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Volumn 10, Issue 1, 2014, Pages 43-52

Betrixaban (PRT054021): Pharmacology, dose selection and clinical studies

Author keywords

atrial fibrillation; betrixaban; direct factor Xa inhibitor; oral anticoagulant; thromboprophylaxis

Indexed keywords

APIXABAN; BETRIXABAN; CLOPIDOGREL; DABIGATRAN; EDOXABAN; ENOXAPARIN; FONDAPARINUX; RIVAROXABAN; WARFARIN;

EID: 84891118494     PISSN: 14796678     EISSN: 17448298     Source Type: Journal    
DOI: 10.2217/fca.13.98     Document Type: Review
Times cited : (33)

References (27)
  • 1
    • 84856772158 scopus 로고    scopus 로고
    • Evidence-based management of anticoagulant therapy: Antithrombotic therapy and prevention of thrombosis, 9th ed: American college of chest physicians evidence-based clinical practice guidelines
    • Holbrook A, Schulman S, Witt DM et al. Evidence-based management of anticoagulant therapy: Antithrombotic therapy and prevention of thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines. Chest 141(Suppl. 2), e152S-e184S (2012
    • (2012) Chest , vol.141 , Issue.SUPPL. 2
    • Holbrook, A.1    Schulman, S.2    Witt, D.M.3
  • 2
    • 70349306707 scopus 로고    scopus 로고
    • Dabigatran versus warfarin in patients with atrial fibrillation
    • Connolly SJ, Ezekowitz MD, Yusuf S et al. Dabigatran versus warfarin in patients with atrial fibrillation. N. Engl. J. Med. 361(12), 1139-1151 (2009
    • (2009) N. Engl. J. Med , vol.361 , Issue.12 , pp. 1139-1151
    • Connolly, S.J.1    Ezekowitz, M.D.2    Yusuf, S.3
  • 3
    • 80052592404 scopus 로고    scopus 로고
    • Rivaroxaban versus warfarin in nonvalvular atrial fibrillation
    • Patel MR, Mahaffey KW, Garg J et al. Rivaroxaban versus warfarin in nonvalvular atrial fibrillation. N. Engl. J. Med. 365(10), 883-891 (2011
    • (2011) N. Engl. J. Med , vol.365 , Issue.10 , pp. 883-891
    • Patel, M.R.1    Mahaffey, K.W.2    Garg, J.3
  • 4
    • 80052825103 scopus 로고    scopus 로고
    • Apixaban versus warfarin in patients with atrial fibrillation
    • Granger CB, Alexander JH, McMurray JJ et al. Apixaban versus warfarin in patients with atrial fibrillation. N. Engl. J. Med. 365(11), 981-992 (2011
    • (2011) N. Engl. J. Med , vol.365 , Issue.11 , pp. 981-992
    • Granger, C.B.1    Alexander, J.H.2    McMurray, J.J.3
  • 5
    • 84873596181 scopus 로고    scopus 로고
    • Apixaban for extended treatment of venous thromboembolism
    • Agnelli G, Buller HR, Cohen A et al. Apixaban for extended treatment of venous thromboembolism. N. Engl. J. Med. 368(8), 699-708 (2013
    • (2013) N. Engl. J. Med , vol.368 , Issue.8 , pp. 699-708
    • Agnelli, G.1    Buller, H.R.2    Cohen, A.3
  • 6
    • 84859385808 scopus 로고    scopus 로고
    • Oral rivaroxaban for the treatment of symptomatic pulmonary embolism
    • Buller HR, Prins MH, Lensin AW et al. Oral rivaroxaban for the treatment of symptomatic pulmonary embolism. N. Engl. J. Med. 366(14), 1287-1297 (2012
    • (2012) N. Engl. J. Med , vol.366 , Issue.14 , pp. 1287-1297
    • Buller, H.R.1    Prins, M.H.2    Lensin, A.W.3
  • 7
    • 71849117615 scopus 로고    scopus 로고
    • Dabigatran versus warfarin in the treatment of acute venous thromboembolism
