메뉴 건너뛰기




Volumn 210, Issue , 2012, Pages 239-260

PAR-1 inhibitors: A novel class of antiplatelet agents for the treatment of patients with atherothrombosis

Author keywords

Acute coronary syndromes; Antiplatelet agents; Atherothrombosis; PAR 1 inhibitors

Indexed keywords

ACETYLSALICYLIC ACID; ANTITHROMBOCYTIC AGENT; ATOPAXAR; CANGRELOR; CLOPIDOGREL; HEPARIN; PLACEBO; PRASUGREL; PROTEINASE ACTIVATED RECEPTOR 1; PURINERGIC P2Y12 RECEPTOR; SCH 602539; TICAGRELOR; TICLOPIDINE; UNCLASSIFIED DRUG; VORAPAXAR; IMINE; LACTONE; PYRIDINE DERIVATIVE;

EID: 84867163935     PISSN: 01712004     EISSN: 18650325     Source Type: Book Series    
DOI: 10.1007/978-3-642-29423-5_10     Document Type: Article
Times cited : (11)

References (36)
  • 1
    • 61849180442 scopus 로고    scopus 로고
    • Safety and tolerability of SCH 530348 in patients undergoing non-urgent percutaneous coronary intervention: A randomised, doubleblind, placebo-controlled phase II study
    • Becker RC, Moliterno DJ, Jennings LK et al (2009) Safety and tolerability of SCH 530348 in patients undergoing non-urgent percutaneous coronary intervention: a randomised, doubleblind, placebo-controlled phase II study. Lancet 373:919-928
    • (2009) Lancet , vol.373 , pp. 919-928
    • Becker, R.C.1    Moliterno, D.J.2    Jennings, L.K.3
  • 2
    • 71849119604 scopus 로고    scopus 로고
    • Intravenous platelet blockade with cangrelor during PCI
    • Bhatt DL, Lincoff AM, Gibson CM et al (2009) Intravenous platelet blockade with cangrelor during PCI. N Engl J Med 361:2330-2341
    • (2009) N Engl J Med , vol.361 , pp. 2330-2341
    • Bhatt, D.L.1    Lincoff, A.M.2    Gibson, C.M.3
  • 3
    • 44949114152 scopus 로고    scopus 로고
    • Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity
    • Chackalamannil S, Wang Y, Greenlee WJ et al (2008) Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem 51:3061-3064
    • (2008) J Med Chem , vol.51 , pp. 3061-3064
    • Chackalamannil, S.1    Wang, Y.2    Greenlee, W.J.3
  • 4
    • 58149156652 scopus 로고    scopus 로고
    • SCH 530348, a novel oral antiplatelet agent, demonstrated no bleeding risk alone or in combination with aspirin and clopidogrel in cynomolgus monkeys
    • Chintala M, Vemulapalli S, Kurowski S, Sabin C, Reynolds D, Prevete K, Friedrichs G (2008) (2008) SCH 530348, a novel oral antiplatelet agent, demonstrated no bleeding risk alone or in combination with aspirin and clopidogrel in cynomolgus monkeys. Atheroscler Thromb Vasc Biol 28:e32-e149
    • (2008) Atheroscler Thromb Vasc Biol , vol.28
    • Chintala, M.1    Vemulapalli, S.2    Kurowski, S.3    Sabin, C.4    Reynolds, D.5    Prevete, K.6    Friedrichs, G.7
  • 5
    • 78149281431 scopus 로고    scopus 로고
    • SCH 602539, a protease-activated receptor-1 antagonist, inhibits thrombosis alone and in combination with cangrelor in a Folts model of arterial thrombosis in cynomolgus monkeys
    • Chintala M, Strony J, Yang B, Kurowski S, Li Q (2010) SCH 602539, a protease-activated receptor-1 antagonist, inhibits thrombosis alone and in combination with cangrelor in a Folts model of arterial thrombosis in cynomolgus monkeys. Arterioscler Thromb Vasc Biol 30:2143-2149
    • (2010) Arterioscler Thromb Vasc Biol , vol.30 , pp. 2143-2149
    • Chintala, M.1    Strony, J.2    Yang, B.3    Kurowski, S.4    Li, Q.5
  • 6
    • 0033613183 scopus 로고    scopus 로고
