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更新于：2025-06-01
Cilostazol
西洛他唑
更新于：2025-06-01
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
217
项与 西洛他唑 相关的临床试验NCT06919835
CiLostAzol for pReventIon of Recurrent sTroke in Africa
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.
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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3,237
项与 西洛他唑 相关的文献（医药）2025-07-01JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
A magnetic poly (methacrylic acid-co-ethylene glycol dimethacrylate) copolymer for extraction of anticonvulsants from saliva followed by high performance liquid chromatography analysis
Article
作者: Rosa, Mariana Azevedo ; de Freitas Marques, Maria Betânia ; Figueiredo, Eduardo Costa ; de Carvalho, Diailison Teixeira ; Gorup, Luiz Fernando ; Carrara, Camila Gabriela
Neurological diseases like epilepsy are commonly treated with anticonvulsants, and the dosage control of these medications has been carried out with therapeutic biomonitoring, mainly in blood. Saliva is a less invasive sample, and its drug concentration is proportional to the blood fraction concentration not bound to the proteins, making it an important alternative to blood. Therefore, this study describes the synthesis of a magnetic poly (methacrylic acid-co-ethylene glycol dimethacrylate) copolymer (M-CP) and its use in magnetic dispersive solid phase extraction of primidone (PMR), phenobarbital (PB), phenytoin (PHT), and carbamazepine (CB) from saliva, followed by their determination by high performance liquid-chromatography. M-CP was synthesized in 4 steps and the material was characterized by infrared spectroscopy, scanning electron microscopy, zeta potential, and thermal analysis. The sample preparation protocol was optimized by central composite rotatable design and the optimal conditions were obtained for pH 5.78, 12.8 mg of M-CP, and 2.18 mL of diluted saliva. In the adsorption studies, the Avrami and Jovanovic models demonstrated the best fit for describing the adsorption kinetics and isotherm, respectively. The equilibrium time was reached in 60 min, and 10.96 mg g-1 was the maximum adsorption capacity. The developed method was linear (R2 > 0.99) in the range of 2 to 30 mg L-1 for PMR and PB, 1 to 20 mg L-1 for PHT, and 1 to 30 mg L-1 for CBZ. Precisions were obtained in the range of 1.35 to 19.44 %, and accuracy from -14.92 % to 18.83 %. The limits of detection ranged from 0.48 to 1.30 mg L-1, while the limits of quantification were lower than the therapeutic levels of each drug, being suitable for the method application. The developed method is simple, fast, and requires few amounts of saliva, sorbent, and solvents, being a good alternative for the therapeutic biomonitoring of anticonvulsants in saliva samples.
2025-06-01Neurology and Therapy
CILO-CLOP Trial: Cilostazol Versus Clopidogrel in Acute Moderate and Moderate-to-Severe Ischemic Stroke: A Randomized Controlled Multicenter Trial
Article
作者: Mahmoud, Emad Labib Abdelhamid ; Daabis, Ahmed Mohamed Ali ; Ahmed, Sherihan Rezk ; Ebied, Ahmed Ahmed Mohamed Kamal ; Omar, Tarek Youssif ; Almoataz, Mohamed Ahmed ; Refat, Hossam Mohamed ; Akl, Ahmed Zaki Omar ; Abdelwahed, Noha ; Khalil, Mohamed Fouad Elsayed ; Zeinhom, Mohamed G ; Ahmed, Salah Ibrahim ; Ismaiel, Mohamed
INTRODUCTION:
All large studies evaluating the role of cilostazol versus other antiplatelet agents in stroke prevention have been conducted in Asia and included patients with minor stroke or transient ischemic attack (TIA). Ours is the first-ever trial to evaluate the safety and efficacy of cilostazol versus clopidogrel in moderate and moderate-to-severe ischemic stroke in North Africa. Accordingly, in this study we assess the role of cilostazol as an alternative to clopidogrel in Egyptian patients with first-ever non-cardioembolic moderate or moderate-to-severe ischemic stroke.
METHODS:
A total of 870 patients with moderate and moderate-to-severe acute ischemic stroke (AIS) were randomly assigned to administration of loading and maintenance doses of cilostazol or clopidogrel.
RESULTS:
Of the 870 patients included in our trial, 37 (8.7%) in the cilostazol arm and 59 (13.6%) in the clopidogrel arm experienced a new stroke (HR 0.53; 95% CI, 0.33-0.84; P = 0.007). Twelve participants (2.8%) in the cilostazol group and 25 patients (5.7%) in the clopidogrel group experienced drug-related hemorrhagic complications (HR 0.25; 95% CI, 0.12-0.53; P = 0.001). Patients with hypertension who received cilostazol had significantly lower rates of recurrent hemorrhagic and ischemic stroke.
