Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects

Clinical Pharmacology and Therapeutics

Volumn 60, Issue 2, 1996, Pages 124-137

  Weber, Cornelia ^a   Schmitt, Rita ^b   Birnboeck, Herbert ^b   Hopfgartner, Gerard ^b   Van Marie, Sjoerd P ^b   Peeters, Pierre A M ^b   Jonkman, Jan H G ^b   Jones, Charles Richard ^b  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

BOSENTAN; ENDOTHELIN 1; ENDOTHELIN RECEPTOR ANTAGONIST; PLACEBO;

ADULT; AREA UNDER THE CURVE; ARTICLE; BLOOD PRESSURE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG STRUCTURE; DRUG TOLERANCE; HEART RATE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; INTRAVENOUS DRUG ADMINISTRATION; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHARMACODYNAMICS; PHARMACOKINETICS; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; VOLUNTEER;

ADMINISTRATION, ORAL; ADULT; ANALYSIS OF VARIANCE; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; BLOOD PRESSURE; DOUBLE-BLIND METHOD; ENDOTHELIN-1; ENDOTHELIN-3; ENDOTHELINS; HEART RATE; HUMANS; INJECTIONS, INTRADERMAL; INJECTIONS, INTRAVENOUS; MALE; PROTEIN PRECURSORS; RECEPTORS, ENDOTHELIN; REFERENCE VALUES; SKIN; SULFONAMIDES;

EID: 0029860546     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0009-9236(96)90127-7     Document Type: Article

References (31)

1. O'Brien RF, Robbins RJ, McMurtry IF. Endothelial cells in culture produce a vasoconstrictor substance. J Cell Physiol 1987;132:263-70.
2. Yanagisawa M, Kurihara H, Kimura S, Tomobe Y, Kobayashi M, Mitsui Y, et al. A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 1988;332:411-5.
3. Rubanyi GM. Potential physiological and pathological significance of endothelins. Drugs Future 1992;17: 915-36.
4. Haynes WG, Webb DJ. The endothelin family of peptides: local hormones with diverse roles in health and disease? Clin Sci 1993;84:485-500.
5. Douglas SA, Meek TD, Ohlstein EH. Novel receptor antagonists welcome a new era in endothelin biology. Trends Pharmacol Sci 1994;15:313-6.
6. Warner TD. Endothelin receptor antagonists. Cardiovasc Drug Rev 1994;12:110-22.
7. Clozel M, Breu V, Gray GA, Kalina B, Löffler BM, Burri K, et al. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. Pharmacol Exp Ther 1994;270:228-35.
8. Shigeno T, Clozel M, Sakai S, Saito A, Goto K. The effect of bosentan, a new potent endothelin receptor antagonist, on the pathogenesis of cerebral vasospasm. Neurosurgery 1995;37:87-91.
9. Roux S, Löffler BM, Gray GA, Sprecher U, Clozel M, Clozel JP. The role of endothelin in experimental cerebral vasospasm. Neurosurgery 1995;37:78-86.
10. Teerlink JR, Löffler BM, Hess P, Maire JP, Clozel M, Clozel JP. Role of endothelin in the maintenance of blood pressure in conscious rats with chronic heart failure: acute effects of the endothelin receptor antagonist Ro 47-0203 (bosentan). Circulation [in press].
11. Lausecker B, Hopfgartner G. Quantitative analysis of a new endothelin receptor antagonist in human plasma by narrow-bore liquid chromatography and ion spray mass spectrometry. J Chromatogr 1995;712:75-83.
12. Gibaldi M, Perrier D. Pharmacokinetics. 2nd ed. New York: Marcel Dekker, 1982.
13. Benet LZ, Galeazzi RL. Noncompartmental determination of the steady-state volume of distribution. J Pharm Sci 1979;68:1071-4.
14. Loeffler BM, Maire JP. Radioimmunological determination of endothelin peptides in human plasma: a methodological approach. Endothelium 1994;1:273-86.
15. Crossman DC, Brain SD, Fuller RW. Potent vasoactive properties of endothelin 1 in human skin. J Appl Physiol 1991;70:260-6.
16. Beal SL, Sheiner LB. The NONMEM system. Am Stat 1980;34:118-9.
17. Boeckmann AJ, Beal SL, Sheiner LB. NONMEM users guide. San Francisco: NONMEM Project Group, University of California, 1990
18. Levy G. Pharmacologic target-mediated drug disposition. Clin Pharmacol Ther 1994;56:248-52.
19. Yoshimoto S, Ishizaki Y, Sasaki T, Murota SI. Effect of carbon dioxide and oxygen on endothelin production by cultured porcine cerebral endothelial cells. Stroke 1991;22:378-83.
20. Wei CM, Lerman A, Rodeheffer RJ, McGregor CGA, Brandt RR, Wright S, et al. Endothelin in human congestive heart failure. Circulation 1994;89:1580-6.
21. Fukuroda T, Fujikawa T, Ozaki S, Ishikawa K, Yano M, Nishikibe M. Clearance of circulating endothelin-1 by ETB receptors in rats. Biochem Biophys Res Commun 1994;199:1461-5.
22. Loeffler BM, Breu V, Clozel M. Effect of endothelin receptor antagonists and of the novel non-peptide antagonist Ro 46-2005 on endothelin levels in rat plasma. FEBS Lett 1993;333:108-10.
23. MacCumber MW, Ross CR, Glaser BM, Snyder SH. Endothelin: visualization of mRNAs by in situ hybridization provides evidence for local action. Proc Natl Acad Sci USA 1989;86:7285-9.
24. De Nucci G, Thomas R, D'Orleans-Juste P, Antunes E, Walder C, Warner TD, et al. Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor. Proc Natl Acad Sci USA 1988;85:9797-800.
25. 125I]endothelin-1 binding data. Life Sci 1992;51:1869-76.
26. Maggi CA, Giuliani S, Patacchini R, Rovero P, Giachetti A, Meli A. The activity of peptides of the endothelin family in various mammalian smooth muscle preparations. Eur J Pharmacol 1989;174:23-31.
27. Wenzel RR, Noll G, Luscher TF. Endothelin receptor antagonists inhibit endothelin in human skin microcirculation. Hypertension 1994;23:581-6.
28. Haynes WG Webb DJ. Contribution of endogenous generation of endothelin-1 to basal vascular tone. Lancet 1994;344:852-4.
29. Kiowski W, Sutsch G, Hunziker P, Muller P, Kim J, Oechslin E, et al. Evidence of endothelin-1 mediated vasoconstriction in severe chronic heart failure. Lancet 1995;346:732-6.
30. Li JS, Schiffrin EL. Effect of chronic treatment of adult spontaneously hypertensive rats with an endothelin receptor antagonist. Hypertension 1995;25:494-500.
31. Li JS, Lariviere R, Schiffrin EL. Effect of a nonselective endothelin antagonist on vascular remodeling in deoxycorticosterone acetate-salt hypertensive rats. Hypertension 1994;24:183-8.