Affiliation: Nycomed GmbH
- Ciclesonide uptake and metabolism in human alveolar type II epithelial cells (A549)Takashi Nonaka
Teijin Institute for Biomedical Research, Teijin Pharma Limited, 4 3 2 Asahigaoka, Hino, Tokyo 191 8512, Japan
BMC Pharmacol 7:12. 2007..High performance liquid chromatography with tandem mass spectrometry was used to measure the concentrations of both corticosteroids and metabolites...
- Determination of lung deposition following inhalation of ciclesonide using different bioanalytical proceduresRüdiger Nave
Department of Pharmacometrics Pharmacokinetics, Nycomed GmbH, Byk Gulden Str 2, 78467 Konstanz, Germany
Bioanalysis 2:807-14. 2010..The pulmonary bioavailability was more than 60% as assessed for des-CIC in pharmacokinetic studies using HPLC-MS/MS detection as bioanalytical method. Pharmacokinetics in asthmatic patients and healthy subjects are similar...
- Clinical pharmacokinetic and pharmacodynamic profile of inhaled ciclesonideRüdiger Nave
Department of Pharmacometrics Pharmacokinetics, Nycomed GmbH, Konstanz, Germany
Clin Pharmacokinet 48:243-52. 2009..The unique pharmacokinetic and pharmacodynamic profile of ciclesonide offers a rationale that supports the favourable risk-benefit profile observed in clinical trials in patients with persistent asthma...
- In vitro metabolism of beclomethasone dipropionate, budesonide, ciclesonide, and fluticasone propionate in human lung precision-cut tissue slicesRuediger Nave
DMPK, Nycomed GmbH, Konstanz, Germany
Respir Res 8:65. 2007..CIC, a new generation ICS, is hydrolyzed by esterases in the upper and lower airways to its pharmacologically active metabolite desisobutyryl-ciclesonide (des-CIC)...
- Deposition and metabolism of inhaled ciclesonide in the human lungR Nave
Dept of Pharmacometrics, Nycomed GmbH, Byk Gulden Str 2, 78467 Konstanz, Germany
Eur Respir J 36:1113-9. 2010..A substantial portion of ciclesonide was already activated to des-CIC at the first time-point of tissue analysis. Activation of ciclesonide and formation of des-CIC fatty acid conjugates was confirmed in vivo in the human lung...
- In Vitro metabolism of ciclesonide in human lung and liver precision-cut tissue slicesRuediger Nave
ALTANA Pharma AG, Konstanz, Germany
Biopharm Drug Dispos 27:197-207. 2006..Activation and fatty acid esterification in the lung followed by rapid inactivation in the liver may explain the improved safety profile and prolonged anti-inflammatory activity of ciclesonide...
- Pharmacokinetics of ciclesonide and desisobutyryl ciclesonide after administration via aqueous nasal spray or hydrofluoroalkane nasal aerosol compared with orally inhaled ciclesonide: an open-label, single-dose, three-period crossover study in healthy volRuediger Nave
Nycomed GmbH, Konstanz, Germany
Clin Ther 31:2988-99. 2009..However, systemic exposure with ciclesonide HFA nasal aerosol (CIC-HFA) developed for the treatment of allergic rhinitis has not been investigated...
- Lower oropharyngeal deposition of inhaled ciclesonide via hydrofluoroalkane metered-dose inhaler compared with budesonide via chlorofluorocarbon metered-dose inhaler in healthy subjectsRuediger Nave
ALTANA Pharma AG, Byk Gulden Str 2, 78467, Konstanz, Germany
Eur J Clin Pharmacol 61:203-8. 2005..We studied oropharyngeal deposition of ciclesonide, des-CIC, and budesonide...
- Safety, tolerability, and exposure of ciclesonide nasal spray in healthy and asymptomatic subjects with seasonal allergic rhinitisRuediger Nave
ALTANA Pharma AG, Byk Gulden Str 2, 78467 Konstanz, Germany
J Clin Pharmacol 46:461-7. 2006..Ciclesonide was well tolerated and did not appear to affect serum or urine free cortisol levels. The low systemic exposure and favorable safety profile support the continued clinical development of ciclesonide nasal spray...
