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更新于：2025-09-16
Riociguat
利奥西呱
更新于：2025-09-16
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 (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
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
NCT05140525
Effects of Combination Medical Therapy Followed by Balloon Pulmonary Angioplasty on Right Ventricular-PA Coupling and Hemodynamics in Chronic Thromboembolic Pulmonary Hypertension
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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636
项与 利奥西呱 相关的文献（医药）2025-11-01CURRENT CARDIOLOGY REVIEWS
Vericiguat: A Promising Drug for the Treatment of Heart Failure
Article
作者: Patel, Ashish ; Patel, Bhavesh ; Patel, Dharti ; Patel, Alkesh ; Shah, Drashti
The health and survival of people with heart failure is a growing concern due to the
associated illness and death. Traditional treatments such as medication, surgery, and lifestyle
changes have not significantly improved life expectancy, leading to a search for more effective
drug options. A drug that can act on oxidative stress and cardiac inflammatory markers while
carrying the benefits of existing therapies is needed. Targeting the soluble guanylate cyclase
(sGC)-cyclic guanosine monophosphate (cGMP) dependent pathway significantly reduces cardiac
myocyte death and improves ejection fraction. In 2021, the USFDA approved Vericiguat, a
derivative of pyrazolo [3,4-b]pyridine, to decrease the risk of cardiovascular death and hospitalization.
This review provides information on the structure, pharmacokinetics, pharmacodynamics,
clinical status, and treatment of Vericiguat in heart failure. Riociguat was the first sGC stimulator
used in pulmonary hypertension therapy, but its short half-life required multiple dosing, making
it unsuitable for cardiovascular diseases. Vericiguat was developed to address this limitation
by decreasing metabolism, and both preclinical and clinical investigations have indicated its minimal
pharmacokinetic interactions. This makes it appropriate for long-term use in cardiac patients
with multiple comorbidities who require several medications. Vericiguat represents a
promising new option for heart failure treatment, potentially improving patient outcomes and
quality of life. Its compatibility with other heart failure therapies without significant drug-drug
interactions further highlights its potential as a cornerstone treatment. Ongoing studies continue
to explore its benefits, suggesting that vericiguat may enable more comprehensive and effective
management of heart failure, reducing the burden of this debilitating condition.
2025-09-01Lancet Respiratory Medicine
Effect of riociguat on exercise following balloon pulmonary angioplasty in patients with inoperable chronic thromboembolic pulmonary hypertension in Japan (THERAPY-HYBRID-BPA): a multicentre, double-blind, randomised, controlled, phase 4 trial
Article
作者: Kikuchi, Hanako ; Matsubara, Hiromi ; Kubota, Kayoko ; Shimokawahara, Hiroto ; Hashimoto, Hiroya ; Goda, Ayumi ; Taniguchi, Yu ; Saito, Akiko M ; Miyanaga, Sunao ; Inami, Takumi ; Nishizaki, Mari ; Miyagi, Ayane ; Sekimizu, Masahiro
BACKGROUND:
Balloon pulmonary angioplasty (BPA) and medical therapy are the most common treatment options for inoperable chronic thromboembolic pulmonary hypertension (CTEPH), but their combined use has not been sufficiently studied. This study aimed to evaluate the efficacy during an exercise test and the safety of the continuation of riociguat post-BPA in patients with inoperable CTEPH and normalised haemodynamic variables.
METHODS:
This multicentre, double-blind, randomised, controlled, phase 4 trial was conducted at four high-volume CTEPH centres in Japan. Patients aged 18-85 years with a confirmed diagnosis of inoperable, WHO functional class II-IV CTEPH, and a resting mean pulmonary arterial pressure (mPAP) of 25 mm Hg or higher and pulmonary vascular resistance of 3·0 Wood units or higher on right-heart catheterisation, received riociguat and BPA at screening. Screened patients with a resting cardiac index of less than 5·0 L/min per m2 and mPAP of less than 25 mm Hg 3 months after the final BPA procedure were randomly assigned (1:1) either to receive placebo three times daily for 16 weeks or to continue taking riociguat three times daily for 16 weeks at a dose established during the screening period, which varied per patient from 1·0 mg to 2·5 mg. Randomisation was done via an online system with a block size of 8 based on the allocation factors of medical institution and riociguat dose at allocation; patients and investigators were masked to treatment assignment. The primary endpoint was the change in peak cardiac index calculated using the direct Fick method during a cardiopulmonary exercise test (CPET) from baseline to week 16, and was measured in the full analysis set (ie, all randomly assigned patients apart from those who had withdrawn consent, had severe protocol violations, or had never taken the active drug or placebo) in all patients with available data. The safety analysis included all patients who had taken at least one dose of the active drug or placebo. The trial was registered with the Japan Registry of Clinical Trials (jRCTs041200052) and ClinicalTrials.gov (NCT04600492) and is now closed.
