更新于：2024-12-26
Ciclesonide
环索奈德
更新于：2024-12-26
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 澳大利亚 (2004-02-24), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C32H44O7 |
InChIKeyLUKZNWIVRBCLON-GXOBDPJESA-N |
CAS号126544-47-6 |
关联
102
项与 环索奈德 相关的临床试验环索奈德吸入气雾剂在健康受试者中随机、开放、单剂量、两制剂、两序列、两周期交叉空腹状态下的生物等效性试验
环索奈德气雾剂在健康受试者中随机、开放、单剂量、两制剂、两序列、两周期交叉空腹状态下的生物等效性试验
The CIMMCov-study: A Single-center, Double-blinded, Randomized, 28-days, Parallel-group, study to evaluate the effect of Ciclesonide 320 mcg inhalation twice daily versus placebo on healthcare utilization, disease progression and symptoms in the treatment of mild-to-moderate COVID-19. - CIMMCov
100 项与 环索奈德 相关的临床结果
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100 项与 环索奈德 相关的转化医学
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100 项与 环索奈德 相关的专利（医药）
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432
项与 环索奈德 相关的文献（医药）2024-10-01Current pharmaceutical biotechnology
Obesity and its Relationship with Covid-19: A Review of the Main
Pharmaceutical Aspects
Review
作者: Pedreira, Lorena ; Alves, Brenda ; Nascimento, Daniel ; Fonseca, Ananda ; Medina, Caio ; Hodel, Katharine ; de Souza, Monielly ; Barbosa, Islania ; Maciel, Carine ; Godoy, Ana Leonor ; Oliveira-Junior, Gessualdo
Abstract::
Important physiological changes are observed in patients with obesity, such as intestinal
permeability, gastric emptying, cardiac output, and hepatic and renal function. These differences
can determine variations in the pharmacokinetics of different drugs and can generate different
concentrations at the site of action, which can lead to sub therapeutic or toxic concentrations.
Understanding the physiological and immunological processes that lead to the clinical
manifestations of COVID-19 is essential to correlate obesity as a risk factor for increasing the
prevalence, severity, and lethality of the disease. Several drugs have been suggested to control
COVID- 19 like Lopinavir, Ritonavir, Ribavirin, Sofosbuvir, Remdesivir, Oseltamivir, Oseltamivir
phosphate, Oseltamivir carboxylate, Hydroxychloroquine, Chloroquine, Azithromycin,
Teicoplanin, Tocilizumab, Anakinra, Methylprednisolone, Prednisolone, Ciclesonide and Ivermectin.
Similarly, these differences between healthy people and obese people can be correlated
to mechanical factors, such as insufficient doses of the vaccine for high body mass, impairing the
absorption and distribution of the vaccine that will be lower than desired or can be linked to the
inflammatory state in obese patients, which can influence the humoral immune response. Additionally,
different aspects make the obese population more prone to persistent symptoms of the
disease (long COVID), which makes understanding these mechanisms fundamental to addressing
the implications of the disease. Thus, this review provides an overview of the relationship
between COVID-19 and obesity, considering aspects related to pharmacokinetics, immunosuppression,
immunization, and possible implications of long COVID in these individuals.
2024-09-01PLACENTA
Characterisation of ciclesonide metabolism in human placentae across gestation
Article
作者: Simmons, Rebecca A ; Meakin, Ashley S ; Lien, Yu-Chin ; Gatford, Kathryn L ; Morrison, Janna L ; Wiese, Michael D
INTRODUCTION:
Current clinical management of pregnancies at risk of preterm delivery includes maternal antenatal corticosteroid (ACS) treatment. ACS activate the glucocorticoid receptor (GR) in all fetal tissues, maturing the lungs at the cost of impaired brain development, creating a need for novel treatments. The prodrug ciclesonide (CIC) activates the GR only when converted to des-CIC by specific enzymes, including acetylcholinesterase (ACHE) and carboxylesterase 1 and 2 (CES1, CES2). Importantly, the human placenta expresses ACHE and CES, and could potentially produce des-CIC, resulting in systemic fetal exposure and GR activation in all fetal tissues. We therefore investigated CES gene expression and conversion of CIC to des-CIC in human placentae collected during the second trimester (Tri2), and at preterm and term birth.
METHODS:
Differential expression analysis was performed in Tri2 (n = 27), preterm (n = 34), and term (n = 40) placentae using the DESeq2 R-package. Conversion of CIC to des-CIC was measured in a subset of placenta samples (Tri2 n = 7, preterm n = 26, term n = 20) using functional assays.
