Thromboxane receptors antagonists and/or synthase inhibitors

Handbook of Experimental Pharmacology

Volumn 210, Issue , 2012, Pages 261-286

  Davì, Giovanni ^a   Santilli, Francesca ^a   Vazzana, Natale ^a  

^a UNIVERSITY OF CHIETI   (Italy)

Author keywords

Antiplatelet therapy; Atherothrombosis; Ischemic stroke; Platelet activation; Thromboxane biosynthesis; TP antagonists

Indexed keywords

ACETYLSALICYLIC ACID; ANTICOAGULANT AGENT; CLOPIDOGREL; CYCLOOXYGENASE 2 INHIBITOR; DAZOXIBEN; DICLOFENAC; DIPYRIDAMOLE; LUMIRACOXIB; NONSTEROID ANTIINFLAMMATORY AGENT; OZAGREL; PICOTAMIDE; PLACEBO; PROSTAGLANDIN SYNTHASE INHIBITOR; RIDOGREL; SERATRODAST; TERUTROBAN; THROMBOXANE A2 RECEPTOR; THROMBOXANE A2 RECEPTOR BLOCKING AGENT; THROMBOXANE RECEPTOR BLOCKING AGENT; THROMBOXANE SYNTHASE INHIBITOR; THROMBOXANE RECEPTOR; THROMBOXANE SYNTHASE;

ACUTE HEART INFARCTION; ADJUVANT THERAPY; ANTICOAGULATION; ARTICLE; ASTHMA; ATHEROMA; ATHEROSCLEROSIS; BLEEDING; BRAIN ISCHEMIA; CARDIOVASCULAR DISEASE; CARDIOVASCULAR RISK; CEREBROVASCULAR DISEASE; CORONARY ARTERY DISEASE; DIABETES MELLITUS; DOSE RESPONSE; DRUG ANTAGONISM; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG MEGADOSE; DRUG SAFETY; ENZYME INHIBITION; HUMAN; INTRACELLULAR SIGNALING; ISCHEMIC HEART DISEASE; LOW DRUG DOSE; MAXIMUM PLASMA CONCENTRATION; MICROVASCULAR ENDOTHELIAL CELL; MOLECULAR BIOLOGY; NONHUMAN; PERIPHERAL OCCLUSIVE ARTERY DISEASE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); RISK ASSESSMENT; SMOOTH MUSCLE FIBER; THROMBOCYTE AGGREGATION INHIBITION; THROMBOSIS; ULCERATIVE COLITIS; ANIMAL; CEREBROVASCULAR ACCIDENT; CLINICAL TRIAL (TOPIC); PHYSIOLOGY; REVIEW; SIGNAL TRANSDUCTION;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ASPIRIN; ATHEROSCLEROSIS; CLINICAL TRIALS AS TOPIC; HUMANS; RECEPTORS, THROMBOXANE; SIGNAL TRANSDUCTION; STROKE; THROMBOSIS; THROMBOXANE-A SYNTHASE;

EID: 84867153649     PISSN: 01712004     EISSN: 18650325     Source Type: Book Series    
DOI: 10.1007/978-3-642-29423-5_11     Document Type: Article

References (76)

