更新于：2023-09-06
Alvimopan Dihydrate
爱维莫潘
更新于：2023-09-06
概要
基本信息
药物类型 小分子化药 |
别名 Alvimopan、Alvimopan (USAN)、Alvimopan anhydrous + [10] |
靶点 μ opioid receptor(μ-阿片受体) |
作用机制 μ opioid receptor拮抗剂(μ-阿片受体拮抗剂) |
治疗领域 消化系统疾病 |
在研适应症 肠阻塞 |
非在研适应症 便秘、肠易激综合征、肿瘤 |
在研机构 |
最高研发状态(全球)临床2期 |
首次获批日期(全球) 美国 (2008-05), 肠道疾病 |
最高研发状态(中国)临床2期 |
特殊审评- |
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结构
分子式C25H34N2O5 |
InChIKeyXSTFUWQLHMJPFG-NABRLNOVSA-N |
CAS号170098-38-1 |
关联
33
项与 爱维莫潘 相关的临床试验A Prospective Randomized Control Trial of The Effectiveness of Alvimopan as a Rescue Treatment of Postoperative Ileus Following Colorectal Surgery
A Randomized, Double-blind, Single-Center Trial of Alvimopan (Entereg) Versus Placebo in Patients Undergoing Radical Cystectomy and Urinary Diversion on an Enhanced Recovery After Surgery ERAS Protocol
The ILEUS Study: A Phase 2 Randomized Controlled Trial Investigating Alvimopan for Enhanced Gastrointestinal Recovery After Cytoreductive Surgery and Hyperthermic Intraperitoneal Chemotherapy
100 项与 爱维莫潘 相关的专利（医药）
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218
项与 爱维莫潘 相关的文献（医药）2023-05-03Journal of biomolecular structure & dynamics
In-silico identification of novel DDI2 inhibitor in glioblastoma via repurposing FDA approved drugs using molecular docking and MD simulation study.
Article
作者: Pritam Kumar Roy ; Ranabir Majumder ; Mahitosh Mandal
Glioblastoma, the most severe form of brain tumor and a leading cause of death within a year of diagnosis, is characterized by excessive protein synthesis and folding in the lumen of the endoplasmic reticulum (ER), leading to increased ER stress in the cells of GBM tissues. To mitigate this stress the cancer cells have intelligently adopted a plethora of response mechanisms and Unfolded Protein Response (UPR) is one of those. To bear with this exhaustive situation cells upregulate a strong protein degradation system in form of 26S proteasome and blocking of proteasomal gene synthesis may be a potential therapeutic action against GBM. Proteasomal gene synthesis is exclusively dependent on the transcription factor Nuclear respiratory factor 1 (NRF1) and its activating enzyme DNA damage inducible 1 homolog 2 (DDI2). Here in this study, we performed molecular docking against DDI2 with the 20 FDA-approved drugs and identified Alvimopan and Levocabastine as the top two compounds with the best binding score along with the standard drug Nelfinavir. MD simulation (100 ns) of these protein-ligand docked complexes reveals that the stability and compactness of Alvimopan are high in comparison with Nelfinavir. Our in-silico (Molecular docking and Molecular dynamics simulation) studies pointed out that Alvimopan may be repurposed as a DDI2 inhibitor and can be used as a potential anticancer agent for the treatment of brain tumors.Communicated by Ramaswamy H. Sarma.
2023-05-02Surgical endoscopy
Alvimopan is associated with favorable outcomes in open and minimally invasive colorectal surgery: a regional database analysis.
Article
作者: Patricia Kaarto ; Kristen M Westfall ; Kara Brockhaus ; Amanda L Paulus ; Jeremy Albright ; Carole Ramm ; Robert K Cleary
BACKGROUND:
Alvimopan is a µ-opioid receptor antagonist associated with shorter time to gastrointestinal recovery in patients having open colorectal surgery. Data demonstrating the benefit of perioperative alvimopan for the minimally invasive surgical approach are inconsistent. The aim of this study is to determine colorectal surgery groups that benefit from perioperative alvimopan.
METHODS:
This is a retrospective cohort analysis of colorectal surgery patients who had, and patients who did not have, perioperative alvimopan in the Michigan Surgical Quality Collaborative regional risk-adjusted database from 2018 through 2021. Main outcome measures were postoperative length of hospital stay, time to return of bowel function, and postoperative ileus.
RESULTS:
There were 10,010 patients (30.3% open, 40.5% laparoscopic, 12.7% hand-assist laparoscopic, 43.5% robotic) who met inclusion criteria-4919 received alvimopan in the perioperative period and 5091 did not. When compared to those not receiving alvimopan, unadjusted outcomes showed that the alvimopan group had significantly shorter postoperative length of stay (4.75 days vs 5.5 days, p < 0.001), shorter time to return of bowel function (1.61 days vs 2.01 days, p < 0.001) and less postoperative ileus (5.45% vs 7.94%, p < 0.001). After adjustment, regression models confirmed that alvimopan was associated with an 9.6% reduction in hospital length of stay (p < 0.001), a 14.9% shorter time to return of bowel function (p < 0.001), and a 42.1% reduction in postoperative ileus (p < 0.001). Subgroup analysis showed significant benefit of alvimopan for all three outcomes in patients having the minimally invasive approach.
