更新于：2024-05-01
Umirolimus
乌米莫司
更新于：2024-05-01
概要
基本信息
在研机构- |
最高研发阶段批准上市 |
首次获批日期 (2008-04-03), |
最高研发阶段(中国)- |
特殊审评- |
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结构
分子式C55H87NO14 |
InChIKeyYYSFXUWWPNHNAZ-UHFFFAOYSA-N |
CAS号851536-75-9 |
关联
2
项与 乌米莫司 相关的临床试验A prospective, multi center evaluation of the Bioliumus A9 eluting Axxess stent system in de novo coronary artery lesions. The study outcome will measure reduction in major adverse cardiac events compared to a historial control group.
Randomized Clinical Comparison of the Combined Sirolimus Eluting and Endothelial Progenitor Cell Combo™ Stent and the Biolimus Eluting Absorbable Polymer Coated BioMatrix Alpha™ Stent in Patients Treated With Percutaneous Coronary Intervention.
100 项与 乌米莫司 相关的临床结果
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100 项与 乌米莫司 相关的转化医学
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100 项与 乌米莫司 相关的专利（医药）
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558
项与 乌米莫司 相关的文献（医药）2024-02-14ChemMedChem
Insights into the overcoming EGFR Del19/T790M/C797S mutation: A perspective on the 2-aryl-4-aminothienopyrimidine backbone.
Article
作者: Xuan Zhang ; Jie He ; Shidi Xu ; Li Fu ; Pengwu Zheng ; Shan Xu ; Qingshan Pan ; Wufu Zhu
The epithelial growth factor receptor signaling pathway has been proposed to benefit non-small cell lung cancer treatment. In this manuscript, we investigated the modification of 2-aryl-4-aminoquinazoline, the classical backbone of the fourth-generation EGFR inhibitors, in addition to obtaining a series of novel 2-aryl-4-aminothienopyrimidine derivatives (A1~A45), we also gained further understanding of the modification of this framework. The bioactivity of these compounds was evaluated and it's suggested that compound A9 could effectively inhibit the proliferation of A549 and H1975 cells, with an IC50 of 0.77 ± 0.08 and 6.90 ± 0.83 μM, respectively. At concentration of 10 μM, A9 can be employed as the fourth-generation of EGFR inhibitors with the ability to overcome the C797S drug resistance since it can suppress EGFRDel19/T790M/C797S cells and kinase by 98.90% and 85.88%, respectively. Moreover, the tumor-bearing nude mice experiment further shows that A9 can significantly inhibit the growth of tumor in vivo, with the tumor inhibition rate (TIR) of 55.92%, which was equivalent to the positive group. After that, from the result of HE staining experiment and blood biochemical analysis experiment, A9 show low toxicity and good safety, which is worthy of further research and development.
2024-01-23Journal of addiction medicine
Associations of Methadone and BUP/NX Dose Titration Patterns With Retention in Treatment and Opioid Use in Individuals With Prescription-Type Opioid Use Disorder: Secondary Analysis of the OPTIMA Study.
Article
作者: Hamzah Bakouni ; Lexie Haquet ; M Eugenia Socias ; Bernard Le Foll ; Ron Lim ; Keith Ahamad ; Didier Jutras-Aswad ; OPTIMA Research Group within the Canadian Research Initiative in Substance Misuse
INTRODUCTION:
Methadone and buprenorphine/naloxone (BUP/NX) titration parameters (eg, range, duration, and rate) can vary during opioid use disorder (OUD) treatment. We describe methadone and BUP/NX titration patterns and their associations with treatment outcomes among individuals with a prescription-type OUD.
METHODS:
We used data from a 24-week open-label, multicenter randomized controlled trial, including N = 167 participants aged 18-64 years old with prescription-type OUD who received at least a first dose of treatment. Descriptive analyses of methadone and BUP/NX titration patterns were conducted, that is, range and duration from first to maximum dose, and rate (range/duration ratio). Outcomes included percentage of opioid-positive urine drug screens (UDS) and treatment retention. Adjusted linear and logistic regressions were used to study associations between titration patterns and percentage of opioid-positive UDS and treatment retention.
RESULTS:
Methadone doses were increased by a mean dose range of 42.4 mg over a mean duration of 42.2 days. BUP/NX doses were increased by a mean dose range of 8.4 mg over a mean duration of 28.7 days. Only methadone dose titration range (odds ratio: 1.03; 95% CI, 1.01 to 1.05) and duration (odds ratio: 1.03; 95% CI, 1.01 to 1.05) were associated with higher retention. Only methadone dose titration rate was associated with lower percentage of opioid-positive UDS at weeks 12-24 (B: -2.77; 95% CI, -4.72 to -0.81).
CONCLUSIONS:
Specific parameters of methadone titration were associated with treatment outcomes and may help in personalizing treatment schedules. Sustained methadone dose titration, when indicated, may help increase retention, whereas faster dose titration for methadone may help decrease opioid use.
2024-01-12Journal of the American Heart Association
Percutaneous Coronary Interventions Using a Ridaforolimus-Eluting Stent in Patients at High Bleeding Risk.
