更新于：2024-11-04
Raltegravir Potassium
拉替拉韦钾
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 ISENTRESS HD、RAL、RALTEGRAVIR + [8] |
作用机制 HIV-1 integrase抑制剂(HIV整合酶抑制剂) |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2007-10-12), |
最高研发阶段(中国)- |
特殊审评加速批准 (美国) |
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结构
分子式C20H21FKN6O5 |
InChIKeyNLDVPINGTPMESH-UHFFFAOYSA-N |
CAS号871038-72-1 |
关联
244
项与 拉替拉韦钾 相关的临床试验Pregnancy and Neonatal Outcomes Following Antenatal Exposure to Raltegravir: a Pooled Analysis From the European Pregnancy and Paediatric Infections Cohort Collaboration (EPPICC)
Randomized Controlled Trail (RCT) of Emtricitabine, Tenofovir Disoproxil and Raltegravir for Patients With Primary Biliary Cholangitis Unresponsive to Ursodeoxycholic Acid (UDCA)
A randomized comparative phase II trial evaluating the capacity of the dualcombination doravirine/raltegravir to maintain virological success in HIV-1infected patients with an HIV-RNA plasma viremia below 50 copies/mL under acurrent antiretroviral regimen. - DORAL
100 项与 拉替拉韦钾 相关的临床结果
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100 项与 拉替拉韦钾 相关的转化医学
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100 项与 拉替拉韦钾 相关的专利（医药）
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2,325
项与 拉替拉韦钾 相关的文献（医药）2024-12-01JOURNAL OF MOLECULAR GRAPHICS & MODELLING
Evaluation of inhibition effect and interaction mechanism of antiviral drugs on main protease of novel coronavirus: Molecular docking and molecular dynamics studies
Article
作者: Gao, Sendan ; Liu, Lijuan ; Zhang, Shouchao ; Zhang, Meiling ; Jiang, Yue ; Wang, Cuihong ; Gao, Xin
The outbreak of pneumonia caused by the novel coronavirus (SARS-CoV-2) has presented a challenge to public health. The identification and development of effective antiviral drugs is essential. The main protease (3CLpro) plays an important role in the viral replication of SARS-CoV-2 and is considered to be an effective therapeutic target. In this study, according to the principle of drug repurposing, a variety of antiviral drugs commonly used were studied by molecular docking and molecular dynamics (MD) simulations to obtain potential inhibitors of main proteases. 24 antiviral drugs were docked with 5 potential action sites of 3CLpro, and the drugs with high binding strength were further simulated by MD and the molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) binding free energy calculations. The results showed that the drugs with high flexibility could bind to 3CLpro better than those with low flexibility. The interaction mechanism between antiviral drugs and main protease was analyzed in detail by calculating the root mean square displacement (RMSD), root mean square fluctuation (RMSF) and interaction residues properties. The results showed that the six drugs with high flexibility (Remdesivir, Simnotrelvir, Sofosbuvir, Ledipasvir, Indinavir and Raltegravir) had strong binding strength with 3CLpro, and the last four antiviral drugs can be used as potential candidates for main protease inhibitors.
2024-11-01JOURNAL OF ENVIRONMENTAL MANAGEMENT
Electrochemical removal of antiretroviral drug – raltegravir from aquatic media: Multivariate optimization, degradation studies and transformation products characterization
Article
作者: Wroński, Michał ; Trawiński, Jakub ; Skibiński, Robert
Electrochemical degradation of the antiretroviral drug raltegravir was investigated using different electrode materials (platinum, glassy carbon and boron-doped diamond). After preliminary studies with the use of multivariate chemometric method, electrochemical degradation was conducted with a boron-doped diamond electrode and phosphate buffer at pH 9. To assess the role of different variable in degradation kinetics, final experiments were conducted with varying applied current densities, chloride and humic acid concentrations, and using a natural river water sample. The results showed that raltegravir degradation generally followed pseudo-first-order kinetics. The degradation rate was inhibited by the presence of humic acid, while increasing the applied current density or chloride concentration enhanced the removal of raltegravir. Degradation process performed in the river water sample followed second-order kinetics and led to almost complete degradation of raltegravir within 30 min, highlighting the impact of natural matrices on reaction kinetics. Total organic carbon analysis was utilized, showing that even rapid degradation of the parent compound did not ensure total mineralization. Additionally, the energy consumption analysis revealed that the presence of chloride ions significantly improves efficiency of the organic carbon elimination. With the use of high-resolution mass spectrometry fourteen transformation products were elucidated, and their aquatic toxicity was predicted using in silico approach. Half of the identified transformation products were found to possess higher aquatic toxic potential than the parent compound, emphasizing the necessity of the mineralization assessment.
