The pharmacokinetic profile of sitaxsentan, a selective endothelin receptor antagonist, in varying degrees of renal impairment

British Journal of Clinical Pharmacology

Volumn 64, Issue 6, 2007, Pages 733-737

  Dhaun, Neeraj ^a   Melville, Vanessa ^a   Kramer, William ^c   Stavros, Fiona ^c   Coyne, Terrance ^c   Swan, Suzanne ^d   Goddard, Jane ^b   Webb, David J ^a  

^a UNIVERSITY OF EDINBURGH   (United Kingdom)

^b ROYAL INFIRMARY OF EDINBURGH   (United Kingdom)

^c TEXAS BIOTECHNOLOGY CORPORATION   (United States)

^d DAVITA CLINICAL RESEARCH   (United States)

Author keywords

Endothelin; Pharmacokinetic; Renal impairment; Sitaxsentan

Indexed keywords

CREATININE; ENDOTHELIN A RECEPTOR ANTAGONIST; SITAXSENTAN;

ADULT; AGED; AREA UNDER THE CURVE; ARTICLE; CLINICAL ARTICLE; CONTROLLED STUDY; CREATININE CLEARANCE; DISEASE SEVERITY; DOSE RESPONSE; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG HALF LIFE; FEMALE; HUMAN; KIDNEY DISEASE; KIDNEY FUNCTION; MALE; MAXIMUM ALLOWABLE CONCENTRATION; PRIORITY JOURNAL; SINGLE DRUG DOSE;

ADOLESCENT; ADULT; AGED; FEMALE; HUMANS; ISOXAZOLES; KIDNEY DISEASES; MALE; METABOLIC CLEARANCE RATE; MIDDLE AGED; RECEPTOR, ENDOTHELIN A; THIOPHENES;

EID: 36849025519     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2007.02979.x     Document Type: Article

References (13)

1. Kohan DE. Endothelins in the normal and diseased kidney. Am J Kid Dis 1997 29 : 2 26.
2. Karet FE, Davenport AP. Human kidney: endothelin isoforms detected by HPLC with radioimmunoassay and receptor subtypes detected using ligands BQ123 and BQ3020. J Cardiovasc Pharmacol 1993 22 (Suppl. 8 S29 33.
3. Davenport AP, Kuc RE, Hoskins SL, Karet FE, Fitzgerald F. [125I]-PD151242: a selective ligand for endothelin ETA receptors in human kidney which localizes to renal vasculature. Br J Pharmacol 1994 113 : 1303 10.
4. Haynes WG, Webb DJ. Contribution of endogenous generation of endothelin-1 to basal vascular tone. Lancet 1994 344 : 852 4.
5. Fukuroda T, Fujikawa T, Ozakai S, Ishikawa K, Yano M, Nishikibe M. Clearance of circulating endothelin-1 by ETB receptors in rats. Biochem Biophys Res Commun 1994 199 : 1461 5.
6. Rich S, McLaughlin VV. Endothelin receptor blockers in cardiovascular disease. Circulation 2003 108 : 2184 90.
7. Dhaun N, Goddard J, Webb DJ. The endothelin system and its antagonism in chronic kidney disease. J Am Soc Nephrol 2006 17 : 943 55.
8. O'Callaghan DS, Gaine SP. Sitaxsentan: an endothelin-A receptor antagonist for the treatment of pulmonary arterial hypertension. Int J Clin Pract 2006 60 : 475 81.
9. Wu C, Chan MF, Stavros F, Raju B, Okun I, Mong S, Keller KM, Brock T, Kogan TP, Dixon RA. Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J Med Chem 1997 40 : 1690 7.
10. Inveresk Research. A Phase 1 Study to Investigate the Absorption, Distribution, Metabolism, and Excretion of [14C]-Sitaxsentan (TBC11251Na) Following a Single Oral Dose in Healthy Volunteers. Report no. 175869. Protocol FNL-ADME. Edinburgh : Inveresk Research 2004.
11. Cockcroft DW, Gault MH. Prediction of creatinine clearance from serum creatinine. Nephron 1976 16 : 31 41.
12. Battistini B, Berthiaume N, Kelland NF, Webb DJ, Kohan DE. Profile of past and current clinical trials involving endothelin receptor antagonists: the novel '-sentan' class of drug. Soc Exp Biol Med 2006 231 : 653 95.
13. Clinical Trials.gov: a service of the US National Institutes of Health. Available at http://www.clinicaltrials.gov/ct/show/NCT00120328 (last accessed: 21 December 2006).