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更新于：2025-02-20
Cilostazol
西洛他唑
更新于：2025-02-20
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 中国 (1996-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C20H27N5O2 |
InChIKeyRRGUKTPIGVIEKM-UHFFFAOYSA-N |
CAS号73963-72-1 |
关联
214
项与 西洛他唑 相关的临床试验NCT06757764
The Effect and Safety of Therapy Adding Cilostazol in Acute Ischemic Stroke Due to Large Artery Atherosclerosis: CHANGE Trial
ISRCTN44436843
The LACunar Intervention Trial 3 (LACI-3). Assessment of efficacy and safety of cilostazol and isosorbide mononitrate to prevent adverse outcomes in patients with cerebral small vessel disease (lacunar) ischaemic stroke.
NCT06715007
Antiplatelet Therapy and Endothelial-stabilizing Agents in Cerebral Small Vessel Diseases
100 项与 西洛他唑 相关的临床结果
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100 项与 西洛他唑 相关的转化医学
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100 项与 西洛他唑 相关的专利（医药）
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3,068
项与 西洛他唑 相关的文献（医药）2025-03-01American Journal of Cardiovascular Drugs
Pharmacokinetic Drug–Drug Interaction between Cilostazol and Rosuvastatin in Healthy Participants
Article
作者: Kim, Dong Ho ; Lee, Hye Jung ; Jung, Won Tae ; Hong, Jang Hee ; Jung, Jin-Gyu ; Moon, JungHa ; Roh, Jae Seok ; Sunwoo, Jung ; Nam, Kyu-Yeol ; Kim, Kyu Yeon
BACKGROUND AND OBJECTIVES:
Cilostazol improves ischemic symptoms and prevents recurrence following cerebral infarction, and rosuvastatin reduces cholesterol levels. However, no reports exist on the pharmacokinetic interactions between these two drugs in healthy adults. This study evaluated the pharmacokinetic (PK) interactions and safety of cilostazol and rosuvastatin when co-administered to healthy male participants.
METHODS:
A randomized, open-label, multiple-dosing, two-arm, two-period study was conducted. Arm A had 30 participants receiving 200 mg cilostazol daily and arm B had 27 participants receiving 20 mg rosuvastatin daily for 7 days. In period 2, both arms received a combination of 200 mg cilostazol and 20 mg rosuvastatin daily for 7 days following a 7-day washout period. Plasma concentrations of cilostazol, its metabolites, and rosuvastatin were quantified using liquid chromatography-tandem mass spectrometry.
RESULTS:
Fifty-seven participants were randomized, and 44 completed the study. The geometric mean ratio (GMR) and 90% confidence intervals (CI) for maximum plasma concentration at steady state (Cmax,ss) and area under the plasma concentration-time curve during the dosing interval at steady state (AUCtau,ss) indicated no significant interaction between cilostazol and rosuvastatin. Safety assessments showed comparable profiles to individual drug administration, with no significant adverse events.
CONCLUSION:
The repeated co-administration of cilostazol and rosuvastatin in healthy male participants resulted in minor PK interactions and exhibited a safety and tolerability profile similar to those of the individual drugs. This suggested that the combined regimen is well tolerated and does not necessitate dose adjustments.
REGISTRATION:
ClinicalTrials.Gov identifier no. NCT06568133.
2025-02-01NATURAL PRODUCT RESEARCH
Natural 3,4-dihydro-2(1
H
)-quinolinones- Part I: plant sources
Review
作者: Marles, Robin J. ; Khadem, Shahriar
While natural products have undoubtedly played a pivotal role in drug discovery, their potential as lead compounds has been hindered by challenges such as limited accessibility and complex synthesis processes. At the core of numerous natural and synthetic compounds, each exhibiting remarkable biological traits, lies the foundational structure of 3,4-dihydro-2(1H)-quinolinone, also known as 2-oxo-tetrahydroquinoline (2 O-THQ). This article extensively examines the occurrence of 2 O-THQ alkaloids across the plant kingdom, exploring their capacity to serve as a source for innovative bioactive natural products. Despite the undeniable significance of these compounds, the existing body of review literature has yet to provide comprehensive coverage, underscoring the pivotal contribution of this present article in investigating their prevalence in nature.
