Pharmacokinetics and pharmacodynamic effects of ABT-627, an oral ETA selective endothelin antagonist, in humans

British Journal of Clinical Pharmacology

Volumn 49, Issue 6, 2000, Pages 562-573

  Verhaar, Marianne C ^a   Grahn, Amy Y ^c   Van Weerdt, Anton W M ^b   Honing, Marina L H ^a   Morrison, Paul J ^b   Yang, Yonghong P ^c   Padley, Robert J ^c   Rabelink, Ton J ^a  

^a UNIVERSITY MEDICAL CENTER UTRECHT   (Netherlands)

^b U Gene Clinical Pharmacology Unit   (Netherlands)

^c ABBOTT LABORATORIES   (United States)

Author keywords

ABT 627; Endothelin antagonist; Endothelins; Humans

Indexed keywords

ATRASENTAN; ENDOTHELIN 1; ENDOTHELIN RECEPTOR ANTAGONIST; LIDOCAINE; PLACEBO;

ADULT; AGED; ARTICLE; BLOOD PRESSURE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG SELECTIVITY; HEADACHE; HUMAN; MALE; NORMAL HUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; VASCULAR RESISTANCE; VASOCONSTRICTION;

ADULT; AGED; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; ENDOTHELINS; FOREARM; HALF-LIFE; HEMODYNAMIC PROCESSES; HUMANS; MALE; MIDDLE AGED; PYRROLIDINES; RECEPTOR, ENDOTHELIN A; RECEPTORS, ENDOTHELIN; REGIONAL BLOOD FLOW; VASOCONSTRICTION;

EID: 0034076139     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.2000.00171.x     Document Type: Article

References (46)