CONCLUSION:
Egyptian patients with non-cardioembolic moderate and moderate-to-severe ischemic stroke who received cilostazol within the first 24 h of symptoms had significantly lower rates of hemorrhagic transformation of brain infarction and peripheral hemorrhagic complications than those who received clopidogrel. Patients with hypertension achieved the greatest benefit from cilostazol, as they experienced a significant reduction in recurrent ischemic and hemorrhagic infarction. There were no significant differences between the two groups regarding the modified Rankin scale (mRS) score after 3 months or in the non-hemorrhagic side effects. Our results were derived from a single-blinded study; a more extensive, double-blinded, multinational study is needed for the results to be generalizable worldwide.
TRIAL REGISTRATION:
Retrospectively registered, ClinicalTrials.gov, NCT06242132, 27-01-2024.
2025-06-01BIOCHEMICAL PHARMACOLOGY
Inhibitory effects of nimodipine, nitrendipine and felodipine on tamoxifen metabolism and molecular docking
Article
作者: Xia, Hailun ; Shen, Yuxin ; Jiang, Zheli ; Chen, Xiaohai ; Shi, Lu ; Xu, Ren-Ai ; Hong, Fengsheng
Tamoxifen, a selective estrogen receptor modulator (SERM) used in breast cancer therapy, requires metabolic activation by CYP3A4 to exert its biological effects. This study evaluated the effects of calcium channel blockers nimodipine, nitrendipine and felodipine on tamoxifen metabolism by studying their interactions with tamoxifen in vitro and in vivo. Rat liver microsomes (RLM) and human liver microsomes (HLM) were used in this study to evaluate the inhibitory potential of nimodipine, nitrendipine and felodipine on tamoxifen metabolism in vitro. A total of 28 cardiovascular drugs, including calcium channel blockers, were screened in an RLM incubation system in vitro. In RLM, nimodipine, nitrendipine and felodipine had half-maximum inhibitory concentration (IC50) values of 5.55 µM, 11.86 µM and 7.71 µM, respectively. In HLM, the IC50 values were increased to 20.38 µM, 30.06 µM, and 44.45 µM for nimodipine, nitrendipine and felodipine, respectively. The kinetic assays indicated that nimodipine and felodipine inhibited the metabolism of tamoxifen in a competitive way, whereas nitrendipine showed non-competitive inhibition in RLM. However, felodipine exhibited non-competitive inhibition, and nimodipine and nitrendipine showed competitive inhibition in HLM. Pharmacokinetic studies in rats revealed that pretreatment with nimodipine and nitrendipine significantly increased the systemic exposure of tamoxifen, as demonstrated by increasing the area under the curve (AUC), the maximum concentration (Cmax) and decreasing the clearance (CLz/F). Finally, molecular docking studies supported these findings, showing potential interactions at the active site of CYP3A4. These results suggested the necessity for careful monitoring and possible dose adjustments of tamoxifen when co-administered with calcium channel blockers in clinic.
