Pharmacokinetics and pharmacodynamics of the endothelin‐receptor antagonist bosentan in healthy human subjects
@article{Weber1996PharmacokineticsAP, title={Pharmacokinetics and pharmacodynamics of the endothelin‐receptor antagonist bosentan in healthy human subjects}, author={Cornelia Weber and Rita Schmitt and Herbert Birnboeck and G{\'e}rard Hopfgartner and Sjoerd P. Marle and Pierre A. M. Peeters and Jan H. G. Jonkman and Charles‐Richard Jones}, journal={Clinical Pharmacology \& Therapeutics}, year={1996}, volume={60} }
202 Citations
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The pharmacology of bosentan.
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Bosentan is a combined and competitive antagonist of both ETA and ETB receptors that is selective for the endothelin system that potently antagonises the vascular response elicited by the endothelins in vitro and in vivo.
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Preclinical and clinical data suggest that bosentan might become a new approach for the chronic treatment of these cadiovascular and pulmonary diseases.
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A number of endothelin (ET) receptor antagonists have been developed as research tools and as potential medicines and several are at various stages of clinical evaluation.
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Atrasentan pharmacokinetics was linear in the 1 to 23.25 mg dose range, with some dose dependency in the highest dose group, and the apparent volume of distribution was large, consistent with extensive tissue distribution.
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