    • How the protease thrombin talks to cells
    • Coughlin SR (1999) How the protease thrombin talks to cells. Proc Natl Acad Sci USA 96:11023-11027
    • (1999) Proc Natl Acad Sci USA , vol.96 , pp. 11023-11027
    • Coughlin, S.R.1
  • 7
    • 0034648757 scopus 로고    scopus 로고
    • Thrombin signalling and protease-activated receptors
    • Coughlin SR (2000) Thrombin signalling and protease-activated receptors. Nature 407:258-264
    • (2000) Nature , vol.407 , pp. 258-264
    • Coughlin, S.R.1
  • 8
    • 37249068049 scopus 로고    scopus 로고
    • Platelet activation and atherothrombosis
    • Davi G, Patrono C (2007) Platelet activation and atherothrombosis. N Engl J Med 357:2482-2494
    • (2007) N Engl J Med , vol.357 , pp. 2482-2494
    • Davi, G.1    Patrono, C.2
  • 9
    • 1842788585 scopus 로고    scopus 로고
    • Contribution of PAR-1, PAR-4 and GPIbalpha in intracellular signaling leading to the cleavage of the beta3 cytoplasmic domain during thrombin-induced platelet aggregation
    • Dubois C, Steiner B, Meyer Reigner SC (2004) Contribution of PAR-1, PAR-4 and GPIbalpha in intracellular signaling leading to the cleavage of the beta3 cytoplasmic domain during thrombin-induced platelet aggregation. Thromb Haemost 91:733-742
    • (2004) Thromb Haemost , vol.91 , pp. 733-742
    • Dubois, C.1    Steiner, B.2    Meyer Reigner, S.C.3
  • 10
    • 0036846734 scopus 로고    scopus 로고
    • Clopidogrel does not suppress blood markers of coagulation activation in aspirin-treated patients with non-ST-elevation acute coronary syndromes
    • Eikelboom JW, Weitz JI, Budaj A et al (2002) Clopidogrel does not suppress blood markers of coagulation activation in aspirin-treated patients with non-ST-elevation acute coronary syndromes. Eur Heart J 23:1771-1779
    • (2002) Eur Heart J , vol.23 , pp. 1771-1779
    • Eikelboom, J.W.1    Weitz, J.I.2    Budaj, A.3
  • 11
    • 78650740920 scopus 로고    scopus 로고
    • Identification of human liver cytochrome P450 enzymes involved in the metabolism of SCH 530348 (Vorapaxar), a potent oral thrombin proteaseactivated receptor 1 antagonist
    • Ghosal A, Lu X, Penner N et al (2011) Identification of human liver cytochrome P450 enzymes involved in the metabolism of SCH 530348 (Vorapaxar), a potent oral thrombin proteaseactivated receptor 1 antagonist. Drug Metab Dispos 39:30-38
    • (2011) Drug Metab Dispos , vol.39 , pp. 30-38
    • Ghosal, A.1    Lu, X.2    Penner, N.3
  • 12
    • 77649207578 scopus 로고    scopus 로고
    • Safety and exploratory efficacy of the novel thrombin receptor (PAR-1) antagonist SCH 530348 for non-ST-segment elevation acute coronary syndrome
    • Goto S, Yamaguchi T, Ikeda Y, Kato K, Yamaguchi H, Jensen P (2010a) Safety and exploratory efficacy of the novel thrombin receptor (PAR-1) antagonist SCH 530348 for non-ST-segment elevation acute coronary syndrome. J Atheroscler Thromb 17:156-164
    • (2010) J Atheroscler Thromb , vol.17 , pp. 156-164
    • Goto, S.1    Yamaguchi, T.2    Ikeda, Y.3    Kato, K.4    Yamaguchi, H.5    Jensen, P.6
  • 13
    • 78149355554 scopus 로고    scopus 로고
    • Double-blind, placebo-controlled Phase II studies of the protease-activated receptor 1 antagonist E5555 (atopaxar) in Japanese patients with acute coronary syndrome or high-risk coronary artery disease