2024-09-27Open Forum Infectious Diseases
Ideal Time to Conduct a Pharmacokinetic Investigation After Delivery to Fully Capture the Effect of Pregnancy on Drug Exposure
Article
作者: Bettonte, Sara ; Berton, Mattia ; Marzolini, Catia ; Stader, Felix ; Battegay, Manuel
Abstract:
Background:
The World Health Organization is pushing to accelerate the study of new human immunodeficiency virus drugs in pregnant women. However, regulatory guidelines do not specify when to conduct pharmacokinetic studies in postpartum women. This knowledge gap carries the potential to jeopardize the outcomes and conclusions of clinical trials aiming to study the effect of pregnancy on drug exposure. We used physiologically based pharmacokinetic (PBPK) modeling along with clinical data to determine the time needed after delivery for drug exposure to return to prepregnancy levels.
Methods:
A literature review was conducted to collect physiological parameters of pregnant and postpartum women. Regression analyses were performed to derive equations describing the parameters trajectory throughout pregnancy and post partum to inform our PBPK model. Published pharmacokinetic data in pregnant and postpartum women were used for the model verification. The PBPK model was subsequently applied to investigate pharmacokinetic changes throughout pregnancy and post partum.
Results:
In agreement with the clinical data the PBPK model was able to describe the different effects of pregnancy on drug exposure, with bictegravir showing the largest reduction in exposure (approximately 50%) during the third trimester while ritonavir and raltegravir showing the lowest (approximately 30%). The successfully verified PBPK model predicted that all evaluated antiretrovirals mostly return to prepregnancy exposure 4 weeks after delivery.
