메뉴 건너뛰기




Volumn 53, Issue 11, 2013, Pages 1131-1138

Safety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple]dose study in healthy subjects

Author keywords

Endothelin receptor antagonist; Healthy subjects; Macitentan; Pharmacodynamics; Pharmacokinetics

Indexed keywords

6BETA HYDROXYHYDROCORTISONE; ACT 132577; ALANINE AMINOTRANSFERASE; ALKALINE PHOSPHATASE; ASPARTATE AMINOTRANSFERASE; BILE SALT; BILIRUBIN; CYTOCHROME P450 3A4; DRUG METABOLITE; ENDOTHELIN 1; ENDOTHELIN RECEPTOR ANTAGONIST; HYDROCORTISONE; MACITENTAN; PLACEBO; UNCLASSIFIED DRUG;

EID: 84892915544     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1002/jcph.152     Document Type: Article
Times cited : (57)

References (35)
  • 1
    • 70849089564 scopus 로고    scopus 로고
    • Pharmacokinetic and clinical profile of a novel formulation of bosentan in children with pulmonary arterial hypertension: The future1 study
    • Beghetti M, Haworth SG, Bonnet D, et al. Pharmacokinetic and clinical profile of a novel formulation of bosentan in children with pulmonary arterial hypertension: The future1 study. J Clin Pharmacol. 2009;68(6):948-955.
    • (2009) J Clin Pharmacol , vol.68 , Issue.6 , pp. 948-955
    • Beghetti, M.1    Haworth, S.G.2    Bonnet, D.3
  • 3
    • 36849008609 scopus 로고    scopus 로고
    • Endothelin receptor antagonists in cancer therapy
    • Lalich M, McNeel DG, Wilding G, et al. Endothelin receptor antagonists in cancer therapy. Cancer Invest. 2007;25(8):785-794.
    • (2007) Cancer Invest , vol.25 , Issue.8 , pp. 785-794
    • Lalich, M.1    McNeel, D.G.2    Wilding, G.3
  • 4
    • 77951443168 scopus 로고    scopus 로고
    • Pharmacotherapeutic management of pulmonary arterial hypertension
    • Anderson JR, Nawarskas JJ. Pharmacotherapeutic management of pulmonary arterial hypertension. Cardiol Rev. 2010;18(3):148-162.
    • (2010) Cardiol Rev , vol.18 , Issue.3 , pp. 148-162
    • Anderson, J.R.1    Nawarskas, J.J.2
  • 5
    • 44949256178 scopus 로고    scopus 로고
    • Endothelin receptor antagonists for pulmonary arterial hypertension: Rationale and place in therapy
    • Price LC, Howard LS. Endothelin receptor antagonists for pulmonary arterial hypertension: Rationale and place in therapy. Am J Cardiovasc Drugs. 2008;8(3):171-185.
    • (2008) Am J Cardiovasc Drugs , vol.8 , Issue.3 , pp. 171-185
    • Price, L.C.1    Howard, L.S.2
  • 6
    • 70349162027 scopus 로고    scopus 로고
    • Bosentan: A review of its use in the management of digital ulcers associated with systemic sclerosis
    • Dhillon S. Bosentan: A review of its use in the management of digital ulcers associated with systemic sclerosis. Drugs. 2009;69(14): 2005-2024.
    • (2009) Drugs , vol.69 , Issue.14 , pp. 2005-2024
    • Dhillon, S.1
  • 7
    • 84877297353 scopus 로고    scopus 로고
    • Treatment of idiopathic pulmonary fibrosis with ambrisentan: A parallel, randomized trial
    • Raghu G, Behr J, Brown KK, et al. Treatment of idiopathic pulmonary fibrosis with ambrisentan: A parallel, randomized trial. Ann Intern Med. 2013;158(9):641-649.
    • (2013) Ann Intern Med , vol.158 , Issue.9 , pp. 641-649
    • Raghu, G.1    Behr, J.2    Brown, K.K.3
  • 8
    • 84880439899 scopus 로고    scopus 로고
    • Inflammatory responses of airway smooth muscle cells and effects of endothelin receptor antagonism
    • Knobloch J, Lin Y, Konradi J, et al. Inflammatory responses of airway smooth muscle cells and effects of endothelin receptor antagonism. Am J Respir Cell Mol Biol. 2013;49(1):114-127.
    • (2013) Am J Respir Cell Mol Biol , vol.49 , Issue.1 , pp. 114-127
    • Knobloch, J.1    Lin, Y.2    Konradi, J.3
  • 9
    • 33646526270 scopus 로고    scopus 로고
    • Endothelin receptor antagonists
    • Motte S, McEntee K, Naeije R. Endothelin receptor antagonists. Pharmacol Ther. 2006;110(3):386-414.
    • (2006) Pharmacol Ther , vol.110 , Issue.3 , pp. 386-414
    • Motte, S.1    McEntee, K.2    Naeije, R.3
  • 10
    • 84867342891 scopus 로고    scopus 로고
