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Volumn 78, Issue 5, 2014, Pages 1035-1042

Investigation of mutual pharmacokinetic interactions between macitentan, a novel endothelin receptor antagonist, and sildenafil in healthy subjects

Author keywords

Drug drug interaction; Endothelin receptor antagonist; Healthy subjects; Macitentan; Pharmacokinetics; Sildenafil

Indexed keywords

DRUG METABOLITE; MACITENTAN; SILDENAFIL; CYP3A4 PROTEIN, HUMAN; CYTOCHROME P450 3A; ENDOTHELIN RECEPTOR ANTAGONIST; PHOSPHODIESTERASE V INHIBITOR; PIPERAZINE DERIVATIVE; PURINE DERIVATIVE; PYRIMIDINE DERIVATIVE; SULFONAMIDE;

EID: 84918802150     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/bcp.12447     Document Type: Article
Times cited : (21)

References (49)
  • 1
    • 0031031440 scopus 로고    scopus 로고
    • Primary pulmonary hypertension
    • Rubin LJ. Primary pulmonary hypertension. N Engl J Med 1997; 336: 111-7.
    • (1997) N Engl J Med , vol.336 , pp. 111-117
    • Rubin, L.J.1
  • 3
    • 55249105959 scopus 로고    scopus 로고
    • Pulmonary arterial hypertension and its association with HIV infection: An overview
    • Lederman MM, Sereni D, Simonneau G, Voelkel NF. Pulmonary arterial hypertension and its association with HIV infection: an overview. AIDS 2008; 22: (Suppl. 3): S1-6.
    • (2008) AIDS , vol.22 , pp. S1-6
    • Lederman, M.M.1    Sereni, D.2    Simonneau, G.3    Voelkel, N.F.4
  • 4
    • 0032844284 scopus 로고    scopus 로고
    • Pulmonary hypertension related to drugs and toxins
    • Abenhaim L, Humbert M. Pulmonary hypertension related to drugs and toxins. Curr Opin Cardiol 1999; 14: 437-41.
    • (1999) Curr Opin Cardiol , vol.14 , pp. 437-441
    • Abenhaim, L.1    Humbert, M.2
  • 6
    • 54049111932 scopus 로고    scopus 로고
    • Pulmonary arterial hypertension: An overview of current pharmacologic treatment
    • Reinhart K, Salerno E, White CM. Pulmonary arterial hypertension: an overview of current pharmacologic treatment. Conn Med 2008; 72: 531-4.
    • (2008) Conn Med , vol.72 , pp. 531-534
    • Reinhart, K.1    Salerno, E.2    White, C.M.3
  • 7
    • 23844552809 scopus 로고    scopus 로고
    • Management of heart failure with pulmonary hypertension
    • Osman MN, Dunlap ME. Management of heart failure with pulmonary hypertension. Curr Cardiol Rep 2005; 7: 196-203.
    • (2005) Curr Cardiol Rep , vol.7 , pp. 196-203
    • Osman, M.N.1    Dunlap, M.E.2
  • 8
    • 2942544581 scopus 로고    scopus 로고
    • Comparative analysis of clinical trials and evidence-based treatment algorithm in pulmonary arterial hypertension
    • Galie N, Seeger W, Naeije R, Simonneau G, Rubin LJ. Comparative analysis of clinical trials and evidence-based treatment algorithm in pulmonary arterial hypertension. J Am Coll Cardiol 2004; 43: 81S-8S.
    • (2004) J Am Coll Cardiol , vol.43 , pp. 81S-8S
    • Galie, N.1    Seeger, W.2    Naeije, R.3    Simonneau, G.4    Rubin, L.J.5
  • 9
    • 33847320631 scopus 로고    scopus 로고
    • Combination therapy and new types of agents for pulmonary arterial hypertension
    • ix
    • O'Callaghan DS, Gaine SP. Combination therapy and new types of agents for pulmonary arterial hypertension. Clin Chest Med 2007; 28: 169-85, ix.
