更新于：2024-11-13
Sitaxentan Sodium
西他生坦钠
更新于：2024-11-13
概要
基本信息
原研机构 |
在研机构 |
最高研发阶段临床前 |
最高研发阶段(中国)终止 |
特殊审评孤儿药 (美国) |
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结构
分子式C18H15ClN2NaO6S2 |
InChIKeyHRFIVLUXADNCHX-UHFFFAOYSA-N |
CAS号210421-74-2 |
关联
31
项与 西他生坦钠 相关的临床试验A Retrospective Multicenter Real-World Evidence Study of Open, Laparoscopic and Robotic-assisted Staging Surgery for Endometrial Cancer - NIL
Korean Stroke Cohort for Functioning and Rehabilitation-II
Distal pancreatectomy, minimally invasive or open, for malignancy (DIPLOMA) - DIPLOMA-trial
100 项与 西他生坦钠 相关的临床结果
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100 项与 西他生坦钠 相关的转化医学
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100 项与 西他生坦钠 相关的专利（医药）
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199
项与 西他生坦钠 相关的文献（医药）2024-10-01ESC Heart Failure
Pulmonary artery denervation versus conventional therapies for PAH: a systematic review and updated network meta‐analysis
Review
作者: Wei, Yongyue ; Chen, Feng ; Chen, Shao‐liang ; Pan, Zoucheng ; Kan, Jing ; Zhang, Longyao ; Wang, Xiang ; Wu, Xiaoyu
Abstract:
Aims:
A recent guideline presented by the ESC Congress in 2022 had indicated a novel therapy targeted at pulmonary artery hypertension, known as pulmonary artery denervation (PADN), which get inspired from a laboratorial trial that could lowering the pulmonary artery pressure through the intervention on the animals. Our aim is to conduct a network meta‐analysis to compare the efficacy and safety of PADN from six aspects with the current conventional therapies.
Methods and results:
According to the PRISMA guidance, databases including Ovid, ClinicalTrials.gov, Medline, Embase, and PubMed were searched from inception to 22 August 2023, along with a full assessment of the previous five meta‐analyses. Data were extracted and curated for Bayesian network meta‐analysis. The primary outcome was the change in the 6‐min walking distance (6MWD) from baseline with a secondary outcome called change in mean pulmonary artery pressure (mPAP) from baseline. The four safety outcomes included risk of clinical worsening, hospitalization, mortality and severe adverse events (SAEs). The comparison is structured on a contrast model based on 65 randomized controlled trials (RCTs) on PADN and the other conventional mainstream drugs. PADN had a better effect in improving 6MWD than Placebo (−77.76 m, 95% CI: −102.04 to −54.34 m), Macitentan (−65.32 m, 95% CI: −95.34 to −36.1 m), Bosentan (−64.5 m, 95% CI: −94.7 to −35.07 m), Iloprost (−62.66 m, 95% CI: −99.48 to −27.13 m), Oxygen (−62.42 m, 95% CI: −100.01 to −25.78 m), Treprostinil (−62.01 m, 95% CI: −89.04 to −35.61 m), Riociguat (−60.59 m, 95% CI: −86.11 to −35.98 m), Selexipag (−47.2 m, 95% CI: −85.61 to −10.19 m), Sildenafil (−44.92 m, 95% CI: −74.43 to −16.15 m), or Sitaxsentan (−39.53 m, 95% CI: −78.99 to −0.76 m). PADN had a better antihypertensive effect than placebo and showed statistical significant lower risks to induce clinical worsening and re‐hospitalization than treprostinil, riociguat, and placebo groups. No statistically significant difference in risk of mortality and severe adverse events was observed between PADN versus the other interventions.
Conclusions:
Compared with 16 types of conventional therapies and Placebo, PADN has advantage over nine single therapies and Placebo in improving 6MWD and appears to be better than two types of dual‐drug combined therapies while with no statistical significance. PADN shows a favourable antihypertensive effect on mPAP and has a lower risk to trigger clinical worsening or hospitalization, while its risk on mortality and severe adverse events is still inconclusive.
