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更新于：2025-03-25
Riociguat
利奥西呱
更新于：2025-03-25
概要
基本信息
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2013-10-08), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国)、孤儿药 (韩国)、孤儿药 (日本) |
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结构/序列
分子式C20H19FN8O2 |
InChIKeyWXXSNCNJFUAIDG-UHFFFAOYSA-N |
CAS号625115-55-1 |
关联
78
项与 利奥西呱 相关的临床试验NCT05140525
Effects of Combination Medical Therapy Followed by Balloon Pulmonary Angioplasty on Right Ventricular-PA Coupling and Hemodynamics in Chronic Thromboembolic Pulmonary Hypertension
CTR20250018
利奥西呱片（2.5 mg）单次给药餐后状态下在健康男性受试者中的生物等效性试验
CTR20243669
利奥西呱片（2.5 mg）单次给药空腹/餐后状态下在健康男性受试者中的生物等效性试验
100 项与 利奥西呱 相关的临床结果
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100 项与 利奥西呱 相关的转化医学
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100 项与 利奥西呱 相关的专利（医药）
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632
项与 利奥西呱 相关的文献（医药）2025-06-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Development and robust optimization of the RP-HPLC method for the determination of riociguat and its four impurities in tablets using the AQbD approach
Article
作者: Otašević, Biljana ; Rašević, Marija ; Protić, Ana ; Zečević, Mira ; Rmandić, Milena ; Malenović, Anđelija ; Stanković, Jelena
The aim of this work was to develop and optimize the RP-HPLC method for the qualitative and quantitative analysis of riociguat and its four impurities using the Analytical Quality by Design concept. Risk assessment was carried out as a combination of Ishikawa diagram - Control, Noise and eXperimental - Failure mode and effect analysis from where critical method parameters for this study were selected (i.e. acetonitrile content in the mobile phase, concentration of ammonium acetate in aqueous part of mobile phase and column temperature). Their effects on critical method attributes (retention factor of the last eluting peak and separation of critical peak pairs) were further analyzed using the Design of Experiments methodology. The Design Space was defined as the area in which the robustness of the qualitative performance of the developed method is confirmed. Monte Carlo simulations were applied to achieve the defined quality by propagating the error resulting from the calculated coefficients of the mathematical models. The optimal chromatographic conditions included separation on an Xterra® RP18 (150 × 4.6 mm, 3.5 µm) column with a mobile phase consisting of 34 % of acetonitrile and 66 % of aqueous 15 mM ammonium acetate solution pH 5.5, at a column temperature of 36°C. The flow rate was 1 mL/min, the detection wavelength was 210 nm, while the injection volume was 20 µL. Validation of the developed method was performed, which confirmed its reliability in determining the content of riociguat and its four impurities in tablets.
2025-04-01Cardiovascular Intervention and Therapeutics
Effect of balloon pulmonary angioplasty on chronic thromboembolic pulmonary hypertension: an assessment of the learning curve in a Japanese university hospital
Article
作者: Kawaura, Noriyuki ; Ishigami, Tomoaki ; Ono, Fumiaki ; Suzuki, Toru ; Nakayama, Mina ; Konishi, Masaaki ; Hosoda, Junya ; Komura, Naohiro ; Hibi, Kiyoshi ; Mo, Makoto ; Sugano, Teruyasu ; Iwahashi, Noriaki
Abstract:
Balloon pulmonary angioplasty (BPA) is an innovative treatment for chronic thromboembolic pulmonary hypertension (CTEPH). We retrospectively examined the clinical outcomes and complications of BPA at Yokohama City University Hospital (YCUH) between 2012 and 2018. In 2012, we began to conduct BPA sessions in 46 patients with inoperable CTEPH; 34 completed the BPA scheme and the follow-up plan. A longitudinal sub-analysis was performed with cohorts 1 and 2 receiving BPA before and after April 2015. Significant improvements in the mean pulmonary arterial pressure, pulmonary vascular resistance, and other parameters were detected after BPA. The total rate of thoracic complications was 25%. Specifically, the increase in SaO2 and home oxygen therapy discontinuation rate, and oral riociguat discontinuation rate was significantly higher in cohort 2 (+ 7.7, 75, and 59%) compared to cohort 1 (+ 3.1, 27, and 10%) (P < 0.05). Moreover, the need for non-invasive positive pressure ventilation was significantly lower: 0% (cohort 2) vs. 7% (cohort 1) (P < 0.05). The BPA sessions conducted at the YCUH resulted in significant improvements in patients with CTEPH. This study demonstrates a clear learning curve regarding the effectiveness of BPA both in normalizing SaO2 and facilitating the cessation of home oxygen therapy, as well as in reducing the incidence of severe complications.Graphical abstract
2025-02-01JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
A simple HPLC-UV method for monitoring therapeutic adherence in pulmonary arterial hypertension
Article
作者: Kunicki, Paweł K ; Kopeć, Grzegorz ; Grymm, Maciej T ; Waligóra, Marcin ; Pawiński, Tomasz ; Szulczyk, Daniel
A considerable percentage of ineffective treatment in pulmonary arterial hypertension (PAH) may be related to subtherapeutic dosage or non-adherence. The aim of the study was to develop a simple analytical method suitable for plasma determination of selected drugs: riociguat (RIO), bosentan (BOS) and macitentan (MAC) administered to PAH patients. An isocratic HPLC-UV system (Spectra Physics - Shimadzu) with a manual injector (50 μL loop) was applied. Chromatographic analysis was performed using a Suplecosil LC-CN column (150 × 4.6 mm, 5 μm) protected with a Supelguard precolumn at room temperature. The separation was carried out using the mobile phase: CH3CN:H2O:0.5 M KH2PO4:85 % H3PO4 (172:324.2:3.7:0.1, v/v) at a flow rate of 1.8 mL/min. Ethyl acetate (4 mL) was used for 10-min liquid-liquid extraction from 0.4 mL alkalized plasma sample. Detection was performed at λ = 245 nm chosen as a compromise between signal intensity and matrix interference. The analytes were eluted at retention times of 4.4 min (RIO), 5.4 min (BOS), 8.9 min (MAC) and 7.8 min for gallopamil (internal standard, GAL). The method was found linear and calibrated in the ranges: 5-1000 ng/mL for RIO, 10-2000 ng/mL for BOS and 20-2000 ng/mL for MAC, with r2 of 0.9991 for RIO, 0.9983 for BOS, and 0.9949 for MAC, respectively. Within the given ranges, the method ensured reliable results with the required precision and accuracy: ≤15 % (≤20 % for LLOQ). There was no significant carryover effect. The method has been successfully used in pilot study on adherence in patients treated for PAH, enabling monitoring of RIO, BOS and MAC. Drug concentrations were assessed in samples taken before (C0) and 3 h after drug administration (C3). For RIO, BOS and MAC, the developed method was suitable for both C0 and C3 samples, allowing steady-state drug determination if used. The presented method can be recommended to laboratories equipped with basic HPLC apparatus as an attractive analytical tool for both TDM and adherence studies.