Article
作者: Ran Kornowski ; Maayan Konigstein ; Michael Jonas ; Abid Assali ; Hana Vaknin-Assa ; Amit Segev ; Haim Danenberg ; Majdi Halabi ; Ariel Roguin ; Arthur Kerner ; Eli Lev ; Grigoris V Karamasis ; Thomas W Johnson ; Richard Anderson ; Jonathan Blaxill ; Sachin Jadhav ; Stephen Hoole ; Guy Witberg ; Melek Ozgu Issever ; Ori Ben-Yehuda ; Andreas Baumbach
BACKGROUND:
Patients treated with percutaneous coronary intervention are often considered to be at a high bleeding risk (HBR). Drug-eluting stents have been shown to be superior to bare-metal stents in patients with HBR, even when patients were given abbreviated periods of dual antiplatelet therapy (DAPT). Short DAPT has not been evaluated with the EluNIR ridaforolimus-eluting stent. The aim of this study was to evaluate the safety and efficacy of a shortened period of DAPT following implantation of the ridaforolimus-eluting stent in patients with HBR.
METHODS AND RESULTS:
This was a prospective, multicenter, binational, single-arm, open-label trial. Patients were defined as HBR according to the LEADERS-FREE (Prospective Randomized Comparison of the BioFreedom Biolimus A9 Drug-Coated Stent versus the Gazelle Bare-Metal Stent in Patients at High Bleeding Risk) trial criteria. After percutaneous coronary intervention, DAPT was given for 1 month to patients presenting with stable angina. In patients presenting with an acute coronary syndrome, DAPT was given for 1 to 3 months, at the investigator's discretion. The primary end point was a composite of cardiac death, myocardial infarction, or stent thrombosis up to 1 year (Academic Research Consortium definite and probable). Three hundred fifteen patients undergoing percutaneous coronary intervention were enrolled, and 56.4% presented with acute coronary syndrome; 33.7% were receiving oral anticoagulation. At 1 year, the primary end point occurred in 15 patients (4.9%), meeting the prespecified performance goal of 14.1% (P<0.0001). Stent thrombosis (Academic Research Consortium definite and probable) occurred in 2 patients (0.6%). Bleeding Academic Research Consortium type 3 and 5 bleeding occurred in 6 patients (1.9%).
CONCLUSIONS:
We observed favorable results in patients with HBR who underwent percutaneous coronary intervention with a ridaforolimus-eluting stent and received shortened DAPT, including a low rate of ischemic events and low rate of stent thrombosis.
REGISTRATION:
URL: https://www.clinicaltrials.gov; Unique identifier: NCT03877848.
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 冠状动脉再狭窄 | 批准上市 | - | - |
| 冠心病 | 临床阶段不明 | 西班牙 更多 | |
| 冠状动脉疾病 | 无进展 | 日本 更多 |
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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 | - | - | Biolimus-eluting stent | 製鬱觸選願襯選觸壓襯(鏇鹹觸夢鑰築艱鏇廠積) = 衊餘觸顧壓襯製壓範願 顧膚鹹獵醖膚壓膚蓋選 (壓艱鏇蓋築壓鏇網構獵 ) 更多 | 积极 | 2005-05-01 | |
Biolimus A9 | 製鬱觸選願襯選觸壓襯(鏇鹹觸夢鑰築艱鏇廠積) = 糧餘簾廠簾觸願憲齋選 顧膚鹹獵醖膚壓膚蓋選 (壓艱鏇蓋築壓鏇網構獵 ) 更多 | ||||||
临床4期 | 2,341 | (Ultrathin-strut BP-SES) | 廠餘壓構鬱廠鬱選繭鑰(襯觸鏇構襯觸糧膚顧淵) = 衊鬱襯簾齋齋淵鹽鬱鑰 餘選鹽鏇網餘願鹹獵簾 (艱顧顧觸糧鹽齋廠廠繭 ) | - | 2023-01-01 | ||
(Thick-strut BP-BES) | 廠餘壓構鬱廠鬱選繭鑰(襯觸鏇構襯觸糧膚顧淵) = 憲餘顧築鏇衊蓋願簾憲 餘選鹽鏇網餘願鹹獵簾 (艱顧顧觸糧鹽齋廠廠繭 ) | ||||||
N/A | - | 鏇遞鹹膚選蓋鏇艱範願(獵壓鑰範觸鬱鹽蓋蓋餘) = 壓積衊繭築簾憲廠觸範 範憲鹽淵築蓋艱願遞繭 (構願鏇鏇積構顧糧蓋糧 ) 更多 | - | 2017-08-28 | |||
zotarolimus-eluting Endeavor (ZES-E) | 鏇遞鹹膚選蓋鏇艱範願(獵壓鑰範觸鬱鹽蓋蓋餘) = 餘選構齋遞齋簾築襯蓋 範憲鹽淵築蓋艱願遞繭 (構願鏇鏇積構顧糧蓋糧 ) 更多 | ||||||
N/A | - | 109 | Biolimus A9 | 鬱簾構蓋餘鑰衊範觸製(簾齋範艱夢醖鹽餘遞鹹) = 廠壓構艱糧膚製廠衊鏇 糧製鹹簾製構淵鹽築願 (憲遞夢範積範醖壓膚蓋 ) 更多 | 积极 | 2020-08-28 | |
Biolimus A9 | 鬱簾構蓋餘鑰衊範觸製(簾齋範艱夢醖鹽餘遞鹹) = 鹽鑰衊鬱獵鹽網獵觸鏇 糧製鹹簾製構淵鹽築願 (憲遞夢範積範醖壓膚蓋 ) 更多 |
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