    • Goto S, Ogawa H, Takeuchi M, Flather MD, Bhatt DL (2010b) Double-blind, placebo-controlled Phase II studies of the protease-activated receptor 1 antagonist E5555 (atopaxar) in Japanese patients with acute coronary syndrome or high-risk coronary artery disease. Eur Heart J 31:2601-2613
    • (2010) Eur Heart J , vol.31 , pp. 2601-2613
    • Goto, S.1    Ogawa, H.2    Takeuchi, M.3    Flather, M.D.4    Bhatt, D.L.5
  • 14
    • 76349089295 scopus 로고    scopus 로고
    • Combination antithrombotic therapies
    • Gurbel PA, Tantry US (2010) Combination antithrombotic therapies. Circulation 121:569-583
    • (2010) Circulation , vol.121 , pp. 569-583
    • Gurbel, P.A.1    Tantry, U.S.2
  • 15
    • 13244273430 scopus 로고    scopus 로고
    • Impaired hemostasis and protection against thrombosis in protease-activated receptor 4-deficient mice is due to lack of thrombin signaling in platelets
    • Hamilton JR, Cornelissen I, Coughlin SR (2004) Impaired hemostasis and protection against thrombosis in protease-activated receptor 4-deficient mice is due to lack of thrombin signaling in platelets. J Thromb Haemost 2:1429-1435
    • (2004) J Thromb Haemost , vol.2 , pp. 1429-1435
    • Hamilton, J.R.1    Cornelissen, I.2    Coughlin, S.R.3
  • 16
    • 71849087338 scopus 로고    scopus 로고
    • Platelet inhibition with cangrelor in patients undergoing PCI
    • Harrington RA, Stone GW, McNulty S et al (2009) Platelet inhibition with cangrelor in patients undergoing PCI. N Engl J Med 361:2318-2329
    • (2009) N Engl J Med , vol.361 , pp. 2318-2329
    • Harrington, R.A.1    Stone, G.W.2    McNulty, S.3
  • 18
    • 36448931550 scopus 로고    scopus 로고
    • Antithrombotic and bleeding time effects of E5555, an orally active protease-activated receptor-1 antagonist, in guinea pigs
    • Abstract
    • Kogushi M, Kobayashi H, Matsuoka T et al (2003) Antithrombotic and bleeding time effects of E5555, an orally active protease-activated receptor-1 antagonist, in guinea pigs. Circulation 108:280, Abstract
    • (2003) Circulation , vol.108 , pp. 280
    • Kogushi, M.1    Kobayashi, H.2    Matsuoka, T.3
  • 20
    • 79952487685 scopus 로고    scopus 로고
    • The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs
    • Kogushi M, Matsuoka T, Kawata T et al (2011a) The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs. Eur J Pharmacol 657:131-137
    • (2011) Eur J Pharmacol , vol.657 , pp. 131-137
    • Kogushi, M.1    Matsuoka, T.2    Kawata, T.3
  • 21
    • 79959999841 scopus 로고    scopus 로고
    • Oral administration of the thrombin receptor antagonist E5555 (atopaxar) attenuates intimal thickening following balloon injury in rats
    • Kogushi M, Matsuoka T, Kuramochi H et al (2011b) Oral administration of the thrombin receptor antagonist E5555 (atopaxar) attenuates intimal thickening following balloon injury in rats. Eur J Pharmacol 666:158-164
    • (2011) Eur J Pharmacol , vol.666 , pp. 158-164
    • Kogushi, M.1    Matsuoka, T.2    Kuramochi, H.3
  • 22
    • 77955677366 scopus 로고    scopus 로고
    • Rationale and design of the randomized, doubleblind trial testing INtraveNous and Oral administration of elinogrel, a selective and reversible P2Y12-receptor inhibitor, versus clopidogrel to eVAluate Tolerability and Efficacy in nonurgent Percutaneous Coronary Interventions patients (INNOVATE-PCI)