    • An evaluation of reproductive and developmental toxicity of sitaxentan (thelin) in rats
    • Cross DM, Horsley E, Derzi M, et al. An evaluation of reproductive and developmental toxicity of sitaxentan (thelin) in rats. Birth Defects Res B Dev Reprod Toxicol. 2012;95(5):327-336.
    • (2012) Birth Defects Res B Dev Reprod Toxicol , vol.95 , Issue.5 , pp. 327-336
    • Cross, D.M.1    Horsley, E.2    Derzi, M.3
  • 11
    • 84867396866 scopus 로고    scopus 로고
    • Frequency of edema in patients with pulmonary arterial hypertension receiving ambrisentan
    • Shapiro S, Pollock DM, Gillies H, et al. Frequency of edema in patients with pulmonary arterial hypertension receiving ambrisentan. Am J Cardiol. 2012;110(9):1373-1377.
    • (2012) Am J Cardiol , vol.110 , Issue.9 , pp. 1373-1377
    • Shapiro, S.1    Pollock, D.M.2    Gillies, H.3
  • 12
    • 84867578454 scopus 로고    scopus 로고
    • Endothelin receptor antagonists for the treatment of pulmonary artery hypertension
    • Rubin LJ. Endothelin receptor antagonists for the treatment of pulmonary artery hypertension. Life Sci. 2012;91(13-14):517-521.
    • (2012) Life Sci , vol.91 , Issue.13-14 , pp. 517-521
    • Rubin, L.J.1
  • 13
    • 10944231356 scopus 로고    scopus 로고
    • Clinical pharmacology of bosentan, a dual endothelin receptor antagonist
    • Dingemanse J, van Giersbergen PL. Clinical pharmacology of bosentan, a dual endothelin receptor antagonist. Clin Pharmacokinet. 2004;43(15):1089-1115.
    • (2004) Clin Pharmacokinet , vol.43 , Issue.15 , pp. 1089-1115
    • Dingemanse, J.1    Van Giersbergen, P.L.2
  • 14
    • 0033991960 scopus 로고    scopus 로고
    • Molecular cloning and characterization of the murine bile salt export pump
    • Green RM, Hoda F, Ward KL. Molecular cloning and characterization of the murine bile salt export pump. Gene. 2000;241(1):117-123.
    • (2000) Gene , vol.241 , Issue.1 , pp. 117-123
    • Green, R.M.1    Hoda, F.2    Ward, K.L.3
  • 15
    • 0035036050 scopus 로고    scopus 로고
    • The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: A potential mechanism for hepatic adverse reactions
    • Fattinger K, Funk C, Pantze M, et al. The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: A potential mechanism for hepatic adverse reactions. Clin Pharmacol Ther. 2001;69(4):223-231.
    • (2001) Clin Pharmacol Ther , vol.69 , Issue.4 , pp. 223-231
    • Fattinger, K.1    Funk, C.2    Pantze, M.3
  • 16
    • 84866307803 scopus 로고    scopus 로고
    • The discovery of N[5(4bromophenyl)6[2[(5bromo2pyrimidinyl)oxy]ethoxy] 4pyrimidinyl] N0 propylsulfamide (macitentan), an orally active, potent dual endothelin receptor antagonist
    • Bolli MH, Boss C, Binkert C, et al. The discovery of N[5(4 bromophenyl)6[2[(5bromo2pyrimidinyl)oxy]ethoxy]4pyrimidinyl] N0 propylsulfamide (macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem. 2012;55(17): 7849-7861.
    • (2012) J Med Chem , vol.55 , Issue.17 , pp. 7849-7861
    • Bolli, M.H.1    Boss, C.2    Binkert, C.3
  • 17
    • 84867562420 scopus 로고    scopus 로고
    • Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells
    • Gatfield J, Mueller Grandjean C, Sasse T, et al. Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells. PLoS ONE. 2012;7(10):e47662.
    • (2012) PLoS ONE , vol.7 , Issue.10
    • Gatfield, J.1    Mueller Grandjean, C.2    Sasse, T.3
  • 18
    • 84870740909 scopus 로고    scopus 로고
    • Macitentan, a new dual endothelin receptor antagonist, improves its efficacy in a rat model of pulmonary fibrosis associated with pulmonary arterial hypertension (abstract)
    • Iglarz M, Landskroner K, Rey M, et al. Macitentan, a new dual endothelin receptor antagonist, improves its efficacy in a rat model of pulmonary fibrosis associated with pulmonary arterial hypertension (abstract). Am J Respir Crit Care Med. 2011;183:A6445.
    • (2011) Am J Respir Crit Care Med , vol.183
    • Iglarz, M.1    Landskroner, K.2    Rey, M.3
  • 19
    • 57349133022 scopus 로고    scopus 로고