    • (2007) Clin Chest Med , vol.28 , pp. 169-185
    • O'callaghan, D.S.1    Gaine, S.P.2
  • 10
    • 34247132582 scopus 로고    scopus 로고
    • Management of pulmonary arterial hypertension with a focus on combination therapies
    • Benza RL, Park MH, Keogh A, Girgis RE. Management of pulmonary arterial hypertension with a focus on combination therapies. J Heart Lung Transplant 2007; 26: 437-46.
    • (2007) J Heart Lung Transplant , vol.26 , pp. 437-446
    • Benza, R.L.1    Park, M.H.2    Keogh, A.3    Girgis, R.E.4
  • 11
    • 10444246635 scopus 로고    scopus 로고
    • Combination therapy with bosentan and sildenafil in idiopathic pulmonary arterial hypertension
    • Hoeper MM, Faulenbach C, Golpon H, Winkler J, Welte T, Niedermeyer J. Combination therapy with bosentan and sildenafil in idiopathic pulmonary arterial hypertension. Eur Respir J 2004; 24: 1007-10.
    • (2004) Eur Respir J , vol.24 , pp. 1007-1010
    • Hoeper, M.M.1    Faulenbach, C.2    Golpon, H.3    Winkler, J.4    Welte, T.5    Niedermeyer, J.6
  • 13
    • 84893041865 scopus 로고    scopus 로고
    • Macitentan: First global approval
    • Patel T, McKeage K. Macitentan: first global approval. Drugs 2014; 74: 127-33.
    • (2014) Drugs , vol.74 , pp. 127-133
    • Patel, T.1    McKeage, K.2
  • 14
    • 84896696727 scopus 로고    scopus 로고
    • Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertension
    • Dingemanse J, Sidharta PN, Maddrey WC, Rubin LJ, Mickail H. Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertension. Expert Opin Drug Saf 2014; 13: 391-405.
    • (2014) Expert Opin Drug Saf , vol.13 , pp. 391-405
    • Dingemanse, J.1    Sidharta, P.N.2    Maddrey, W.C.3    Rubin, L.J.4    Mickail, H.5
  • 15
    • 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, Clozel M, Nayler O. Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells. PLoS ONE 2012; 7: e47662.
    • (2012) PLoS ONE , vol.7
    • Gatfield, J.1    Mueller Grandjean, C.2    Sasse, T.3    Clozel, M.4    Nayler, O.5
  • 17
    • 84873713624 scopus 로고    scopus 로고
    • Interaction profile of macitentan, a new non-selective endothelin-1 receptor antagonist, in vitro
    • Weiss J, Theile D, Ruppell MA, Speck T, Spalwisz A, Haefeli WE. Interaction profile of macitentan, a new non-selective endothelin-1 receptor antagonist, in vitro. Eur J Pharmacol 2013; 701: 168-75.
    • (2013) Eur J Pharmacol , vol.701 , pp. 168-175
    • Weiss, J.1    Theile, D.2    Ruppell, M.A.3    Speck, T.4    Spalwisz, A.5    Haefeli, W.E.6
  • 18
    • 84904557356 scopus 로고    scopus 로고
    • Investigation of the effect of macitentan on the pharmacokinetics and pharmacodynamics of warfarin in healthy male subjects
    • Sidharta PN, Dietrich H, Dingemanse J. Investigation of the effect of macitentan on the pharmacokinetics and pharmacodynamics of warfarin in healthy male subjects. Clin Drug Investig 2014; 34: 545-52
    • (2014) Clin Drug Investig , vol.34 , pp. 545-552
    • Sidharta, P.N.1    Dietrich, H.2    Dingemanse, J.3
  • 19
    • 84857627857 scopus 로고    scopus 로고
    • Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist
    • Bruderer S, Aanismaa P, Homery MC, Hausler S, Landskroner K, Sidharta PN, Treiber A, Dingemanse J. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J 2012; 14: 68-78.