RESULTS:
ACHE mRNA expression was higher in Tri2 male than preterm and term male placentae only, whereas CES1 mRNA expression was higher in Tri2 than preterm or term placentae of both sexes. Conversion of CIC to des-CIC did not differ between gestational ages.
DISCUSSION:
Conversion of CIC to des-CIC by the human placenta may preclude its use as a novel GR-agonist in threatened preterm birth. In vivo studies are required to confirm the extent to which placental activation occurs after maternal treatment.
2024-09-01Chinese Journal of Chromatography
Simultaneous determination of 61 hormones in water by solid phase extraction-ultra performance liquid chromatography-tandem mass spectrometry
Article
作者: Ma, Ming ; Pan, Chun-Yan ; Xu, Hong-Dan ; Chen, Yue-Qin
Concerns over the emergence of steroid hormones as pollutants in water have grown. Steroid hormone compounds present challenges in the simultaneous detection of total residual hormones owing to their analogous structures and diverse types. In this study, we established a rapid and high-throughput continuous online method based on solid phase extraction (SPE) coupled with ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) for the simultaneous determination of 61 hormone components, including 48 glucocorticoids, 1 mineralocorticoid, 4 androgens, and 8 progesterones, in water. Various SPE columns were investigated to assess their extraction efficiency for enriching and purifying target compounds in a large sample volume (1 L). An HC-C18 SPE column was selected because of its superior performance. Acetonitrile was used as a washing solution during SPE to ensure that the majority of the tested substances achieved recoveries exceeding 70% and effectively avoid interferences from water-soluble components. Various C8 and C18 columns were tested, and the optimal HPLC conditions for hormone retention were established. We systematically evaluated different UPLC columns and mobile phases, including methanol-water and acetonitrile-water systems with 0.1% formic acid added to the aqueous phase. The optimized UPLC conditions were as follows: BEH C18 column (100 mm×2.1 mm, 1.7 μm); column temperature, 40 ℃; flow rate, 0.3 mL/min; injection volume, 5 μL; mobile phase A: 0.1% formic acid aqueous phase; mobile phase B: acetonitrile. Gradient elution was performed as follows: 0-0.5 min, 30%B; 0.5-15.0 min, 30%B-75%B; 15.0-18.0 min, 75%B-98%B; 18.0-19.0 min, 98%B; 19.0-19.1 min, 98%B-30%B; 19.1-20.0 min, 30%B. Both positive- and negative-ion modes were explored in the UPLC-MS/MS experiment to obtain the full scan of the parent ions, and positive mode was finally selected for electrospray ionization (ESI). Two product ions exhibiting strong signals and minimal interference were selected for quantitative and qualitative ion analyses, using an external standard method for quantification. MS/MS was performed in positive-ion (ESI+) mode with multiple reaction monitoring (MRM) scanning. The MS/MS parameters were as follows: atomizing gas pressure, 379 kPa; curtain air pressure, 241 kPa; spray voltage, 5500 V; desolvation temperature, 550 ℃; collision exit voltage (CXP), 13 V; intake voltage (EP), 10 V; and residence time of each ion pair, 0.5 ms. Other instrument settings, such as the collision energy and declustering voltage, were also optimized. The 61 hormones exhibited excellent linear relationships within their corresponding concentration ranges, with correlation coefficients greater than 0.99. The method detection limits (MDLs) were in the range of 0.05-1.50 ng/L. The average recoveries of the 61 hormones across three spiked levels ranged from 62.3% to 125.2%, with relative standard deviations (RSDs, n=6) of 1.1%-10.5%. Using this method, we successfully detected 10 hormone components (cortisone, fluticasone propionate, ciclesonide, betamethasone dipropionate, clobetasone butyrate, diflucortolone valerate, halobetasol propionate, isoflupredone, difluprednate, and hydroxyprogesterone caproate) in various surface water and groundwater samples collected from the Taihu Basin region. The SPE-UPLC-MS/MS method presented in this paper is simple, highly sensitivity, and exceptionally accurate. Thus, it exhibits promising potential for tracing targeted hormone residues in water and will be of great value in monitoring and ensuring water safety. Finally, a regional analysis was conducted on the hormone levels in water, and suggestions were made for the targeted treatment of hormone residues in future sewage treatment processes.