    • Leonardi S, Rao SV, Harrington RA et al (2010) Rationale and design of the randomized, doubleblind trial testing INtraveNous and Oral administration of elinogrel, a selective and reversible P2Y12-receptor inhibitor, versus clopidogrel to eVAluate Tolerability and Efficacy in nonurgent Percutaneous Coronary Interventions patients (INNOVATE-PCI). Am Heart J 160:65-72
    • (2010) Am Heart J , vol.160 , pp. 65-72
    • Leonardi, S.1    Rao, S.V.2    Harrington, R.A.3
  • 23
    • 36448941387 scopus 로고    scopus 로고
    • Inhibitory effect of E5555, an orally active thrombin receptor antagonist, on intimal hyperplasia following balloon injury
    • Matsuoka T, Kogushi M, Kawata T et al (2004) Inhibitory effect of E5555, an orally active thrombin receptor antagonist, on intimal hyperplasia following balloon injury. J Am Coll Cardiol 43:68A
    • (2004) J Am Coll Cardiol , vol.43
    • Matsuoka, T.1    Kogushi, M.2    Kawata, T.3
  • 24
    • 68949156886 scopus 로고    scopus 로고
    • Evaluation of a novel antiplatelet agent for secondary prevention in patients with a history of atherosclerotic disease: Design and rationale for the Thrombin-Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events (TRA 2-P)-TIMI 50 trial
    • Morrow DA, Scirica BM, Fox KA et al (2009) Evaluation of a novel antiplatelet agent for secondary prevention in patients with a history of atherosclerotic disease: design and rationale for the Thrombin-Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events (TRA 2-P)-TIMI 50 trial. Am Heart J 158:335.e3-341.e3
    • (2009) Am Heart J , vol.158
    • Morrow, D.A.1    Scirica, B.M.2    Fox, K.A.3
  • 25
    • 84859555815 scopus 로고    scopus 로고
    • Vorapaxar in the secondary prevention of atherothrombotic events
    • Morrow DA, Braunwald E, Bonaca MP et al (2012) Vorapaxar in the secondary prevention of atherothrombotic events. N Engl J Med 366(15):1404-1413
    • (2012) N Engl J Med , vol.366 , Issue.15 , pp. 1404-1413
    • Morrow, D.A.1    Braunwald, E.2    Bonaca, M.P.3
  • 26
    • 85027946204 scopus 로고    scopus 로고
    • Safety and tolerability of atopaxar in the treatment of patients with acute coronary syndromes/clinical perspective
    • O'Donoghue ML, Bhatt DL, Wiviott SD et al (2011) Safety and tolerability of atopaxar in the treatment of patients with acute coronary syndromes/clinical perspective. Circulation 123:1843-1853
    • (2011) Circulation , vol.123 , pp. 1843-1853
    • O'Donoghue, M.L.1    Bhatt, D.L.2    Wiviott, S.D.3
  • 28
    • 67749086022 scopus 로고    scopus 로고
    • The in-vitro effects of E5555, a protease-activated receptor (PAR)-1 antagonist, on platelet biomarkers in healthy volunteers and patients with coronary artery disease
    • Serebruany VL, Kogushi M, Dastros-Pitei D, Flather M, Bhatt DL (2009) The in-vitro effects of E5555, a protease-activated receptor (PAR)-1 antagonist, on platelet biomarkers in healthy volunteers and patients with coronary artery disease. Thromb Haemost 102:111-119
    • (2009) Thromb Haemost , vol.102 , pp. 111-119
    • Serebruany, V.L.1    Kogushi, M.2    Dastros-Pitei, D.3    Flather, M.4    Bhatt, D.L.5
  • 29
    • 84860134566 scopus 로고    scopus 로고
    • Safety of the novel protease-activated receptor-1 antagonist Vorapaxar in Japanese patients with a history of ischemic stroke