    • Pharmacology of macitentan, an orally active tissuetargeting dual endothelin receptor antagonist
    • Iglarz M, Binkert C, Morrison K, et al. Pharmacology of macitentan, an orally active tissuetargeting dual endothelin receptor antagonist. J Pharmacol Exp Ther. 2008;327(3):736-745.
    • (2008) J Pharmacol Exp Ther , vol.327 , Issue.3 , pp. 736-745
    • Iglarz, M.1    Binkert, C.2    Morrison, K.3
  • 20
    • 80054771944 scopus 로고    scopus 로고
    • Macitentan: Entryinto humans study with a new endothelin receptor antagonist
    • Sidharta PN, van Giersbergen PL, Halabi A, et al. Macitentan: Entryinto humans study with a new endothelin receptor antagonist. Eur J Clin Pharmacol. 2011;67(10):977-984.
    • (2011) Eur J Clin Pharmacol , vol.67 , Issue.10 , pp. 977-984
    • Sidharta, P.N.1    Van Giersbergen, P.L.2    Halabi, A.3
  • 21
    • 34547558919 scopus 로고    scopus 로고
    • Results of european postmarketing surveillance of bosentan in pulmonary hypertension
    • Humbert M, Segal ES, Kiely DG, et al. Results of european postmarketing surveillance of bosentan in pulmonary hypertension. Eur Respir J. 2007;30(2):338-344.
    • (2007) Eur Respir J , vol.30 , Issue.2 , pp. 338-344
    • Humbert, M.1    Segal, E.S.2    Kiely, D.G.3
  • 22
    • 0347361482 scopus 로고    scopus 로고
    • Urinary 6bhydroxycortisol: A validated test for evaluating drug induction or drug inhibition mediated through cyp3a in humans and animals
    • GalteauMM, Shamsa F. Urinary 6bhydroxycortisol: A validated test for evaluating drug induction or drug inhibition mediated through cyp3a in humans and animals. Eur J Clin Pharmacol. 2003;59: 713-733.
    • (2003) Eur J Clin Pharmacol , vol.59 , pp. 713-733
    • Galteaumm Shamsa, F.1
  • 23
    • 70349807555 scopus 로고    scopus 로고
    • Comparison of the dissolution and pharmacokinetic profiles of two galenical formulations of the endothelin receptor antagonist macitentan
    • Kummer O, Haschke M, Hammann F, et al. Comparison of the dissolution and pharmacokinetic profiles of two galenical formulations of the endothelin receptor antagonist macitentan. Eur J Pharm Sci. 2009;38(4):384-388.
    • (2009) Eur J Pharm Sci , vol.38 , Issue.4 , pp. 384-388
    • Kummer, O.1    Haschke, M.2    Hammann, F.3
  • 24
    • 0029094562 scopus 로고
    • Assessment of dose proportionality: Report from the statisticians in the pharmaceutical industry/pharmacokinetics uk joint working party
    • Gough K, Hutchison M, Keene O, et al. Assessment of dose proportionality: Report from the statisticians in the pharmaceutical industry/pharmacokinetics uk joint working party. Drug Inf J. 1995;29:1039-1048.
    • (1995) Drug Inf J , vol.29 , pp. 1039-1048
    • Gough, K.1    Hutchison, M.2    Keene, O.3
  • 25
    • 84857627857 scopus 로고    scopus 로고
    • Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissuetargeting dual endothelin receptor antagonist
    • Bruderer S, Aanismaa P, Homery MC, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissuetargeting dual endothelin receptor antagonist. AAPS J. 2012; 14(1):68-78.
    • (2012) AAPS J , vol.14 , Issue.1 , pp. 68-78
    • Bruderer, S.1    Aanismaa, P.2    Homery, M.C.3
  • 26
    • 84872192521 scopus 로고    scopus 로고
    • Effect of macitentan on morbidity and mortality in pulmonary arterial hypertension (PAH): Results from the seraphin trial
    • Rubin LJ, Pulido T, Channick R, et al. Effect of macitentan on morbidity and mortality in pulmonary arterial hypertension (PAH): Results from the seraphin trial. Am Coll Chest Physicians - Chest. 2012;142(4-meeting abstracts):1026A.
    • (2012) Am Coll Chest Physicians-Chest , vol.142
    • Rubin, L.J.1    Pulido, T.2    Channick, R.3
  • 27
    • 84880767255 scopus 로고    scopus 로고
    • Lack of clinically relevant pharmacokinetic interactions between the dual endothelin receptor antagonist macitentan and sildenafil in healthy subjects
