
AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI
VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG
GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE
VITSSPLK
Drugs and Modes of Action
Approved Drug(s) [+] 11 Approved Drugs +
1 Apixaban Drug Info Approved Thrombosis [2], [3]
2 BETRIXABAN Drug Info Approved Venous thromboembolism [4], [5]
3 Certoparin sodium Drug Info Approved Deep vein thrombosis [6]
4 Coagulation Factor IX Drug Info Approved Haemophilia B [7], [8]
5 Danaparoid Drug Info Approved Deep venous clot [9], [10]
6 DU-176b Drug Info Approved Atrial fibrillation [11], [12]
7 Emicizumab Drug Info Approved Factor VIII deficiency [5]
8 Fondaparinux sodium Drug Info Approved Venous thrombosis [13]
9 Lmw heparin Drug Info Approved Hematologic disease [6]
10 Nadroparin calcium Drug Info Approved Coagulation defect [6]
11 Rivaroxaban Drug Info Approved Deep vein thrombosis [14], [15]
Clinical Trial Drug(s) [+] 15 Clinical Trial Drugs +
1 Human coagulation factor X Drug Info BLA submitted Renal cell carcinoma [16]
2 PRT4445 Drug Info Phase 3 Bleeding disorder [17]
3 Semuloparin Drug Info Phase 3 Venous thromboembolism [18], [19]
4 SSR-126517E Drug Info Phase 3 Thrombosis [20]
5 SR-123781A Drug Info Phase 2/3 Venous thrombosis [21]
6 Antistasin Drug Info Phase 2 Attention deficit hyperactivity disorder [22]
7 EP-217609 Drug Info Phase 2 Thrombosis [23]
8 GW-813893 Drug Info Phase 2 Thrombosis [24]
9 LY-517717 Drug Info Phase 2 Thrombosis [25]
10 BI-11634 Drug Info Phase 1 Thrombosis [26]
11 BIBT986 Drug Info Phase 1 Thrombosis [27]
12 EP-42675 Drug Info Phase 1 Thrombosis [28]
13 GCC-4401 Drug Info Phase 1 Thrombosis [29]
14 R-1663 Drug Info Phase 1 Coagulation defect [30]
15 SSR-128428 Drug Info Phase 1 Thrombosis [31]
Discontinued Drug(s) [+] 19 Discontinued Drugs +
1 Darexaban maleate Drug Info Discontinued in Phase 3 Acute coronary syndrome [32]
2 Idraparinux Drug Info Discontinued in Phase 3 Thrombosis [33]
3 Otamixaban Drug Info Discontinued in Phase 3 Angina pectoris [34]
4 Valspodar Drug Info Discontinued in Phase 3 Acute myeloid leukaemia [35]
5 Octopamine Drug Info Discontinued in Phase 2a Thrombosis [36], [37]
6 DX-9065 Drug Info Discontinued in Phase 2 Coagulation defect [38], [39]
7 DX-9065a Drug Info Discontinued in Phase 2 Angina pectoris [39]
8 PD-348292 Drug Info Discontinued in Phase 2 Thrombosis [40]
9 R-68151 Drug Info Discontinued in Phase 2 Psoriasis vulgaris [41]
10 TAK-442 Drug Info Discontinued in Phase 2 Thrombosis [42]
11 AVE-3247 Drug Info Discontinued in Phase 1 Thrombosis [43]
12 DPC 423 Drug Info Discontinued in Phase 1 Thrombosis [44]
13 EMD-503982 Drug Info Discontinued in Phase 1 Thrombosis [45]
14 JTV-803 Drug Info Discontinued in Phase 1 Thrombosis [46]
15 YM-75466 Drug Info Discontinued in Phase 1 Thrombosis [47]
16 ZD-4927 Drug Info Discontinued in Phase 1 Thrombosis [48]
17 Draculin Drug Info Terminated Thrombosis [51]
18 Hirufaxin Drug Info Terminated Thrombosis [52]
19 Nematode anticoagulant proteins Drug Info Terminated Angina pectoris [53]
Preclinical Drug(s) [+] 2 Preclinical Drugs +
1 CS-3030 Drug Info Preclinical Thrombosis [49]
2 Trimidox Drug Info Preclinical Solid tumour/cancer [50]
Mode of Action [+] 4 Modes of Action +
Inhibitor [+] 63 Inhibitor drugs +
1 Apixaban Drug Info [1], [54]
2 Danaparoid Drug Info [59]
3 Fondaparinux sodium Drug Info [61], [62]
4 MELAGATRAN Drug Info [65]
5 Semuloparin Drug Info [18], [19]
6 SSR-126517E Drug Info [18], [19]
7 Antistasin Drug Info [67]
8 GW-813893 Drug Info [18], [19]
9 LY-517717 Drug Info [18], [19]
10 BI-11634 Drug Info [18], [19]
11 BIBT986 Drug Info [69]
12 GCC-4401 Drug Info [18], [19]
13 R-1663 Drug Info [18], [19]
14 Darexaban maleate Drug Info [72]
15 Idraparinux Drug Info [73]
16 Otamixaban Drug Info [73]
17 Valspodar Drug Info [74], [67]
18 Octopamine Drug Info [75], [76]