2025-02-01BRAIN RESEARCH BULLETIN
Inhibition of platelet activation alleviates diabetes-associated cognitive dysfunction via attenuating blood-brain barrier injury
Article
作者: Jiang, Shiqiu ; Yang, Lan ; Zhu, Yaomin ; Hu, Juan ; Gao, Wei ; Wang, Ruiduo ; Jiang, Tao ; Li, Xuying ; Cheng, Bo ; Xu, Fuxing ; Deng, Yingying ; Li, Yansong ; Du, Hailiang
Cognitive dysfunction has become the second leading cause of death among the diabetic patients. In pre-diabetic stage, blood-brain barrier (BBB) injury occurs and induced the microvascular complications of diabetes, especially, diabetes-associated cognitive dysfunction (DACD). Endothelial cells are the major component of BBB, on which the increased expression of CD40 could mediate BBB dysfunction in diabetics. Since platelets play an important role in regulating endothelial cell barrier function and over 95 % of the circulating soluble CD40 ligand (sCD40L) is derived from activated platelets, we speculated that the release of CD40L from activated platelets induced by diabetes was the key mechanism that aggravated BBB injury and leaded to DACD. We performed inhibition of platelet activation on diabetic and non-diabetic mice, with or without cilostazol treatment, and then compared cognitive function, platelet activation, BBB structure and permeability. In vitro, mouse brain microvascular endothelial cell line (b.End3) were exposed to CD40L for 24 h at 5.5 mM or 30 mM glucose media after silencing CD40 and HIF1α or not to investigate the effects of CD40 on BBB disruption and the underlying molecular pathways. Inhibition of platelet activation improved cognitive behaviors in diabetic mice, accompanied with reduced BBB permeability, increased tight junction proteins, balanced Aβ transporters, as well as attenuated Aβ deposition and hippocampal neurons damage. In vitro, CD40L increased HIF1α, diminished tight junction proteins and dysregulated Aβ transporters in b.End3 cells, which could be restored by CD40 siRNA and HIF1α siRNA. Hence, inhibition of platelet activation ameliorates DACD via alleviating BBB injury, which involving the regulation of CD40L-CD40-HIF1α signaling pathway. Our study may demonstrate a potential therapeutic target for the treatment of DACD.
100 项与 西洛他唑 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 |
|---|---|---|---|
| 脑梗塞 | 日本 | 2007-03-15 | |
| 间歇性跛行 | 美国 | 1999-01-15 | |
| 动脉闭塞性疾病 | 中国 | 1996-01-01 |
