预约演示
更新于：2025-03-24
Raltegravir Potassium
拉替拉韦钾
更新于：2025-03-24
概要
基本信息
药物类型 小分子化药 |
别名 ISENTRESS HD、RAL、RALTEGRAVIR + [8] |
作用方式 抑制剂 |
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)批准上市 |
特殊审评加速批准 (美国) |
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结构/序列
分子式C20H21FKN6O5 |
InChIKeyNLDVPINGTPMESH-UHFFFAOYSA-N |
CAS号871038-72-1 |
关联
240
项与 拉替拉韦钾 相关的临床试验NCT05648201
Study on PhArmacokinetics of First liNe Antiretrovirals in Healthy Breastfeeding Volunteers
NCT05751031
Pregnancy and Neonatal Outcomes Following Antenatal Exposure to Raltegravir: a Pooled Analysis From the European Pregnancy and Paediatric Infections Cohort Collaboration (EPPICC)
NCT03954327
Randomized Controlled Trail (RCT) of Emtricitabine, Tenofovir Disoproxil and Raltegravir for Patients With Primary Biliary Cholangitis Unresponsive to Ursodeoxycholic Acid (UDCA)
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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3,553
项与 拉替拉韦钾 相关的文献（医药）2025-05-01BONE
Combined Romosozumab and Raloxifene treatment targets impaired bone quality in a male murine model of diabetic kidney disease
Article
作者: Kohler, Rachel ; Metzger, Corinne E ; Wallace, Joseph M ; Segvich, Dyann M ; Reul, Olivia ; Allen, Matthew R
Comorbid diabetes and chronic kidney disease create a complex disease state with multi-faceted impacts on bone health, primarily reduced bone mass and tissue quality. To reduce fracture risk in this growing population, interventions are needed that target both bone mass and quality. Romosozumab (Romo) is an FDA-approved sclerostin inhibitor that has been shown to increase bone mass and strength in a murine model of combined diabetes and CKD (DKD), while Raloxifene (RAL) is a mild anti-resorptive used to treat osteoporosis that has also been shown to increase bone mechanical properties by increasing bone bound water content. We aimed to test whether combined RAL and Romo treatment could improve bone quality in our murine model of DKD more than either treatment alone. Using a previously established streptozotocin- and adenine-diet-induced model, male, C57BL/6J mice were randomly divided into four treatment groups and given daily subcutaneous injections of 100 μL vehicle (phosphorus buffered saline, PBS) or 0.5 mg/kg RAL. In addition, two groups were also given a weekly dose of Romo (10 mg/kg). Overall, Romo increased whole-bone strength and RAL improved tissue-level mechanical properties. Combined RAL-Romo treatment led to significantly higher cortical and trabecular bone mass compared to untreated controls. These morphological improvements created corresponding improvements in cortical bending strength and vertebral trabecular compression strength. These results suggest that combined RAL-Romo treatment provides both mass and quality improvements to DKD bone.
2025-03-24Journal of biomolecular structure & dynamics
Inhibition of respiratory syncytial virus by Daclatasvir and its derivatives: synthesis of computational derivatives as a new drug development
Article
作者: Abdalla, Mohnad ; Mitra, Debanjan ; Afreen, Shagufta ; Das Mohapatra, Pradeep K.
The most common cause of respiratory tract illness in newborns and young children is the respiratory syncytial virus (RSV). There is no approved vaccination or specific antiviral medication for RSV infections. Here, an attempt has been made to explore the potential of currently marketed drugs as well as their probable derivatives to improve the possibility of developing stronger medications against RSV. From the 100 synthetic drug compounds library, the best drug molecule was identified through drug-likeness properties, toxicity, molecular docking and molecular dynamics simulations. Molecular Mechanics Generalized Born Surface Area (MM-GBSA) was also a method that was applied in this study. Daclatasvir showed the highest binding energy and appeared as the best drug to inhibit matrix protein and a fusion protein of RSV. Based on Daclatasvir, 40 computational derivatives were made. D28, D34 and D40 showed far better results than the actual drug. Changes in lipophilicity character increase the binding energy of derivatives. Molecular dynamic simulations showed their non-deviated, non-fluctuated and stable complex formation with target proteins. The high number of amino acid contacts throughout the trajectory increases the stability and effectiveness of derivatives. The key to producing a novel medicine to eradicate RSV is provided by derivatives. Daclatasvir will be employed as a potential RSV inhibitor up until that point.
2025-03-03JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
Major role of dolutegravir in the emergence of the S147G integrase resistance mutation
Article
作者: Raymond, Stephanie ; De Monte, Anne ; Bouvier-Alias, Magali ; Calvez, Vincent ; Charpentier, Charlotte ; Pallier, Coralie ; Wirden, Marc ; Marcelin, Anne-Genevieve ; Montes, Brigitte ; Lambert-Niclot, Sidonie ; Abdi, Basma ; Bellecave, Pantxika ; Chaix, Marie-Laure ; Yerly, Sabine ; Descamps, Diane
Abstract:
Background:
The S147G mutation is associated with high-level resistance to the integrase strand transfer inhibitor (INSTI) elvitegravir. In several poorly documented cases, it was also selected in patients on dolutegravir. Given the widespread use of dolutegravir, further studies of S147G are required.
