Contribution of in vivo models of thrombosis to the discovery and development of novel antithrombotic agents

Journal of Pharmacological and Toxicological Methods

Volumn 43, Issue 2, 2000, Pages 101-116

  Leadley Jr , Robert J ^a   Chi, Liguo ^a   Rebello, Sam S ^b   Gagnon, Alison ^b  

^a PFIZER INC   (United States)

^b SANOFI   (France)

Author keywords

Animal models; Anti thrombotics; Factor Xa; In vivo; Thrombosis

Indexed keywords

ABCIXIMAB; ALTEPLASE; ANTICOAGULANT AGENT; ARGATROBAN; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; BLOOD CLOTTING FACTOR 7A; CLOPIDOGREL; ENOXAPARIN; EPTIFIBATIDE; FIBRINOGEN RECEPTOR ANTAGONIST; LEPIRUDIN; LOW MOLECULAR WEIGHT HEPARIN; THROMBIN INHIBITOR; TIROFIBAN; TISSUE PLASMINOGEN ACTIVATOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CARDIOVASCULAR DISEASE; CEREBROVASCULAR DISEASE; CONTROLLED STUDY; DRUG SAFETY; DRUG TARGETING; GENE THERAPY; HEMOPHILIA; MOLECULAR MODEL; MORTALITY; NONHUMAN; SPECIES DIFFERENCE; THROMBOSIS;

ANIMALS; DISEASE MODELS, ANIMAL; FACTOR XA; FIBRINOLYTIC AGENTS; HEMOSTASIS; HUMANS; MICE; MICE, KNOCKOUT; SPECIES SPECIFICITY; THROMBOSIS;

EID: 0034527312     PISSN: 10568719     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1056-8719(00)00095-2     Document Type: Article

References (133)