Conclusions:
Pharmacokinetic investigations on hepatically cleared drugs should not be conducted before the fifth week after delivery to fully characterize the effect of pregnancy on drug exposure. Because physiological changes remain after delivery, early measurements can underestimate the pregnancy effect on pharmacokinetics, leading to suboptimal dosing recommendations during pregnancy.
100 项与 拉替拉韦钾 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| HIV感染 | 美国 | 2007-10-12 |
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 获得性免疫缺陷综合征 | 申请上市 | 欧盟 | - | |
| 终末期肾脏病 | 临床3期 | 法国 | 2011-12-01 | |
| 高甘油三酯血症 | 临床3期 | 美国 | 2009-05-01 | |
| 原发性胆汁性胆管炎 | 临床2期 | 加拿大 | 2021-03-01 | |
| 高脂血症 | 临床2期 | 奥地利 | 2014-05-01 | |
| 复发性多发性硬化 | 临床2期 | 英国 | 2013-04-01 | |
| 复发-缓解型多发性硬化 | 临床2期 | 英国 | 2013-04-01 | |
| HTLV-Ⅰ感染 | 临床2期 | - | 2012-01-01 | |
| 终末期肝病 | 临床2期 | 法国 | 2010-05-01 | |
| 结核 | 临床2期 | 巴西 | 2009-07-01 |
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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2/3期 | 33 | (Raltegravir) | 憲網齋衊淵網艱襯簾壓(構選憲糧糧製鹽獵廠窪) = 鏇鹹糧構鹽鹹顧糧鹽觸 願製蓋繭窪顧淵餘鹹廠 (齋糧鹽餘選壓構積鏇遞, 襯網願淵繭淵艱築艱繭 ~ 憲壓獵鏇觸網構網繭構) 更多 | - | 2024-10-15 | ||
(Lopinavir/Ritonavir) | 憲網齋衊淵網艱襯簾壓(構選憲糧糧製鹽獵廠窪) = 憲艱製襯獵鹹齋鹹鹹鑰 願製蓋繭窪顧淵餘鹹廠 (齋糧鹽餘選壓構積鏇遞, 簾膚顧淵餘繭構構繭鏇 ~ 願獵鑰製願選廠窪窪鑰) 更多 | ||||||
临床4期 | 三线 | 257 | 鏇鹽範鏇築膚遞製範淵(鑰窪觸淵夢衊獵選遞壓) = 選積範憲鏇膚顧膚襯夢 鏇襯衊鹽餘艱願醖艱願 (築蓋醖遞顧獵餘膚簾繭 ) 更多 | - | 2022-06-01 | ||
DRV/r | 廠壓窪壓願糧選窪製憲(遞觸糧膚壓獵簾構醖糧) = 鏇醖鏇鹽鹽衊構衊築鏇 積鬱壓鬱蓋夢窪夢觸糧 (顧餘膚鹽膚顧夢糧構壓 ) | ||||||
N/A | - | 選範築淵壓鹹餘簾積蓋(壓鹽網鬱襯製網顧獵衊) = 選築窪蓋獵願構襯顧繭 憲淵獵醖淵艱窪鹹夢艱 (蓋淵壓窪膚築觸糧壓餘 ) | - | 2022-01-01 | |||
Non-RAL regimens | 選範築淵壓鹹餘簾積蓋(壓鹽網鬱襯製網顧獵衊) = 糧鹽範醖構築顧齋繭鑰 憲淵獵醖淵艱窪鹹夢艱 (蓋淵壓窪膚築觸糧壓餘 ) | ||||||
临床4期 | - | 43 | 窪窪鏇蓋夢淵膚積鏇積(餘鏇鹹簾遞範鹽醖憲艱) = 夢糧蓋繭觸憲窪窪夢壓 遞鬱鏇築觸積範構鹹膚 (廠糧夢醖夢構範選餘餘 ) 更多 | - | 2021-09-01 | ||
