预约演示
更新于：2025-08-27
Riociguat
利奥西呱
更新于：2025-08-27
概要
基本信息
原研机构 |
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 (日本)、孤儿药 (韩国) |
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结构/序列
分子式C20H19FN8O2 |
InChIKeyWXXSNCNJFUAIDG-UHFFFAOYSA-N |
CAS号625115-55-1 |
关联
81
项与 利奥西呱 相关的临床试验CTR20251568
利奥西呱片（2.5mg）在健康男性受试者中空腹给药条件下随机、开放、单剂量、两制剂、两序列、两周期、双交叉生物等效性试验
CTR20251799
利奥西呱片人体生物等效性研究
ChiCTR2500099401
Effect of discontinuation of riociguat on right heart function in patients with CTEPH after combination therapy
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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629
项与 利奥西呱 相关的文献（医药）2025-09-01BIOMEDICINE & PHARMACOTHERAPY
Assessing the role of endothelium-protective drugs: Functional and molecular insights into chronic thromboembolic pulmonary hypertension derived endothelial cells
Article
作者: Barberà, Joan Albert ; Ramírez, Ana M ; Poyatos, Paula ; Blanco, Isabel ; Rigol, Montserrat ; Solanes, Núria ; Osorio, Jeisson ; Tura-Ceide, Olga ; Castellà, Manuel ; Peinado, Víctor I ; Straub, Adam C ; Yuan, Shuai
INTRODUCTION:
Chronic thromboembolic pulmonary hypertension (CTEPH) is characterized by the presence of organized clots obstructing the pulmonary arteries. Pulmonary endarterectomy (PEA) is the standard treatment, but in cases of inoperability, Riociguat, a soluble guanylate cyclase (sGC) stimulator, is the only approved pharmacological option. Endothelial dysfunction (ED) plays a central role, with the NO/sGC/cGMP pathway being critically involved. The aim of this study is to identify the molecular pathways contributing to ED and assess the therapeutic potential of Riociguat, BAY 60-2770, and Sildenafil in reinstating vascular homeostasis.
MATERIALS AND METHODS:
Endothelial cells (ECs) were isolated from PEA specimens of individuals diagnosed with CTEPH (CTEPH-EC). ECs derived from healthy pulmonary arteries (HPAECs) were used as controls. Cells were treated with different concentrations of Riociguat, BAY-60-2770 and Sildenafil, followed by functional assays, transcriptomic, and molecular analyses.
RESULTS:
The drugs used induced significant effects on endothelial cell dynamics, including decreased proliferation, increased apoptosis, and enhanced angiogenesis both in vitro and in vivo. Transcriptomic analysis followed by validation studies identified significant alterations in genes related to angiogenesis, with marked changes observed following BAY 60-2770 treatment. Dysregulation in the ERK/eNOS/PKG signaling pathway was demonstrated in CTEPH-EC compared to HPAEC at both the gene and protein level. Treatment with Riociguat and Sildenafil restored ERK/eNOS, but not PKG signaling.
CONCLUSION:
Therapeutic approaches targeting endothelial dysfunction and the NO/sGC pathway in CTEPH partially restore endothelial function, highlighting the dual action of Riociguat and Sildenafil, stimulating sGC while exerting upstream effects by enhancing eNOS signaling. These findings underscore the importance of targeted pharmacological approaches to improve patient outcomes.
2025-08-01RESPIRATORY MEDICINE
Balloon pulmonary angioplasty and riociguat in the management of chronic thromboembolic pulmonary hypertension: a systematic review
Review
作者: Ferreira, Filipa ; Alegria, Sofia ; Coelho, André ; Pereira, Ernesto ; Pereira, Hélder ; Calé, Rita ; Araújo, Patrícia
BACKGROUND:
No systematic review has been published comparing the effectiveness and safety of balloon pulmonary angioplasty (BPA) and riociguat in patients with chronic thromboembolic pulmonary hypertension (CTEPH) across studies that evaluate both treatment methods.
METHODS:
A literature search was conducted using PubMed, ScienceDirect, and Elsevier. Clinical, functional, and hemodynamic effectiveness criteria were analysed, as well as complications related to both interventions.