    • Schulman S, Kearon C, Kakkar AK et al. Dabigatran versus warfarin in the treatment of acute venous thromboembolism. N. Engl. J. Med. 361(24), 2342-2352 (2009
    • (2009) N. Engl. J. Med , vol.361 , Issue.24 , pp. 2342-2352
    • Schulman, S.1    Kearon, C.2    Kakkar, A.K.3
  • 8
    • 77957932391 scopus 로고    scopus 로고
    • Evaluation of the novel factor xa inhibitor edoxaban compared with warfarin in patients with atrial fibrillation: Design and rationale for the effective anticoagulation with factor xa next generation in atrial fibrillation-thrombozlysis in myocardial infarction study 48 (engage af-timi 48
    • Ruff CT, Giugliano RP, Antman EM et al. Evaluation of the novel factor Xa inhibitor edoxaban compared with warfarin in patients with atrial fibrillation: Design and rationale for the effective anticoagulation with factor Xa next generation in atrial fibrillation-thrombozlysis in myocardial infarction study 48 (ENGAGE AF-TIMI 48). Am. Heart J. 160(4), 635-641 (2010
    • (2010) Am. Heart J. , vol.160 , Issue.4 , pp. 635-641
    • Ruff, C.T.1    Giugliano, R.P.2    Antman, E.M.3
  • 9
    • 63149141508 scopus 로고    scopus 로고
    • Discovery of betrixaban (prt054021), n-(5-chloropyridin-2-yl)-2-(4-(n, n-dimethylcarbamimidoyl)benzamido)-5-methoxybenz amide, ahighly potent, selective, and orally efficacious factor xa inhibitor
    • Zhang P, Huang W, Wang L et al. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N, N-dimethylcarbamimidoyl)benzamido)-5- methoxybenz amide, ahighly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg. Med. Chem. Lett. 19(8), 2179-2185 (2009
    • (2009) Bioorg. Med. Chem. Lett , vol.19 , Issue.8 , pp. 2179-2185
    • Zhang, P.1    Huang, W.2    Wang, L.3
  • 10
    • 60849097858 scopus 로고    scopus 로고
    • A randomized evaluation of betrixaban, an oral factor xa inhibitor, for prevention of thromboembolic events after total knee replacement (expert
    • Turpie AG, Bauer KA, Davidson BL et al. A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT). Thromb. Haemost. 101(1), 68-76 (2009
    • (2009) Thromb. Haemost , vol.101 , Issue.1 , pp. 68-76
    • Turpie, A.G.1    Bauer, K.A.2    Davidson, B.L.3
  • 11
    • 84878290471 scopus 로고    scopus 로고
    • Betrixaban compared with warfarin in patients with atrial fibrillation: Results of a phase 2, randomized, dose-ranging study (explore-xa
    • Connolly SJ, Eikelboom J, Dorian P et al. Betrixaban compared with warfarin in patients with atrial fibrillation: Results of a Phase 2, randomized, dose-ranging study (EXPLORE-Xa). Eur. Heart J. 34(20), 1498-1505 (2013
    • (2013) Eur. Heart J. , vol.34 , Issue.20 , pp. 1498-1505
    • Connolly, S.J.1    Eikelboom, J.2    Dorian, P.3
  • 12
    • 34249303314 scopus 로고    scopus 로고
    • Animal models of thrombosis help predict the human therapeutic concentration of prt54021, apotent oral factor xa inhibitor
    • Abe K, Siu G, Edwards S et al. Animal models of thrombosis help predict the human therapeutic concentration of PRT54021, apotent oral factor Xa inhibitor. Blood 108(11), A270-A270 (2006
    • (2006) Blood , vol.108 , Issue.11
    • Abe, K.1    Siu, G.2    Edwards, S.3