100 项与 利奥西呱 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 | 澳大利亚 | 2014-04-14 | |
| 家族性肺动脉高压 | 欧盟 | 2014-03-27 | |
| 家族性肺动脉高压 | 冰岛 | 2014-03-27 | |
| 家族性肺动脉高压 | 列支敦士登 | 2014-03-27 | |
| 家族性肺动脉高压 | 挪威 | 2014-03-27 | |
| 特发性肺动脉高压 | 欧盟 | 2014-03-27 | |
| 特发性肺动脉高压 | 冰岛 | 2014-03-27 | |
| 特发性肺动脉高压 | 列支敦士登 | 2014-03-27 | |
| 特发性肺动脉高压 | 挪威 | 2014-03-27 | |
| 与结缔组织病相关的肺动脉高压 | 欧盟 | 2014-03-27 | |
| 与结缔组织病相关的肺动脉高压 | 冰岛 | 2014-03-27 | |
| 与结缔组织病相关的肺动脉高压 | 列支敦士登 | 2014-03-27 | |
| 与结缔组织病相关的肺动脉高压 | 挪威 | 2014-03-27 | |
| 慢性血栓栓塞性肺动脉高压 | 美国 | 2013-10-08 | |
| 肺动脉高压 | 美国 | 2013-10-08 |
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 |
|---|---|---|---|---|
| 心脏病 | 临床2期 | 美国 | 2018-06-13 | |
| 肺血管疾病 | 临床2期 | 美国 | 2018-06-13 | |
| 血栓栓塞 | 临床2期 | 美国 | 2018-06-13 | |
| 指溃疡 | 临床2期 | 美国 | 2016-09-01 | |
| 硬皮病相关的手指溃疡 | 临床2期 | 美国 | 2016-09-01 | |
| 系统性硬皮病 | 临床2期 | 美国 | 2016-09-01 | |
| 弥漫性硬皮病 | 临床2期 | 美国 | 2015-01-15 | |
| 弥漫性硬皮病 | 临床2期 | 日本 | 2015-01-15 | |
| 弥漫性硬皮病 | 临床2期 | 澳大利亚 | 2015-01-15 | |
| 弥漫性硬皮病 | 临床2期 | 比利时 | 2015-01-15 |
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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
N/A | - | Riociguat monotherapy | 鹹壓襯積選襯夢鬱鏇鏇(夢憲簾淵鹹構廠齋糧願) = 4% 醖簾獵願憲窪鏇壓繭壓 (構遞獵醖艱鬱構鏇蓋廠 ) 更多 | - | 2024-05-19 | ||
Riociguat combination therapy | |||||||
临床2期 | 130 | (Riociguat) | 襯鏇鹹糧獵網廠膚衊願 = 醖憲繭構積簾構築鏇選 範淵夢鹽範窪製願淵鹹 (淵壓鹹艱築蓋淵網願顧, 獵鹹襯廠餘艱觸網鏇選 ~ 憲鏇顧願膚壓憲顧鬱醖) 更多 | - | 2023-07-19 | ||
Placebo (Placebo) | 襯鏇鹹糧獵網廠膚衊願 = 遞艱觸鑰蓋膚齋繭築獵 範淵夢鹽範窪製願淵鹹 (淵壓鹹艱築蓋淵網願顧, 繭鑰鏇壓範餘淵觸艱製 ~ 襯範衊簾衊鑰鹹製夢膚) 更多 | ||||||
临床3期 | 24 | 夢鏇範鬱淵製鑰選築簾(夢繭繭遞齋齋構衊窪製) = 鑰繭積鹽糧淵艱壓壓糧 鏇積觸餘獵願膚築窪糧 (淵襯鹽製襯選壓獵構獵 ) | 积极 | 2022-07-01 | |||
Pubmed 人工标引  | N/A | 31 | 蓋獵積憲遞願範蓋鏇艱(憲鑰醖遞夢鹽築鹹窪膚) = from 394 ± 91 m at baseline to 458 ± 100 m 遞觸蓋鹽鹽鏇築鑰淵糧 (鬱艱糧積壓襯鬱遞遞憲 ) | 积极 | 2022-05-09 | ||
临床2期 | 21 | 顧鹽觸壓鏇膚窪淵醖構(選鏇醖醖鏇餘醖繭壓醖) = Riociguat did not alter CFTR activity (change in sweat chloride) at doses up to 1.0 mg tid after 28 days. 簾壓構衊醖構壓獵獵獵 (範窪繭夢窪壓窪積築壓 ) 更多 | 不佳 | 2021-08-19 | |||
Placebo | |||||||
临床4期 | 16 | 鹹艱鬱窪鹹糧餘獵顧鬱(蓋壓觸顧鹽繭顧構夢鹹) = 餘製夢淵鹹窪範觸糧醖 構衊艱夢齋鬱糧積夢膚 (窪窪簾簾壓餘遞膚廠觸, -7.5 ~ +91.4) | 积极 | 2021-08-04 | |||
Placebo | 鹹艱鬱窪鹹糧餘獵顧鬱(蓋壓觸顧鹽繭顧構夢鹹) = 鬱淵衊齋簾鹽鏇淵製範 構衊艱夢齋鬱糧積夢膚 (窪窪簾簾壓餘遞膚廠觸, -176.8 ~ 60) | ||||||
临床2期 | 14 | Pulmonary endarterectomy+Riociguat (Riociguat) | 積蓋構窪憲網積積鬱淵(願觸鏇鹹醖選鑰齋淵鬱) = 遞範簾選網選窪顧選繭 遞壓選鏇餘積構範膚齋 (壓網觸獵顧鑰鹹網鑰蓋, 16.2) 更多 | - | 2021-06-22 | ||
Pulmonary endarterectomy (Placebo) | 積蓋構窪憲網積積鬱淵(願觸鏇鹹醖選鑰齋淵鬱) = 鬱鏇淵蓋鹹醖糧衊願製 遞壓選鏇餘積構範膚齋 (壓網觸獵顧鑰鹹網鑰蓋, 27.9) 更多 | ||||||
临床3期 | 16 | 窪製餘淵簾膚鑰襯鬱構(衊鹽蓋選衊襯願襯廠淵) = 艱蓋醖襯憲襯築糧蓋簾 窪構鏇鏇窪選壓憲窪簾 (遞構夢襯鬱製鬱顧鹽願, -7.5 ~ +91.4) | 积极 | 2021-05-03 | |||
Placebo | 窪製餘淵簾膚鑰襯鬱構(衊鹽蓋選衊襯願襯廠淵) = 鹹襯齋蓋簾築衊鹽餘網 窪構鏇鏇窪選壓憲窪簾 (遞構夢襯鬱製鬱顧鹽願, -176.8 ~ 60) | ||||||
临床4期 | - | 齋鑰觸製憲夢構鑰襯醖(窪鏇艱壓蓋鏇顧鹹積廠): OR = 2.78 (95% CI, 1.53 ~ 5.06), P-Value = 0.0007 | 积极 | 2021-05-03 | |||
PDE5i | |||||||
临床4期 | 225 | (Riociguat) | 艱蓋鬱鏇蓋醖淵憲簾顧 = 餘艱蓋構廠糧艱顧艱夢 簾淵淵鏇鬱鏇醖襯夢糧 (齋積鹽淵糧鹹鏇窪獵廠, 餘夢廠餘顧壓襯製鏇築 ~ 鹹獵餘憲餘夢構糧憲廠) 更多 | - | 2021-01-22 | ||
(PDE-5i) | 艱蓋鬱鏇蓋醖淵憲簾顧 = 鹽衊選鏇鏇鏇艱鏇觸網 簾淵淵鏇鬱鏇醖襯夢糧 (齋積鹽淵糧鹹鏇窪獵廠, 齋鏇醖願積鬱願餘獵鬱 ~ 憲獵獵獵壓夢獵築願顧) 更多 |
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