1. Ali S, Davis MG, Becker MW, Dorn GW2nd (1993) Thromboxane A2 stimulates vascular smooth muscle hypertrophy by up-regulating the synthesis and release of endogenous basic fibroblast growth factor. J Biol Chem 268:17397-17403
2. Ashton AW, Ware GM, Kaul DK, Ware JA (2003) Inhibition of tumor necrosis factor alphamediated NFkappaB activation and leukocyte adhesion, with enhanced endothelial apoptosis, by G protein-linked receptor (TP) ligands. J Biol Chem 278:11858-11866
3. Baigent C, Blackwell L, Collins R, Emberson J, Godwin J, Peto R, Buring J, Hennekens C, Kearney P, Meade T, Patrono C, Roncaglioni MC, Zanchetti A (2009) Aspirin in the primary and secondary prevention of vascular disease: collaborative meta-analysis of individual participant data from randomised trials. Lancet 373:1849-1860
4. Bal Dit Sollier C, Crassard I, Simoneau G, Bergmann JF, Bousser MG, Drouet L (2009) Effect of the thromboxane prostaglandin receptor antagonist terutroban on arterial thrombogenesis after repeated administration in patients treated for the prevention of ischemic stroke. Cerebrovasc Dis 28:505-513
5. Basili S, Raparelli V, Vestri A, Di Tanna GL, Violi F (2010) Comparison of efficacy of antiplatelet treatments for patients with claudication. A meta-analysis. Thromb Haemost 103:766-773
6. Belhassen L, Pelle G, Dubois-Rande JL, Adnot S (2003) Improved endothelial function by the thromboxane A2 receptor antagonist S 18886 in patients with coronary artery disease treated with aspirin. J Am Coll Cardiol 41:1198-1204
7. Bousser MG, Amarenco P, Chamorro A, Fisher M, Ford I, Fox K, Hennerici MG, Mattle HP, Rothwell PM (2009) Rationale and design of a randomized, double-blind, parallel-group study of terutroban 30 mg/day versus aspirin 100 mg/day in stroke patients: the prevention of cerebrovascular and cardiovascular events of ischemic origin with terutroban in patients with a history of ischemic stroke or transient ischemic attack (PERFORM) study. Cerebrovasc Dis 27:509-518
8. Bousser MG, Amarenco P, Chamorro A, Fisher M, Ford I, Fox KM, Hennerici MG, Mattle HP, Rothwell PM, de Cordoue A, Fratacci MD (2011) Terutroban versus aspirin in patients with cerebral ischaemic events (PERFORM): a randomised, double-blind, parallel-group trial. Lancet 377:2013-2022
9. Cathcart MC, Reynolds JV, O'Byrne KJ, Pidgeon GP (2010) The role of prostacyclin synthase and thromboxane synthase signaling in the development and progression of cancer. Biochim Biophys Acta 1805:153-166
10. Cathcart MC, Gately K, Cummins R, Kay E, O'Byrne KJ, Pidgeon GP (2011) Examination of thromboxane synthase as a prognostic factor and therapeutic target in non-small cell lung cancer. Mol Cancer 10:25
11. Cayatte AJ, Du Y, Oliver-Krasinski J, Lavielle G, Verbeuren TJ, Cohen RA (2000) The thromboxane receptor antagonist S18886 but not aspirin inhibits atherogenesis in apo E-deficient mice: evidence that eicosanoids other than thromboxane contribute to atherosclerosis. Arterioscler Thromb Vasc Biol 20:1724-1728
12. Chamorro A (2009) TP receptor antagonism: a new concept in atherothrombosis and stroke prevention. Cerebrovasc Dis 27(Suppl 3):20-27
13. Chen ZM, Sandercock P, Pan HC, Counsell C, Collins R, Liu LS, Xie JX, Warlow C, Peto R (2000) Indications for early aspirin use in acute ischemic stroke: a combined analysis of 40 000 randomized patients from the chinese acute stroke trial and the international stroke trial. On behalf of the CAST and IST collaborative groups. Stroke 31:1240-1249
