Research Topics
| J DingemanseSummaryAffiliation: Actelion Pharmaceuticals Ltd Country: Switzerland Publications
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Detail Information
Publications
Investigation of the mutual pharmacokinetic interactions between bosentan, a dual endothelin receptor antagonist, and simvastatinJasper Dingemanse
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Clin Pharmacokinet 42:293-301. 2003..In vitro, bosentan has been shown to be a mild inducer of cytochrome P450 (CYP) 2C9 and 3A4...- Influence of mild liver impairment on the pharmacokinetics of tezosentan, a drug excreted unchanged into bileJasper Dingemanse
Department of Clinical Pharmacology, Gewerbestrasse 18, 4123 Allschwil, Switzerland
Br J Clin Pharmacol 57:344-8. 2004..To investigate the effect of mild liver impairment on the pharmacokinetics of tezosentan... - Clinical pharmacology of bosentan, a dual endothelin receptor antagonistJasper Dingemanse
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Clin Pharmacokinet 43:1089-115. 2004..In a pharmacokinetic-pharmacodynamic study in PAH patients, the haemodynamic effects lagged the plasma concentrations of bosentan... - Comparison of the pharmacokinetics, pharmacodynamics and tolerability of tezosentan between caucasian and Japanese subjectsJasper Dingemanse
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Allschwil, Switzerland
Br J Clin Pharmacol 61:405-13. 2006..To investigate the pharmacokinetics, pharmacodynamics and tolerability of the dual endothelin receptor antagonist tezosentan in caucasian and Japanese subjects... - Integrated pharmacokinetics and pharmacodynamics in drug developmentJasper Dingemanse
Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Clin Pharmacokinet 46:713-37. 2007.... - Influence of severe renal dysfunction on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonistJ Dingemanse
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Allschwil, Switzerland
Int J Clin Pharmacol Ther 40:310-6. 2002..One of the potential indications of bosentan, a dual endothelin receptor antagonist, is chronic heart failure. Patients with chronic heart failure frequently also suffer from impaired renal function... - World Federation of Sleep Research and Sleep Medicine Societies (worldsleep07)--5th Congress. 2-6 September 2007, Cairns, QLD, AustraliaJasper Dingemanse
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse 16, 4123 Allschwil, Switzerland
IDrugs 10:775-7. 2007 - Influence of liver cirrhosis on the pharmacokinetics, pharmacodynamics, and safety of tezosentanJasper Dingemanse
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse 16, 4123 Allschwil, Switzerland
J Clin Pharmacol 49:455-64. 2009..Moderate/severe liver impairment is associated with increased exposure to tezosentan, which is more pronounced in patients with elevated bilirubin levels, necessitating dose reduction... - Entry-into-humans study with tezosentan, an intravenous dual endothelin receptor antagonistJasper Dingemanse
Actelion Pharmaceuticals Ltd, Department of Preclinical Pharmacology, Allschwil, Switzerland
J Cardiovasc Pharmacol 39:795-802. 2002..Tezosentan warrants further clinical development in view of its tolerability and pharmacokinetic profile, which appears advantageous for application in emergency situations... - Pharmacokinetics and pharmacodynamics of tezosentan, an intravenous dual endothelin receptor antagonist, following chronic infusion in healthy subjectsJasper Dingemanse
Actelion Pharmaceuticals Ltd, Department of Preclinical Pharmacology, Gewerbestrasse 18, 4123 Allschwil, Switzerland
Br J Clin Pharmacol 53:355-62. 2002..The purpose of this study was to investigate the tolerability, pharmacokinetics, and pharmacodynamics of tezosentan, an intravenous dual endothelin receptor antagonist, during chronic infusions in healthy male subjects... - Mutual pharmacokinetic interactions between bosentan and lopinavir/ritonavir in healthy participantsJasper Dingemanse
Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Antivir Ther 15:157-63. 2010..We aimed to investigate the extent of pharmacokinetic drug interactions between bosentan and a fixed combination of lopinavir/ritonavir... - Nemifitide. InnapharmaJasper Dingemanse
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland
Curr Opin Investig Drugs 4:859-62. 2003..By June 2001, the first phase II trial of nemifitide in moderate to severely depressed individuals had been completed and in February 2003, Innapharma anticipated that phase III trials would commence later that year... - In vitro and in vivo pharmacokinetic characteristics of clazosentan, an intravenous endothelin receptor antagonist, in humansP L M van Giersbergen
Department of Clinical Pharmacology, Actelin Pharmaceuticals Ltd, Allschwil, Switzerland
Int J Clin Pharmacol Ther 47:169-77. 2009..In this study, the distribution, metabolism and excretion of the endothelin receptor antagonist clazosentan were investigated... - Inhibitory and inductive effects of rifampin on the pharmacokinetics of bosentan in healthy subjectsP L M van Giersbergen
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland
Clin Pharmacol Ther 81:414-9. 2007..The initial increase in bosentan concentrations can be explained by an inhibitory effect of rifampin on hepatic drug transporters... - Influence of ethnic origin and sex on the pharmacokinetics of clazosentanPaul L M van Giersbergen
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse 16, 4123 Allschwil, Switzerland
J Clin Pharmacol 47:1374-80. 2007..7 hours. The data suggest that Caucasian and Japanese patients can be treated with a similar dosing regimen of clazosentan. At the doses infused, administration of clazosentan was safe and well tolerated in both ethnic groups... - Comparative investigation of the pharmacokinetics of bosentan in Caucasian and Japanese healthy subjectsPaul L M van Giersbergen
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse 18, 4123 Allschwil, Switzerland
J Clin Pharmacol 45:42-7. 2005..The results suggest that, based on pharmacokinetic grounds, no dose adjustment of bosentan is necessary when used to treat Japanese patients in comparison to Caucasian patients... - Effect of gender on the tolerability, safety and pharmacokinetics of clazosentan following long-term infusionPaul L M van Giersbergen
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Clin Drug Investig 27:797-802. 2007..The purpose of this study was to investigate the effect of gender on the tolerability, safety and pharmacokinetics of clazosentan, an intravenous endothelin receptor antagonist... - Effect of severe renal impairment on the pharmacokinetics and tolerability of the parenteral endothelin antagonist tezosentanP L M van Giersbergen
Actelion Pharmaceuticals Ltd, Clinical Pharmacology, Allschwil, Switzerland
Int J Clin Pharmacol Ther 41:261-6. 2003..Tezosentan, an endothelin receptor antagonist, is under development for the treatment of acute heart failure. Impaired renal function is a frequent comorbidity in these patients... - Pharmacokinetic interaction between bosentan and the oral contraceptives norethisterone and ethinyl estradiolP L M van Giersbergen
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Int J Clin Pharmacol Ther 44:113-8. 2006..Bosentan has been shown in vitro and in vivo to induce the cytochrome P450 enzymes CYP2C9 and CYP3A4. The present study was conducted to investigate the effect of bosentan on the pharmacokinetics of a combined oral contraceptive... - Influence of food intake and formulation on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonistJasper Dingemanse
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Allschwil, Switzerland
J Clin Pharmacol 42:283-9. 2002..In conclusion, bosentan bioavailability from the newly developed 125 mg tablet formulation is similar to that of the suspension, and food intake does not influence its pharmacokinetics to a clinically relevant extent... - In vivo and in vitro disposition profile of tezosentan, an intravenous dual endothelin receptor antagonist, in humansA Treiber
Actelion Pharmaceuticals Ltd, Departments of Preclinical Pharmacokinetics and Metabolism, and Clinical Pharmacology, Gewerbestrasse 16, CH-4123 Allschwil, Switzerland
Xenobiotica 33:399-414. 2003..5. In human blood, tezosentan was highly bound to plasma proteins, mainly albumin, and hardly penetrated into red blood cells... - Orexin receptor antagonism, a new sleep-promoting paradigm: an ascending single-dose study with almorexantP Hoever
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Clin Pharmacol Ther 87:593-600. 2010..Population pharmacokinetic/pharmacodynamic modeling suggested that doses of ~500 mg almorexant and 10 mg zolpidem are equivalent with respect to subjectively assessed alertness... - Influence of food intake on the pharmacokinetics of miglustat, an inhibitor of glucosylceramide synthasePaul L M van Giersbergen