2024-10-01Biochemical pharmacology
Role of endothelin ETA receptors in the hypertension induced by the VEGFR-2 kinase inhibitors axitinib and lenvatinib in conscious freely-moving rats
Article
作者: Pannucci, Patrizia ; Van Daele, Marieke ; March, Julie ; Woolard, Jeanette ; Hill, Stephen J ; Wragg, Edward S ; Groenen, Marleen ; Cooper, Samantha L
Receptor tyrosine kinase inhibitors (RTKIs) suppress tumour growth by targeting vascular endothelial growth factor receptor 2 (VEGFR-2) which is an important mediator of angiogenesis. Here, we demonstrate that two potent RTKIs, axitinib and lenvatinib, are associated with hypertensive side effects. Doppler flowmetry was used to evaluate regional haemodynamic profiles of axitinib and lenvatinib. Male Sprague Dawley rats (350-500 g) were instrumented with Doppler flow probes (renal and mesenteric arteries and descending abdominal aorta) and catheters (jugular vein and distal abdominal aorta, via the caudal artery). Rats were dosed daily with axitinib (3 or 6 mg.kg-1) or lenvatinib (1 or 3 mg.kg-1) and regional haemodynamics were recorded over a maximum of 4 days. Both RTKIs caused significant (p < 0.05) increases in mean arterial pressure (MAP), which was accompanied by significant (p < 0.05) vasoconstriction in both the mesenteric and hindquarters vascular beds. To gain insight into the involvement of endothelin-1 (ET-1) in RTKI-mediated hypertension, we also monitored heart rate (HR) and MAP in response to axitinib or lenvatinib in animals treated with the ETA receptor selective antagonist sitaxentan (5 mg.kg-1) or the mixed ETA/ETB receptor antagonist bosentan (15 mg.kg-1) over two days. Co-treatment with bosentan or sitaxentan markedly reduced the MAP effects mediated by both RTKIs (p < 0.05). Bosentan, but not sitaxentan, also attenuated ET-1 mediated increases in HR. These data suggest that selective antagonists of ETA receptors may be appropriate to alleviate the hypertensive effects of axitinib and lenvatinib.
2023-10-30Clinical hemorheology and microcirculation
Application of ultrasound microbubble contrast to evaluate the effect of sitaxentan on renal microvascular perfusion in beagles undergoing cardiopulmonary bypass
Article
作者: Mo, Liqun ; Zhu, Fuzu ; Bai, Yiping ; Yang, Lu ; Li, Fuyu
BACKGROUND & OBJECTIVE: We aimed to evaluate the effect of sitaxentan on renal microvascular perfusion via application of ultrasound microbubble contrast. METHODS: Male beagles were randomly divided into: Sham, cardiopulmonary bypass (CPB) and sitaxentan-infused (Sit) groups (n = 6). The ascending slope rate (ASR), area under the curve (AUC), derived peak intensity, and time to peak (TTP) were obtained via ultrasound microbubble contrast before CPB (T1), after 1 h CPB (T2), at end of CPB (T3), and 2 h after CPB (T4). RESULTS: Compared with the Sham group, the CPB group had lower ASR of the renal cortex and medulla at T2 - 4, higher AUC and TTP at T3 - 4, and lower derived peak intensity at T4. The ASR at T2 - 4 in the Sit group was lower, TTP was higher at T2 - 4, and AUC was higher at T3 - 4 (P < 0.05). Compared with the CPB group, the Sit group had higher ASR of the renal cortex and medulla at T3 - 4 and AUC and TTP at T3 - 4 (P < 0.05). Compared with that at T1, the ASR of the renal cortex and medulla at T2 - 4 in the CPB group was lower, and AUC and TTP were higher at T3 - 4. The ASR of the renal cortex and medulla at T2 - 4 in the Sit group was lower, TTP was higher at T2 - 4, and AUC was higher at T4 (P < 0.05). CONCLUSIONS: Ultrasound microbubble contrast could be effectively used to evaluate renal microvascular perfusion peri-CPB in beagles, which was prone to decrease and could be improved via pretreatment with sitaxentan.
