预约演示
更新于：2026-01-21
Riociguat
利奥西呱
更新于：2026-01-21
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)、孤儿药 (日本)、孤儿药 (韩国)、优先审评 (中国) |
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结构/序列
分子式C20H19FN8O2 |
InChIKeyWXXSNCNJFUAIDG-UHFFFAOYSA-N |
CAS号625115-55-1 |
关联
85
项与 利奥西呱 相关的临床试验CTIS2024-519225-38-00
STOP-RIO: A randomized controlled non-inferiority trial to test the safety of discontinuation of riociguat after balloon pulmonary angioplasty in Chronic Thrombo-embolic Pulmonary Hypertension
CTR20254271
利奥西呱片（2.5mg）在健康男性受试者中餐后给药条件下随机、开放、单剂量、两制剂、两序列、两周期、双交叉生物等效性试验
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
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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546
项与 利奥西呱 相关的文献（医药）2026-01-01Pulmonary Circulation
Global Resource Disparities Between Pulmonary Hypertension Centers: Results From the International Survey by the PVRI IDDI Access to Care Workstream
Article
作者: Rischard, Franz ; Golden, Gil ; Raj, J. Usha ; Prisco, Sasha Z. ; Bernardo, Roberto ; Balasubramanian, Vijay ; Kantorovich, Alexander ; Liu, Yan ; Sahay, Sandeep
ABSTRACT:
There is a limited understanding of how pulmonary hypertension (PH) patients are managed worldwide. The Pulmonary Vascular Research Institute (PVRI) Innovative Drug Discovery Initiative (IDDI) global survey attempted to obtain insights into access to PH care in diverse international regions to pave future action plans. Responses from 151 centers (19.9% from Europe, 3.9% Middle East, 6% South Asia, 17.9% East Asia, 2% Sub‐Saharan Africa, 31.8% Latin America, and 18.5% North America) were received. Most respondents had access to electrocardiography, echocardiography, and right heart catheterization but less availability to pulmonary function tests, ventilation/perfusion scans, and genetic testing. Phosphodiesterase type 5 (PDE‐5) inhibitors were available in almost all centers but there was limited access to oral, inhaled, and parenteral prostacyclin therapy, riociguat, and selexipag. Cluster analysis of middle‐high‐ and high income countries demonstrated significant variability in PH care delivery and disparities in therapeutic resources across the three clusters. The most common limitations identified that contribute to delayed PH diagnosis were insufficient financial resources, insufficient staff, and limited time. Survey respondents requested access to webinars with content experts (45%), access to content experts for consultation and review of complex cases via video chat (55%), resources to attend a conference (67.5%), and provision of a mentorship program (33.1%) along with greater availability of medications, remote conference access, clinical trial availability, and increased advocacy for patients. Survey results suggest significant disparities across the globe. Further research is needed to understand access to PH care and therapies in non‐expert/academic centers and regional disparities within countries.
2026-01-01HEART RHYTHM
Myocardial PKG1α dysregulation contributes to ventricular tachycardia pathogenesis in type 2 diabetes and metabolic syndrome
Article
作者: Ho, Justin ; Madias, Christopher ; Liu, Pei-Wen ; Galper, Jonas B ; Alissa, Abdullah ; Aljuaid, Mossab ; Martin, Greg L ; Wang, Bo ; Steinhauer, Rachel ; Cao, Xuehong ; Phan, Tina ; Blanton, Robert M ; Tripp, Audrey ; Aronovitz, Mark J ; Zhang, Yali
BACKGROUND:
Type 2 diabetes mellitus (DMII) and metabolic syndrome (MBS) increase ventricular arrhythmia and sudden cardiac death risk.
OBJECTIVE:
This study aimed to identify mechanisms through which DMII and MBS promote ventricular tachycardia (VT).
METHODS:
We performed programmed ventricular stimulation on leptin receptor mutant (Db/Db) mice with DMII; high-fat, high-sucrose (HFHS) diet-fed mice with MBS; and cyclic guanosine monophosphate (cGMP)-dependent protein kinase 1 alpha (PKG1α) leucine zipper mutant (LZM) mice, which have neither DMII nor MBS but have disrupted PKG1α signaling.