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse 16, 4123 Allschwil, Switzerland
J Clin Pharmacol 47:1277-82. 2007..The observed effects of food intake on the pharmacokinetics of miglustat are not considered to be of clinical relevance... - Cyclosporin increases the exposure to tezosentan, an intravenous dual endothelin receptor antagonistPaul L M van Giersbergen
Actelion Pharmaceuticals Ltd, Clinical Pharmacology, Gewerbestrasse 18, 4123 Allschwil, Switzerland
Eur J Clin Pharmacol 58:243-5. 2002..To investigate in 12 healthy subjects the pharmacokinetics and tolerability of tezosentan, an endothelin receptor antagonist, when given concomitantly with cyclosporin... - Determination of tezosentan, a parenteral endothelin receptor antagonist, in human plasma by liquid chromatography-tandem mass spectrometryPaul L M van Giersbergen
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Gewerbestrasse 18, 4123 Allschwil, Switzerland
J Chromatogr B Analyt Technol Biomed Life Sci 792:369-73. 2003..2%. Intra- and inter-assay coefficients of variation were below 10%. Stability tests revealed that tezosentan is stable under the different conditions tested... - Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjectsPatricia N Sidharta
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil Switzerland
J Clin Pharmacol 49:1168-75. 2009..No consistent effect was found on any of the pharmacodynamic variables measured. The results of this entry-into-humans study warrant further investigation of the therapeutic potential of palosuran... - Effect of the urotensin-II receptor antagonist palosuran on secretion of and sensitivity to insulin in patients with Type 2 diabetes mellitusPatricia N Sidharta
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, CH 4123 Allschwil, Switzerland
Br J Clin Pharmacol 68:502-10. 2009.... - In vivo and in vitro studies exploring the pharmacokinetic interaction between bosentan, a dual endothelin receptor antagonist, and glyburidePaul L M van Giersbergen
Department of Preclinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Clin Pharmacol Ther 71:253-62. 2002..This study was conducted to investigate a possible pharmacokinetic interaction between bosentan and glyburide... - Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptorPaul L M van Giersbergen
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Gewerbestrasse 18, 4123 Allschwil, Switzerland
Eur J Pharmacol 450:115-21. 2002..The findings provide a molecular mechanism for the interactions observed between bosentan and several drugs... - Influence of severe renal impairment on the pharmacokinetics of clazosentanShirin Bruderer
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse 3, 4123 Allschwil, Switzerland
J Clin Pharmacol 51:413-21. 2011..Administration of clazosentan was well tolerated in both groups. The data suggest that there is no need for dose adjustment of clazosentan in patients with renal impairment... - Pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonary arterial hypertensionRobyn J Barst
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse, Allscwil, Switzerland
Clin Pharmacol Ther 73:372-82. 2003..Little is known about the effects of bosentan in children. This study was conducted to investigate the pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonary arterial hypertension... - Single- and multiple-dose pharmacokinetics of bosentan and its interaction with ketoconazolePaul L M van Giersbergen
Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse 18, 4123 Allschwil, Switzerland
Br J Clin Pharmacol 53:589-95. 2002..The present study was conducted to characterize the single- and multiple-dose pharmacokinetics of bosentan, a dual endothelin receptor antagonist, and to investigate a possible pharmacokinetic interaction with ketoconazole... - Pharmacodynamics and pharmacokinetics of the urotensin II receptor antagonist palosuran in macroalbuminuric, diabetic patientsPatricia N Sidharta
Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Clin Pharmacol Ther 80:246-56. 2006..We have investigated whether palosuran, a potent, selective, and competitive antagonist of the urotensin II receptor, has effects in patients who are prone to the development of renal disease... - Tolerability, pharmacokinetics, and pharmacodynamics of clazosentan, a parenteral endothelin receptor antagonistPaul L M van Giersbergen
