Absorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humans

Xenobiotica

Volumn 42, Issue 9, 2012, Pages 901-910

  Bruderer, Shirin ^a   Hopfgartner, Gérard ^b   Seiberling, Michael ^c   Wank, Janine ^b   Sidharta, Patricia N ^a   Treiber, Alexander ^a   Dingemanse, Jasper ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

^b Swiss BioAnalytics AG   (Switzerland)

^c Swiss BioAnalytics AG ^*  (Switzerland)

Author keywords

Mass balance; metabolite profiling; pharmacokinetics; Phase I

Indexed keywords

ACT 080803; ACT 132577; ACT 373898; CARBON 14; DRUG METABOLITE; M 323U; M 706U; MACITENTAN; UNCLASSIFIED DRUG;

ADULT; AGED; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG METABOLISM; DRUG TOLERABILITY; FECES ANALYSIS; HEADACHE; HEMATOCHEZIA; HUMAN; HUMAN EXPERIMENT; MALE; MASS SPECTROMETRY; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; RADIOACTIVITY; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; URINALYSIS;

CARBON RADIOISOTOPES; CHROMATOGRAPHY, LIQUID; FECES; HUMANS; MALE; METABOLIC NETWORKS AND PATHWAYS; MIDDLE AGED; MOLECULAR STRUCTURE; PYRIMIDINES; RECEPTORS, ENDOTHELIN; SCINTILLATION COUNTING; SULFONAMIDES; TANDEM MASS SPECTROMETRY;

EID: 84865010567     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498254.2012.664665     Document Type: Article

References (8)

1. Bruderer S, Marjason J, Sidharta PN, Dingemanse J. (2011). Pharmacokinetics, tolerability, and safety of the dual endothelin receptor antagonist macitentan in Japanese and Caucasian healthy subjects. Supplement of Clin Pharmacol & Ther, 89, 83.
2. Iglarz M, Binkert C, Morrison K, Fischli W, Gatfield J, Treiber A, Weller,T, Bolli M., Boss C, Buchmann S, Capeleto B, Hess P, Qiu C, Clozel M. (2008). Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther, 327, 736-745.
3. Kummer O, Haschke M, Hammann F, Bodmer M, Bruderer S, Regnault Y, Dingemanse J, Krahenbuhl S. (2009). Comparison of the dissolution and pharmacokinetic profiles of two galenical formulations of the endothelin receptor antagonist macitentan. Eur J Pharm Sci, 38, 384-388.
4. Roffey SJ, Obach RS, Gedge JI, Smith DA. (2007). What is the objective of the mass balance study? A retrospective analysis of data in animal and human excretion studies employing radiolabelled drugs. Drug Metab Rev, 39, 17-43.
5. Sidharta PN, Atsmon J, Dingemanse J. (2010). Investigation of the effect of ketoconazole on the pharmacokinetics of macitentan in healthy male subjects. (Abstract). Br J Clin Pharmacol, 70, 730-731.
6. Sidharta PN, Dingemanse J. (2008). Multiple-dose tolerability, safety, pharmacokinetics, and pharmacodynamics of the dual endothelin receptor antagonist ACT-064992 in healthy human subjects. (Abstract). J Clin Pharmacol, 48, 1114.
7. Sidharta PN, Van Giersbergen PL, Halabi A, Dingemanse J. (2011). Macitentan: Entry-into-humans study with a new endothelin receptor antagonist. Eur J Clin Pharmacol, 67, 977-984.
8. Valentin J. (2007). The 2007 Recommendations of the International Commission on Radiological Protections. Ann ICRP, 37, 1-332.