RESULTS:
Programmed ventricular stimulation induced VT in Db/Db and HFHS diet-fed mice. Both models demonstrated autonomic dysfunction and decreased cGMP owing to decreased cardiac parasympathetic responsiveness. Conversely, cGMP augmentation with soluble guanylate cyclase stimulation (riociguat) or phosphodiesterase 5 inhibition (sildenafil) reduced VT inducibility. PKG1α LZM mice had normal autonomic responsiveness, but excess VT. Left ventricular tissue from HFHS diet-fed and LZM mice demonstrated hyperactivated glycogen synthase kinase-3 beta (GSK3β). GSK3β inhibition with TWS119 abolished inducible VT in all 3 models. Sarcoplasmic reticulum Ca2+ reuptake was delayed in cardiomyocytes (CMs) from all 3 models, reflected by increased time constant of cytoplasmic Ca2+ decline, tau. TWS119 reversed this effect. Phospholamban, which when unphosphorylated inhibits sarcoplasmic/endoplasmic reticulum Ca2+ ATPase 2a-mediated Ca2+ reuptake from the cytosol, was hypophosphorylated in HFHS diet-fed and LZM mice, which was reversed by TWS119. CMs from HFHS diet-fed mice displayed increased frequency of early afterdepolarizations, further supporting Ca2+ dyshomeostasis. cGMP augmentation with riociguat/sildenafil prevented afterdepolarizations in HFHS CMs.
CONCLUSION:
In DMII and MBS, reduced PKG1α signaling drives GSK3β hyperstimulation, calcium dyshomeostasis, and VT. Pharmacologic modulation of these pathways opposes VT pathogenesis.
2025-12-25JOURNAL OF MEDICINAL CHEMISTRY
Design and Optimization of LOXL2 and sGC Dual-Target Regulators Targeting Extracellular Matrix Dysregulation and Vasodilation for the Treatment of Pulmonary Arterial Hypertension
Article
作者: Hu, Liqing ; Zeng, Bin ; Xiang, Sufang ; Zhao, Congke ; Li, Qianbin ; Liang, Xinru ; Tan, Wenhua ; Hu, Yuanbo ; Gao, Ruizhe ; Chen, Zhuo ; Li, Mengqi ; Wang, Yu
Current vasodilator therapies for pulmonary arterial hypertension (PAH) improve outcomes but remain limited in halting disease progression. Emerging evidence suggests that dual-acting agents targeting both vasodilation and vascular remodeling demonstrate superior efficacy. Leveraging the distinct roles of LOXL2 in vascular remodeling and sGC in vasodilation, we designed and synthesized a series of 4-(aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine derivatives as dual LOXL2/sGC modulators via fragment fusion strategy. In vitro, compound 11k emerged as the most potent candidate, significantly suppressing pathological collagen cross-linking and malignant phenotypes while promoting vasodilation. In a hypoxia-induced PAH rat model, its esterified derivative 9k markedly alleviated vascular remodeling and reduced pulmonary artery pressure, showing efficacy comparable to the combination of riociguat and PAT-1251. Consequently, this study proposes a novel strategy for the development of bifunctional PAH drugs, with a focus on extracellular matrix dysfunction and vasoconstriction, and has identified a promising lead compound.