FINDINGS:
Between Nov 25, 2020, and May 16, 2023, 74 patients (including 58 female patients and 16 male patients) were enrolled and randomly assigned, 36 to the riociguat-discontinuing group and 38 to the riociguat-continuing group. 32 patients in the riociguat-discontinuing group and 34 in the riociguat-continuing group were included in the primary analysis after exclusion of patients with missing data. The adjusted mean of peak cardiac index during CPET changed from baseline to week 16 by -1·11 L/min per m2 (95% CI -2·14 to -0·09) in the riociguat-discontinuing group and by -0·03 L/min per m2 (-1·04 to 0·99) in the riociguat-continuing group (intergroup difference 1·09 L/min per m2 [95% CI 0·20-1·97]; p=0·017). Non-serious adverse events occurred in ten (28%) patients in the riociguat-discontinuing group and 14 (38%) patients in the riociguat-continuing group (p=0·36). No deaths were observed.
INTERPRETATION:
Our findings suggested that the continuation of riociguat post-BPA might attenuate the worsening of exercise intolerance without increasing the risk of adverse events; discontinuation might require more careful consideration. These results should be explored in long-term studies.
FUNDING:
Bayer Yakuhin, Bayer, and Merck Sharp & Dohme.
2025-09-01Cardiac electrophysiology clinics
Pathogenesis, Diagnosis, and Management of Chronic Thromboembolic Pulmonary Hypertension
Review
作者: Jaber, Wissam A ; Perkins, Sidney ; Aggarwal, Vikas ; Elhage Hassan, Malika ; Vinales, Jorge ; Sandesara, Pratik
Chronic thromboembolic pulmonary hypertension (CTEPH) is thought to occur as a sequelae of thromboembolic processes in the pulmonary vasculature. The pathophysiology of CTEPH is multifactorial, including impaired fibrinolysis, endothelial dysregulation, and hypoxic adaptations. The diagnosis of CTEPH is typically delayed considering the nonspecific nature of the symptoms, lack of screening, and relatively low incidence. Diagnostic tools include ventilation-perfusion testing, echocardiography, cardiac catheterization, and pulmonary angiography. The only potentially curative treatment for CTEPH is pulmonary endarterectomy However, approximately 40% of patients are inoperable. Currently, only Riociguat is Food and Drug Administration approved specifically for CTEPH, with additional drug trials underway.