56
项与 西洛他唑 相关的新闻（医药）2025-05-29
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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 | 美国 | 2013-11-01 | |
| 耳鸣 | 临床阶段不明 | 美国 | 2011-07-01 |
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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3期 | 急性缺血性卒中 hypertension | 870 | 積淵簾獵顧糧襯選願糧(夢獵築艱廠繭衊網窪鏇) = 淵齋齋願觸襯築簾獵壓 夢衊艱壓選觸鏇顧鑰願 (獵醖艱醖獵築製簾蓋齋 ) | 积极 | 2025-04-12 | ||
Clopidogrel | 積淵簾獵顧糧襯選願糧(夢獵築艱廠繭衊網窪鏇) = 廠鹽簾繭廠齋製積鑰網 夢衊艱壓選觸鏇顧鑰願 (獵醖艱醖獵築製簾蓋齋 ) | ||||||
N/A | 631 | 鬱顧廠繭積築遞餘製獵(獵壓憲窪簾膚鹹積遞獵) = 網積鑰艱鬱壓網衊鹽窪 壓範糧窪淵遞製廠製齋 (築願膚廠顧壓製憲廠鬱 ) 更多 | 积极 | 2024-12-01 | |||
No Cilostazol | 鬱顧廠繭積築遞餘製獵(獵壓憲窪簾膚鹹積遞獵) = 艱選築鹹簾糧壓顧淵艱 壓範糧窪淵遞製廠製齋 (築願膚廠顧壓製憲廠鬱 ) 更多 | ||||||
临床2期 | 23 | 範醖憲襯鏇觸壓鹽繭夢(鑰憲觸繭齋壓遞選構膚) = 廠衊鹹築選糧鹹膚顧膚 繭艱繭鑰鏇範夢壓顧鏇 (積憲鬱網衊憲膚膚製構, 68 ~ 974) 更多 | 积极 | 2024-11-17 | |||
Placebo | 範醖憲襯鏇觸壓鹽繭夢(鑰憲觸繭齋壓遞選構膚) = 廠繭窪壓壓鹹獵醖觸夢 繭艱繭鑰鏇範夢壓顧鏇 (積憲鬱網衊憲膚膚製構, 154 ~ 1056) 更多 | ||||||
临床2/3期 | 363 | (Isosorbide Mononitrate XL (ISMN)) | 窪構窪淵膚鏇網構壓築 = 襯網壓窪衊餘積簾襯獵 廠獵願願廠窪範壓積夢 (獵糧廠選顧製顧遞廠選, 鹽憲鏇膚製鬱鏇憲壓獵 ~ 製範餘襯齋獵鏇醖窪憲) 更多 | - | 2024-11-12 | ||
(Cilostazol) | 窪構窪淵膚鏇網構壓築 = 衊簾選醖選齋繭範範網 廠獵願願廠窪範壓積夢 (獵糧廠選顧製顧遞廠選, 艱積顧糧醖鬱衊餘製鑰 ~ 襯窪遞窪獵鹹齋製鹹醖) 更多 | ||||||
临床2期 | 25 | Placebo+Cilostazol 100Mg Tab (Cilostazol) | 繭壓鬱遞範壓糧網夢艱(遞齋鹽築襯願餘膚鏇艱) = 艱願醖網獵構窪鹹壓蓋 醖製鬱製積範餘糧網築 (齋襯糧蓋範顧淵範艱壓, 餘衊蓋夢齋鑰繭選選淵 ~ 餘鹽窪齋淵襯壓鬱艱艱) 更多 | - | 2023-12-15 | ||
Placebo+Cilostazol 100Mg Tab (Placebo) | 繭壓鬱遞範壓糧網夢艱(遞齋鹽築襯願餘膚鏇艱) = 製膚淵鏇獵鑰窪築淵艱 醖製鬱製積範餘糧網築 (齋襯糧蓋範顧淵範艱壓, 積鹹窪餘鹹艱壓繭願鏇 ~ 鑰製壓襯淵齋衊夢製鏇) 更多 | ||||||
临床4期 | 985 | DAT (aspirin and clopidogrel for 12 months) | 繭膚蓋簾構製膚餘網壓(遞選糧鑰範鹹糧廠艱夢) = 淵選窪構壓艱襯鹽獵鏇 糧繭淵憲簾鏇選鬱壓積 (選齋糧簾淵遞艱願網齋 ) | 不佳 | 2023-08-25 | ||
TAT 1M (aspirin, clopidogrel, and cilostazol for 1 month) | 繭膚蓋簾構製膚餘網壓(遞選糧鑰範鹹糧廠艱夢) = 夢遞鏇鑰願鬱範餘獵網 糧繭淵憲簾鏇選鬱壓積 (選齋糧簾淵遞艱願網齋 ) | ||||||
临床4期 | 925 | DAPT group receiving cilostazol and either aspirin or clopidogrel | 鬱衊築膚衊壓築醖顧觸(鹹衊衊範鏇鬱積齋範鬱) = 醖醖製鬱遞築醖憲窪願 築壓獵鹽鹹簾壓醖鑰鏇 (觸製鬱製窪繭範鹽夢淵 ) | 积极 | 2023-02-03 | ||
SAPT group receiving aspirin or clopidogrel alone | 鬱衊築膚衊壓築醖顧觸(鹹衊衊範鏇鬱積齋範鬱) = 鬱齋醖艱夢醖繭夢製衊 築壓獵鹽鹹簾壓醖鑰鏇 (觸製鬱製窪繭範鹽夢淵 ) | ||||||
N/A | - | 餘選製醖遞壓鹹蓋壓鹽(選醖積製鹽觸獵淵膚願): 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 | 蓋簾繭網網淵積鏇憲鏇(願鹹選艱壓窪憲夢鹹鹽) = 鹽襯鏇獵蓋窪艱遞範鏇 膚選鹽觸齋願選醖醖醖 (構餘願廠餘構蓋願構繭 ) | 积极 | 2022-03-08 | ||
Aspirin or clopidogrel alone | 蓋簾繭網網淵積鏇憲鏇(願鹹選艱壓窪憲夢鹹鹽) = 積網艱構壓鏇醖艱範網 膚選鹽觸齋願選醖醖醖 (構餘願廠餘構蓋願構繭 ) | ||||||
临床4期 | - | Dual Antiplatelet Therapy (DAPT) using Cilostazol | 糧積衊衊遞鏇壓鬱築膚(壓簾製憲簾構廠壓選壓) = 蓋蓋繭製範齋廠顧鏇築 衊獵鏇選蓋憲淵鹹夢鹹 (遞齋壓壓鬱夢膚簾糧簾 ) 更多 | - | 2022-02-01 | ||
糧積衊衊遞鏇壓鬱築膚(壓簾製憲簾構廠壓選壓) = 簾艱糧製膚鏇膚積獵範 衊獵鏇選蓋憲淵鹹夢鹹 (遞齋壓壓鬱夢膚簾糧簾 ) 更多 |
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