    • Shinohara Y, Goto S, Doi M, Jensen P (2012) Safety of the novel protease-activated receptor-1 antagonist Vorapaxar in Japanese patients with a history of ischemic stroke. J Stroke Cerebrovasc Dis 1(4):318-24
    • (2012) J Stroke Cerebrovasc Dis , vol.1 , Issue.4 , pp. 318-324
    • Shinohara, Y.1    Goto, S.2    Doi, M.3    Jensen, P.4
  • 30
    • 0035899289 scopus 로고    scopus 로고
    • Effects of clopidogrel in addition to aspirin in patients with acute coronary syndromes without ST-segment elevation
    • The Clopidogrel In Unstable Angina To Prevent Recurrent Events Trial Investigators
    • The Clopidogrel in Unstable Angina to Prevent Recurrent Events Trial Investigators (2001) Effects of clopidogrel in addition to aspirin in patients with acute coronary syndromes without ST-segment elevation. N Engl J Med 345:494-502
    • (2001) N Engl J Med , vol.345 , pp. 494-502
  • 31
    • 85058720552 scopus 로고    scopus 로고
    • The Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome (TRA-CER) trial: Study design and rationale
    • The TRACER Executive Steering C
    • The TRACER Executive Steering C (2009) The Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome (TRA-CER) trial: study design and rationale. Am Hear J 158:327-334
    • (2009) Am Hear J , vol.158 , pp. 327-334
  • 32
    • 83655177669 scopus 로고    scopus 로고
    • Thrombin-receptor antagonist vorapaxar in acute coronary syndromes
    • Tricoci P, Huang Z, Held C et al (2012) Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. N Engl J Med 366(1):20-33
    • (2012) N Engl J Med , vol.366 , Issue.1 , pp. 20-33
    • Tricoci, P.1    Huang, Z.2    Held, C.3
  • 33
    • 37849002889 scopus 로고    scopus 로고
    • Prasugrel achieves greater and faster P2Y12receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite in aspirin-treated patients with coronary artery disease
    • Wallentin L, Varenhorst C, James S et al (2008) Prasugrel achieves greater and faster P2Y12receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite in aspirin-treated patients with coronary artery disease. Eur Heart J 29:21-30
    • (2008) Eur Heart J , vol.29 , pp. 21-30
    • Wallentin, L.1    Varenhorst, C.2    James, S.3
  • 34
    • 70149101223 scopus 로고    scopus 로고
    • Ticagrelor versus clopidogrel in patients with acute coronary syndromes
    • Wallentin L, Becker RC, Budaj A et al (2009) Ticagrelor versus clopidogrel in patients with acute coronary syndromes. N Engl J Med 361:1045-1057
    • (2009) N Engl J Med , vol.361 , pp. 1045-1057
    • Wallentin, L.1    Becker, R.C.2    Budaj, A.3
  • 35
    • 36148983750 scopus 로고    scopus 로고
    • Prasugrel versus clopidogrel in patients with acute coronary syndromes
    • Wiviott SD, Braunwald E, McCabe CH et al (2007) Prasugrel versus clopidogrel in patients with acute coronary syndromes. N Engl J Med 357:2001-2015
    • (2007) N Engl J Med , vol.357 , pp. 2001-2015
    • Wiviott, S.D.1    Braunwald, E.2    McCabe, C.H.3
  • 36
    • 85027951718 scopus 로고    scopus 로고
    • Randomized trial of atopaxar in the treatment of patients with coronary artery disease/clinical perspective
    • Wiviott SD, FlatherMD, O'DonoghueML et al (2011) Randomized trial of atopaxar in the treatment of patients with coronary artery disease/clinical perspective. Circulation 123:1854-1863
    • (2011) Circulation , vol.123 , pp. 1854-1863
    • Wiviott, S.D.1    O'Donoghueml, F.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.