1. 1 Arai H, Hori S, Aramori I, Ohkubo H, Nakanishi S. Cloning and expression of a cDNA encoding an endothelin receptor. Nature 1990; 348: 730-732.
2. 2 Sakurai T, Yanagisawa M, Takuwa Y, et al. Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature 1990; 348: 732-735.
3. 3 De Nucci G, Thomas R, D'Orleans Juste P, 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: 9797-9800.
4. 4 Tsukahara H, Ende H, Magazine HI, Bahou WF, Goligorsky MS. Molecular and functional characterization of the non-isopeptide-selective ETB receptor in endothelial cells. Receptor coupling to nitric oxide synthase. J Biol Client 1994; 269: 21778-21785.
5. 5 Davenport AP, O'Reilly G, Molenaar P, et al. Human endothelin receptors characterized using reverse transcriptase-polymerase chain reaction, in situ hybridization, and subtype-selective ligands. BQ, 123 BQ : evidence for expression of ETB receptors in human vascular smooth muscle. J Cardiovasc Pharmacol 1993; 22(Suppl 8): S22-S25.
6. 6 Clozel M, Gray GA, Breu V, Loffler BM, Osterwalder R. The endothelin ETB receptor mediates both vasodilation and vasoconstriction in vivo. Biochem Biophys Res Commun 1992; 186: 867-873.
7. 7 Seo B, Oemar BS, Siebenmann R, von Segesser L, Luscher TF. Both ETA and ETB receptors mediate contraction to endothelin-1 in human blood vessels. Circulation 1994; 89: 1203-1208.
8. 8 Haynes WG, Strachan FE, Webb DJ. Endothelin ETA and ETB receptors cause vasoconstriction of human resistance and capacitance vessels in vivo. Circulation 1995; 92: 357-363.
9. 9 Yanagisawa M, Kurihara H, Kimura S, et al. A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 1988; 332: 411-415.
10. 10 Battistini B, Chailler P, D'Orleans Juste P, Briere N, Sirois P. Growth regulatory properties of endothelins. Peptides 1993; 14: 385-399.
11. 11 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.
12. 12 Sutsch G, Kiowski W, Yan XW, et al. Short-term oral endothelin-receptor antagonist therapy in conventionally treated patients with symptomatic severe chronic heart failure. Circulation 1998; 98: 2262-2268.
13. 13 Krum H, Viskoper RJ, Lacourciere Y, Budde M, Charlon V. The effect of an endothelin-receptor antagonist, bosentan, on blood pressure in patients with essential hypertension. N Engl J Med 1998; 338: 784-790.
14. 14 Mallat A, Fouassier L, Preaux AM, et al. Growth inhibitory properties of endothelin-1 in human hepatic myofibroblastic Ito cells. J Clin Invest 1995; 96: 42-49.
15. 15 Ong ACM, Jowett TP, Firth JD, Burton S, Karet FE, Fine LG. An endothelin-1 mediated automne growth loop involved in human renal tubular regeneration. Kidney Int 1995; 48: 390-401.
16. B receptors. Am J Physiol 1995; 269: H686-H695.
17. B receptor. Br J Pharmacol 1993; 109: 530-534.
18. B receptor increases peripheral vascular resistence in healthy men. Hypertension 1999; 33 (1 Part 2): 581-585.
19. 19 Verhaar MC, Strachan FE, Newby DE, et al. Endothelin-A receptor antagonist-mediated vasodilatation is attenuated by inhibition of nitric oxide synthesis and by endothelin-B receptor blockade. Circulation 1998; 97: 752-756.
20. 20 Webb DJ, Monge JC, Rabelink TJ, Yanagisawa M. Endothelin: new discoveries and rapid progress in the clinic. Trends Pharmacol Sci 1998; 19: 5-8.
21. A-selective receptor antagonist. J Pharmacol Exp Ther 1996; 276: 473-481.
22. 22 Haynes WG, Webb DJ. Contribution of endogenous generation of endothelin-1 to basal vascular tone. Lancet 1994; 344: 852-854.
23. 23 Chang PC, Verlinde R, Bruning T, van Brummelen P. A microcomputer-based, R-wave triggered system for hemodynamic measurements in the forearm. Comput Biol Med 1988; 18: 157-163.
24. 24 Salandin V, Zussa C, Risica G, et al. Comparison of cardiac output estimation by thoracic electrical bioimpedance, thermodilution, and Fick methods. Crit Care Med 1988; 16: 1157-1158.
25. 25 Northridge DB, Findlay IN, Wilson J, Henderson E, Dargie HJ. Non-invasive determination of cardiac output by Doppler echocardiography and electrical bioimpedance. Br Heart J 1990; 63: 93-97.
26. 26 Benjamin N, Calver A, Collier J, Robinson B, Vallance P, Webb D. Measuring forearm blood flow and interpreting the responses to drugs and mediators. Hypertension 1995; 25: 918-923.
27. 27 Panza JA, Epstein SE, Quyyumi AA. Circadian variation in vascular tone and its relation to alpha sympathetic vasoconstriction. N Engl J Med 1991; 325: 986-990.
28. 1adrenergic modulation does not play a predominant role in the genesis of postprandial effects. Br J Clin Pharmacol 1993; 36: 427-435.
29. 29 de Mey C, Enterling D, Brendel E, Meineke I. Postprandial changes in supine and erect heart rate, systemic blood pressure and plasma noradrenaline and renin activity in normal subjects. Eur J Clin Pharmacol 1987; 32: 471-476.
30. 30 Pedrinelli R, Taddei S, Salvetti A. Calcium-entry blockade and α-adrenergic vascular reactivity in human beings: differences between nicardipine and verapamil. Clin Pharmacol Ther 1989; 45: 285-290.
31. 31 Hilal-Dandan R, Villegas S, Gonzalez A, Brunton LL. The quasi-irreversible nature of endothelin binding and G protein-linked signaling in cardiac myocytes. J Pharmacol Exp Ther 1997; 281: 267-273.
32. 32 Haynes WG, Ferro CJ, O'Kane KP, Somerville D, Lomax CC, Webb DJ. Systemic endothelin receptor blockade decreases peripheral vascular resistance and blood pressure in humans. Circulation 1996; 93: 1860-1870.
33. 33 Wei CM, Lerman A, Rodeheffer RJ, et al. Endothelin in human congestive heart failure. Circulation 1994; 89: 1580-1586.
34. 34 Saito Y, Nakao K, Mukoyama M, Imura H. Increased plasma endothelin levels in patients with essential hypertension. N Engl J Med 1990; 322: 205.
35. 35 Kiowski W, Sutsch G, Hunziker P, et al. Evidence for endothelin-1-mediated vasoconstriction in severe chronic heart failure. Lancet 1995; 346: 732-736.
36. 36 Boarder MR, Marriott DB. Characterization of endothelin-1 stimulation of catecholamine release from adrenal chromaffin cells. J Cardiovasc Pharmacol 1989; 13(Suppl 5): S223-S224.
37. 37 Kawaguchi H, Sawa H, Yasuda H. Endothelin stimulates angiotensin I to angiotensin II conversion in cultured pulmonary artery endothelial cells. J Mol Cell Cardiol 1990; 22: 839-842.
38. 38 Matsumura K, Abe I, Tsuchihashi T, Tominaga M, Kobayashi K, Fujishima M. Central effect of endothelin on neurohormonal responses in conscious rabbits. Hypertension 1991; 17: 1192-1196.
39. 39 Borgeson DD, Grantham JA, Williamson EE, et al. Chronic oral endothelin type A receptor antagonism in experimental heart failure. Hypertension 1998; 31: 766-770.
40. A receptor reduces neointimal hyperplasia after balloon-induced vascular injury in pigs. J Cardiovasc Pharmacol 1997; 30: 33-41.
41. 41 Potter GS, Johnson RJ, Fink GD. Role of endothelin in hypertension of experimental chronic renal failure. Hypertension 1997; 30: 1578-1584.
42. 42 Rajagopalan S, Laursen JB, Borthayre A, et al. Role for endothelin-1 in angiotensin II mediated hypertension. Hypertension, 1997 :30[part 1]: 29-34.
43. 43 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: 1461-1465.
44. 44 Loffler BM, Breu V, Clozel M. Effect of different endothelin receptor antagonists and of the novel non-peptide antagonist Ro 46-2005 on endothelin levels in rat plasma. FEBS Lett 1993; 333: 108-110.
45. 45 Plumpton C, Ferro CJ, Haynes WG, Webb DJ, Davenport AP. 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. Br J Pharmacol 1996; 119: 311-314.
46. 46 Wenzel RR, Fleisch M, Shaw S, et al. Hemodynamic and coronary effects of the endothelin antagonist bosentan in patients with coronary artery disease. Circulation 1998; 98: 2235-2240.