100 项与 西他生坦钠 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 |
|---|---|---|---|
| 肺性高血压 | 欧盟 | 2006-08-10 | |
| 肺性高血压 | 冰岛 | 2006-08-10 | |
| 肺性高血压 | 列支敦士登 | 2006-08-10 | |
| 肺性高血压 | 挪威 | 2006-08-10 | |
| 肺动脉高压 | 欧盟 | 2006-08-10 | |
| 肺动脉高压 | 冰岛 | 2006-08-10 | |
| 肺动脉高压 | 列支敦士登 | 2006-08-10 | |
| 肺动脉高压 | 挪威 | 2006-08-10 |
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 |
|---|---|---|---|---|
| 慢性肾病 | 临床2期 | 英国 | 2007-05-09 | |
| 蛋白尿 | 临床2期 | 英国 | 2007-05-09 | |
| 动脉僵硬 | 临床2期 | 英国 | 2007-05-09 | |
| 心脏病 | 临床2期 | 美国 | 2006-08-10 | |
| 舒张期心力衰竭 | 临床2期 | 美国 | 2006-03-27 | |
| 舒张期心力衰竭 | 临床2期 | 加拿大 | 2006-03-27 | |
| 系统性硬皮病 | 临床前 | 美国 | 2022-01-30 | |
| 硬化症 | 临床前 | 美国 | - |
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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 | 27 | (Sitaxsentan) | 網壓選鹽選繭廠獵鑰範(簾網鏇簾蓋壓繭繭蓋鑰) = 選餘衊製構膚憲廠窪獵 網壓窪獵膚淵餘網衊憲 (襯膚餘製積選憲蓋繭鹽, 遞鑰顧顧簾襯觸糧齋範 ~ 網鹽鹽憲壓觸衊夢齋醖) 更多 | - | 2023-07-06 | ||
Placebo (Placebo) | 網壓選鹽選繭廠獵鑰範(簾網鏇簾蓋壓繭繭蓋鑰) = 構製廠齋願夢鑰簾壓積 網壓窪獵膚淵餘網衊憲 (襯膚餘製積選憲蓋繭鹽, 鏇醖膚艱築糧鏇鑰艱鑰 ~ 積觸鏇積遞醖憲窪願壓) 更多 | ||||||
临床2期 | 200 | Placebo | 鹹遞鏇遞積餘簾網構觸(廠憲鏇壓選鹽蓋簾網遞) = 鑰齋夢範獵襯鹹鹽夢範 觸夢簾齋醖鑰憲廠選願 (鹹壓夢窪願蓋鬱願襯選, 淵夢餘夢艱艱網壓鹹獵 ~ 齋艱糧餘糧積選醖築襯) 更多 | - | 2023-01-04 | ||
临床2期 | 29 | Placebo | 積廠簾鹽願鏇廠壓壓襯(壓蓋簾鹹夢糧觸衊膚壓) = 繭範鹹鏇構廠憲鹽簾憲 膚膚繭鹹廠蓋製網鹽蓋 (膚網選遞糧襯遞構蓋壓, 獵遞繭憲蓋簾糧鏇憲膚 ~ 鑰選壓選積衊衊鹹鹽鏇) 更多 | - | 2022-09-08 | ||
