Pharmacodynamics and pharmacokinetics of the urotensin II receptor antagonist palosuran in macroalbuminuric, diabetic patients

Clinical Pharmacology and Therapeutics

Volumn 80, Issue 3, 2006, Pages 246-256

  Sidharta, Patricia N ^a   Wagner, Frank D ^a   Bohnemeier, Holger ^a   Jungnik, Arvid ^a   Halabi, Atef ^a   Krähenbühl, Stephan ^a   Chadha Boreham, Harbajan ^a   Dingemanse, Jasper ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

DIPEPTIDYL CARBOXYPEPTIDASE INHIBITOR; PALOSURAN; UNCLASSIFIED DRUG;

ADULT; AGED; ALBUMINURIA; ARTICLE; CLINICAL ARTICLE; CLINICAL TRIAL; CONFIDENCE INTERVAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DIABETES MELLITUS; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG SAFETY; DRUG TOLERABILITY; FATIGUE; FEMALE; FEVER; GEOMETRY; HEADACHE; HEMODYNAMICS; HUMAN; KIDNEY FUNCTION; MALE; MICROALBUMINURIA; PRIORITY JOURNAL; RHINOPHARYNGITIS; VERTIGO;

AGED; ALBUMINURIA; ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; AREA UNDER CURVE; CREATININE; DIABETES MELLITUS, TYPE 2; DIABETIC NEPHROPATHIES; FATIGUE; FEMALE; GLOMERULAR FILTRATION RATE; HEADACHE; HUMANS; HYPERTENSION; MALE; MIDDLE AGED; NASOPHARYNGITIS; QUINOLINES; RECEPTORS, G-PROTEIN-COUPLED; RENAL CIRCULATION; TREATMENT OUTCOME; UREA;

EID: 33748148272     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.clpt.2006.05.013     Document Type: Article

References (49)