    • Sidharta PN, van Giersbergen PL, Wolzt M, et al. Lack of clinically relevant pharmacokinetic interactions between the dual endothelin receptor antagonist macitentan and sildenafil in healthy subjects. Am J Respir Crit Care Med. 2012;185:A4802.
    • (2012) Am J Respir Crit Care Med , vol.185
    • Sidharta, P.N.1    Van Giersbergen, P.L.2    Wolzt, M.3
  • 28
    • 84888166435 scopus 로고    scopus 로고
    • Macitentan for the treatment of idiopathic pulmonary fibrosis: The randomised controlled MUSIC trial
    • doi: 10.1183/09031936.00104612
    • Raghu G, MillionRousseau R, Morganti A, et al. Macitentan for the treatment of idiopathic pulmonary fibrosis: The randomised controlled MUSIC trial. Eur Respir J. 2013, doi: 10.1183/09031936.00104612
    • (2013) Eur Respir J
    • Raghu, G.1    Millionrousseau, R.2    Morganti, A.3
  • 29
    • 0033061022 scopus 로고    scopus 로고
    • Transaminase elevation on placebo during phase i trials: Prevalence and significance
    • Rosenzweig P, Miget N, Brohier S. Transaminase elevation on placebo during phase I trials: Prevalence and significance. Br J Clin Pharmacol. 1999;48(1):19-23.
    • (1999) Br J Clin Pharmacol , vol.48 , Issue.1 , pp. 19-23
    • Rosenzweig, P.1    Miget, N.2    Brohier, S.3
  • 30
    • 79952277323 scopus 로고    scopus 로고
    • Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwichcultured human hepatocytes
    • Hartman JC, Brouwer K, Mandagere A, et al. Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwichcultured human hepatocytes. Can J Physiol Pharmacol. 2010;88(6):682-691.
    • (2010) Can J Physiol Pharmacol , vol.88 , Issue.6 , pp. 682-691
    • Hartman, J.C.1    Brouwer, K.2    Mandagere, A.3
  • 31
    • 0028333046 scopus 로고
    • Clearance of circulating endothelin1 by ETB receptors in rats
    • Fukuroda T, Fujikawa T, Ozaki S, et al. Clearance of circulating endothelin1 by ETB receptors in rats. Biochem Biophys Res Commun. 1994;199(3):1461-1465.
    • (1994) Biochem Biophys Res Commun , vol.199 , Issue.3 , pp. 1461-1465
    • Fukuroda, T.1    Fujikawa, T.2    Ozaki, S.3
  • 32
    • 84880807894 scopus 로고    scopus 로고
    • Investigation of the effects of ketoconazole on the pharmacokinetics of macitentan, a novel dual endothelin receptor antagonist, in healthy subjects
    • Atsmon J, Dingemanse J, Shaikevich D, et al. Investigation of the effects of ketoconazole on the pharmacokinetics of macitentan, a novel dual endothelin receptor antagonist, in healthy subjects. Clin Pharmacokinet. 2013;52(8):685-692.
    • (2013) Clin Pharmacokinet , vol.52 , Issue.8 , pp. 685-692
    • Atsmon, J.1    Dingemanse, J.2    Shaikevich, D.3
  • 33
    • 0033158340 scopus 로고    scopus 로고
    • Multipledose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers
    • Weber C, Schmitt R, Birnboeck H, et al. Multipledose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers. J Clin Pharmacol. 1999;39 (7):703-714.
    • (1999) J Clin Pharmacol , vol.39 , Issue.7 , pp. 703-714
    • Weber, C.1    Schmitt, R.2    Birnboeck, H.3
  • 34
    • 0032801792 scopus 로고    scopus 로고
    • Morning spot and 24hour urinary 6 betahydroxycortisol to cortisol ratios: Intraindividual variability and correlation under basal conditions and conditions of cyp 3a4 induction
    • Tran JQ, Kovacs SJ, McIntosh TS, et al. Morning spot and 24hour urinary 6 betahydroxycortisol to cortisol ratios: Intraindividual variability and correlation under basal conditions and conditions of cyp 3a4 induction. J Clin Pharmacol. 1999;39(5):487-494.
    • (1999) J Clin Pharmacol , vol.39 , Issue.5 , pp. 487-494
    • Tran, J.Q.1    Kovacs, S.J.2    McIntosh, T.S.3
  • 35
    • 36749017545 scopus 로고    scopus 로고
    • Drugs as cyp3a probes, inducers, and inhibitors
    • Liu YT, Hao HP, Liu CX, et al. Drugs as cyp3a probes, inducers, and inhibitors. Drug Metab Rev. 2007;39(4):699-721.
    • (2007) Drug Metab Rev , vol.39 , Issue.4 , pp. 699-721
    • Liu, Y.T.1    Hao, H.P.2    Liu, C.X.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.