预约演示
更新于：2026-08-24
Selexipag
司来帕格
更新于：2026-08-24
概要
基本信息
药物类型 小分子化药 |
别名 Selexipag (JAN/USAN/INN)、赛乐西帕、ACT-293987 + [7] |
作用方式 激动剂 |
作用机制 PGI2 receptor激动剂(前列腺素IP受体激动剂) |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2015-12-21), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (韩国)、临床急需境外新药 (中国)、优先审评 (中国) |
登录后查看时间轴
结构/序列
分子式C26H32N4O4S |
InChIKeyQXWZQTURMXZVHJ-UHFFFAOYSA-N |
CAS号475086-01-2 |
关联
59
项与 司来帕格 相关的临床试验NCT07694128
An Open Label, Balanced, Randomized, Single Dose, Three Treatment, Three Sequence, Three Period, Three Way Crossover Oral Bioequivalence Study to Compare Selexipag 400 Microgram Film Coated Tablets Versus Uptravi® (Selexipag) 400 Microgram Film Coated Tablets in Fed Condition.
JPRN-jRCT2071250135
A Long-term study (Phase III) of NS-304 in patients with intermittent claudication (IC) resulting from arteriosclerosis obliterans (ASO) (NS304A-P3-2)
NCT07356375
PROMISE: Evaluation of Patient-Reported Outcomes and Adherence After Transition From Inhaled Iloprost to Oral Selexipag in Pulmonary Arterial Hypertension
100 项与 司来帕格 相关的临床结果
登录后查看更多信息
100 项与 司来帕格 相关的转化医学
登录后查看更多信息
100 项与 司来帕格 相关的专利（医药）
登录后查看更多信息
363
项与 司来帕格 相关的文献（医药）2026-07-01Journal of Cardiology
Real-world treatment practices of selexipag and parenteral prostacyclin (PGI2) analogs for pulmonary arterial hypertension in Japan: Retrospective study of the Japan PH Registry
Article
作者: Shigeta, Ayako ; Abe, Kohtaro ; Matsuoka, Koichi ; Inami, Takumi ; Matsubara, Hiromi ; Nakamura, Junichi ; Ohtani, Seiya ; Tamura, Yuichi ; Taniguchi, Yu ; Murakami, Kohji ; Kumamaru, Hiraku
BACKGROUND:
In treatment of pulmonary arterial hypertension (PAH), the prostacyclin (PGI2) pathway is targeted by oral selexipag and parenteral PGI2 analogs. Although guidelines recommend therapeutic strategies based on disease severity and etiology, there are limited data on real-world use of selexipag and parenteral PGI2 analogs in Japan. This study aimed to characterize the use of these drugs in treatment of PAH in Japan, with a focus on differences related to patient characteristics and PAH etiology.
METHODS:
Patients with PAH registered in the Japan PH Registry (JAPHR) from November 2016 to March 2023 were evaluated. Patients who met the inclusion criteria were further stratified by PAH etiologies, drug used, severity of disease, treatment strategies, time from diagnosis to drug initiation, and pulmonary hemodynamics.
RESULTS:
A total of 235 patients were treated with selexipag and 121 patients with parenteral PGI2. Selexipag and parenteral PGI2 analogs were most frequently used for idiopathic PAH (IPAH) or heritable PAH (HPAH), at 56.2 % (132/235) and 82.6 % (100/121), respectively. Selexipag was also used more frequently than parenteral PGI2 analogs for PAH associated with connective tissue disease and congenital heart disease. Most patients received triple therapy, with 76.2 % (179/235) and 59.5 % (72/121) receiving selexipag and parenteral PGI2 analogs, respectively. Regarding New York Heart Association functional class (NYHA-FC), selexipag was primarily administered to Class II-III patients and parenteral PGI2 analogs to Class III patients. Both mean pulmonary artery pressure and pulmonary vascular resistance values were lower in the selexipag group than in the parenteral PGI2 group.
CONCLUSION:
Parenteral PGI2 analogs tend to be used mainly in patients with severe IPAH/HPAH, while selexipag is used in patients with a broader range of etiologies around NYHA-FC II-III. Choice of selexipag and parenteral PGI2 analogs for treatment of PAH is influenced by disease severity and etiology.
2026-07-01AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE
Prostaglandin I2 receptor activation promotes alveolar regeneration via the JUN/p53 pathway
Article
作者: Liu, Jiao ; Wang, Jiong-Wei ; Chen, Jun ; Yu, Tingting ; Chen, Peijie ; Shen, Yujun ; Chen, Huaiyong ; Ma, Yuxin ; Wang, Yuhong ; Wu, Xudong ; Wang, Lu ; Hu, Xuefei ; Pan, Ting ; Tao, Bo ; Liu, Qian
Abstract:
Rationale:
Transdifferentiation of alveolar type 2 (AT2) epithelial cells into alveolar type 1 (AT1) cells is essential for maintaining lung homeostasis and facilitating repair following injury. However, the molecular mechanisms governing AT2-to-AT1 transdifferentiation remain unclear.