19 DX-9065 Drug Info [18], [19]
20 DX-9065a Drug Info [77]
21 PD-348292 Drug Info [1], [78]
22 R-68151 Drug Info [79]
23 TAK-442 Drug Info [80]
24 AVE-3247 Drug Info [18], [19]
25 DPC 423 Drug Info [81]
26 EMD-503982 Drug Info [18], [19]
27 JTV-803 Drug Info [18], [19]
28 YM-75466 Drug Info [18], [19]
29 ZD-4927 Drug Info [18], [19]
30 CS-3030 Drug Info [18], [19]
31 Trimidox Drug Info [82]
32 Hirufaxin Drug Info [18], [19]
33 YM60828 Drug Info [67]
34 1,2,3,4,6-penta-O-galloyl-beta-D-glucose Drug Info [85]
35 3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate Drug Info [86]
36 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Drug Info [87]
37 5-desgalloylstachyurin Drug Info [85]
38 Azaphenylalanine derivative Drug Info [88]
39 Beta-Hydroxy Aspartic Acid Drug Info [89]
40 BMS-269223 Drug Info [90]
41 BMS-344577 Drug Info [90]
42 BMS-740808 Drug Info [91]
43 CASUARIIN Drug Info [85]
44 D-Pro-Phe-Arg chloromethyl ketone Drug Info [94]
45 Gamma-Carboxy-Glutamic Acid Drug Info [95]
46 GC-2107 Drug Info [18], [19]
47 Lefaxin Drug Info [67]
48 M55113 Drug Info [96]
49 Molecule 11 Drug Info [97]
50 PEDUNCULAGIN Drug Info [85]
51 PhSO2-Gly-(Me-Gly)-Arg-(2-thiazole) Drug Info [98]
52 PRT-064445 Drug Info [18], [19]
53 RAZAXABAN Drug Info [91]
54 SC-83157 Drug Info [99]
55 SF303 Drug Info [81]
56 SK509 Drug Info [81]
57 SK549 Drug Info [100]
58 SK554 Drug Info [67]
59 SN429 Drug Info [99]
60 Tellimagrandin II Drug Info [85]
61 YM-96765 Drug Info [101]
62 ZK-810388 Drug Info [102]
63 ZK-814048 Drug Info [102]
Modulator [+] 19 Modulator drugs +
1 BETRIXABAN Drug Info [55]
2 Certoparin sodium Drug Info [13], [56], [57]
3 DU-176b Drug Info [60]
4 Emicizumab Drug Info [5]
5 Lmw heparin Drug Info [13], [63]
6 Nadroparin calcium Drug Info [64], [13]
7 Rivaroxaban Drug Info [6]
8 Human coagulation factor X Drug Info [18], [19]
9 PRT4445 Drug Info [18], [19]
10 SR-123781A Drug Info [66]
11 EP-217609 Drug Info [68]
12 EP-42675 Drug Info [70]
13 SSR-128428 Drug Info [71]
14 Draculin Drug Info [83]
15 Nematode anticoagulant proteins Drug Info [84]
16 CI-1031 Drug Info [92], [93]
17 Recombinant coagulation factors Drug Info [18], [19]
18 Recombinant Factor X Drug Info [18], [19]
19 ZK-813039 Drug Info [102]
Activator [+] 1 Activator drugs +
1 Coagulation Factor IX Drug Info [58]
Antagonist [+] 2 Antagonist drugs +
1 DT-831j Drug Info [18], [19]
2 EP-37 Drug Info [18], [19]
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
KEGG Pathway [+] 1 KEGG Pathways +
1 Complement and coagulation cascades
Panther Pathway [+] 1 Panther Pathways +
1 Blood coagulation
Pathwhiz Pathway [+] 1 Pathwhiz Pathways +
1 Coagulation
PID Pathway [+] 1 PID Pathways +
1 Beta2 integrin cell surface interactions
Reactome [+] 6 Reactome Pathways +
1 Extrinsic Pathway of Fibrin Clot Formation
2 Intrinsic Pathway of Fibrin Clot Formation
3 Common Pathway of Fibrin Clot Formation
4 Gamma-carboxylation of protein precursors
5 Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus
6 Removal of aminoterminal propeptides from gamma-carboxylated proteins
WikiPathways [+] 5 WikiPathways +
1 Complement and Coagulation Cascades
2 Human Complement System
3 PTM: gamma carboxylation, hypusine formation and arylsulfatase activation
4 Blood Clotting Cascade
5 Formation of Fibrin Clot (Clotting Cascade)
Target-Related Models and Studies
Target Validation
References
REF 1 Pfizer. Product Development Pipeline. March 31 2009.
REF 2 URL: 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 3 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
REF 4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018
REF 5 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
REF 6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 7 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
REF 8 Drug information of Coagulation Factor IX, 2008. eduDrugs.