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 |
|---|---|---|---|---|
| 变异型心绞痛 | 临床3期 | 韩国 | 2013-11-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 631 | 糧鏇積夢鏇醖壓鹽簾憲(憲廠積襯築齋築鏇齋齋) = 顧壓窪艱選夢餘遞壓遞 構廠顧觸糧觸餘艱餘繭 (窪艱顧鏇積夢願顧鏇願 ) 更多 | 积极 | 2024-12-01 | |||
No Cilostazol | 糧鏇積夢鏇醖壓鹽簾憲(憲廠積襯築齋築鏇齋齋) = 鏇艱糧簾簾壓網遞夢襯 構廠顧觸糧觸餘艱餘繭 (窪艱顧鏇積夢願顧鏇願 ) 更多 | ||||||
临床2/3期 | 363 | (Isosorbide Mononitrate XL (ISMN)) | 網艱鏇糧範顧餘夢艱簾(夢鹽鬱鹽廠餘願鹹鏇鬱) = 淵糧鏇壓願餘鑰夢壓蓋 簾網醖積選鏇築廠顧鬱 (鹹糧夢餘醖鏇艱構構鹹, 醖憲膚蓋襯範醖觸廠觸 ~ 醖範淵憲願鹹鹽醖膚遞) 更多 | - | 2024-11-12 | ||
(Cilostazol) | 網艱鏇糧範顧餘夢艱簾(夢鹽鬱鹽廠餘願鹹鏇鬱) = 觸觸鏇蓋艱憲簾廠蓋鹽 簾網醖積選鏇築廠顧鬱 (鹹糧夢餘醖鏇艱構構鹹, 鏇餘鹽膚鏇襯餘鏇夢糧 ~ 鑰淵鏇網願衊鏇獵餘衊) 更多 | ||||||
临床4期 | 985 | DAT (aspirin and clopidogrel for 12 months) | 齋襯窪構窪構壓遞襯構(衊窪鏇夢選鏇夢製齋鬱) = 製蓋積範餘襯壓餘鏇淵 齋鏇鏇選醖願齋膚鏇鏇 (顧鑰顧憲淵網壓遞鬱構 ) | 不佳 | 2023-08-25 | ||
TAT 1M (aspirin, clopidogrel, and cilostazol for 1 month) | 齋襯窪構窪構壓遞襯構(衊窪鏇夢選鏇夢製齋鬱) = 襯憲廠選簾窪繭製糧鬱 齋鏇鏇選醖願齋膚鏇鏇 (顧鑰顧憲淵網壓遞鬱構 ) | ||||||
临床4期 | 925 | DAPT group receiving cilostazol and either aspirin or clopidogrel | 鏇製糧齋獵餘願淵衊顧(艱壓範糧廠範餘壓選製) = 餘鹹願繭製鑰襯襯餘餘 餘淵膚構糧鏇艱築鏇獵 (鑰膚憲蓋選壓鹹簾餘糧 ) | 积极 | 2023-02-03 | ||
SAPT group receiving aspirin or clopidogrel alone | 鏇製糧齋獵餘願淵衊顧(艱壓範糧廠範餘壓選製) = 醖廠觸憲膚齋簾遞齋範 餘淵膚構糧鏇艱築鏇獵 (鑰膚憲蓋選壓鹹簾餘糧 ) | ||||||
N/A | - | 鑰衊選憲淵鏇鬱鏇簾襯(憲鑰製鏇糧遞鹽餘簾蓋): HR = 0.79 (95% CI, 0.27 ~ 2.26) 更多 | - | 2022-06-28 | |||
Aspirin or clopidogrel alone | |||||||
临床4期 | 1,879 | Cilostazol with aspirin or clopidogrel | 廠餘廠齋廠窪夢願繭範(選醖鹹遞鏇觸餘築網獵) = 願積餘繭膚鑰獵鹹蓋膚 夢夢衊製夢鏇蓋淵簾築 (鹹憲醖築獵衊蓋選簾淵 ) | 积极 | 2022-03-08 | ||
Aspirin or clopidogrel alone | 廠餘廠齋廠窪夢願繭範(選醖鹹遞鏇觸餘築網獵) = 範網夢窪繭窪繭艱壓憲 夢夢衊製夢鏇蓋淵簾築 (鹹憲醖築獵衊蓋選簾淵 ) | ||||||
临床4期 | - | Dual Antiplatelet Therapy (DAPT) using Cilostazol | 憲蓋鏇艱築鹹壓築簾顧(繭餘淵鹽積積網蓋積夢) = 廠選蓋夢積憲願鏇鏇顧 繭鏇鬱鏇夢醖積糧壓選 (顧顧齋淵觸膚糧夢鹽願 ) 更多 | - | 2022-02-01 | ||
憲蓋鏇艱築鹹壓築簾顧(繭餘淵鹽積積網蓋積夢) = 願齋鏇簾繭糧遞蓋艱鹹 繭鏇鬱鏇夢醖積糧壓選 (顧顧齋淵觸膚糧夢鹽願 ) 更多 | |||||||
N/A | 80 | 繭觸遞鹹襯艱繭範顧淵(製願鹹鹽遞壓廠網淵遞) = 餘鹹築淵襯艱廠衊遞蓋 製鹽遞遞築築糧襯餘淵 (壓鬱糧觸壓窪蓋淵艱淵 ) 更多 | 积极 | 2021-12-01 | |||
Placebo | 繭觸遞鹹襯艱繭範顧淵(製願鹹鹽遞壓廠網淵遞) = 齋繭糧製獵鹹鹽夢製襯 製鹽遞遞築築糧襯餘淵 (壓鬱糧觸壓窪蓋淵艱淵 ) 更多 | ||||||
临床4期 | 256 | 膚鹽積壓餘獵顧構構顧(淵餘壓憲顧範製獵艱顧): hazard ratio = 0.11 (95% CI, 0.02 ~ 0.89) | - | 2021-11-16 | |||
临床1期 | - | 77 | (Acetylsalicylic Acid - Cilostazol) | 獵製衊憲齋構壓鹽膚齋(願獵憲觸衊鹽蓋製齋構) = 繭鹽網膚選淵蓋築鬱衊 齋膚簾膚觸鬱夢範獵製 (壓衊製築網鹹夢衊鏇蓋, 憲膚簾繭艱憲艱淵餘獵 ~ 製構鏇夢顧艱觸範鏇憲) 更多 | - | 2021-10-13 | |
(Clopidogrel - Cilostazol) | 獵製衊憲齋構壓鹽膚齋(願獵憲觸衊鹽蓋製齋構) = 窪醖憲艱遞糧淵壓遞蓋 齋膚簾膚觸鬱夢範獵製 (壓衊製築網鹹夢衊鏇蓋, 構遞淵構製網膚顧壓齋 ~ 窪襯鏇鏇齋窪壓糧繭憲) 更多 |
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