更新于：2024-11-15
Beraprost Sodium
贝前列素钠
更新于：2024-11-15
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 日本 (1992-01-21), |
最高研发阶段(中国)批准上市 |
特殊审评临床急需境外新药 (中国) |
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结构
分子式C24H30NaO5 |
InChIKeyLJCCZMFYFWMMDN-UHFFFAOYSA-N |
CAS号88475-69-8 |
关联
48
项与 贝前列素钠 相关的临床试验贝前列素钠片人体生物等效性试验
健康受试者空腹和餐后状态下单剂量口服贝前列素钠片（40μg）的随机、开放、两制剂、两序列、四周期、完全重复交叉生物等效性试验
贝前列素钠片在中国健康受试者中进行的单中心、随机、开放、单次（空腹/餐后）口服给药、两制剂、两序列交叉的人体生物等效性试验
100 项与 贝前列素钠 相关的临床结果
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100 项与 贝前列素钠 相关的转化医学
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100 项与 贝前列素钠 相关的专利（医药）
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505
项与 贝前列素钠 相关的文献（医药）2024-07-01Journal of veterinary internal medicine
Pulmonary thrombotic pulmonary hypertension managed using antithrombotic and pulmonary vasodilator treatment
Article
作者: Saito, Takahiro ; Horikawa, Rina ; Yuchi, Yunosuke ; Satomi, Shuji ; Teshima, Takahiro ; Matsumoto, Hirotaka ; Suzuki, Ryohei
Abstract:
An 8‐year‐old Leonberger receiving immunosuppressive treatment with clinical signs of acute dyspnea, cyanosis, and difficulty standing was referred to our institution (Day 1). Treatment including oxygen, clopidogrel, and low‐molecular‐weight heparin was initiated for suspected pulmonary thrombosis. However, exertional dyspnea persisted until Day 10, and increased tricuspid regurgitation velocity, pulmonary vascular resistance, and McConnell's signs also were observed. Thus, beraprost sodium was administered PO on Day 11 to treat suspected pulmonary hypertension. On Day 13, contrast‐enhanced computed tomography identified extensive contrast defects in the pulmonary arteries, and IV monteplase was administered on Days 14 and 18, with marked improvement in respiratory status and exertional dyspnea on Day 20. Right ventricular function and McConnell signs also improved, and tricuspid regurgitation velocity and pulmonary vascular resistance decreased. On Day 250, echocardiography indicated further improvement in pulmonary hypertension pathophysiology. The patient was still progressing well with antithrombotic and pulmonary vasodilator treatment 400 days later.
2024-05-01British journal of pharmacology
Inhibition of TRPM8 function by prostacyclin receptor agonists requires coupling to Gq/11 proteins
Article
作者: Offermanns, Stefan ; Tunaru, Sorin ; Huţanu, Debora-Elena ; Stratulat, Teodora ; Babes, Alexandru ; Badea, Rodica ; Sisignano, Marco ; Trif, Cosmin ; Banica, Alexandra-Maria ; Oprita, George ; Anghel, Sorina Andreea ; Selescu, Tudor ; Petrescu, Stefana M ; Manolache, Alexandra
Abstract:
Background and Purpose:
The TRPM8 ion channel is involved in innocuous cold sensing and has a potent anti‐inflammatory action. Its activation by lower temperature or chemical agonists such as menthol and icilin induces analgesic effects, reversing hypersensitivity and reducing chronic pain. On the other hand, prostacyclin (PGI2) enhances pain and inflammation by activating the IP receptors. Due to the critical roles of TRPM8 and IP receptors in the regulation of inflammatory pain, and considering their overlapping expression pattern, we analysed the functional interaction between human TRPM8 and IP receptors.
Experimental Approach:
We transiently expressed human TRPM8 channels and IP receptors in HEK293T cells and carried out intracellular calcium and cAMP measurements. Additionally, we cultured neurons from the dorsal root ganglia (DRGs) of mice and determined the increase in intracellular calcium triggered by the TRPM8 agonist, icilin, in the presence of the IP receptor agonist cicaprost, the IP receptor antagonist Cay10441, and the Gq/11 inhibitor YM254890.
Key Results:
Activation of IP receptors by selective agonists (cicaprost, beraprost, and iloprost) inhibited TRPM8 channel function, independently of the Gs‐cAMP pathway. The potent inhibition of TRPM8 channels by IP receptor agonists involved Gq/11 coupling. These effects were also observed in neurons isolated from murine DRGs.
Conclusions and Implications:
Our results demonstrate an unusual signalling pathway of IP receptors by coupling to Gq/11 proteins to inhibit TRPM8 channel function. This pathway may contribute to a better understanding of the role of TRPM8 channels and IP receptors in regulating pain and inflammation.
2024-03-01Vascular pharmacology
Comparative effectiveness of oral therapies targeting the prostacyclin pathway in pulmonary arterial hypertension: A systematic review and network meta-analysis
Review
作者: Papa, Silvia ; Badagliacca, Roberto ; Manzi, Giovanna ; Recchioni, Tommaso ; Mariani, Marco Valerio ; Vizza, Carmine Dario ; Scoccia, Gianmarco ; Filomena, Domenico
BACKGROUND:
Oral prostanoids are recommended in patients with pulmonary arterial hypertension (PAH) and an unsatisfactory response to first-line therapy.