REF 9 URL: 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 10 A comparison of danaparoid and lepirudin in heparin-induced thrombocytopenia. Thromb Haemost. 2001 Jun;85(6):950-7.
REF 11 URL: 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 12 ClinicalTrials.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 13 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
REF 14 URL: 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 15 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
REF 16 FDA Accepts BPL's Amended BLA Submission for Coagadex (Coagulation Factor X, Human). BPL Bio Products Laboratory USA, Inc.
REF 17 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031853)
REF 18 Semuloparin for the prevention of venous thromboembolic events in cancer patients. Drugs Today (Barc). 2012 Jul;48(7):451-7.
REF 19 Venous thromboembolism in the patient with cancer: focus on burden of disease and benefits of thromboprophylaxis. Cancer. 2011 Apr 1;117(7):1334-49.
REF 20 ClinicalTrials.gov (NCT00345618) Clinical Study Assessing SSR126517E Injections Once-weekly in Pulmonary Embolism Therapeutic Approach. U.S. National Institutes of Health.
REF 21 ClinicalTrials.gov (NCT00338897) Dose Ranging Study in Elective Total Hip Replacement Surgery. U.S. National Institutes of Health.
REF 22 The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor. Nat Rev Drug Discov. 2011 Jan;10(1):61-75.
REF 23 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033781)
REF 24 ClinicalTrials.gov (NCT00541320) Phase IIa Venous Thromboembolism (VTE) Prevention Study In Total Knee Replacement (TKR). U.S. National Institutes of Health.
REF 25 ClinicalTrials.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 26 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041083)
REF 27 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024917)
REF 28 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023539)
REF 29 ClinicalTrials.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 30 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024856)
REF 31 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020651)
REF 32 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020726)
REF 33 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010432)
REF 34 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015497)
REF 35 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001281)
REF 36 URL: 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 37 Juvenile hormone and octopamine in the regulation of division of labor in honey bee colonies. Horm Behav. 2002 Sep;42(2):222-31.
REF 38 DX-9065a Daiichi. Curr Opin Investig Drugs. 2003 Sep;4(9):1105-12.
REF 39 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004028)
REF 40 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024432)
REF 41 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003630)
REF 42 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027537)
REF 43 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012558)
REF 44 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012496)
REF 45 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022087)
REF 46 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014748)
REF 47 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010496)
REF 48 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009534)
REF 49 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022617)
REF 50 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004681)
REF 51 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004668)
REF 52 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012166)
REF 53 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006763)
REF 54 Effects 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 55 Company report (Portola)
REF 56 Low molecular weight heparins for venous thromboembolism. Drug Ther Bull. 1998 Apr;36(4):25-9.