1. The comparative effects of recombinant hirudin (CGP 39393) and standard heparin on thrombus growth in rabbits
2. Experimental models of thrombosis
3. Hirudin in acute myocardial infarction: Safety report from the thrombolysis and thrombin inhibition in myocardial infarction (TIMI) 9A trial
4. Hirudin in acute myocardial infarction: Thrombolysis and thrombin inhibition in myocardial infarction (TIMI) 9B trial
5. Models to study thrombotic disorders
6. Mechanism of arterial thrombosis in non-parallel streamlines: Platelet thrombi grow on the apex of stenotic severely injured vessel wall
7. Lack of usefulness of prolonged bleeding times in predicting hemorrhagic events in patients receiving the 7E3 glycoprotein IIb/IIIa platelet antibody
8. Further characterization of Factor VIII-deficient mice created by gene targeting: RNA and protein studies
9. Laboratory evaluation of platelet dysfunction
10. Animal models of atherosclerosis and interpretation of drug intervention studies
11. RPR120844, a novel, specific inhibitor of coagulation factor Xa, inhibits venous thrombus formation in the rabbit
12. Anti-thrombotic activity of RG13965, a novel platelet fibrinogen receptor antagonist
13. Plasminogen deficiency causes severe thrombosis but is compatible with development and reproduction
14. The receptor for urokinase-type plasminogen activator is not essential for mouse development or fertility
15. Fatal embryonic bleeding events in mice lacking tissue factor, the cell-associated initiator of blood coagulation
16. In vivo models of arterial thrombosis and thrombolysis
17. Antithrombotic effects of synthetic pentasaccharide with high affinity for plasma antithrombin III in non-human primates
18. New developments in the molecular biology of coagulation and fibrinolysis
19. Role of tissue factor in embryonic blood vessel development
20. Physiological consequences of loss of plasminogen activator gene function in mice
21. Plasminogen activator inhibitor-1 gene-deficient mice
22. In vivo models of thrombosis
23. A murine model of myocardial thrombosis
24. A comparison of low-molecular-weight heparin with unfractioned heparin for unstable coronary artery disease. Efficacy and Safety of Subcutaneous Enoxaparin in Non-Q-Wave Coronary Events Study Group
25. Coronary thrombolysis with recombinant human tissue-type plasminogen activator: A prospective, randomized, placebo-controlled trial
26. Antithrombotic effect of a monoclonal antibody to the platelet glycoprotein IIb/IIa receptor in an experimental animal model
27. Role of the thrombin receptor in development and evidence for a second receptor
28. Nonpeptide glycoprotein IIb/IIIa inhibitors: 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217
29. Platelet aggregation and fibrinogen binding in human, rhesus monkey, guinea-pig, hamster and rat blood: Activation by ADP and thrombin receptor peptide and inhibition by glycoprotein IIb/IIIa antagonists
30. Pentamadine: A non-peptide GPIIb/IIIa antagonist - In vitro studies on platelets from humans and other species
31. Fatal haemorrhage and incomplete block to embryogenesis in mice lacking coagulation factor V
32. Administration of abciximab during percutaneous coronary intervention reduces both ex vivo platelet thrombus formation and fibrin deposition
33. A mouse model of severe von Willebrand disease: Defects in hemostasis and thrombosis
34. Generation and characterization of urokinase receptor-deficient mice
35. A comparison of recombinant hirudin with a low-molecular-weight heparin to prevent thromboembolic complications after total hip replacement
36. Canine hemophilia B resulting from a point mutation with unusual consequences
37. Role of thrombin and thromboxane A2 in reocclusion following coronary thrombolysis with tissue-type plasminogen activator
38. An in vivo model of experimental arterial stenosis, intimal damage, and periodic thrombosis
39. A murine model of factor XI deficiency
40. Evidence for a rebound coagulation phenomenon after cessation of a 4-hour infusion of a specific thrombin inhibitor in patients with unstable angina pectoris
41. Animal models for arterial thrombolysis and prevention of reocclusion
42. Randomized trial of intravenous heparin versus recombinant hirudin for acute coronary syndromes
43. A comparison of recombinant hirudin with heparin for the treatment of acute coronary syndromes
44. DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa
45. Species differences in anticoagulant and anti-Xa activity of DX-9065a, a highly selective factor Xa inhibitor
46. Experimental arterial thrombosis in nonhuman primates
47. Synthetic Inhibitors of thrombin and Factor Xa: From bench to bedside
48. Absence of the blood-clotting regulator thrombomodulin causes embryonic lethality in mice before development of a functional cardiovascular system
49. Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis
50. Hirudin, heparin, and placebo during deep arterial injury in the pig: The in vivo role of thrombin in platelet-mediated thrombosis
51. DX 9065A, a novel, synthetic selective and orally active inhibitor of factor Xa: In vitro and in vivo studies
52. Long-term correction of canine hemophilia B by gene transfer of blood coagulation factor IX mediated by adeno-associated viral vector
53. 3-integrin-deficient mice are a model for Glanzmann thrombasthenia showing placental defects and reduced survival
54. 3
55. Tissue factor pathway inhibitor gene disruption produces intrauterine lethality in mice
56. Animal models of acute ischaemic stroke: Can they predict clinically successful neuroprotective drugs?
57. Inactivation of the gene for anticoagulant protein C causes lethal perinatal consumptive coagulopathy in mice
58. The utility of animal models in the preclinical study of interventions to prevent human coronary artery restenosis: Analysis and recommendations
59. A dual thrombin receptor system for platelet activation
60. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals
61. Comparative studies of an orally-active factor Xa inhibitor, YM-60828, with other antithrombotic agents in a rat model of arterial thrombosis
62. Evidence for gene transfer and expression of factor IX in haemophilia B patients with an AAV vector
63. Transient interruption of arterial thrombosis by inhibition of factor Xa results in long-term antithrombotic effects in baboons
64. Human FIX corrects bleeding diathesis of mice with hemophilia B
65. Rat model of arterial thrombosis induced by ferric chloride
66. 3 signalling and platelet function
67. Inhibition of repetitive thrombus formation in the stenosed canine coronary artery by enoxaparin, but not by unfractionated heparin
68. Pharmacodynamic activity and antithrombotic efficacy of RPR120844, a novel inhibitor of coagulation factor Xa
69. Selective inhibition of Factor Xa is more efficient than Factor VIIa-Tissue Factor complex at facilitating coronary thrombolysis in the canine model
70. 1 receptor-null mice