    • (2012) AAPS J , vol.14 , pp. 68-78
    • Bruderer, S.1    Aanismaa, P.2    Homery, M.C.3    Hausler, S.4    Landskroner, K.5    Sidharta, P.N.6    Treiber, A.7    Dingemanse, J.8
  • 20
    • 84918839849 scopus 로고    scopus 로고
    • Summary of Product Characteristics: Opsumit® (macitentan) 10 mg tablets, for oral use. Actelion Registration, Ltd. 2013
    • Summary of Product Characteristics: Opsumit® (macitentan) 10 mg tablets, for oral use. Actelion Registration, Ltd. 2013.
  • 22
    • 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, Volokhov I, Sidharta PN. Investigation of the effects of ketoconazole on the pharmacokinetics of macitentan, a novel dual endothelin receptor antagonist, in healthy subjects. Clin Pharmacokinet 2013; 52: 685-92.
    • (2013) Clin Pharmacokinet , vol.52 , pp. 685-692
    • Atsmon, J.1    Dingemanse, J.2    Shaikevich, D.3    Volokhov, I.4    Sidharta, P.N.5
  • 24
    • 84892915544 scopus 로고    scopus 로고
    • Safety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple-dose study in healthy subjects
    • Sidharta PN, van Giersbergen PL, Dingemanse J. Safety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple-dose study in healthy subjects. J Clin Pharmacol 2013; 53: 1131-8.
    • (2013) J Clin Pharmacol , vol.53 , pp. 1131-1138
    • Sidharta, P.N.1    Van Giersbergen, P.L.2    Dingemanse, J.3
  • 25
    • 0347361482 scopus 로고    scopus 로고
    • Urinary 6beta-hydroxycortisol: A validated test for evaluating drug induction or drug inhibition mediated through CYP3A in humans and in animals
    • Galteau MM, Shamsa F. Urinary 6beta-hydroxycortisol: a validated test for evaluating drug induction or drug inhibition mediated through CYP3A in humans and in animals. Eur J Clin Pharmacol 2003; 59: 713-33.
    • (2003) Eur J Clin Pharmacol , vol.59 , pp. 713-733
    • Galteau, M.M.1    Shamsa, F.2
  • 26
    • 84918770016 scopus 로고    scopus 로고
    • Product Information: Revatio® (sildenafil), Pfizer Ltd, August 2008
    • Product Information: Revatio® (sildenafil), Pfizer Ltd, August 2008.
  • 27
    • 34547212999 scopus 로고    scopus 로고
    • Bosentan is a substrate of human OATP1B1 and OATP1B3: Inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil
    • Treiber A, Schneiter R, Hausler S, Stieger B. Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Drug Metab Dispos 2007; 35: 1400-7.
    • (2007) Drug Metab Dispos , vol.35 , pp. 1400-1407
    • Treiber, A.1    Schneiter, R.2    Hausler, S.3    Stieger, B.4
  • 28
    • 38049089932 scopus 로고    scopus 로고
    • Mutual pharmacokinetic interactions between steady-state bosentan and sildenafil
    • Burgess G, Hoogkamer H, Collings L, Dingemanse J. Mutual pharmacokinetic interactions between steady-state bosentan and sildenafil. Eur J Clin Pharmacol 2008; 64: 43-50.
    • (2008) Eur J Clin Pharmacol , vol.64 , pp. 43-50
    • Burgess, G.1    Hoogkamer, H.2    Collings, L.3    Dingemanse, J.4
  • 29
    • 84918790906 scopus 로고    scopus 로고
    • Prescribing Information: Opsumit® (macitentan) tablets, for oral use
    • Prescribing Information: Opsumit® (macitentan) tablets, for oral use. Actelion Pharmaceuticals US, Inc. 2013.
    • (2013) Actelion Pharmaceuticals US, Inc.
  • 30
    • 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, Bodmer M, Bruderer S, Regnault Y, Dingemanse J, Krahenbuhl S. Comparison of the dissolution and pharmacokinetic profiles of two galenical formulations of the endothelin receptor antagonist macitentan. Eur J Pharm Sci 2009; 38: 384-8.