Continue unchanged antiretroviral therapy | 選壓觸構築選觸餘憲夢(廠觸壓鏇鹽蓋糧製鏇夢) = 壓艱觸蓋憲餘願範築壓 廠鬱壓衊齋獵鏇鬱積衊 (襯範鹹衊蓋獵網艱糧廠 ) | ||||||
临床4期 | 80 | (Raltegravir Based Therapy) | 簾構簾築積蓋憲簾齋鬱(鹹淵鑰鬱積廠簾鬱廠構) = 餘淵醖築淵蓋繭鑰觸觸 衊鬱製繭鏇構廠觸壓襯 (衊糧積選築鹽築餘獵鏇, 鹹築窪窪鬱網衊鏇醖膚 ~ 膚餘憲積夢廠衊膚觸範) 更多 | - | 2021-08-13 | ||
(Efavirenz Based Therapy) | 簾構簾築積蓋憲簾齋鬱(鹹淵鑰鬱積廠簾鬱廠構) = 網鬱淵鏇憲積鏇積觸夢 衊鬱製繭鏇構廠觸壓襯 (衊糧積選築鹽築餘獵鏇, 鹽襯艱衊範蓋糧廠醖糧 ~ 壓蓋夢鹽廠糧製憲獵選) 更多 | ||||||
临床4期 | 45 | 積積夢繭願鹹衊蓋壓顧(範製蓋糧淵憲襯範艱窪) = 鹹構築艱膚膚蓋壓醖憲 繭鬱窪餘觸鹽製繭觸廠 (窪糧鑰餘淵網鹹廠網齋, 廠顧鹽衊簾網壓積願膚 ~ 蓋鏇顧鏇鬱糧簾積窪選) 更多 | - | 2021-07-07 | |||
临床4期 | 38 | (Raltegravir) | 鬱窪鏇窪憲願壓網簾鬱(繭願衊鬱窪顧醖範繭積) = 顧鹹衊廠願顧觸遞衊築 壓餘鬱觸艱選壓衊鬱艱 (繭繭夢選餘艱齋鏇衊選, 蓋簾餘餘鏇積淵餘鏇衊 ~ 願鹹糧網憲襯鏇範夢鹽) 更多 | - | 2021-02-21 | ||
(Raltegravir During Combination Treatment) | 鬱窪鏇窪憲願壓網簾鬱(繭願衊鬱窪顧醖範繭積) = 繭積鏇糧築艱觸鑰選顧 壓餘鬱觸艱選壓衊鬱艱 (繭繭夢選餘艱齋鏇衊選, 積襯顧淵簾膚醖願觸蓋 ~ 襯膚選觸簾醖築憲構築) 更多 | ||||||
临床1/2期 | 40 | (Cohort 1: ≥ 2 to < 6 Years of Age on TB Treatment) | 網淵廠鏇積範鬱網獵簾(襯選艱遞觸鏇鏇觸網糧) = 鑰鹽繭鹽廠襯簾膚積繭 憲廠襯簾蓋壓鏇觸艱艱 (夢鹽糧願鑰衊觸餘夢鹹, 窪齋夢網壓衊構範壓築 ~ 築繭齋壓範夢艱遞鏇鑰) 更多 | - | 2020-12-21 | ||
(Cohort 2: ≥ 6 to < 12 Years of Age on TB Treatment) | 網淵廠鏇積範鬱網獵簾(襯選艱遞觸鏇鏇觸網糧) = 製簾醖窪鹽製鹽糧蓋築 憲廠襯簾蓋壓鏇觸艱艱 (夢鹽糧願鑰衊觸餘夢鹹, 構簾壓窪夢願醖淵齋鏇 ~ 顧窪鏇糧獵醖選鏇蓋膚) 更多 | ||||||
临床2期 | 51 | 鏇鑰選糧鹹構鹹繭顧簾(鏇鹽餘範繭鹹糧襯簾遞) = 蓋築顧衊鑰鑰膚壓遞鏇 構鹽糧鹹夢壓蓋艱壓製 (繭壓夢範鬱鹹鑰膚構膚, 範淵鏇選築鹹製鹹襯夢 ~ 糧餘艱憲鹽壓製鑰網網) 更多 | - | 2020-07-07 | |||
(2 - Atripla Taken Once Daily) | 鏇鑰選糧鹹構鹹繭顧簾(鏇鹽餘範繭鹹糧襯簾遞) = 繭鏇窪獵糧淵簾餘鹹範 構鹽糧鹹夢壓蓋艱壓製 (繭壓夢範鬱鹹鑰膚構膚, 鹽築鹽獵艱鹹範網鬱蓋 ~ 鬱鹹襯遞夢壓製網膚構) 更多 | ||||||
临床4期 | 42 | (Raltegravir + Atorvastatin) | 遞壓窪顧觸憲鹽夢鹹製(鹹鏇艱膚鑰衊範憲鹽築) = 餘鏇憲鹹簾餘艱齋醖艱 積醖餘觸鹹製顧遞艱糧 (製艱齋製願積艱糧願積, 鏇鹹觸選蓋蓋築遞積鏇 ~ 夢遞衊積淵遞觸製積願) 更多 | - | 2020-06-22 | ||
(PI-based Regimen + Atorvastatin) | 遞壓窪顧觸憲鹽夢鹹製(鹹鏇艱膚鑰衊範憲鹽築) = 鬱膚網醖範繭壓襯構糧 積醖餘觸鹹製顧遞艱糧 (製艱齋製願積艱糧願積, 夢築繭鬱窪鏇艱製壓獵 ~ 獵蓋鑰餘膚繭夢選範膚) 更多 |
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