14. Cheng Y, Austin SC, Rocca B, Koller BH, Coffman TM, Grosser T, Lawson JA, FitzGerald GA (2002) Role of prostacyclin in the cardiovascular response to thromboxane A2. Science 296:539-541
15. Davi G, Falco A (2005) Oxidant stress, inflammation and atherogenesis. Lupus 14:760-764
16. Davi G, Patrono C (2007) Platelet activation and atherothrombosis. N Engl J Med 357:2482-2494
17. Davi G, Catalano I, Averna M, Notarbartolo A, Strano A, Ciabattoni G, Patrono C (1990) Thromboxane biosynthesis and platelet function in type II diabetes mellitus. N Engl J Med 322:1769-1774
18. Davi G, Ciabattoni G, Consoli A, Mezzetti A, Falco A, Santarone S, Pennese E, Vitacolonna E, Bucciarelli T, Costantini F, Capani F, Patrono C (1999) In vivo formation of 8-iso-prostaglandin f2alpha and platelet activation in diabetes mellitus: effects of improved metabolic control and vitamin E supplementation. Circulation 99:224-229
19. Dogne JM, de Leval X, Hanson J, Frederich M, Lambermont B, Ghuysen A, Casini A, Masereel B, Ruan KH, Pirotte B, Kolh P (2004) New developments on thromboxane and prostacyclin modulators part I: thromboxane modulators. Curr Med Chem 11:1223-1241
20. Dogne JM, Hanson J, Pratico D (2005) Thromboxane, prostacyclin and isoprostanes: therapeutic targets in atherogenesis. Trends Pharmacol Sci 26:639-644
21. Egan KM, Wang M, Fries S, Lucitt MB, Zukas AM, Pure E, Lawson JA, FitzGerald GA (2005) Cyclooxygenases, thromboxane, and atherosclerosis: plaque destabilization by cyclooxygenase-2 inhibition combined with thromboxane receptor antagonism. Circulation 111:334-342
22. Eikelboom JW, Hirsh J, Weitz JI, Johnston M, Yi Q, Yusuf S (2002) Aspirin-resistant thromboxane biosynthesis and the risk of myocardial infarction, stroke, or cardiovascular death in patients at high risk for cardiovascular events. Circulation 105:1650-1655
23. Feletou M, Verbeuren TJ, Vanhoutte PM (2009) Endothelium-dependent contractions in SHR: a tale of prostanoid TP and IP receptors. Br J Pharmacol 156:563-574
24. Feletou M, Cohen RA, Vanhoutte PM, Verbeuren TJ (2010) TP receptors and oxidative stress hand in hand from endothelial dysfunction to atherosclerosis. Adv Pharmacol 60:85-106
25. Ferroni P, Basili S, Falco A, Davi G (2004) Platelet activation in type 2 diabetes mellitus. J Thromb Haemost 2:1282-1291
26. Fiessinger JN, Bounameaux H, Cairols MA, Clement DL, Coccheri S, Fletcher JP, Hoffmann U, Turpie AG (2010) Thromboxane Antagonism with terutroban in Peripheral Arterial Disease: the TAIPAD study. J Thromb Haemost 8:2369-2376
27. FitzGerald GA, Reilly IA, Pedersen AK (1985) The biochemical pharmacology of thromboxane synthase inhibition in man. Circulation 72:1194-1201
28. Gaussem P, Reny JL, Thalamas C, Chatelain N, Kroumova M, Jude B, Boneu B, Fiessinger JN (2005) The specific thromboxane receptor antagonist S18886: pharmacokinetic and pharmacodynamic studies. J Thromb Haemost 3:1437-1445
29. Gelosa P, Ballerio R, Banfi C, Nobili E, Gianella A, Pignieri A, Brioschi M, Guerrini U, Castiglioni L, Blanc-Guillemaud V, Lerond L, Tremoli E, Sironi L (2010) Terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, increases survival in strokeprone rats by preventing systemic inflammation and endothelial dysfunction: comparison with aspirin and rosuvastatin. J Pharmacol Exp Ther 334:199-205
30. Giannarelli C, Zafar MU, Badimon JJ (2010) Prostanoid and TP-receptors in atherothrombosis: is there a role for their antagonism? Thromb Haemost 104:949-954
31. Guthikonda S, Lev EI, Patel R, DeLao T, Bergeron AL, Dong JF, Kleiman NS (2007) Reticulated platelets and uninhibited COX-1 and COX-2 decrease the antiplatelet effects of aspirin. J Thromb Haemost 5:490-496