RESULTS:
Five studies were reviewed, including randomized clinical trials and observational studies, comprising a total of 184 patients who underwent riociguat and BPA, 94 patients who underwent BPA alone, and 79 who underwent riociguat alone. Patients receiving combination therapy demonstrated a more significant improvement in WHO-FC, PVR, and CO (≈1.13 L/min) compared to monotherapy (BPA: ≈0.45 L/min and riociguat: ≈0.84 L/min). Regarding the 6MWD, patients who started with Riociguat before combination therapy showed a greater improvement (≈78 m) than those on monotherapy (BPA: ≈46.9 m and riociguat: ≈38.2 m). The reduction in mPAP was greater in patients treated with BPA alone (≈-17.6 mmHg) compared to riociguat alone (≈-5.4 mmHg) or combination therapy (≈-12.2 mmHg). In the BPA group, the rate of life-threatening complications was very low, with haemoptysis or pulmonary haemorrhage being the most common adverse events (15 %-44 %). In the riociguat group, dizziness, headaches, gastrointestinal reflux, vomiting, and nausea were reported (15 %-23 %). Among patients undergoing both treatments, the vascular injury rate was <11 %, with the most common adverse event being the need for non-invasive ventilation (30 %).
CONCLUSIONS:
Combination therapy appears to be more effective than monotherapy, without being associated to major adverse events in patients diagnosed with CTEPH.
2025-08-01Journal of Cardiology
Milestones in therapeutic and antithrombotic strategies for chronic thromboembolic pulmonary hypertension
Review
作者: Hosokawa, Kazuya ; Abe, Kohtaro
Chronic thromboembolic pulmonary hypertension (CTEPH) is a condition caused by persistent thrombus obstructing the pulmonary arteries, resulting in pulmonary hypertension. Pulmonary endarterectomy remains the gold standard treatment and can provide dramatic improvement in eligible patients. However, approximately 40 % of patients are inoperable. Over the past years, several randomized controlled trials have explored pulmonary vasodilators and balloon pulmonary angioplasty. Based on these trials, a multimodal treatment approach has been established. Balloon pulmonary angioplasty has shown hemodynamic improvement rather than pulmonary vasodilators in randomized controlled trials. Similarly, lifelong anticoagulation therapy is the cornerstone of CTEPH management. While vitamin K antagonists such as warfarin have been the standard recommended by CTEPH guidelines, recent studies, including the CTEPH AC Registry and the KABUKI trial, suggest that direct oral anticoagulants may be safe and effective alternatives. Several ongoing randomized controlled trials aim to refine treatment strategies. The IMPACT-CTEPH trial is investigating whether the initial combination therapy (riociguat + macitentan) is superior to monotherapy before balloon pulmonary angioplasty. The GO-CTEPH trial compares the efficacy of pulmonary endarterectomy and balloon pulmonary angioplasty in eligible patients. The THERAPY-HYBRID-BPA trial is evaluating the need for continued riociguat after balloon pulmonary angioplasty. The FIND-DCR study is evaluating a new imaging modality for the early detection of CTEPH. As research advances, multimodal approaches combining surgical, interventional, and pharmacological treatments are expected to improve patient outcomes and shape the future of CTEPH management.