OBJECTIVE:
To compare the effectiveness of oral therapies targeting the prostacyclin pathway in PAH patients.
METHODS:
An online search of Medline, Cochrane Registry, Scopus and EMBASE libraries (from inception to May, 12,020) was conducted. Eight randomized controlled studies were included in the meta-analysis involving 3023 patients, with 828 receiving oral treprostinil, 607 patients receiving selexipag, 125 patients receiving beraprost, and 1463 patients receiving placebo.
RESULTS:
Compared to placebo, oral treprostinil (WMD 9.05, 95% CI 3.0280-15.0839, p = 0.0032) and beraprost (WMD 21.98, 95% CI 5.0536-38.9063, p = 0.0109) were associated with a significant increase in 6-min walking distance (6MWD) at follow-up from baseline, whereas selexipag use was associated with a non-significant increase in 6MWD (WMD 15.41, 95% CI -0.6074; 31.4232, p = 0.0593). Compared to placebo, the risk of clinical worsening was significantly lowered by selexipag (RR 0.47, 95% CI 0.35-0.65, p < 0.001) and oral treprostinil (RR 0.65, 95% CI 0.46-0.90, p 0.012), whereas a non-significant reduction of the outcome was related to beraprost use (RR 0.70, 95% CI 0.36-1.38, p 0.31). No significant difference in 6MWD change and clinical worsening reduction were found among oral treprostinil and selexipag. Beraprost use less frequently caused adverse events as compared to selexipag and oral treprostinil.
CONCLUSIONS:
No differences in 6MWD change, clinical worsening reduction and adverse events rates were found among oral treprostinil and selexipag, resulting in similar efficacy and safety profiles.
100 项与 贝前列素钠 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 |
|---|---|---|---|
| 外周血管疾病 | 中国 | 2003-08-15 | |
| 肺动脉高压 | 中国 | 2003-08-15 | |
| 肺性高血压 | 日本 | 1999-09-22 | |
| 动脉闭塞 | 日本 | 1992-01-21 |
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 |
|---|---|---|---|---|
| 肾硬化 | 临床3期 | 中国 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 中国 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 中国 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 日本 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 日本 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 日本 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 马来西亚 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 马来西亚 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 马来西亚 | 2011-06-02 | |
| 肾硬化 | 临床3期 | 韩国 | 2011-06-02 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 36 | 積觸範淵糧窪襯繭網顧(衊壓衊鑰鹽鏇餘艱鑰築) = 繭鏇範艱壓膚淵膚獵壓 鹹窪鹹構製醖蓋遞簾糧 (窪衊鹽餘鹽鏇壓夢鹹顧, 憲顧簾願築壓觸蓋鏇鹽 ~ 廠襯遞壓獵願獵憲衊構) 更多 | - | 2020-09-30 | |||
临床2期 | 18 | 範積壓積鏇獵鹹醖積簾(積鑰鬱簾膚窪鹹鹹糧獵) = 遞積夢鑰網襯憲醖夢蓋 糧糧膚窪壓窪廠構憲蓋 (觸衊糧蓋鬱製鹹鏇簾鬱, 顧膚夢築淵範艱鹽獵鹽 ~ 醖艱網範選窪築衊壓鹹) 更多 | - | 2019-12-26 | |||
N/A | - | - | 鬱簾鹹網膚簾願選醖鏇(壓鹹鏇夢簾衊襯廠築遞) = 簾襯積糧淵構壓鬱衊壓 獵鏇艱糧簾鹹願簾糧齋 (鬱獵膚構餘糧鏇襯壓襯 ) | 积极 | 2017-05-26 | ||
鬱簾鹹網膚簾願選醖鏇(壓鹹鏇夢簾衊襯廠築遞) = 製壓構廠壓構壓製遞窪 獵鏇艱糧簾鹹願簾糧齋 (鬱獵膚構餘糧鏇襯壓襯 ) | |||||||
N/A | - | 築願餘鏇簾淵鏇鏇觸憲(網餘窪觸艱衊鬱鑰醖鏇) = 廠膚壓願窪顧齋鏇築蓋 製繭繭遞壓壓網遞齋齋 (廠鬱夢築願艱鹽鑰廠鏇 ) 更多 | - | 2016-10-01 | |||
築願餘鏇簾淵鏇鏇觸憲(網餘窪觸艱衊鬱鑰醖鏇) = 願窪壓衊蓋鬱顧選願鹹 製繭繭遞壓壓網遞齋齋 (廠鬱夢築願艱鹽鑰廠鏇 ) 更多 | |||||||
临床3期 | - | - | 範範廠製淵鏇構鏇窪廠(積選齋艱鹹艱鹹繭淵壓) = Beraprost-314d relaxed constricted PAs with a 4-fold greater potency than beraprost 鏇壓醖鏇網網觸繭膚醖 (願顧齋壓範觸鏇範獵鑰 ) 更多 | - | 2015-09-01 | ||
临床2/3期 | - | 糧膚獵餘醖網顧獵觸鏇(簾鏇鬱淵願製夢鑰鹹願) = 醖窪範壓膚膚願膚構蓋 窪壓繭鹹簾鏇糧築鏇衊 (鏇範繭顧醖鹹齋窪糧範 ) | 积极 | 2013-11-05 |
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