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Gewerbestrasse 18, 4123 Allschwil, Switzerland
Eur J Clin Pharmacol 63:151-8. 2007..The purpose of this study was to investigate in healthy male subjects the tolerability, pharmacokinetics, and pharmacodynamics of ascending doses of clazosentan, an intravenous endothelin receptor antagonist... - Influence of mild liver impairment on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonistPaul L M van Giersbergen
Actelion Pharmaceuticals, Ltd, Department of Clinical Pharmacology, Gewerbestrasse 18, 4123 Allschwil, Switzerland
J Clin Pharmacol 43:15-22. 2003..Bosentan was well tolerated in this study. In conclusion, the pharmacokinetics, metabolism, and tolerability of bosentan are similar in healthy subjects and patients with mild liver impairment... - Promotion of sleep by targeting the orexin system in rats, dogs and humansCatherine Brisbare Roch
Research and Development, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil, Switzerland
Nat Med 13:150-5. 2007..No signs of cataplexy were observed, in contrast to the rodent, dog or human narcolepsy syndromes. These results open new perspectives for investigating the role of endogenous orexins in sleep-wake regulation... - Mutual pharmacokinetic interactions between steady-state bosentan and sildenafilGary Burgess
PGRD, Pfizer Ltd, Sandwich, Kent, UK
Eur J Clin Pharmacol 64:43-50. 2008.... - Effect of the catechol-O-methyltransferase inhibitor entacapone on the steady-state pharmacokinetics and pharmacodynamics of warfarinJasper Dingemanse
Jacor Research, Bottmingen, Switzerland
Br J Clin Pharmacol 53:485-91. 2002..To investigate the influence of a multiple-dose regimen with the catechol-O-methyltransferase inhibitor entacapone on the pharmacokinetics and pharmacodynamics of warfarin... - Lack of renal improvement with nonselective endothelin antagonism with tezosentan in type 2 hepatorenal syndromeFlorence Wong
Division of Gastroenterology, Department of Medicine, Toronto General Hospital, University of Toronto, Toronto, Canada
Hepatology 47:160-8. 2008..Caution should be taken in future studies using endothelin receptor antagonists in these patients... - Effects of the endothelin receptor antagonist bosentan on hemodynamics, symptoms and functional capacity in Japanese patients with severe pulmonary hypertensionShigetake Sasayama
Hamamatsu Rosai Hospital, Japan
Circ J 69:131-7. 2005..CONCLUSION: Bosentan was well tolerated and improved the hemodynamics, symptoms, exercise capacity, and quality of life of Japanese patients with PAH. Thus, bosentan can be a valuable therapeutic option in Japanese patients... - The hemodynamic and neurohormonal effects of low doses of tezosentan (an endothelin A/B receptor antagonist) in patients with acute heart failureGad Cotter
The Cardiology Department, Assaf Harofeh Medical Center, 70300 Zerifin, Israel
Eur J Heart Fail 6:601-9. 2004..v.)-balanced dual endothelin (ET-A/B) antagonist, in doses of 50 and 100 mg/h, improved the hemodynamics but not the clinical outcome of patients with acute heart failure (AHF)... - Treatment of secondary pulmonary hypertension with bosentan and its pharmacokinetic monitoring in ESRDLutz Liefeldt
Division of Nephrology Department of Pathology, Center for Cardiovascular Research (CCR, Charit, Humboldt-University, Berlin, Germany
Am J Kidney Dis 43:923-6. 2004..5 mL/min. Bosentan for the treatment of secondary PH seems to be safe as well as effective in end-stage renal disease patients and no adjustment of the bosentan dosing regimen appears necessary... - Pharmacokinetic interaction between tadalafil and bosentan in healthy male subjectsRebecca E Wrishko
Lilly Research Laboratories, Lilly Corporate Center, DC 0730, Indianapolis, IN 46285, USA
J Clin Pharmacol 48:610-8. 2008..In conclusion, after 10 days of coadministration, bosentan decreased tadalafil exposure by 41.5% with minimal and clinically irrelevant differences (<20%) in bosentan exposure... - Pseudohallucinations after zolpidem intake: a case reportSanne de Haas
J Clin Psychopharmacol 27:728-30. 2007 - Multiple-dose pharmacokinetics of intranasally administered IS-159 in healthy subjectsPaul L M van Giersbergen
The Medicines Company, Gasstrasse 1, CH-4056 Basel, Switzerland
Eur J Drug Metab Pharmacokinet 28:49-54. 2003..The results showed dose-proportional pharmacokinetics of IS-159 in the dose range tested and a low propensity for drug accumulation...