Multiple-dose pharmacokinetics, pharmacodynamics and tolerability of the oral ETA endothelin-receptor antagonist SPP301 in man

International Journal of Clinical Pharmacology and Therapeutics

Volumn 43, Issue 4, 2005, Pages 178-186

  Dieterle, W ^a   Mann, Jessica ^b   Kutz, K ^c  

^a Drug Disposition Consultants   (Germany)

^b Speedel Pharma AG   (Switzerland)

^c AccelPharm   (Switzerland)

Author keywords

ET 1 selective endothelin receptor antagonist; Pharmacodynamics; Pharmacokinetics; SPP301; Tolerability

Indexed keywords

5 HYDROXYMETHYL PYRIDINE 2 SULFONIC ACID [6 METHOXY 5 (2METHOXY PHENOXY) 2 (PYRIDIN 4 YL) PYRIMIDIN 4 YL] AMIDE; 5 METHYL PYRIDINE 2 SULFONIC ACID [6 METHOXY 5 (2 METHOXY PHENOXY) 2 [(PYRIDIN 4 YL)] PYRIMIDIN 4 YL]; AMINOTRANSFERASE; DRUG METABOLITE; ENDOTHELIN 1; ENDOTHELIN A RECEPTOR; ENDOTHELIN RECEPTOR ANTAGONIST; PLACEBO; RO 68 5925; SPP 301; UNCLASSIFIED DRUG;

AMINOTRANSFERASE BLOOD LEVEL; AREA UNDER THE CURVE; ARTICLE; BLOOD ANALYSIS; BLOOD PRESSURE MEASUREMENT; BLOOD SAMPLING; CLINICAL ARTICLE; CLINICAL TRIAL; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG DOSE REGIMEN; DRUG ELIMINATION; DRUG FEVER; DRUG HALF LIFE; DRUG MEGADOSE; DRUG METABOLISM; DRUG SAFETY; DRUG STABILITY; DRUG STRUCTURE; DRUG TOLERABILITY; EYE PAIN; HEADACHE; HUMAN; HUMAN EXPERIMENT; LIVER TOXICITY; MALAISE; MALE; MULTIPLE DRUG DOSE; NAUSEA; NORMAL HUMAN; PROTEIN BLOOD LEVEL; PULSE RATE; RHINITIS; RHINOPHARYNGITIS; SINGLE DRUG DOSE; SORE THROAT; STEADY STATE; SYMPTOMATOLOGY; TINNITUS; URINALYSIS; URINARY EXCRETION; VOMITING;

EID: 17444390855     PISSN: 09461965     EISSN: None     Source Type: Journal    
DOI: 10.5414/CPP43178     Document Type: Article

References (13)

1. Barst RJ, Langleben D, Frost A, Horn EM, Oudiz R, Shapiro S et al 2004 Sitaxsentan therapy for pulmonary arterial hypertension. Am J Respir Crit Care Med 69: 441-447
2. A-selective endothelin receptor antagonist SPP301 in healthy human subjects. J Clin Pharmacol 44: 59-66
3. Gibaldi M, Perrier D 1982 Pharmacokinetics (2nd ed). Marcel Dekker, New York
4. Grant K, Loizidou M, Taylor I 2003 Endothelin-I: a multifunctional molecule in cancer. Br J Cancer 88: 163-166
5. Gray GA, Webb DJ 1996 The endothelin system and its potential as a therapeutic target in cardiovascular disease. Pharmacol Ther 72: 109-148
6. Inoue A, Yanagisawa M, Kimura S, Kasuya Y, Miyauchi T, Goto K et al 1989 The human endothelin family: three structurally and pharmacologically distinct isopeptides and three separate genes. Proc Natl Acad Sci USA 86: 2863-2867
7. A receptor blockade prevents left ventricular remodeling and deterioration of cardiac function in experimental heart failure. Cardiovasc Res 39: 600-608
8. Noll G, Wenzel RR, Luescher TF 1996 Endothelin and endothelin antagonists: potential role in cardiovascular and renal diseases. Mol Cell Biochem 157: 259-267
9. Opgenorth TJ 1995 Endothelin receptor antagonism. Adv Pharmacol (New York) 33: 1-65
10. Remuzzi G, Perico N, Benigni A 2002 New therapeutics that antagonize endothelin: promises and frustrations. Nature Rev 1: 986-1001
11. Rubin LJ, Badesch DB, Barst RJ et al 2002 Bosentan therapy for pulmonary arterial hypertension. N Engl J Med 346: 896-903
12. Weber C, Schmitt R, Birnboeck H, Hopfgartner G, Eggers H, Meyer J et al 1999 Multiple-dose pharmacokinetics, safety and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers. J Clin Pharmacol 39: 703-714
13. Yanagisawa M, Kurihara H, Kimura S, Tomobe Y, Kobayashi M, Mitsui Y et al 1988 A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 332: 411-415