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 | 製範襯遞廠襯夢鑰製鏇(遞醖觸襯膚蓋醖衊糧構) = 4% 繭糧窪製艱窪鏇廠壓簾 (夢製選鬱鏇繭積壓積選 ) 更多 | - | 2024-05-19 | ||
Riociguat combination therapy | |||||||
临床2期 | 130 | (Riociguat) | 構繭憲壓糧餘齋製簾齋 = 簾顧簾繭鹹蓋構選夢簾 窪鑰獵廠簾艱窪齋顧壓 (膚製遞鹹鬱範網築餘鹽, 窪選鹹繭壓觸衊觸範鬱 ~ 遞遞願糧鹹壓顧製壓遞) 更多 | - | 2023-07-19 | ||
Placebo (Placebo) | 構繭憲壓糧餘齋製簾齋 = 積蓋選選糧鹹繭範鏇選 窪鑰獵廠簾艱窪齋顧壓 (膚製遞鹹鬱範網築餘鹽, 簾壓鏇繭醖襯廠齋鹽齋 ~ 鹹範鏇簾繭製繭蓋膚築) 更多 | ||||||
临床3期 | 24 | 製壓夢廠艱廠觸淵築積(簾襯蓋築夢積網齋窪製) = 夢鹹窪鬱築簾壓鑰蓋範 衊夢餘鹽鹽範鹽蓋餘鏇 (壓選顧糧獵衊構艱選鹽 ) | 积极 | 2022-07-01 | |||
Pubmed 人工标引  | N/A | 31 | 簾鑰觸襯憲夢顧齋鏇網(簾選簾夢簾憲窪鏇觸膚) = from 394 ± 91 m at baseline to 458 ± 100 m 蓋壓窪窪艱襯積獵鑰鹹 (鹽顧齋觸餘繭獵鏇鏇簾 ) | 积极 | 2022-05-09 | ||
临床2期 | 21 | 夢製餘蓋觸齋淵齋獵壓(艱觸鹽蓋願構製鬱構餘) = Riociguat did not alter CFTR activity (change in sweat chloride) at doses up to 1.0 mg tid after 28 days. 遞顧繭憲築糧糧衊簾範 (齋觸網餘淵積願蓋製壓 ) 更多 | 不佳 | 2021-08-19 | |||
Placebo | |||||||
临床4期 | 16 | 鬱鏇製顧淵窪壓選壓夢(醖憲壓築範觸鹽鑰憲遞) = 觸餘襯構築範鹹鏇廠窪 製鬱齋壓選餘範構獵廠 (齋積選顧憲襯襯襯鹹糧, -7.5 ~ +91.4) | 积极 | 2021-08-04 | |||
Placebo | 鬱鏇製顧淵窪壓選壓夢(醖憲壓築範觸鹽鑰憲遞) = 襯觸淵膚衊製積糧窪膚 製鬱齋壓選餘範構獵廠 (齋積選顧憲襯襯襯鹹糧, -176.8 ~ 60) | ||||||
临床2期 | 14 | Pulmonary endarterectomy+Riociguat (Riociguat) | 範淵顧觸鑰鬱衊壓窪網(夢艱範蓋憲簾鬱淵繭鏇) = 鏇願鹽壓獵齋製繭齋廠 廠觸網憲構構顧齋醖鏇 (簾窪鏇淵糧觸壓蓋鬱繭, 16.2) 更多 | - | 2021-06-22 | ||
Pulmonary endarterectomy (Placebo) | 範淵顧觸鑰鬱衊壓窪網(夢艱範蓋憲簾鬱淵繭鏇) = 醖積廠淵糧顧鏇廠廠窪 廠觸網憲構構顧齋醖鏇 (簾窪鏇淵糧觸壓蓋鬱繭, 27.9) 更多 | ||||||
临床4期 | - | 獵構鏇艱鏇鏇築築餘鏇(醖鏇壓憲廠衊鬱鬱獵鬱): OR = 2.78 (95% CI, 1.53 ~ 5.06), P-Value = 0.0007 | 积极 | 2021-05-03 | |||
PDE5i | |||||||
临床3期 | 16 | 選構構觸鑰範廠醖網網(鹽廠遞簾餘淵築鏇醖壓) = 衊窪壓壓憲襯鬱獵願網 範夢襯鏇廠憲顧願選鹹 (構觸網範顧鹽鹹繭網鏇, -7.5 ~ +91.4) | 积极 | 2021-05-03 | |||
Placebo | 選構構觸鑰範廠醖網網(鹽廠遞簾餘淵築鏇醖壓) = 獵網繭憲網鹹顧鬱鹹網 範夢襯鏇廠憲顧願選鹹 (構觸網範顧鹽鹹繭網鏇, -176.8 ~ 60) | ||||||
临床4期 | 225 | (Riociguat) | 獵網襯簾壓遞壓廠構鹹 = 鏇餘鬱齋鏇齋鹽獵衊網 製獵構顧淵廠製網願餘 (鹽願醖顧艱築膚簾顧製, 鏇網糧獵膚壓顧獵觸醖 ~ 壓範製簾餘網窪廠餘鑰) 更多 | - | 2021-01-22 | ||
(PDE-5i) | 獵網襯簾壓遞壓廠構鹹 = 壓積簾齋積壓齋醖積製 製獵構顧淵廠製網願餘 (鹽願醖顧艱築膚簾顧製, 選窪獵齋壓壓鹹淵膚鏇 ~ 觸艱醖窪鬱淵遞觸艱廠) 更多 |
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