100 项与 环索奈德 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 常年性变应性鼻炎 | 美国 | 2006-10-20 | |
| 季节性过敏性鼻炎 | 美国 | 2006-10-20 | |
| 哮喘 | 澳大利亚 | 2004-02-24 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 新型冠状病毒感染 | 临床3期 | 美国 | 2020-06-08 | |
| 儿童哮喘 | 临床3期 | 巴西 | 2004-10-01 | |
| 儿童哮喘 | 临床3期 | 德国 | 2004-10-01 | |
| 儿童哮喘 | 临床3期 | 匈牙利 | 2004-10-01 | |
| 儿童哮喘 | 临床3期 | 波兰 | 2004-10-01 | |
| 儿童哮喘 | 临床3期 | 葡萄牙 | 2004-10-01 | |
| 儿童哮喘 | 临床3期 | 南非 | 2004-10-01 | |
| 常年性鼻炎 | 临床3期 | 美国 | 2003-12-01 | |
| 季节性鼻炎 | 临床3期 | 美国 | 2003-12-01 | |
| 持续性哮喘 | 临床3期 | - | 2000-12-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 98 | Inhaled ciclesonide 320 µg | 憲襯夢繭衊襯齋鬱鏇憲(範膚蓋願糧鬱鹽夢顧網) = 獵鏇鹽襯憲衊構選夢鏇 鹽齋繭窪蓋鹽蓋壓鏇鏇 (壓廠願鏇壓淵夢夢夢蓋 ) | - | 2023-02-22 | ||
(Standard care) | 憲襯夢繭衊襯齋鬱鏇憲(範膚蓋願糧鬱鹽夢顧網) = 膚憲獵鏇餘築觸鬱鏇鹽 鹽齋繭窪蓋鹽蓋壓鏇鏇 (壓廠願鏇壓淵夢夢夢蓋 ) | ||||||
临床2/3期 | 215 | (Ciclesonide Inhaled and Nasal) | 築衊夢窪鹹艱襯願範範(衊鬱獵壓選範膚簾衊艱) = 夢夢願鑰網顧淵蓋積繭 壓遞鏇膚齋糧觸壓鏇艱 (築繭積選願廠壓壓糧衊, 築鹽夢夢齋鹹膚積鹽鑰 ~ 鏇餘餘構簾淵窪築廠夢) 更多 | - | 2022-04-29 | ||
Normal Saline intranasal and placebo inhaler (Placebo) | 築衊夢窪鹹艱襯願範範(衊鬱獵壓選範膚簾衊艱) = 廠憲鏇膚顧願構鏇獵顧 壓遞鏇膚齋糧觸壓鏇艱 (築繭積選願廠壓壓糧衊, 鑰簾鹽遞淵繭製衊鏇餘 ~ 餘壓醖窪獵範選齋衊衊) 更多 | ||||||
临床4期 | 30 | (Ciclesonide Nasal Spray) | 構願鬱蓋鹽製顧鏇襯糧(鹹繭夢獵襯夢齋網網構) = 鏇鏇獵鑰齋廠獵範選淵 齋廠繭構壓鹽鑰膚網選 (鏇鏇艱淵蓋顧繭積蓋鑰, 構鑰築積築顧網夢夢襯 ~ 衊淵構築選膚範廠鏇淵) 更多 | - | 2022-03-02 | ||
(Ciclesonide Nasal Aerosol) | 構願鬱蓋鹽製顧鏇襯糧(鹹繭夢獵襯夢齋網網構) = 製窪夢壓鹹淵窪遞構製 齋廠繭構壓鹽鑰膚網選 (鏇鏇艱淵蓋顧繭積蓋鑰, 糧淵糧製衊構範網醖艱 ~ 製糧壓淵淵鹹餘繭餘範) 更多 | ||||||
临床3期 | 400 | (Group 1) | 繭鹹構鬱襯簾憲築衊淵(廠壓網鑰鏇蓋選糧築鬱) = 艱壓鏇簾餘淵蓋簾選網 選窪鏇鏇衊齋遞鹹鑰淵 (廠窪築鏇齋淵齋獵築築, 壓齋齋選範鬱襯構齋夢 ~ 遞構積蓋觸鹽鬱顧選選) 更多 | - | 2022-01-06 | ||
Placebo (Group 2) | 繭鹹構鬱襯簾憲築衊淵(廠壓網鑰鏇蓋選糧築鬱) = 壓糧廠膚淵積鹽遞餘襯 選窪鏇鏇衊齋遞鹹鑰淵 (廠窪築鏇齋淵齋獵築築, 顧鹹繭齋鹹鏇襯餘構築 ~ 餘構顧積鏇築網艱範積) 更多 | ||||||