  • 13
    • 77956319689 scopus 로고    scopus 로고
    • Antithrombotic activity of PRT54021, a potent oral direct factor Xa inhibitor, can be monitored using a novel prothrombinase inhibition bioassay
    • Sinha U, Edwards ST, Wong PW et al. Antithrombotic activity of PRT54021, a potent oral direct factor Xa inhibitor, can be monitored using a novel prothrombinase inhibition bioassay. Blood 108(11), A272-A272 (2006
    • (2006) Blood , vol.108 , Issue.11
    • Sinha, U.1    Edwards, S.T.2    Wong, P.W.3
  • 14
    • 84871563191 scopus 로고    scopus 로고
    • Absence of QTc prolongation with betrixaban: A randomized, double-blind, placebo-and positive-controlled thorough ECG study
    • Morganroth J, Gretler DD, Hollenbach SJ, Lambing JL, Sinha U. Absence of QTc prolongation with betrixaban: A randomized, double-blind, placebo-and positive-controlled thorough ECG study. Expert Opin. Pharmacother. 14(1), 5-13 (2013
    • (2013) Expert Opin. Pharmacother , vol.14 , Issue.1 , pp. 5-13
    • Morganroth, J.1    Gretler, D.D.2    Hollenbach, S.J.3    Lambing, J.L.4    Sinha, U.5
  • 16
    • 77955951754 scopus 로고    scopus 로고
    • Extended-duration venous thromboembolism prophylaxis in acutely ill medical patients with recently reduced mobility: A randomized trial
    • Hull RD, Schellong SM, Tapson VF et al. Extended-duration venous thromboembolism prophylaxis in acutely ill medical patients with recently reduced mobility: A randomized trial. Ann. Intern. Med. 153(1), 8-18 (2010
    • (2010) Ann. Intern. Med , vol.153 , Issue.1 , pp. 8-18
    • Hull, R.D.1    Schellong, S.M.2    Tapson, V.F.3
  • 17
    • 83155193223 scopus 로고    scopus 로고
    • Apixaban versus enoxaparin for thromboprophylaxis in medically ill patients
    • Goldhaber SZ, Leizorovicz A, Kakkar AK et al. Apixaban versus enoxaparin for thromboprophylaxis in medically ill patients. N. Engl. J. Med. 365(23), 2167-2177 (2011
    • (2011) N. Engl. J. Med , vol.365 , Issue.23 , pp. 2167-2177
    • Goldhaber, S.Z.1    Leizorovicz, A.2    Kakkar, A.K.3
  • 18
    • 84873514413 scopus 로고    scopus 로고
    • Rivaroxaban for thromboprophylaxis in acutely ill medical patients
    • Cohen AT, Spiro TE, Buller HR et al. Rivaroxaban for thromboprophylaxis in acutely ill medical patients. N. Engl. J. Med. 368(6), 513-523 (2013
    • (2013) N. Engl. J. Med , vol.368 , Issue.6 , pp. 513-523
    • Cohen, A.T.1    Spiro, T.E.2    Buller, H.R.3
  • 19
    • 84878460192 scopus 로고    scopus 로고
    • A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa
    • Lu G, Deguzman FR, Hollenbach SJ et al. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat. Med. 19(4), 446-451 (2013
    • (2013) Nat. Med , vol.19 , Issue.4 , pp. 446-451
    • Lu, G.1    Deguzman, F.R.2    Hollenbach, S.J.3
  • 20
    • 34547106820 scopus 로고    scopus 로고
    • Preclinical and clinical characteristics of rivaroxaban: A novel, oral, direct factor Xa inhibitor
    • Laux V, Perzborn E, Kubitza D, Misselwitz F. Preclinical and clinical characteristics of rivaroxaban: A novel, oral, direct factor Xa inhibitor. Semin. Thromb. Hemost. 33(5), 515-523 (2007
    • (2007) Semin. Thromb. Hemost , vol.33 , Issue.5 , pp. 515-523