REF 57 Low-molecular-weight heparins in pregnancy. Pharmacotherapy. 1999 Sep;19(9):1013-25.
REF 58 Haemophilia B: Christmas disease. Expert Opin Pharmacother. 2005 Aug;6(9):1517-24.
REF 59 Effect of factor X inhibition on coagulation activation and cytokine induction in human systemic inflammation. J Infect Dis. 2002 Nov 1;186(9):1270-6.
REF 60 URL: 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 61 Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb. 2002 Sep-Dec;32(5-6):218-24.
REF 62 Fondaparinux, 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 63 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 64 Serum zinc concentrations: contamination from laboratory equipment. JPEN J Parenter Enteral Nutr. 1979 May-Jun;3(3):179-81.
REF 65 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
REF 66 SR123781A, a synthetic heparin mimetic. Thromb Haemost. 2001 May;85(5):852-60.
REF 67 Novel approaches to the treatment of thrombosis. Trends Pharmacol Sci. 2002 Jan;23(1):25-32.
REF 68 Specificity and selectivity profile of EP217609: a new neutralizable dual-action anticoagulant that targets thrombin and factor Xa.Blood.2012 Mar 8;119(10):2187-95.
REF 69 Pharmacokinetics 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 70 EP42675, 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 71 Company report (Sanofi) (drug: FY2008)
REF 72 The 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 73 Pharma & Vaccines. Product Development Pipeline. April 29 2009.
REF 74 Non-hemostatic activity of coagulation factor Xa: potential implications for various diseases. Curr Opin Pharmacol. 2001 Apr;1(2):169-75.
REF 75 Description 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.
REF 76 AVE5026, a new hemisynthetic ultra-low-molecular-weight heparin for the prevention of venous thromboembolism in patients after total knee replaceme... J Thromb Haemost. 2009 Apr;7(4):566-72.
REF 77 DX-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 78 Nilotinib: a novel, selective tyrosine kinase inhibitor. Semin Oncol. 2011 Apr;38 Suppl 1:S3-9.
REF 79 Synthesis 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 80 Clinical pipeline report, company report or official report of Takeda (2009).
REF 81 The design and synthesis of noncovalent factor Xa inhibitors. Curr Top Med Chem. 2001 Jun;1(2):137-49.
REF 82 Computer-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 83 Expression 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 84 JPET 283:9199, 1997
REF 85 Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade. J Nat Prod. 1998 Nov;61(11):1356-60.
REF 86 3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa. J Med Chem. 2005 Dec 1;48(24):7592-603.
REF 87 Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.
REF 88 Thrombin inhibitors built on an azaphenylalanine scaffold. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1563-7.
REF 89 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 90 Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9.
REF 91 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... J Med Chem. 2007 Nov 1;50(22):5339-56.
REF 92 Effects of ZK-807834, a novel inhibitor of factor Xa, on arterial and venous thrombosis in rabbits. J Cardiovasc Pharmacol. 2000 May;35(5):796-805.
REF 93 Effect of vascular injury on inhibition of venous thrombosis with ZK-807834, a direct inhibitor of factor Xa. J Thromb Haemost. 2003 Sep;1(9):1955-8.
REF 94 Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. J Med Chem. 2008 Jun 12;51(11):3077-80.
REF 95 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 96 Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor. Chem Pharm Bull (Tokyo). 2001 Oct;49(10):1237-44.
REF 97 Role of tissue factor pathway inhibitor in the regulation of tissue factor-dependent blood coagulation. Cardiovasc Drug Rev. 2002 Winter;20(1):67-80.
REF 98 Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. Bioorg Med Chem. 2008 Feb 15;16(4):1562-95.
REF 99 Pharmacological 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 100 Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2. J Med Chem. 1999 Jul 29;42(15):2760-73.
REF 101 Synthesis 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 102 Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. J Med Chem. 2007 Jun 28;50(13):2967-80.

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