32. Halkes PH, van Gijn J, Kappelle LJ, Koudstaal PJ, Algra A (2006) Aspirin plus dipyridamole versus aspirin alone after cerebral ischaemia of arterial origin (ESPRIT): randomised controlled trial. Lancet 367:1665-1673
33. Ishizuka T, Suzuki K, Kawakami M, Hidaka T, Matsuki Y, Nakamura H (1996) Thromboxane A2 receptor blockade suppresses intercellular adhesion molecule-1 expression by stimulated vascular endothelial cells. Eur J Pharmacol 312:367-377
34. Ishizuka T, Kawakami M, Hidaka T, Matsuki Y, Takamizawa M, Suzuki K, Kurita A, Nakamura H (1998) Stimulation with thromboxane A2 (TXA2) receptor agonist enhances ICAM-1, VCAM-1 or ELAM-1 expression by human vascular endothelial cells. Clin Exp Immunol 112:464-470
35. Kiff PS, Bergman G, Atkinson L, Jewitt DE, Westwick J, Kakkar VV (1983) Haemodynamic and metabolic effects of dazoxiben at rest and during atrial pacing. Br J Clin Pharmacol 15:73S-77S
36. Lesault PF, Boyer L, Pelle G, Covali-Noroc A, Rideau D, Akakpo S, Teiger E, Dubois-Rande JL, Adnot S (2011) Daily administration of the TP receptor antagonist terutroban improved endothelial function in high-cardiovascular-risk patients with atherosclerosis. Br J Clin Pharmacol 71:844-851
37. Mayeux PR, Morton HE, Gillard J, Lord A, Morinelli TA, Boehm A, Mais DE, Halushka PV (1988) The affinities of prostaglandin H2 and thromboxane A2 for their receptor are similar in washed human platelets. Biochem Biophys Res Commun 157:733-739
38. Meade EA, Smith WL, DeWitt DL (1993) Differential inhibition of prostaglandin endoperoxide synthase (cyclooxygenase) isozymes by aspirin and other non-steroidal anti-inflammatory drugs. J Biol Chem 268:6610-6614
39. Meadows TA, Bhatt DL (2007) Clinical aspects of platelet inhibitors and thrombus formation. Circ Res 100:1261-1275
40. Mehta P, Mehta J, Lawson D, Krop I, Letts LG (1986) Leukotrienes potentiate the effects of epinephrine and thrombin on human platelet aggregation. Thromb Res 41:731-738
41. Meja KK, Barnes PJ, Giembycz MA (1997) Characterization of the prostanoid receptor(s) on human blood monocytes at which prostaglandin E2 inhibits lipopolysaccharide-induced tumour necrosis factor-alpha generation. Br J Pharmacol 122:149-157
42. Miggin SM, Kinsella BT (1998) Expression and tissue distribution of the mRNAs encoding the human thromboxane A2 receptor (TP) alpha and beta isoforms. Biochim Biophys Acta 1425:543-559
43. Moussa O, Ashton AW, Fraig M, Garrett-Mayer E, Ghoneim MA, Halushka PV, Watson DK (2008) Novel role of thromboxane receptors beta isoform in bladder cancer pathogenesis. Cancer Res 68:4097-4104
44. Moussa O, Ciupek A, Watson DK, Halushka PV (2011) Urinary thromboxane B(2) and thromboxane receptors in bladder cancer: opportunity for detection and monitoring. Prostaglandins Other Lipid Mediat 96(1-4):41-44
45. Nakahata N (2008) Thromboxane A2: physiology/pathophysiology, cellular signal transduction and pharmacology. Pharmacol Ther 118:18-35
46. Neri Serneri GG, Coccheri S, Marubini E, Violi F (2004) Picotamide, a combined inhibitor of thromboxane A2 synthase and receptor, reduces 2-year mortality in diabetics with peripheral arterial disease: the DAVID study. Eur Heart J 25:1845-1852
47. Patrono C (1990) Biosynthesis and pharmacological modulation of thromboxane in humans. Circulation 81:I12-I15, discussion I22-I23
48. Patrono C, Falco A, Dave G (2005a) Isoprostane formation and inhibition in atherothrombosis. Curr Opin Pharmacol 5:198-203
49. Patrono C, Garcia Rodriguez LA, Landolfi R, Baigent C (2005b) Low-dose aspirin for the prevention of atherothrombosis. N Engl J Med 353:2373-2383