    • Laux, V.1    Perzborn, E.2    Kubitza, D.3    Misselwitz, F.4
  • 21
    • 22844442726 scopus 로고    scopus 로고
    • In vitro and in vivo studies of the novel antithrombotic agent bay 59-7939 -an oral, direct factor xa inhibitor
    • Perzborn E, Strassburger J, Wilmen A et al. In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939 -an oral, direct factor Xa inhibitor. J. Thromb. Haemost. 3(3), 514-521 (2005
    • (2005) J. Thromb. Haemost , vol.3 , Issue.3 , pp. 514-521
    • Perzborn, E.1    Strassburger, J.2    Wilmen, A.3
  • 22
    • 66449099711 scopus 로고    scopus 로고
    • Metabolism and excretion of rivaroxaban, an oral, direct factor Xa inhibitor, in rats, dogs, and humans
    • Weinz C, Schwarz T, Kubitza D, Mueck W, Lang D. Metabolism and excretion of rivaroxaban, an oral, direct factor Xa inhibitor, in rats, dogs, and humans. Drug Metab. Dispos. 37(5), 1056-1064 (2009
    • (2009) Drug Metab. Dispos , vol.37 , Issue.5 , pp. 1056-1064
    • Weinz, C.1    Schwarz, T.2    Kubitza, D.3    Mueck, W.4    Lang, D.5
  • 23
    • 42149172523 scopus 로고    scopus 로고
    • Apixaban, an oral, direct and highly selective factor Xa inhibitor: In vitro, antithrombotic and antihemostatic studies
    • Wong PC, Crain EJ, Xin B et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: In vitro, antithrombotic and antihemostatic studies. J. Thromb. Haemost. 6(5), 820-829 (2008
    • (2008) J. Thromb. Haemost , vol.6 , Issue.5 , pp. 820-829
    • Wong, P.C.1    Crain, E.J.2    Xin, B.3
  • 24
    • 80052351015 scopus 로고    scopus 로고
    • Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor
    • Wong PC, Pinto DJ, Zhang D. Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor. J. Thromb. Thrombolysis 31(4), 478-492 (2011
    • (2011) J. Thromb. Thrombolysis , vol.31 , Issue.4 , pp. 478-492
    • Wong, P.C.1    Pinto, D.J.2    Zhang, D.3
  • 25
    • 67650809062 scopus 로고    scopus 로고
    • Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans
    • Zhang D, He K, Raghavan N et al. Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans. Drug Metab. Dispos. 37(8), 1738-1748 (2009
    • (2009) Drug Metab. Dispos , vol.37 , Issue.8 , pp. 1738-1748
    • Zhang, D.1    He, K.2    Raghavan, N.3
  • 26
    • 84869109465 scopus 로고    scopus 로고
    • Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans
    • Bathala MS, Masumoto H, Oguma T, He L, Lowrie C, Mendell J. Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans. Drug Metab. Dispos. 40(12), 2250-2255 (2012
    • (2012) Drug Metab. Dispos , vol.40 , Issue.12 , pp. 2250-2255
    • Bathala, M.S.1    Masumoto, H.2    Oguma, T.3    He, L.4    Lowrie, C.5    Mendell, J.6
  • 27
    • 49849099533 scopus 로고    scopus 로고
    • DU-176b, a potent and orally active factor Xa inhibitor: In vitro and in vivo pharmacological profiles
    • Furugohri T, Isobe K, Honda Y et al. DU-176b, a potent and orally active factor Xa inhibitor: In vitro and in vivo pharmacological profiles. J. Thromb. Haemost. 6(9), 1542-1549 (2008
    • (2008) J. Thromb. Haemost , vol.6 , Issue.9 , pp. 1542-1549
    • Furugohri, T.1    Isobe, K.2    Honda, Y.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.