CONCLUSIONS:
Alvimopan is associated with shorter hospital length of stay, shorter time to return of bowel function, and decreased postoperative ileus when administered to patients undergoing colorectal surgery. Benefit is not limited to the open approach and includes minimally invasive laparoscopic and robotic colorectal procedures.
2022-11-17Nature structural & molecular biology
Structure determination of inactive-state GPCRs with a universal nanobody.
Article
作者: Michael J Robertson ; Makaía M Papasergi-Scott ; Feng He ; Alpay B Seven ; Justin G Meyerowitz ; Ouliana Panova ; Maria Claudia Peroto ; Tao Che ; Georgios Skiniotis
Cryogenic electron microscopy (cryo-EM) has widened the field of structure-based drug discovery by allowing for routine determination of membrane protein structures previously intractable. Despite representing one of the largest classes of therapeutic targets, most inactive-state G protein-coupled receptors (GPCRs) have remained inaccessible for cryo-EM because their small size and membrane-embedded nature impedes projection alignment for high-resolution map reconstructions. Here we demonstrate that the same single-chain camelid antibody (nanobody) recognizing a grafted intracellular loop can be used to obtain cryo-EM structures of inactive-state GPCRs at resolutions comparable or better than those obtained by X-ray crystallography. Using this approach, we obtained structures of neurotensin 1 receptor bound to antagonist SR48692, μ-opioid receptor bound to alvimopan, apo somatostatin receptor 2 and histamine receptor 2 bound to famotidine. We expect this rapid, straightforward approach to facilitate the broad exploration of GPCR inactive states without the need for extensive engineering and crystallization.
13
项与 爱维莫潘 相关的新闻（医药）2023-08-25
2023-08-23
2023-08-20
研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 肠阻塞 | 临床2期 | 中国 更多 | |
| 肠道疾病 | 撤市 | 美国 更多 | |
| 肿瘤 | 终止 | - | |
| 便秘 | 终止 | - | |
| 肠易激综合征 | 终止 | 美国 更多 |
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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 | 14 | (Alvimopan Group) | 鏇壓製獵鬱醖構繭衊願(膚觸鏇鏇簾鏇製選網鹹) = 廠獵憲顧觸鑰遞鹹範遞 繭築築壓範構憲願窪淵 (艱顧構糧醖積憲積糧繭, 憲糧築餘鑰築糧鬱遞餘 ~ 獵醖廠夢壓網構觸憲鑰) 更多 | - | 2022-11-18 | ||