1. Nosadini R., Velussi M., Brocco E., Bruseghin M., Abaterusso C., Saller A., et al. Course of renal function in type 2 diabetic patients with abnormalities of albumin excretion rate. Diabetes 49 (2000) 476-484
2. Atkins R.C. The epidemiology of chronic kidney disease. Kidney Int Suppl (2005) S14-S18
3. Tzamaloukas A.H., and Murata G.H. Prevention of nephropathy in patients with type 2 diabetes mellitus. Int Urol Nephrol 37 (2005) 655-663
4. Reboldi G., Gentile G., Angeli F., and Verdecchia P. Microalbuminuria and hypertension. Minerva Med 96 (2005) 261-275
5. Naidoo D.P. The link between microalbuminuria, endothelial dysfunction and cardiovascular disease in diabetes. Cardiovasc J S Afr 13 (2002) 194-199
6. Mogensen C.E. Microalbuminuria and hypertension with focus on type 1 and type 2 diabetes. J Intern Med 254 (2003) 45-66
7. Molitch M.E., DeFronzo R.A., Franz M.J., Keane W.F., Mogensen C.E., and Parving H.H. Diabetic nephropathy. Diabetes Care 26 Suppl 1 (2003) S94-S98
8. Salvetti A., Mattei P., and Sudano I. Renal protection and antihypertensive drugs: current status. Drugs 57 (1999) 665-693
9. Toto R.D. Treatment of hypertension in chronic kidney disease. Semin Nephrol 25 (2005) 435-439
10. Jerums G., and MacIsaac R.J. Treatment of microalbuminuria in patients with type 2 diabetes mellitus. Treat Endocrinol 1 (2002) 163-173
11. Bakris G.L., Weir M.R., Shanifar S., Zhang Z., Douglas J., van Dijk D.J., et al. Effects of blood pressure level on progression of diabetic nephropathy: results from the RENAAL study. Arch Intern Med 163 (2003) 1555-1565
12. Lewis E.J. The role of angiotensin II receptor blockers in preventing the progression of renal disease in patients with type 2 diabetes. Am J Hypertens 15 (2002) 123S-128S
13. Praga M. Slowing the progression of renal failure. Kidney Int Suppl (2002) 18-22
14. Parving H.H., and Hovind P. Microalbuminuria in type 1 and type 2 diabetes mellitus: evidence with angiotensin converting enzyme inhibitors and angiotensin II receptor blockers for treating early and preventing clinical nephropathy. Curr Hypertens Rep 4 (2002) 387-393
15. Abbott K.C., and Bakris G.L. Treatment of the diabetic patient: focus on cardiovascular and renal risk reduction. Prog Brain Res 139 (2002) 289-298
16. Kowey P.R., Dickson T.Z., Zhang Z., Shahinfar S., and Brenner B.M. Losartan and end-organ protection-lessons from the RENAAL study. Clin Cardiol 28 (2005) 136-142
17. Douglas S.A., Tayara L., Ohlstein E.H., Halawa N., and Giaid A. Congestive heart failure and expression of myocardial urotensin II. Lancet 359 (2002) 1990-1997
18. Maguire J.J., Kuc R.E., and Davenport A.P. Orphan-receptor ligand human urotensin II: receptor localization in human tissues and comparison of vasoconstrictor responses with endothelin-1. Br J Pharmacol 131 (2000) 441-446
19. Maguire J.J., and Davenport A.P. Is urotensin-II the new endothelin?. Br J Pharmacol 137 (2002) 579-588
20. Shenouda A., Douglas S.A., Ohlstein E.H., and Giaid A. Localization of urotensin-II immunoreactivity in normal human kidneys and renal carcinoma. J Histochem Cytochem 50 (2002) 885-889
21. Totsune K., Takahashi K., Arihara Z., Sone M., Satoh F., Ito S., et al. Role of urotensin II in patients on dialysis. Lancet 358 (2001) 810-811
22. Richards A.M., Nicholls M.G., Lainchbury J.G., Fisher S., and Yandle T.G. Plasma urotensin II in heart failure. Lancet 360 (2002) 545-546
23. Onan D., Hannan R.D., and Thomas W.G. Urotensin II: the old kid in town. Trends Endocrinol Metab 15 (2004) 175-182
24. Totsune K., Takahashi K., Arihara Z., Sone M., Ito S., and Murakami O. Increased plasma urotensin II levels in patients with diabetes mellitus. Clin Sci (Lond) 104 (2003) 1-5
25. Nicholls H. Urotensin II in human plasma. Trends Endocrinol Metab 12 (2001) 381-382
26. Affolter J., and Webb D.J. Urotensin II: a new mediator in cardiopulmonary regulation?. Lancet 358 (2001) 774-775
27. Douglas S.A., and Ohlstein E.H. Human urotensin-II, the most potent mammalian vasoconstrictor identified to date, as a therapeutic target for the management of cardiovascular disease. Trends Cardiovasc Med 10 (2000) 229-237
28. Clozel M., Binkert C., Birker-Robaczewska M., Boukhadra C., Ding S.S., Fischli W., et al. Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-y l)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System. J Pharmacol Exp Ther 311 (2004) 204-212
29. Clozel M., Hess P., Qiu C., Ding S.S., and Rey M. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J Pharmacol Exp Ther 316 (2006) 1115-1121
30. Sidharta P.N., van Giersbergen P.L.M., Schaarschmidt D., and Dingemanse J. Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy human subjects. J Clin Pharmacol 44 (2004) 1192
31. Sidharta P.N., van Giersbergen P.L.M., Schaarschmidt D., and Dingemanse J. Multiple-dose tolerability, safety, pharmacokinetics, and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy human subjects. Br J Clin Pharmacol 60 (2005) 677-678
32. Cole B.R., Giangiacomo J., Ingelfinger J.R., and Robson A.M. Measurement of renal function without urine collection. A critical evaluation of the constant-infusion technic for determination of inulin and para-aminohippurate. N Engl J Med 287 (1972) 1109-1114
33. Schnurr E., Lahme W., and Kuppers H. Measurement of renal clearance of inulin and PAH in the steady state without urine collection. Clin Nephrol 13 (1980) 26-29
34. Kuehnle H.F., von Dahl K., and Schmidt F.H. Fully enzymatic inulin determination in small volume samples without deproteinization. Nephron 62 (1992) 104-107
35. Marsilio R., Dall'Amico R., Montini G., Murer L., Ros M., Zacchello G., et al. Rapid determination of p-aminohippuric acid in serum and urine by high-performance liquid chromatography. J Chromatogr B Biomed Sci Appl 704 (1997) 359-364
36. Gibaldi M., and Perrier D. Pharmacokinetics. 2nd ed. (1982), Marcel Dekker, New York
37. de Zeeuw D. Should albuminuria be a therapeutic target in patients with hypertension and diabetes?. Am J Hypertens 17 (2004) 11S-15S
38. Brantsma A.H., Bakker S.J., de Zeeuw D., de Jong P.E., and Gansevoort R.T. Urinary albumin excretion as a predictor of the development of hypertension in the general population. J Am Soc Nephrol 17 (2006) 331-335
39. Lane J.T. Microalbuminuria as a marker of cardiovascular and renal risk in type 2 diabetes mellitus: a temporal perspective. Am J Physiol Renal Physiol 286 (2004) F442-F450
40. Björck S., Nyberg G., Mulec H., Granerus G., Herlitz H., and Aurell M. Beneficial effects of angiotensin converting enzyme inhibition on renal function in patients with diabetic nephropathy. Br Med J (Clin Res Ed) 293 (1986) 471-474
41. Buter H., Navis G., Dullaart R.P., de Zeeuw D., and de Jong P.E. Time course of the antiproteinuric and renal haemodynamic responses to losartan in microalbuminuric IDDM. Nephrol Dial Transplant 16 (2001) 771-775
42. Diamond J.R., Tilney N.L., Frye J., Ding G., McElroy J., Pesek-Diamond I., et al. Progressive albuminuria and glomerulosclerosis in a rat model of chronic renal allograft rejection. Transplantation 54 (1992) 710-716
43. Eddy A.A. Molecular insights into renal interstitial fibrosis. J Am Soc Nephrol 7 (1996) 2495-2508
44. Eddy A.A. Proteinuria and interstitial injury. Nephrol Dial Transplant 19 (2004) 277-281
45. Yard B.A., Chorianopoulos E., Herr D., and van der Woude F.J. Regulation of endothelin-1 and transforming growth factor-beta1 production in cultured proximal tubular cells by albumin and heparan sulphate glycosaminoglycans. Nephrol Dial Transplant 16 (2001) 1769-1775
46. Christ D.D. Human plasma protein binding of the angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) and its pharmacologically active metabolite EXP3174. J Clin Pharmacol 35 (1995) 515-520
47. Zini R., d'Athis P., Hoareau A., and Tillement J.P. Binding of four sulphonamides to human albumin. Eur J Clin Pharmacol 10 (1976) 139-145
48. Plum A., Muller L.K., and Jansen J.A. The effects of selected drugs on the in vitro protein binding of repaglinide in human plasma. Methods Find Exp Clin Pharmacol 22 (2000) 139-143
49. Benet L.Z., and Hoener B.A. Changes in plasma protein binding have little clinical relevance. Clin Pharmacol Ther 71 (2002) 115-121