71. A coagulation factor IX-deficient mouse model for human hemophilia B
72. Nonpeptide glycoprotein IIb/IIIa inhibitors: 5. Antithrombotic effects of MK-0383
73. Maintenance of canine coronary artery patency following thrombolysis with front loaded plus low dose maintenance conjunctive therapy. A comparison of factor Xa versus thrombin inhibition
74. Thrombolysis by human tissue plasminogen activator and urokinase in rabbits with experimental pulmonary embolus
75. Antithrombotic and hemorrhagic effects of DX9065a, a direct and selective factor Xa inhibitor: Comparison with a direct thrombin inhibitor and antithrombin III-dependent anticoagulants
76. Experimental models of coronary artery restenosis
77. Tolerability, pharmacokinetics, and pharmacodynamics of DX-9065a, a new synthetic potent anticoagulant and specific factor Xa inhibitor, in healthy male volunteers
78. Selective inhibition of factor Xa during thrombolytic therapy markedly improves coronary artery patency in a canine model of coronary thrombosis
79. Combination of platelet fibrinogen receptor antagonist and direct thrombin inhibitor at low doses markedly improves thrombolysis
80. Purification and characterization of recombinant antistasin: A leech-derived inhibitor of coagulation factor Xa
81. q-deficient mice
82. Combined accelerated tissue-plasminogen activator and platelet glycoprotein IIb/IIIa integrin receptor blockade with integrilin in acute myocardial infarction. Results of a randomized, placebo-controlled, dose-ranging trial
83. Effects of recombinant hirudin (lepirudin) compared with heparin on death, myocardial infarction, refractory angina, and revascularisation procedures in patients with acute myocardial ischaemia without ST elevation: A randomised trial
84. Effect of selective Factor Xa inhibition on arterial thrombus formation triggered by tissue factor/factor VIIa or collagen in an ex vivo model of shear-dependent human thrombogenesis
85. Species variation in the effect of glycoprotein IIb/IIIa antagonists on inhibition of platelet aggregation
86. Use of transgenic mice in the study of thrombosis and hemostasis
87. A comparison of aspirin plus tirofiban with aspirin plus heparin for unstable angina
88. Effects of disruption of the plasminogen gene on thrombosis, growth, and health in mice
89. Design and synthesis of isoxazoline derivatives as factor Xa inhibitors: 2
90. Design and synthesis of isoxazoline derivatives as factor Xa inhibitors: 1
91. Antithrombotic efficacy of a recombinant nematode anticoagulant peptide (rNAP5) in canine models of thrombosis after single subcutaneous administration
92. A critical reappraisal of the bleeding time
93. Electrical induction of coronary artery thrombosis in the ambulatory canine: A model for in vivo evaluation of anti-thrombotic agents
94. Mice lacking factor VII develop normally but suffer fatal perinatal bleeding
95. L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor
96. Antithrombotic effect of YM-75466 is separated from its effect on bleeding time and coagulation time
97. Antithrombotic effects of YM-60828, a newly synthesized factor Xa inhibitor, in rat thrombosis models and its effects on bleeding time
98. YM-60828, a novel factor Xa inhibitor: Separation of its antithrombotic effects from its prolongation of bleeding time
99. Relationship between the antithrombotic effect of YM-75466, a novel factor Xa inhibitor, and coagulation parameters in rats
100. Low-molecular-weight heparin (Fragmin) and thrombin active-site inhibitor (argatroban) compared in experimental arterial and venous thrombosis and bleeding time
101. Prothrombin activation in rabbits
102. Transcription factor NF-E2 is required for platelet formation independent of the actions of thrombopoietin/MGDF in megakaryocyte development
103. Antithrombotic and hemostatic capacity of factor Xa versus thrombin inhibitors in models of venous and arteriovenous thrombosis
104. Conjunctive enhancement of enzymatic thrombolysis and prevention of thrombotic reocclusion with the selective Factor Xa inhibitor, tick anticoagulant peptide
105. Ischemic stroke and intracranial hemorrhage following thrombolytic therapy for acute myocardial infarction: A risk-benefit analysis
106. Intracranial hemorrhage: Diagnosis and emergency management
107. Defects in hemostasis in P-selectin-deficient mice
108. Resolution of spontaneous bleeding events but failure of pregnancy in fibrinogen-deficient mice
109. Prothrombin deficiency results in embryonic and neonatal lethality in mice
110. Biochemical and pharmacological characterization of YM-60828, a newly synthesized and orally active inhibitor of human Factor Xa
111. Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty
112. 2
113. Strategies for anticoagulation wit synthetic protease inhibitors. Xa inhibitors versus thrombin inhibitors
114. Blood-clotting mechanisms of nonhuman primates: Choice of the baboon model to simulate man
115. Targeted disruption of the murine tissue factor gene results in embryonic lethality
116. Gene therapy for arterial thrombosis
117. I. Über die verstopfung der lungenarterie
118. Comparison of the in vivo anticoagulant properties of standard heparin and the highly selective Factor Xa inhibitors antistasin and tick anticoagulant peptide (TAP) in a rabbit model of venous thrombosis
119. Efficacy of a synthetic pentasaccharide, a pure factor Xa inhibitor, as an antithrombotic agent - A pilot study in the setting of coronary angioplasty
120. A factor IX-deficient mouse model for hemophilia B gene therapy
121. Gene therapy to promote thromboresistance: Local overexpression of tissue plasminogen activator to prevent arterial thrombosis in an in vivo rabbit model
122. Local overexpression of thrombomodulin for in vivo prevention of arterial thrombosis in a rabbit model
123. Tick anticoagulant peptide is a novel inhibitor of blood coagulation factor Xa
124. Studies in intravascular coagulation: I. Coagulation changes in isolated venous segments
125. Studies in intravascular coagulation: III. The pathogenesis of serum-induced venous thrombosis
126. Structure-based design of potent, amidine-derived inhibitors of factor Xa: Evaluation of selectivity, anticoagulant activity, and antithrombotic activity
127. Antithrombotic actions of selective inhibitors of blood coagulation factor Xa in rat models of thrombosis
128. Nonpeptide factor Xa inhibitors: I. Studies with SF303 and SK549, a new class of potent antithrombotics
129. Reversibility of platelet thrombosis in vivo
130. Incomplete embryonic lethality and fatal neonatal hemorrhage caused by prothrombin deficiency in mice
131. Effects of DX-9065a, an orally active, newly synthesized and specific inhibitor of factor Xa, against experimental disseminated intravascular coagulation in rats
132. Antithrombotic effects of orally active synthetic antagonist of activated factor X in nonhuman primates
133. Thromboresistance of balloon-injured porcine carotid arteries after local gene transfer of human tissue factor pathway inhibitor