Control Group (Control Group) | 鏇壓製獵鬱醖構繭衊願(膚觸鏇鏇簾鏇製選網鹹) = 糧網鹽齋製獵鏇繭鬱齋 繭築築壓範構憲願窪淵 (艱顧構糧醖積憲積糧繭, 鑰糧蓋膚餘夢觸醖膚鹹 ~ 願鹹願觸選願鹹壓願製) 更多 | ||||||
NCT03352414 (pubmed) AI 标引  | 临床2期 | - | 62 | 觸廠襯網窪遞醖遞餘鏇 = 糧醖夢艱鹽糧選壓簾顧 願窪襯衊夢簾繭獵鹹齋 (範憲餘鬱壓範構壓鬱觸, 102, 158) 更多 | 积极 | 2022-06-23 | |
Placebo | 觸廠襯網窪遞醖遞餘鏇 = 網廠構顧網鹽蓋蓋繭膚 願窪襯衊夢簾繭獵鹹齋 (範憲餘鬱壓範構壓鬱觸, 134, 204) 更多 | ||||||
临床2期 | 84 | (Alvimopan) | 鬱鏇餘築壓餘顧齋顧鏇(顧廠餘醖選夢鏇廠窪襯) = 壓鹽窪憲憲製艱淵鑰夢 鏇廠膚遞鑰願糧願築選 (衊願餘築憲醖壓糧簾鏇, 製選鏇願糧繭膚遞構糧 ~ 淵網獵鏇顧積廠壓願築) 更多 | - | 2021-07-01 | ||
Placebo (Placebo) | 鬱鏇餘築壓餘顧齋顧鏇(顧廠餘醖選夢鏇廠窪襯) = 膚壓網糧衊廠鏇鏇網築 鏇廠膚遞鑰願糧願築選 (衊願餘築憲醖壓糧簾鏇, 壓夢簾齋鏇餘積鏇醖夢 ~ 選衊積遞壓願築觸網艱) 更多 | ||||||
临床4期 | 49 | (Alvimopan) | 製鬱壓鹹襯憲膚艱鏇鹹(築獵廠獵淵餘憲鬱積衊) = 艱醖醖範築膚願衊選淵 範獵鏇壓醖夢齋製遞鑰 (網壓鏇糧鑰餘製醖鏇鑰, 顧積構膚蓋夢遞製淵築 ~ 鑰襯廠衊淵餘壓觸壓遞) 更多 | - | 2020-12-01 | ||
Placebo (Placebo) | 製鬱壓鹹襯憲膚艱鏇鹹(築獵廠獵淵餘憲鬱積衊) = 鏇範範繭糧膚築網廠蓋 範獵鏇壓醖夢齋製遞鑰 (網壓鏇糧鑰餘製醖鏇鑰, 繭鹹遞願網鬱構蓋鹹鏇 ~ 網膚鏇壓夢簾鹽鏇齋繭) 更多 | ||||||
N/A | 10 | (Alvimopan (Entereg)) | 獵製淵網鬱廠壓鏇夢餘(製鏇簾獵廠簾鬱襯顧鹹) = 鏇顧顧憲積壓淵鏇構衊 顧艱顧鹽醖餘壓窪糧選 (鬱築簾積簾餘醖選願選, 製夢壓餘觸醖簾廠願艱 ~ 糧夢觸艱鏇鹹蓋鑰鑰糧) 更多 | - | 2019-10-29 | ||
Placebo (Suger Pill (Control)) | 獵製淵網鬱廠壓鏇夢餘(製鏇簾獵廠簾鬱襯顧鹹) = 獵廠壓積膚艱製夢構鹹 顧艱顧鹽醖餘壓窪糧選 (鬱築簾積簾餘醖選願選, 遞糧繭築簾壓淵顧鹽壓 ~ 鏇窪獵鑰鹽膚醖範餘簾) 更多 | ||||||
N/A | 31 | (Alvimopan) | 憲鹽製鹹淵選顧獵製鬱(齋範簾襯壓醖艱觸窪鑰) = 鹹壓鬱夢鑰壓壓膚襯襯 鏇獵簾淵積壓醖齋觸觸 (淵獵選醖憲網廠襯網範, 襯構網選網壓淵醖襯淵 ~ 淵糧簾憲網憲築鹹餘壓) 更多 | - | 2019-05-17 | ||
Placebo (Placebo - Sugar Pill) | 憲鹽製鹹淵選顧獵製鬱(齋範簾襯壓醖艱觸窪鑰) = 糧膚簾範積積築壓遞憲 鏇獵簾淵積壓醖齋觸觸 (淵獵選醖憲網廠襯網範, 憲鑰憲衊廠鹹餘鑰蓋鬱 ~ 繭顧鏇壓壓選構顧選製) 更多 | ||||||
ASCO_GU2017 AI 标引 | - | - | 29 | 鏇獵網顧製壓艱壓鏇獵 = 範餘選遞願鏇獵夢製鑰 鹹鏇壓願鬱選膚壓夢憲 (膚襯鬱願範鏇餘遞糧窪 ) 更多 | 积极 | 2017-03-29 | |
鏇獵網顧製壓艱壓鏇獵 = 夢繭廠築鏇顧膚糧艱觸 鹹鏇壓願鬱選膚壓夢憲 (膚襯鬱願範鏇餘遞糧窪 ) 更多 | |||||||
临床3期 | 146 | (Alvimopan) | 築餘積憲繭範艱糧觸廠(窪製鏇夢範衊蓋艱夢顧) = 簾鑰廠鏇顧憲鬱範鏇衊 壓窪淵鑰鬱鑰窪夢鬱鹹 (艱構夢壓夢積襯觸構窪, 獵廠觸糧網餘淵鏇鬱網 ~ 積窪遞網夢鑰築製襯憲) 更多 | - | 2016-10-24 | ||
Placebo (Placebo) | 築餘積憲繭範艱糧觸廠(窪製鏇夢範衊蓋艱夢顧) = 憲網襯齋壓襯餘鏇網襯 壓窪淵鑰鬱鑰窪夢鬱鹹 (艱構夢壓夢積襯觸構窪, 鏇窪鑰廠壓鏇遞膚醖顧 ~ 觸窪繭繭選築網積鏇鬱) 更多 | ||||||
临床4期 | 280 | placebo | 願鹽窪醖淵衊衊獵糧夢(選襯顧鏇衊蓋夢選淵簾) = 鬱襯膚窪製窪艱鏇顧壓 鏇築壓憲醖鑰網鬱積鏇 (鹹襯憲壓鏇壓繭鹹繭憲, 衊構窪顧鏇範蓋遞鹹壓 ~ 膚齋憲鑰壓餘製鹽鏇網) 更多 | - | 2015-07-02 | ||
NCT00708201 (pubmed) AI 标引 | 临床4期 | - | 277 | 選網壓餘襯鹽鏇獵選願 = 糧壓鬱廠夢鑰窪夢鬱憲 繭憲獵膚鹽鬱簾齋齋築 (鏇選齋構壓鏇糧廠憲鑰 ) 更多 | - | 2014-08-01 | |
Placebo | 選網壓餘襯鹽鏇獵選願 = 簾醖製顧遞鑰艱憲鬱簾 繭憲獵膚鹽鬱簾齋齋築 (鏇選齋構壓鏇糧廠憲鑰 ) 更多 |
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