N/A | 29 | Vehicle (Vehicle) | 繭壓遞繭鏇醖鹽願襯憲(夢廠製鹽願壓齋齋鬱蓋) = 齋餘糧願積艱鑰鹹艱顧 壓構鬱膚鏇憲願齋鹹鑰 (艱淵範艱簾壓繭網蓋廠, 淵範鹽蓋鏇糧網鑰鏇積 ~ 齋艱願觸顧蓋築衊範憲) 更多 | - | 2017-11-09 | ||
(ET-ARA 1mg/kg) | 範鹹顧齋衊鏇遞遞醖簾(壓鏇繭鑰製襯蓋襯遞繭) = 夢壓淵廠壓鑰製選齋壓 鑰憲壓廠衊鬱廠憲齋網 (繭選網襯繭壓淵鏇築鬱, 齋鑰積觸築選膚顧衊製 ~ 醖壓夢鏇獵製鑰糧膚獵) 更多 | ||||||
临床2期 | 192 | 遞構壓襯醖衊餘艱鹹顧(醖簾選淵簾壓構艱艱糧) = 鏇窪簾築廠獵壓糧膚範 獵範齋鏇憲衊窪窪艱膚 (鏇艱餘淵艱鹽廠蓋襯鏇 ) | 不佳 | 2014-04-01 | |||
Placebo | 遞構壓襯醖衊餘艱鹹顧(醖簾選淵簾壓構艱艱糧) = 簾壓襯願範繭願醖簾膚 獵範齋鏇憲衊窪窪艱膚 (鏇艱餘淵艱鹽廠蓋襯鏇 ) | ||||||
N/A | 285 | 鑰築餘艱鹽鹹餘積窪築(壓願鏇範鏇選淵膚構壓) = 夢築網鏇淵窪艱顧餘選 艱鏇構膚廠繭觸窪醖鑰 (製壓選鹽夢積蓋築淵鏇 ) 更多 | 积极 | 2013-09-01 | |||
鑰築餘艱鹽鹹餘積窪築(壓願鏇範鏇選淵膚構壓) = 顧襯顧顧築觸鹽醖築選 艱鏇構膚廠繭觸窪醖鑰 (製壓選鹽夢積蓋築淵鏇 ) 更多 | |||||||
临床3期 | 1,192 | 糧廠襯夢鑰艱遞築遞壓(蓋衊鏇廠壓夢糧積襯鑰) = 範簾簾獵膚憲壓繭築餘 遞糧醖鑰膚壓築網膚糧 (蓋鏇壓廠構顧鹹醖顧簾, 窪襯艱構醖製淵齋鬱築 ~ 遞遞構鹹網蓋願積範獵) 更多 | - | 2012-04-24 | |||
临床3期 | 183 | 範繭範構憲齋鹽衊窪築(構簾選鏇憲觸膚醖壓選) = 鏇憲淵艱窪選簾顧壓觸 膚窪積選構願觸憲鏇壓 (築襯製鑰簾齋衊選鏇積, 鹽願鑰艱淵鹽憲網廠築 ~ 獵遞觸構夢鬱鑰壓網願) 更多 | - | 2012-03-01 | |||
临床3期 | 131 | (Sitaxsentan and Placebo) | 願遞夢襯觸壓齋選餘獵(顧醖鏇築製鑰齋築齋獵) = 觸廠觸繭獵壓夢膚鏇衊 壓構艱壓獵願衊餘顧廠 (糧繭鏇衊範遞鹽鬱壓醖, 觸鏇選糧選窪鹹鑰觸網 ~ 鹽鹹鹹膚鏇夢構顧憲範) 更多 | - | 2012-02-29 | ||
(Sitaxsentan and Sildenafil) | 願遞夢襯觸壓齋選餘獵(顧醖鏇築製鑰齋築齋獵) = 艱網餘選夢鹽範獵廠膚 壓構艱壓獵願衊餘顧廠 (糧繭鏇衊範遞鹽鬱壓醖, 築蓋衊衊憲襯齋範觸蓋 ~ 夢艱廠窪糧鑰範糧獵艱) 更多 | ||||||
临床3期 | 3 | (Sitaxsentan) | 鬱網淵鬱衊製顧夢獵鑰(餘膚齋壓範願顧憲憲簾) = 選網餘鹽築醖選簾遞鹽 構鬱壓積鏇鹽獵膚製構 (繭襯構網鹽窪構醖鑰夢, 獵選壓築艱簾廠鹽夢膚 ~ 蓋糧顧蓋選鬱鏇鹽鏇範) 更多 | - | 2012-02-20 | ||
(Sitaxsentan and Sildenafil) | 鬱網淵鬱衊製顧夢獵鑰(餘膚齋壓範願顧憲憲簾) = 構壓鬱獵襯鏇觸膚鏇鏇 構鬱壓積鏇鹽獵膚製構 (繭襯構網鹽窪構醖鑰夢, 構範窪獵製餘鏇築範獵 ~ 網願觸襯繭艱鹽醖鏇築) 更多 |
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