Comparative investigation of the pharmacokinetics of bosentan in Caucasian and Japanese healthy subjects

Journal of Clinical Pharmacology

Volumn 45, Issue 1, 2005, Pages 42-47

  Van Giersbergen, Paul L M ^a   Dingemanse, Jasper ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

Bosentan; Caucasian and Japanese subjects; Endothelin receptor antagonist; Pharmacokinetics

Indexed keywords

BOSENTAN; ENDOTHELIN RECEPTOR ANTAGONIST; PYRIMIDINE DERIVATIVE; RO 48 5033; RO 48-5033; SULFONAMIDE;

ADULT; AREA UNDER THE CURVE; ARTICLE; ASIAN; CAUCASIAN; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE TIME EFFECT RELATION; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; ETHNIC GROUP; FEMALE; HEADACHE; HUMAN; JAPAN; LIQUID CHROMATOGRAPHY; MALE; NORMAL HUMAN; RACE DIFFERENCE; SINGLE DRUG DOSE; TANDEM MASS SPECTROMETRY; ANALYSIS OF VARIANCE; BLOOD; COMPARATIVE STUDY; CONFIDENCE INTERVAL; DOSE RESPONSE; METABOLISM; MIDDLE AGED; RANDOMIZED CONTROLLED TRIAL;

ADULT; ANALYSIS OF VARIANCE; AREA UNDER CURVE; ASIAN CONTINENTAL ANCESTRY GROUP; CONFIDENCE INTERVALS; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; EUROPEAN CONTINENTAL ANCESTRY GROUP; FEMALE; HUMANS; MALE; MIDDLE AGED; PYRIMIDINES; SULFONAMIDES;

EID: 16644388500     PISSN: 00912700     EISSN: None     Source Type: Journal    
DOI: 10.1177/0091270004270833     Document Type: Article

References (20)

1. Rubin LJ. Primary pulmonary hypertension. N Engl J Med. 1997;336:111-117.
2. Barst RJ. Primary pulmonary hypertension in children. In: Ruhin LJ, Rich S, eds. Primary Pulmonary Hypertension. New York: Marcel Dekker; 1987:179-225.
3. Barst RJ, Ruhin LJ, Long WA, et al. A comparison of continuous intravenous epoprostenol (prostacyclin) with conventional therapy for primary pulmonary hypertension. N Engl J Med. 1996;334:296-302.
4. Channick RN, Simonneau G, Sitbon O, et al. Effects of the dual endothelin-receptor antagonist bosentan in patients with pulmonary hypertension: a randomised placebo-controlled study. Lancet. 2001;358:1119-1123.
5. Rubin LJ, Badesch DB, Barst RJ, et al. Bosentan therapy for pulmonary arterial hypertension. N Engl J Med. 2002;346:896-903.
6. Dingemanse J, van Giersbergen PLM. Clinical pharmacology of bosentan, a dual endothelin receptor antagonist. Clin Pharmacokinet. In press.
7. Weber C, Schmitt R, Birnboeck H, et al. Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin Pharmacol Ther. 1996;60:124-137.
8. Dingemanse J, Bodin F, Weidekamm E, Kutz K, van Giersbergen P. Influence of food intake and formulation on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist. J Clin Pharmacol. 2002;42:283-289.
9. Weber C, Gasser R, Hopfgartner G. Absorption, excretion, and metabolism of the endothelin receptor antagonist bosentan in healthy male subjects. Drug Metab Disp. 1999;27:810-815.
10. Xie H-G, Kim RB, Wood AJJ, Stein CM. Molecular basis of ethnic differences in dug disposition and response. Annu Rev Pharmacol Toxicol. 2001;41:815-850.
11. Dell D, Lausecker B, Hopfgartner G, van Giersbergen PLM, Dingemanse J. Evolving bioanalytical methods for the cardiovascular drug bosentan. Chromatographia. 2002;55(suppl):S115-S119.
12. Gibaldi M, Perrier D: Pharmacokinetics. 2nd ed. New York: Marcel Dekker; 1982.
13. 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 Info J. 1995;29:1039-1048.
14. Johnson JA. Predictability of the effects of race or ethnicity on pharmacokinetics of drugs. Int J Clin Pharmacol Ther. 2000;38:53-60.
15. Bjornsson TD, Wagner JA, Donahue SR, et al. A review and assessment of potential sources of ethnic differences in drug responsiveness. J Clin Pharmacol. 2003;43:943-967.
16. Muck W, Tanaka T, Ahr G, Kuhlmann J. No interethnic differences in stereoselective disposition of oral nimodipine between Caucasian and Japanese subjects. Int J Clin Pharmacol Ther. 1996;34:163-171.
17. Rashid TJ, Martin U, Clarke H, Waller DG, Renwick AG, George CF. Factors affecting the absolute bioavailability of nifedipine. Br J Clin Pharmacol. 1995;40:51-58.
18. Shimada T, Yamazaki H, Mimura M, Inui Y, Guengerich FP. Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians. J Pharmacol Exp Ther. 1994;270:414-423.
19. Tateishi T, Watanabe M, Nakura H, et al. CYP3A activity in European American and Japanese men using midazolam as an in vivo probe. Clin Pharmacol Ther. 2001;69:333-339.
20. Hooiveld GJEJ, van Montfoort JE, Meijer DKF, Müller M. Function and regulation of ATP-binding cassette transport proteins involved in hepatobiliary transport. Eur J Pharmaceut Sci. 2000;12:13-30.