- Protein binding and its potential for eliciting minimal systemic side effects with a novel inhaled corticosteroid, ciclesonideShashank Rohatagi
Sanofi Aventis, Bridgewater, New Jersey 2ALTANA Pharma AG, Konstanz, Germany
Am J Ther 12:201-9. 2005..The very low fraction of unbound des-CIC in the systemic circulation suggests minimal systemic exposure of unbound des-CIC, thus suggesting a low potential for systemic adverse effects after administration of inhaled ciclesonide...
- Equivalent pharmacokinetics of the active metabolite of ciclesonide with and without use of the AeroChamber Plus spacer for inhalationAnton Drollmann
ALTANA Pharma AG, Konstanz, Germany
Clin Pharmacokinet 45:729-36. 2006..A spacer may be used in combination with the hydrofluoroalkane metered-dose inhaler (HFA-MDI) to maintain inhaled corticosteroid delivery to the lung in patients with poor inhalation technique...
- Pharmacokinetics of [14C]ciclesonide after oral and intravenous administration to healthy subjectsRuediger Nave
ALTANA Pharma AG, Konstanz, Germany
Clin Pharmacokinet 43:479-86. 2004..Ciclesonide is a novel inhaled corticosteroid developed for the treatment of asthma...
- Uptake and metabolism of ciclesonide and retention of desisobutyryl-ciclesonide for up to 24 hours in rabbit nasal mucosaHideyuki Sato
Teijin Institute for Biomedical Research, Teijin Pharma Limited, Asahigaoka, Hino, Tokyo, Japan
BMC Pharmacol 7:7. 2007..Retention and formation of fatty acid conjugates of des-CIC were also measured in nasal mucosa extracts postadministration of a hypotonic ciclesonide suspension (143-mug single dose)...
- Comparative in vitro metabolism of 14C-ciclesonide in hepatocytes from the mouse, rat, rabbit, dog, and humanZheming Gu
XenoBiotic Laboratories Inc, Plainsboro, NJ, USA
Am J Ther 14:280-90. 2007....
- The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissueElaine Mutch
Toxicology Unit, Clinical and Laboratory Sciences, The University of Newcastle, Newcastle upon Tyne, UK
Biochem Pharmacol 73:1657-64. 2007....
- In vitro metabolism of ciclesonide in human nasal epithelial cellsHideyuki Sato
Teijin Institute for Biomedical Research, Teijin Pharma Limited, Hino, Tokyo, Japan
Biopharm Drug Dispos 28:43-50. 2007..In conclusion, ciclesonide was rapidly converted to des-CIC by carboxylesterases and cholinesterases, and des-CIC underwent reversible fatty acid conjugation in HNEC...
- High lung deposition of 99mTc-labeled ciclesonide administered via HFA-MDI to patients with asthmaSteve Newman
Pharmaceutical Profiles, Nottingham, UK
Respir Med 100:375-84. 2006..To examine the deposition and pharmacokinetics of ciclesonide administered via hydrofluoroalkane-metered dose inhaler (HFA-MDI) in patients with asthma...
- Comparison of the oropharyngeal deposition of inhaled ciclesonide and fluticasone propionate in patients with asthmaKai Richter
Pulmonary Research Institute at Hospital Grosshansdorf, Center for Pneumology and Thoracic Surgery, Woehrendamm 80, 22927 Grosshansdorf, Germany
J Clin Pharmacol 45:146-52. 2005..Furthermore, there is little activation of ciclesonide to its active metabolite in the oropharynx, suggesting a decreased likelihood of inhaled ciclesonide-associated oropharyngeal side effects...
- Risk-benefit value of inhaled glucocorticoids: a pharmacokinetic/pharmacodynamic perspectiveShashank Rohatagi
Aventis Pharmaceuticals, Bridgewater, NJ 08807 0800, USA
J Clin Pharmacol 44:37-47. 2004..Currently available inhaled glucocorticoids do not provide the complete pharmacokinetic/pharmacodynamic parameters to optimize RBV, leaving room for improvement in the development of future agents...