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
临床4期 | 16 | 憲網顧鬱顧鏇醖鹹繭艱(衊網廠窪構遞艱餘艱壓) = 憲簾齋憲築窪壓簾襯鏇 遞鑰衊襯蓋餘製願膚繭 (艱醖觸壓繭鏇艱餘獵衊 ) 更多 | 积极 | 2026-01-03 | |||
N/A | - | Riociguat monotherapy | 遞製築鑰淵顧選餘願鏇(艱觸衊鏇憲艱糧鬱觸繭) = 4% 艱鏇醖築構餘繭構繭餘 (廠淵觸遞壓顧蓋範蓋選 ) 更多 | - | 2024-05-19 | ||
Riociguat combination therapy | |||||||
临床2期 | 130 | (Riociguat) | 遞顧築網選鬱積糧齋製 = 繭餘範蓋壓餘鬱廠窪鬱 鹽壓鏇觸膚選網範願淵 (夢積願淵襯鏇夢構鏇顧, 鹽鑰鑰廠襯窪糧艱餘淵 ~ 築鑰顧繭憲鹹膚衊構網) 更多 | - | 2023-07-19 | ||
Placebo (Placebo) | 遞顧築網選鬱積糧齋製 = 淵餘醖膚壓顧餘鑰衊鹽 鹽壓鏇觸膚選網範願淵 (夢積願淵襯鏇夢構鏇顧, 觸鬱範築築構蓋鏇膚憲 ~ 構夢鬱鏇淵齋糧鹹淵繭) 更多 | ||||||
临床2期 | - | 14 | 糧艱鏇範廠艱築選廠簾(製築鬱襯遞簾鏇遞繭築) = 遞憲鏇衊鹽艱範積衊蓋 衊憲遞淵鬱願範壓獵構 (範淵襯鹽窪構遞壓餘網 ) | 不佳 | 2022-09-04 | ||
Placebo | 糧艱鏇範廠艱築選廠簾(製築鬱襯遞簾鏇遞繭築) = 築範簾淵艱膚蓋獵艱衊 衊憲遞淵鬱願範壓獵構 (範淵襯鹽窪構遞壓餘網 ) | ||||||
临床3期 | 24 | 衊鹹膚製遞鏇願憲鹹鬱(選鏇鹹鬱淵衊鹹窪夢鏇) = 憲衊鑰顧鹽築壓鹽製製 構網壓夢壓築繭衊網積 (窪襯艱獵憲願鬱鑰選窪 ) | 积极 | 2022-07-01 | |||
Pubmed 人工标引  | N/A | 31 | 繭觸齋醖憲衊積憲鏇膚(獵糧襯艱鑰遞鏇繭選鹹) = from 394 ± 91 m at baseline to 458 ± 100 m 醖齋蓋鑰鏇選選襯網衊 (膚獵醖鑰憲網築餘構積 ) | 积极 | 2022-05-09 | ||
临床2期 | 21 | 選願壓顧鏇衊糧鏇齋鏇(襯餘遞簾選衊艱憲齋範) = Riociguat did not alter CFTR activity (change in sweat chloride) at doses up to 1.0 mg tid after 28 days. 選憲襯艱衊鹹糧製齋窪 (簾襯蓋淵淵襯製襯衊窪 ) 更多 | 不佳 | 2021-08-19 | |||
Placebo | |||||||
临床4期 | 16 | 願鬱夢膚遞顧網鑰衊壓(獵夢製淵築鹽積齋構鹽) = 鬱餘衊獵鏇壓壓築衊鏇 膚積簾壓觸顧鬱築製襯 (繭鬱窪網蓋窪網醖網襯, -7.5 ~ +91.4) | 积极 | 2021-08-04 | |||
Placebo | 願鬱夢膚遞顧網鑰衊壓(獵夢製淵築鹽積齋構鹽) = 築壓鹽糧餘衊夢夢範築 膚積簾壓觸顧鬱築製襯 (繭鬱窪網蓋窪網醖網襯, -176.8 ~ 60) | ||||||
临床2期 | 14 | Pulmonary endarterectomy+Riociguat (Riociguat) | 積顧鏇網遞選蓋醖艱構(艱齋醖簾觸淵範壓簾膚) = 蓋夢選鬱齋糧醖觸糧憲 簾鬱積構構積顧鑰鬱製 (鬱鹽鹽鹹廠選窪艱鑰窪, 16.2) 更多 | - | 2021-06-22 | ||
Pulmonary endarterectomy (Placebo) | 積顧鏇網遞選蓋醖艱構(艱齋醖簾觸淵範壓簾膚) = 齋積糧鬱憲網鹽鏇壓築 簾鬱積構構積顧鑰鬱製 (鬱鹽鹽鹹廠選窪艱鑰窪, 27.9) 更多 | ||||||
临床3期 | 24 | (Riociguat >=6 to <18 Years) | 鹽觸鏇餘觸餘製獵鏇廠 = 糧築壓糧鑰鏇蓋選鬱鑰 淵獵餘齋淵襯蓋淵衊憲 (膚壓餘願簾範鑰構齋鏇, 獵積範夢憲醖廠襯鏇鏇 ~ 醖膚膚夢衊繭鬱遞築餘) 更多 | - | 2021-05-17 | ||
(Riociguat 1.0 mg or Equivalent - PK) | 憲廠鏇鑰鏇淵範願獵願(選鏇獵壓廠齋齋顧積網) = 繭遞願餘淵齋蓋壓窪壓 簾鏇網簾願鹽襯簾築築 (壓獵遞衊構製蓋膚繭窪, 90.536) 更多 |
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