    • (2009) Eur J Pharm Sci , vol.38 , pp. 384-388
    • Kummer, O.1    Haschke, M.2    Hammann, F.3    Bodmer, M.4    Bruderer, S.5    Regnault, Y.6    Dingemanse, J.7    Krahenbuhl, S.8
  • 31
    • 0035039489 scopus 로고    scopus 로고
    • Identification of the cytochrome P450 enzymes involved in the N-demethylation of sildenafil
    • Hyland R, Roe EG, Jones BC, Smith DA. Identification of the cytochrome P450 enzymes involved in the N-demethylation of sildenafil. Br J Clin Pharmacol 2001; 51: 239-48.
    • (2001) Br J Clin Pharmacol , vol.51 , pp. 239-248
    • Hyland, R.1    Roe, E.G.2    Jones, B.C.3    Smith, D.A.4
  • 32
    • 57449121379 scopus 로고    scopus 로고
    • Pharmacokinetics and safety of ambrisentan in combination with sildenafil in healthy volunteers
    • Spence R, Mandagere A, Dufton C, Venitz J. Pharmacokinetics and safety of ambrisentan in combination with sildenafil in healthy volunteers. J Clin Pharmacol 2008; 48: 1451-9.
    • (2008) J Clin Pharmacol , vol.48 , pp. 1451-1459
    • Spence, R.1    Mandagere, A.2    Dufton, C.3    Venitz, J.4
  • 33
    • 33747866680 scopus 로고    scopus 로고
    • Role of the liver-specific transporters OATP1B1 and OATP1B3 in governing drug elimination
    • Smith NF, Figg WD, Sparreboom A. Role of the liver-specific transporters OATP1B1 and OATP1B3 in governing drug elimination. Expert Opin Drug Metab Toxicol 2005; 1: 429-45.
    • (2005) Expert Opin Drug Metab Toxicol , vol.1 , pp. 429-445
    • Smith, N.F.1    Figg, W.D.2    Sparreboom, A.3
  • 34
    • 84918785389 scopus 로고    scopus 로고
    • Prescribing Information: Tracleer® (bosentan tablets), Actelion Pharmaceuticals US, Inc. 2012
    • Prescribing Information: Tracleer® (bosentan tablets), Actelion Pharmaceuticals US, Inc. 2012.
  • 37
    • 70149121675 scopus 로고    scopus 로고
    • Acute hemodynamic effects of single-dose sildenafil when added to established bosentan therapy in patients with pulmonary arterial hypertension: Results of the COMPASS-1 study
    • Gruenig E, Michelakis E, Vachiery JL, Vizza CD, Meyer FJ, Doelberg M, Bach D, Dingemanse J, Galie N. Acute hemodynamic effects of single-dose sildenafil when added to established bosentan therapy in patients with pulmonary arterial hypertension: results of the COMPASS-1 study. J Clin Pharmacol 2009; 49: 1343-52.
    • (2009) J Clin Pharmacol , vol.49 , pp. 1343-1352
    • Gruenig, E.1    Michelakis, E.2    Vachiery, J.L.3    Vizza, C.D.4    Meyer, F.J.5    Doelberg, M.6    Bach, D.7    Dingemanse, J.8    Galie, N.9
  • 39
    • 36549059303 scopus 로고    scopus 로고
    • Clinically important drug interactions potentially involving mechanism-based inhibition of cytochrome P450 3A4 and the role of therapeutic drug monitoring
    • Zhou SF, Xue CC, Yu XQ, Li C, Wang G. Clinically important drug interactions potentially involving mechanism-based inhibition of cytochrome P450 3A4 and the role of therapeutic drug monitoring. Ther Drug Monit 2007; 29: 687-710.
    • (2007) Ther Drug Monit , vol.29 , pp. 687-710
    • Zhou, S.F.1    Xue, C.C.2    Yu, X.Q.3    Li, C.4    Wang, G.5
  • 40
    • 0031015345 scopus 로고    scopus 로고
    • Human P450 metabolism of warfarin
    • Kaminsky LS, Zhang ZY. Human P450 metabolism of warfarin. Pharmacol Ther 1997; 73: 67-74.