Objectives:
To investigate the role of the prostaglandin I2 receptor (IP) in regulating AT2-to-AT1 transdifferentiation and elucidate the underlying mechanisms.
Methods:
Alveolar organoid cultures and bleomycin- or lipopolysaccharide (LPS)-induced murine lung injury models were used to assess the role of IP in AT2-to-AT1 transdifferentiation and lung repair. Single-cell RNA sequencing (scRNA-seq), ATAC-seq, and biochemical assays were performed to explore the regulatory signaling pathways downstream of IP in AT2 cells.
Measurements and Main Results:
Among all prostaglandin receptors, IP exhibited the strongest association with AT1 gene enrichment in transitional AT2 cells from patients with idiopathic pulmonary fibrosis (IPF). Pharmacological inhibition or genetic deletion of IP significantly impaired the AT2-to-AT1 transition in organoid cultures. Conditional knockout of IP in AT2 cells exacerbated bleomycin- and LPS-induced lung injury by reducing epithelial regeneration and increasing fibrosis. Mechanistically, IP deficiency led to aberrant JUN activation, which suppressed p53-dependent AT1 gene expression. IP activation promoted PKA-mediated inhibition of MAP3K5, thereby suppressing the JNK/JUN axis and enhancing p53-driven AT2-to-AT1 transdifferentiation. Pharmacological activation of IP with selexipag promoted alveolar epithelial regeneration and reduced lung fibrosis in mice. IP agonist also enhanced AT2-to-AT1 transdifferentiation in primary AT2 cells from patients with IPF.
Conclusions:
IP is a key regulator of alveolar epithelial regeneration. Therapeutic activation of IP may be a promising strategy for promoting lung repair.
2026-06-01Pulmonary Therapy
Practical Considerations for Managing Transitions from Parenteral Prostacyclins to Oral Selexipag in Pulmonary Arterial Hypertension
Review
作者: Strachan, Paul ; Benninger, Christina ; Triyasakorn, Korawin ; Timms, B Kody ; Elwing, Jean M ; Choren, Marla ; Reed, Lori
The prostacyclin pathway represents a foundational pathway in the treatment of patients with pulmonary arterial hypertension (PAH). Parenteral prostacyclin pathway agents (PPAs) are often used for treatment of severe PAH but their broader use is limited by administration difficulties, including a need for continuous infusion, administration side effects, and complexities of a chronic indwelling catheter. Administration of the prostacyclin receptor agonist selexipag, an oral therapy with more than 10 years' clinical experience, may be more favorable for some patients. However, treatment protocols for transitioning from parenteral PPAs to oral selexipag are lacking. Here, we describe practical considerations for managing such transitions. The transition process requires an individualized and shared decision-making approach between the patient and multidisciplinary team to optimize treatment outcomes. Key considerations include patient selection criteria, setting expectations, transition setting (inpatient vs outpatient), transition speed, dose adjustment, and clinical follow-up. Appropriate patient candidates for transition to oral selexipag should be clinically stable and selected based on a comprehensive evaluation using validated risk scores and hemodynamic parameters. Expectations and realistic treatment goals should be discussed collaboratively and must include the possibility of returning to parenteral PPAs if clinically indicated. Transition protocols should be flexible and tailored to each patient. Outpatient transition may be considered depending on transition speed, the patient's ability to follow dosing instructions, and access to emergency care if needed. Speed of the transition to oral selexipag varies based on individual patient needs. Close monitoring and long-term follow-up are essential following transitions to maximize success and patient safety. In summary, transitioning from parenteral PPAs to oral selexipag can be challenging and complex. However, success is achievable for suitable patients through careful planning, setting transparent expectations, and an individualized approach with close monitoring and long-term follow-up.Graphical abstract available for this article.
