Entry-into-humans study with tezosentan, an intravenous dual endothelin receptor antagonist

Journal of Cardiovascular Pharmacology

Volumn 39, Issue 6, 2002, Pages 795-802

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

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

Entry into humans; Pharmacodynamics; Pharmacokinetics; Tezosentan

Indexed keywords

ENDOTHELIN 1; ENDOTHELIN RECEPTOR ANTAGONIST; TEZOSENTAN;

ADULT; ARTICLE; CHONDROPATHY; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DISTRIBUTION VOLUME; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG HALF LIFE; DRUG MECHANISM; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; FLUSHING; HEADACHE; HEMATOMA; HUMAN; MAJOR CLINICAL STUDY; MALE; NAUSEA; PHARMACODYNAMICS; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; RHINOPHARYNGITIS; SYNCOPE; VERTIGO; VISUAL FIELD DEFECT; VOMITING;

ADULT; ANALYSIS OF VARIANCE; AREA UNDER CURVE; CONFIDENCE INTERVALS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; HUMANS; INFUSIONS, INTRAVENOUS; MALE; PYRIDINES; RECEPTORS, ENDOTHELIN; TETRAZOLES;

EID: 0036112348     PISSN: 01602446     EISSN: None     Source Type: Journal    
DOI: 10.1097/00005344-200206000-00004     Document Type: Article

References (28)

1. Long-lasting coronary vasoconstrictor effects and myocardial uptake of endothelin-1 in humans
2. A novel potent vasoconstrictor peptide produced by vascular endothelial cells
3. Endothelin in renal pathophysiology: From experimental to therapeutic application
4. Endothelin-1 in heart failure: A new therapeutic target?
5. Endothelins and endothelin receptor antagonists: Therapeutic considerations for a novel class of cardiovascular drugs
6. Endothelin-receptor antagonists: Current and future perspectives
7. Evidence for endothelin-1 mediated vasoconstriction in severe chronic heart failure
8. Bosentan and the endothelin system in congestive heart failure
9. Endothelin in human congestive heart failure
10. Pharmacology of tezosentan, new endothelin receptor antagonist for parenteral use
11. Opportunities for integration of pharmacokinetics, pharmacodynamics, and toxico-kinetics in rational drug development
12. The pharmacology of bosentan
13. Pharmacological characterization of bosentan, a new potent orally active non-peptide endothelin receptor antagonist
14. Craniovascular selectivity of eletriptan and sumatriptan in human isolated blood vessels
15. Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects
16. Pharmacokinetics and pharmacodynamics of SB 209670, an endothelin receptor antagonist: Effects on the regulation of renal vascular tone
17. Pharmacokinetics and pharmacodynamic effects of ABT-627, an oral ETA selective endothelin antagonist, in humans
18. The effect of an endothelin-receptor antagonist, bosentan, on blood pressure in patients with essential hypertension
19. Endothelin-A receptor antagonist-mediated vasodilatation is attenuated by inhibition of nitric oxide synthesis and by endothelin-B receptor blockade
20. Effect of different endothelin receptor antagonists and of the novel non-peptide antagonist Ro 46-2005 on endothelin levels in rat plasma
21. Short-term oral endothelin-receptor antagonist therapy in conventionally treated patients with symptomatic severe chronic heart failure
22. B receptors in rats
23. The increase in human plasma immunoreactive endothelin but not big endothelin-1 or its C-terminal fragment induced by systemic administration of the endothelin antagonist TAK-044
24. Human endothelin-1 clearance kinetics revealed by a radiotracer technique
25. Plasma- and cerebrospinal fluid-immunoreactive endothelin-1: Effects of nonpeptide endothelin receptor antagonists with diverse affinity profiles for endothelin-A and endothelin-B receptors