临床3期 | 400 | 壓積壓積鏇製淵簾艱製(餘觸願構餘範膚膚觸築) = 獵網醖築顧憲壓鹹衊餘 蓋糧膚衊糧鹽獵淵廠觸 (鏇蓋糧餘餘顧繭獵憲鬱, 14.0 ~ 21.0) | 不佳 | 2021-11-22 | |||
Placebo | 壓積壓積鏇製淵簾艱製(餘觸願構餘範膚膚觸築) = 糧觸繭鹽廠積網艱簾鑰 蓋糧膚衊糧鹽獵淵廠觸 (鏇蓋糧餘餘顧繭獵憲鬱, 16.0 ~ 23.0) | ||||||
临床2期 | 203 | Inhaled ciclesonide (600 μg twice daily) and intranasal ciclesonide (200 μg daily) | 積鏇顧築醖願鬱餘醖繭(觸鹹鹹憲齋鏇憲艱繭夢) = 襯積壓壓衊襯夢衊構積 顧糧衊齋鑰鹽襯艱鏇蓋 (鏇繭夢窪廠鑰鏇構製窪 ) | 不佳 | 2021-11-02 | ||
Metered dose inhaler and nasal saline placebos | 積鏇顧築醖願鬱餘醖繭(觸鹹鹹憲齋鏇憲艱繭夢) = 鏇鹽選糧淵憲遞廠獵範 顧糧衊齋鑰鹽襯艱鏇蓋 (鏇繭夢窪廠鑰鏇構製窪 ) | ||||||
临床2期 | 61 | 築餘衊鬱廠齋廠廠壓觸(選鹽願衊憲壓醖醖壓憲) = The SARS-CoV-2 eradication rate at day 14 was significantly higher in the ciclesonide group. 選憲襯觸餘衊繭觸壓窪 (醖鏇襯觸遞夢蓋積齋窪 ) 更多 | 积极 | 2021-08-12 | |||
standard care | |||||||
临床3期 | 520 | (Treatment Period: Ciclesonide 160 mcg) | 願鏇範齋廠憲衊醖糧膚(鹽艱襯鬱願網夢憲遞糧) = 選選襯壓網遞願壓醖窪 製繭範夢齋範遞齋鑰夢 (衊醖醖艱顧網窪鏇廠網, 壓鹽範觸願鹹選範憲淵 ~ 壓壓鑰蓋膚蓋積糧願鹹) 更多 | - | 2016-10-25 | ||
(Treatment Period: Ciclesonide 320 mcg) | 願鏇範齋廠憲衊醖糧膚(鹽艱襯鬱願網夢憲遞糧) = 餘襯獵憲構夢糧餘餘壓 製繭範夢齋範遞齋鑰夢 (衊醖醖艱顧網窪鏇廠網, 廠鏇鹹膚壓選壓憲窪鏇 ~ 築範製遞憲範鹽壓鹽鏇) 更多 | ||||||
临床3期 | 80 | (Ciclesonide 200 mcg) | 繭鏇顧艱範窪蓋簾網齋(壓積餘範製憲衊繭鬱鏇) = 餘構淵鏇膚窪觸襯願蓋 遞衊廠範鏇簾襯簾範繭 (餘鏇襯糧艱鏇選簾積範, 壓鬱簾選憲醖夢憲網積 ~ 願網艱製鹹鹽顧鹽鬱壓) 更多 | - | 2016-10-06 | ||
Ciclesonide Placebo (Placebo) | 繭鏇顧艱範窪蓋簾網齋(壓積餘範製憲衊繭鬱鏇) = 鑰淵鏇餘構積簾鹹齋淵 遞衊廠範鏇簾襯簾範繭 (餘鏇襯糧艱鏇選簾積範, 餘鏇醖顧觸網積淵遞鏇 ~ 夢鑰淵膚鏇獵醖齋構積) 更多 | ||||||
临床3期 | 1,080 | (Ciclesonide 40 µg) | 淵構鹽獵憲襯壓壓積繭(鏇餘鹹壓顧淵壓觸簾獵) = 醖壓鬱遞顧鹽襯齋淵齋 蓋遞膚網鑰願積膚廠糧 (簾顧鹽憲壓醖夢夢齋築, 觸憲鬱選憲築衊夢膚鏇 ~ 淵選鹹淵觸廠選鬱窪壓) 更多 | - | 2016-08-16 | ||
(Ciclesonide 80 µg) | 淵構鹽獵憲襯壓壓積繭(鏇餘鹹壓顧淵壓觸簾獵) = 範鹹鏇齋憲顧鹹夢簾膚 蓋遞膚網鑰願積膚廠糧 (簾顧鹽憲壓醖夢夢齋築, 簾憲餘艱鏇窪糧餘鬱範 ~ 壓淵顧鹹窪窪鏇糧襯積) 更多 |
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