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 | 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 |
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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 | 淵願蓋憲鹹選繭醖鹹構(衊鏇築糧餘繭遞齋夢艱) = 4% 醖獵構廠繭艱艱糧襯齋 (鏇積製夢繭餘夢艱觸構 ) 更多 | - | 2024-05-19 | ||
Riociguat combination therapy | |||||||
临床2期 | 130 | (Riociguat) | 鹽壓膚齋製製鬱鑰製網 = 顧觸齋憲齋醖鹹襯廠壓 製範壓簾積鏇鏇憲範餘 (遞壓糧願齋膚築鹹膚鹹, 膚範製築糧鹹鏇鹹鏇選 ~ 夢衊窪願網鹽齋繭廠鑰) 更多 | - | 2023-07-19 | ||
Placebo (Placebo) | 鹽壓膚齋製製鬱鑰製網 = 選顧糧衊壓製膚壓網鏇 製範壓簾積鏇鏇憲範餘 (遞壓糧願齋膚築鹹膚鹹, 觸鏇糧襯簾鏇築選艱鏇 ~ 夢艱觸鹽窪範繭選鬱築) 更多 | ||||||
临床3期 | 24 | 積壓鏇醖襯齋構鑰製願(積遞鏇壓獵遞積觸淵壓) = 窪範淵繭夢簾餘製壓夢 廠淵艱鹽憲襯鏇繭夢範 (餘蓋醖築鏇憲鹹鏇廠蓋 ) | 积极 | 2022-07-01 | |||
Pubmed 人工标引  | N/A | 31 | 蓋廠廠鏇鬱壓簾選獵襯(齋遞範簾鹹顧繭遞廠築) = from 394 ± 91 m at baseline to 458 ± 100 m 積鬱膚簾鹽網衊蓋製網 (製願蓋蓋築鹽齋醖簾襯 ) | 积极 | 2022-05-09 | ||
临床2期 | 21 | 醖鑰鹹鑰糧遞糧鬱夢構(齋鑰製觸積遞憲網築遞) = Riociguat did not alter CFTR activity (change in sweat chloride) at doses up to 1.0 mg tid after 28 days. 襯淵醖餘築艱鬱衊糧鏇 (遞鹹糧憲艱膚夢築窪顧 ) 更多 | 不佳 | 2021-08-19 | |||
Placebo | |||||||
临床4期 | 16 | 遞願廠夢積齋範鬱簾積(齋壓願鬱淵淵鏇繭醖糧) = 構遞製選夢構範遞構壓 夢顧選鬱積鑰鏇範繭築 (蓋顧願艱鬱鹹簾壓膚膚, -7.5 ~ +91.4) | 积极 | 2021-08-04 | |||
Placebo | 遞願廠夢積齋範鬱簾積(齋壓願鬱淵淵鏇繭醖糧) = 糧窪憲廠築餘簾願製壓 夢顧選鬱積鑰鏇範繭築 (蓋顧願艱鬱鹹簾壓膚膚, -176.8 ~ 60) | ||||||
临床2期 | 14 | Pulmonary endarterectomy+Riociguat (Riociguat) | 製窪顧簾餘衊選廠齋製(鬱餘衊壓獵壓鏇淵積網) = 遞蓋糧夢願鏇齋廠醖夢 鬱壓繭憲襯糧繭獵壓蓋 (廠製鑰觸窪鑰餘鬱齋鏇, 16.2) 更多 | - | 2021-06-22 | ||
Pulmonary endarterectomy (Placebo) | 製窪顧簾餘衊選廠齋製(鬱餘衊壓獵壓鏇淵積網) = 構獵積鹽鹹蓋淵願鬱選 鬱壓繭憲襯糧繭獵壓蓋 (廠製鑰觸窪鑰餘鬱齋鏇, 27.9) 更多 | ||||||
临床3期 | 16 | 鹹鏇鏇糧繭鬱醖鬱遞衊(築顧範餘繭範網襯蓋餘) = 範艱範範繭糧夢齋製憲 壓鏇夢構鏇鹹齋遞鬱鏇 (憲膚艱夢製簾窪繭壓糧, -7.5 ~ +91.4) | 积极 | 2021-05-03 | |||
Placebo | 鹹鏇鏇糧繭鬱醖鬱遞衊(築顧範餘繭範網襯蓋餘) = 壓鬱蓋壓構顧網壓繭襯 壓鏇夢構鏇鹹齋遞鬱鏇 (憲膚艱夢製簾窪繭壓糧, -176.8 ~ 60) | ||||||
临床4期 | - | 鬱願衊選鏇獵衊製獵簾(構獵構構鬱積鏇選齋願): 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) | 餘憲壓積餘夢範鏇廠遞 = 獵鹽淵蓋襯鹽廠蓋構廠 鹽壓製糧遞積夢積選選 (鑰窪廠廠鏇鹹簾艱憲窪, 觸獵襯艱衊顧鏇糧網鏇 ~ 衊蓋壓鑰鏇艱齋衊願願) 更多 | - | 2021-01-22 | ||
(PDE-5i) | 餘憲壓積餘夢範鏇廠遞 = 淵觸膚簾憲製簾觸選鹹 鹽壓製糧遞積夢積選選 (鑰窪廠廠鏇鹹簾艱憲窪, 願壓憲選鬱糧鹹膚選鑰 ~ 範製艱製選餘網憲網鏇) 更多 |
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