50. Patrono C, Baigent C, Hirsh J, Roth G (2008) Antiplatelet drugs: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition). Chest 133:199S-233S
51. Patscheke H (1990) Thromboxane A2/prostaglandin H2 receptor antagonists. A new therapeutic principle. Stroke 21:IV139-IV142
52. Praticó D, Cheng Y, FitzGerald GA (2000) TP or not TP: primary mediators in a close runoff? Arterioscler Thromb Vasc Biol 20:1695-1698
53. Rovati GE, Sala A, Capra V, Dahlen SE, Folco G (2010) Dual COXIB/TP antagonists: a possible new twist in NSAID pharmacology and cardiovascular risk. Trends Pharmacol Sci 31:102-107
54. Sacco RL, Diener HC, Yusuf S, Cotton D, Ounpuu S, Lawton WA, Palesch Y, Martin RH, Albers GW, Bath P, Bornstein N, Chan BP, Chen ST, Cunha L, Dahlof B, De Keyser J, Donnan GA, Estol C, Gorelick P, Gu V, Hermansson K, Hilbrich L, Kaste M, Lu C, Machnig T, Pais P, Roberts R, Skvortsova V, Teal P, Toni D, Vandermaelen C, Voigt T, Weber M, Yoon BW (2008) Aspirin and extended-release dipyridamole versus clopidogrel for recurrent stroke. N Engl J Med 359:1238-1251
55. Santilli F, Rocca B, De Cristofaro R, Lattanzio S, Pietrangelo L, Habib A, Pettinella C, Recchiuti A, Ferrante E, Ciabattoni G, Davi G, Patrono C (2009) Platelet cyclooxygenase inhibition by low-dose aspirin is not reflected consistently by platelet function assays: implications for aspirin "resistance". J Am Coll Cardiol 53:667-677
56. Santilli F, Davi G, Basili S, Lattanzio S, Cavoni A, Guizzardi G, De Feudis L, Traisci G, Pettinella C, Paloscia L, Minuz P, Meneguzzi A, Ciabattoni G, Patrono C (2010) Thromboxane and prostacyclin biosynthesis in heart failure of ischemic origin: effects of disease severity and aspirin treatment. J Thromb Haemost 8:914-922
57. Santilli F, Mucci L, Davi G (2011) TP receptor activation and inhibition in atherothrombosis: the paradigm of diabetes mellitus. Intern Emerg Med 6:203-212
58. Santos-Garcia D, Blanco M, Serena J, Arias S, Millan M, Rodriguez-Yanez M, Leira R, Davalos A, Castillo J (2009) Brachial arterial flow mediated dilation in acute ischemic stroke. Eur J Neurol 16:684-690
59. Savage MP, Goldberg S, Bove AA, Deutsch E, Vetrovec G, Macdonald RG, Bass T, Margolis JR, Whitworth HB, Taussig A (1995) Effect of thromboxane A2 blockade on clinical outcome and restenosis after successful coronary angioplasty. Multi-Hospital Eastern Atlantic Restenosis Trial (M-HEART II). Circulation 92:3194-3200
60. Schramm TK, Gislason GH, Kober L, Rasmussen S, Rasmussen JN, Abildstrom SZ, Hansen ML, Folke F, Buch P, Madsen M, Vaag A, Torp-Pedersen C (2008) Diabetes patients requiring glucose-lowering therapy and nondiabetics with a prior myocardial infarction carry the same cardiovascular risk: a population study of 3.3 million people. Circulation 117:1945-1954
61. Selg E, Buccellati C, Andersson M, Rovati GE, Ezinga M, Sala A, Larsson AK, Ambrosio M, Lastbom L, Capra V, Dahlen B, Ryrfeldt A, Folco GC, Dahlen SE (2007) Antagonism of thromboxane receptors by diclofenac and lumiracoxib. Br J Pharmacol 152:1185-1195
62. Serruys PW, Rutsch W, Heyndrickx GR, Danchin N, Mast EG, Wijns W, Rensing BJ, Vos J, Stibbe J (1991) Prevention of restenosis after percutaneous transluminal coronary angioplasty with thromboxane A2-receptor blockade. A randomized, double-blind, placebo-controlled trial. Coronary Artery Restenosis Prevention on Repeated Thromboxane-Antagonism Study (CARPORT). Circulation 84:1568-1580