    • (1997) Pharmacol Ther , vol.73 , pp. 67-74
    • Kaminsky, L.S.1    Zhang, Z.Y.2
  • 41
    • 79960647787 scopus 로고    scopus 로고
    • Recent progress in anticoagulant therapy: Oral direct inhibitors of thrombin and factor Xa
    • Bauer KA. Recent progress in anticoagulant therapy: oral direct inhibitors of thrombin and factor Xa. J Thromb Haemost 2011; 9: (Suppl. 1): 12-9.
    • (2011) J Thromb Haemost , vol.9 , pp. 12-19
    • Bauer, K.A.1
  • 42
    • 84876226603 scopus 로고    scopus 로고
    • New oral anticoagulants: Comparative pharmacology with vitamin K antagonists
    • Scaglione F. New oral anticoagulants: comparative pharmacology with vitamin K antagonists. Clin Pharmacokinet 2013; 52: 69-82.
    • (2013) Clin Pharmacokinet , vol.52 , pp. 69-82
    • Scaglione, F.1
  • 43
    • 84918803535 scopus 로고    scopus 로고
    • Product Information: Xarelto® (rivaroxaban) tablets, for oral use
    • Product Information: Xarelto® (rivaroxaban) tablets, for oral use. Janssen Pharmaceuticals Inc, 2011.
    • (2011) Janssen Pharmaceuticals Inc
  • 44
    • 0034038457 scopus 로고    scopus 로고
    • Contraceptive effectiveness: Cytochromes and induction
    • Shader RI, Oesterheld JR. Contraceptive effectiveness: cytochromes and induction. J Clin Psychopharmacol 2000; 20: 119-21.
    • (2000) J Clin Psychopharmacol , vol.20 , pp. 119-121
    • Shader, R.I.1    Oesterheld, J.R.2
  • 45
    • 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: 1089-115.
    • (2004) Clin Pharmacokinet , vol.43 , pp. 1089-1115
    • Dingemanse, J.1    Van Giersbergen, P.L.2
  • 46
    • 21744438514 scopus 로고    scopus 로고
    • Bosentan decreases the plasma concentration of sildenafil when coprescribed in pulmonary hypertension
    • Paul GA, Gibbs JS, Boobis AR, Abbas A, Wilkins MR. Bosentan decreases the plasma concentration of sildenafil when coprescribed in pulmonary hypertension. Br J Clin Pharmacol 2005; 60: 107-12.
    • (2005) Br J Clin Pharmacol , vol.60 , pp. 107-112
    • Paul, G.A.1    Gibbs, J.S.2    Boobis, A.R.3    Abbas, A.4    Wilkins, M.R.5
  • 47
    • 27744508710 scopus 로고    scopus 로고
    • The efficacy and safety of PDE5 inhibitors
    • Rashid A. The efficacy and safety of PDE5 inhibitors. Clin Cornerstone 2005; 7: 47-56.
    • (2005) Clin Cornerstone , vol.7 , pp. 47-56
    • Rashid, A.1
  • 48
    • 33846445687 scopus 로고    scopus 로고
    • Tolerability, pharmacokinetics, and pharmacodynamics of clazosentan, a parenteral endothelin receptor antagonist
    • van Giersbergen PL, Dingemanse J. Tolerability, pharmacokinetics, and pharmacodynamics of clazosentan, a parenteral endothelin receptor antagonist. Eur J Clin Pharmacol 2007; 63: 151-8.
    • (2007) Eur J Clin Pharmacol , vol.63 , pp. 151-158
    • Van Giersbergen, P.L.1    Dingemanse, J.2
  • 49
    • 84875425349 scopus 로고    scopus 로고
    • The effect of sodium nitroprusside on cerebral hemodynamics and headache in healthy subjects
    • Guo S, Ashina M, Olesen J, Birk S. The effect of sodium nitroprusside on cerebral hemodynamics and headache in healthy subjects. Cephalalgia 2013; 33: 301-7.
    • (2013) Cephalalgia , vol.33 , pp. 301-307
    • Guo, S.1    Ashina, M.2    Olesen, J.3    Birk, S.4


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