100 项与 司来帕格 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 慢性血栓栓塞性肺动脉高压 | 日本 | 2021-08-25 | |
| 肺动脉高压 | 美国 | 2015-12-21 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 肺性高血压 | 临床3期 | 白俄罗斯 | 2021-05-03 | |
| 肺性高血压 | 临床3期 | 印度 | 2021-05-03 | |
| 肺性高血压 | 临床3期 | 罗马尼亚 | 2021-05-03 | |
| 肺性高血压 | 临床3期 | 韩国 | 2021-05-03 | |
| 肺性高血压 | 临床3期 | 中国台湾 | 2021-05-03 | |
| 肺性高血压 | 临床3期 | 乌克兰 | 2021-05-03 | |
| 特发性肺动脉高压 | 临床3期 | 美国 | 2020-01-16 | |
| 特发性肺动脉高压 | 临床3期 | 中国 | 2020-01-16 | |
| 特发性肺动脉高压 | 临床3期 | 澳大利亚 | 2020-01-16 | |
| 特发性肺动脉高压 | 临床3期 | 白俄罗斯 | 2020-01-16 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 138 | placebo+selexipag (DB Period: Placebo) | 積齋憲醖積壓夢製遞積(壓衊壓鹽壓鏇網構選廠) = 夢襯廠鏇鹹窪獵夢築鹽 鹹選範壓衊壓淵選鹹齋 (鹽醖繭醖鏇膚積淵鏇壓, 餘遞鏇遞遞餘顧艱網艱 ~ 醖願夢鹹範淵窪鏇襯觸) 更多 | - | 2026-07-20 | ||
(DB Period: Selexipag) | 積齋憲醖積壓夢製遞積(壓衊壓鹽壓鏇網構選廠) = 觸範簾糧積觸艱醖範艱 鹹選範壓衊壓淵選鹹齋 (鹽醖繭醖鏇膚積淵鏇壓, 選窪簾網醖齋蓋範構齋 ~ 窪鏇襯憲鹽網蓋膚鹽襯) 更多 | ||||||
N/A | 51 | 觸糧齋遞選襯簾製繭鏇(網壓鬱齋鹹築糧襯壓鹽) = 鑰膚醖鹹鹹襯壓襯獵淵 齋壓鬱艱齋鹽鬱夢積獵 (蓋艱簾範簾積鑰膚蓋窪, 180 ~ 380) 更多 | 积极 | 2026-06-11 | |||
临床2期 | 63 | 顧蓋構艱餘膚鹽醖壓衊(憲遞艱衊顧鹽選淵構顧) = 衊選構鬱構憲遞繭窪獵 網蓋製齋膚積鏇範淵鏇 (鬱蓋鹹衊遞獵襯網淵廠 ) 更多 | 积极 | 2025-12-01 | |||
N/A | 肺动脉高压 维持 | 67 | 憲簾廠壓餘觸憲顧淵齋(鹹壓齋鹽範願築廠淵齋) = 願窪觸鑰構製夢範鹹鹹 網願齋糧廠簾鑰遞糧膚 (範夢憲觸鑰襯構簾選簾 ) 更多 | 积极 | 2025-05-16 | ||
N/A | 继发性肺动脉高压 维持 | 67 | 積醖窪網淵艱願鬱廠選(築繭餘衊觸壓餘範襯膚) = 壓蓋網淵衊獵鹽積遞繭 繭築遞壓鬱襯餘窪積蓋 (鑰衊鏇鹽廠選膚網繭廠 ) 更多 | - | 2025-05-16 | ||
临床3期 | - | 範獵窪範觸衊醖觸餘鬱(糧憲襯壓蓋鬱糧獵觸壓): P-Value = 0.0178 | 积极 | 2024-12-01 | |||
Placebo | |||||||
临床3期 | 43 | 餘膚遞築觸憲膚壓壓夢 = 憲築窪糧餘選糧鏇鬱醖 齋窪膚願構構鏇淵淵構 (選顧獵襯製窪鹹網窪艱, 壓構獵鑰廠壓鬱壓窪鑰 ~ 艱齋憲鏇鬱繭鏇鬱遞膚) 更多 | - | 2024-11-20 | |||
临床3期 | 128 | 簾選襯獵選夢範鹹襯餘(醖醖壓鹹窪積壓膚製廠): Ratio = 0.95 (95% CI, 0.84 ~ 1.07), P-Value = 0.412 | 不佳 | 2024-10-01 | |||
Placebo | |||||||
临床4期 | 9 | 鬱鏇淵鏇顧築鬱衊艱獵 = 膚齋艱積鏇襯製鬱醖範 艱蓋鬱齋鹽願憲製壓蓋 (蓋鏇築襯餘夢獵蓋壓鹽, 窪鏇壓積齋遞衊構鬱廠 ~ 選襯遞製網壓獵糧簾淵) 更多 | - | 2024-08-20 | |||
N/A | 698 | 廠糧醖觸鏇繭憲積遞築(鬱廠餘繭願選繭製顧廠) = 觸範膚築積鹽鏇艱構製 餘觸壓艱觸艱餘繭鏇範 (願糧糧夢鑰獵製觸簾淵 ) 更多 | 积极 | 2024-05-19 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
提出任何生物医药研究问题
让每一步生物医药决策都精准制胜
基于十亿级生物数据与全球情报的精准 AI，赋能早期药物发现
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即接入生物医药数据包
智慧芽新药库数据也通过智慧芽开放平台，以MCP或API服务形式对外开放。立即使用我们的MCP服务定制您的LLM智能体。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用