63. Shikano M, Ito T, Ogawa K, Satake T (1987) Effects of a selective thromboxane synthetase inhibitor (OKY-046) in patients with coronary artery disease during exercise. Jpn Heart J 28:663-674
64. Shinohara Y, Katayama Y, Uchiyama S, Yamaguchi T, Handa S,Matsuoka K, Ohashi Y, Tanahashi N, Yamamoto H, Genka C, Kitagawa Y, Kusuoka H, Nishimaru K, Tsushima M, Koretsune Y, Sawada T, Hamada C (2010) Cilostazol for prevention of secondary stroke (CSPS 2): an aspirincontrolled, double-blind, randomised non-inferiority trial. Lancet Neurol 9:959-968
65. SwinnenM, Vanhoutte D, Van Almen GC, Hamdani N, SchellingsMW, D'Hooge J, Van der Velden J,WeaverMS, SageEH, Bornstein P,Verheyen FK,VandenDriessche T,ChuahMK,Westermann D, PaulusWJ, Van de Werf F, Schroen B, Carmeliet P, Pinto YM, Heymans S (2009) Absence of thrombospondin-2 causes age-related dilated cardiomyopathy. Circulation 120:1585-1597
66. Thaulow E, Dale J, Myhre E (1984) Effects of a selective thromboxane synthetase inhibitor, dazoxiben, and of acetylsalicylic acid on myocardial ischemia in patients with coronary artery disease. Am J Cardiol 53:1255-1258
67. The Ridogrel Versus Aspirin Patency Trial (1994) Randomized trial of ridogrel, a combined thromboxane A2 synthase inhibitor and thromboxane A2/prostaglandin endoperoxide receptor antagonist, versus aspirin as adjunct to thrombolysis in patients with acute myocardial infarction. Circulation 89:588-595
68. Toth P, Rozsa B, Springo Z, Doczi T, Koller A (2011) Isolated human and rat cerebral arteries constrict to increases in flow: role of 20-HETE and TP receptors. J Cereb Blood Flow Metab 31:2096-2105
69. Tytgat GN, Van Nueten L, Van De Velde I, Joslyn A, Hanauer SB (2002) Efficacy and safety of oral ridogrel in the treatment of ulcerative colitis: two multicentre, randomized, double-blind studies. Aliment Pharmacol Ther 16:87-99
70. Uehara Y, Ishimitsu T, Kimura K, Ishii M, Ikeda T, Sugimoto T (1988) Regulatory effects of eicosanoids on thymidine uptake by vascular smooth muscle cells of rats. Prostaglandins 36:847-857
71. Uyama O, Nagatsuka K, Nakabayashi S, Isaka Y, Yoneda S, Kimura K, Abe H (1985) The effect of a thromboxane synthetase inhibitor, OKY-046, on urinary excretion of immunoreactive thromboxane B2 and 6-keto-prostaglandin F1 alpha in patients with ischemic cerebrovascular disease. Stroke 16:241-244
72. Vandeplassche G, Hermans C, Somers Y, Van de Werf F, de Clerck F (1993) Combined thromboxane A2 synthase inhibition and prostaglandin endoperoxide receptor antagonism limits myocardial infarct size after mechanical coronary occlusion and reperfusion at doses enhancing coronary thrombolysis by streptokinase. J Am Coll Cardiol 21:1269-1279
73. Violi F, Hiatt W (2007) A critical review of antiplatelet treatment in peripheral arterial disease. Intern Emerg Med 2:84-87
74. Watala C, Boncler M, Gresner P (2005) Blood platelet abnormalities and pharmacological modulation of platelet reactivity in patients with diabetes mellitus. Pharmacol Rep 57 (Suppl):42-58
75. Yui Y, Hattori R, Takatsu Y, Nakajima H, Wakabayashi A, Kawai C, Kayama N, Hiraku S, Inagawa T, Tsubojima M et al (1984) Intravenous infusion of a selective inhibitor of thromboxane A2 synthetase in man: influence on thromboxane B2 and 6-keto-prostaglandin F1 alpha levels and platelet aggregation. Circulation 70:599-605
76. Zuccollo A, Shi C, Mastroianni R, Maitland-Toolan KA, Weisbrod RM, Zang M, Xu S, Jiang B, Oliver-Krasinski JM, Cayatte AJ, Corda S, Lavielle G, Verbeuren TJ, Cohen RA (2005) The thromboxane A2 receptor antagonist S18886 prevents enhanced atherogenesis caused by diabetes mellitus. Circulation 112:3001-3008