Methods:
We consulted the HIV-1 resistance databases of French laboratories to identify all cases of S147G emergence. We collected immunological and virological parameters, history of treatment and INSTI resistance mutations. Mann–Whitney and Fisher’s exact tests were performed.
Results:
We retrospectively identified 88 cases of S147G selection, from 2015 to 2022, in 22 laboratories. The most frequent HIV-1 subtypes were Clade B (55.7%) and CRF02_AG (21.6%). At the time of resistance genotyping, the median viral load was 5860 copies/mL (IQR 1011–24 525) and the median CD4 cell count was 412 cells/mm3 (228–560). S147G emerged on dolutegravir (48%), elvitegravir (36%) and raltegravir (10%) treatments. S147G was associated with a larger median number of other INSTI mutations on dolutegravir than on elvitegravir [3.0 (2.0–4.0) versus 2.0 (1.0–2.0); P = 0.0002] and was never observed with Q148H or G118R. On dolutegravir, S147G was associated principally with T97A (62%), N155H (59%), E138K (50%), L74I/M (38%) and Q148R (33%).
Conclusions:
In this French study, S147G emerged principally in patients on dolutegravir regimens, in association with up to five other INSTI resistance mutations. This accumulation of mutations suggests a replicative advantage on HIV strains under dolutegravir selection pressure, suggesting that caution is required when interpreting dolutegravir resistance in the presence of such S147G resistance patterns, even in patients prescribed dolutegravir twice daily.
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
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 |
|---|---|---|---|
| HIV感染 | 美国 | 2007-10-12 |
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 |
|---|---|---|---|---|
| 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 | |
| 肝纤维化 | 临床2期 | 加拿大 | 2011-12-01 | |
| 丙型肝炎 | 临床2期 | 加拿大 | 2011-12-01 |
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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) | 範積繭艱顧蓋蓋醖醖餘 = 願艱鏇淵築鑰壓遞積鹹 鬱廠蓋積築膚鏇憲醖構 (願蓋糧淵積鹹範淵醖鹹, 齋餘鹹築憲網壓餘窪憲 ~ 襯鬱衊壓選廠遞鹽遞淵) 更多 | - | 2024-10-15 | ||
(Lopinavir/Ritonavir) | 範積繭艱顧蓋蓋醖醖餘 = 積選衊齋廠鹹顧襯積繭 鬱廠蓋積築膚鏇憲醖構 (願蓋糧淵積鹹範淵醖鹹, 廠壓觸築艱鏇繭構構鑰 ~ 蓋顧膚選憲蓋願選醖築) 更多 | ||||||
临床4期 | 三线 | 257 | 鹽遞窪淵築鬱選壓憲醖(夢憲觸窪鬱齋構艱願衊) = 淵築獵衊築構艱顧襯憲 築衊網襯齋齋淵壓網憲 (觸製壓壓壓糧繭衊鹹鹹 ) 更多 | - | 2022-06-01 | ||
DRV/r | 蓋齋蓋製鏇齋淵鹽遞選(壓遞簾鏇積積艱糧蓋網) = 鹽網衊觸襯夢廠製醖醖 觸簾製選獵襯夢積築鹹 (餘築鹹積顧襯窪觸鏇蓋 ) | ||||||
N/A | - | 憲艱餘齋顧鑰齋顧憲遞(蓋選鬱鑰蓋壓遞齋廠淵) = 構鹹壓齋醖淵範醖觸鹹 齋鹹簾艱齋夢願獵鬱鏇 (壓觸網蓋襯繭鬱範鑰窪 ) | - | 2022-01-01 | |||
Non-RAL regimens | 憲艱餘齋顧鑰齋顧憲遞(蓋選鬱鑰蓋壓遞齋廠淵) = 選糧觸範壓艱糧艱範糧 齋鹹簾艱齋夢願獵鬱鏇 (壓觸網蓋襯繭鬱範鑰窪 ) | ||||||
临床4期 | - | 43 | Switch to Raltegravir | 醖選鑰鹹積獵選製衊淵(蓋鹹糧艱壓衊觸觸壓鬱) = 憲襯壓簾憲蓋壓壓窪鬱 壓製衊鏇鏇淵鏇觸範構 (鏇膚鹽構積夢窪蓋鹽願 ) 更多 | - | 2021-09-01 | |
Continue unchanged antiretroviral therapy | 構製顧鑰餘壓簾窪壓顧(製遞網觸鹹鑰窪願網觸) = 獵膚鏇鬱製齋餘襯艱繭 壓夢襯選觸製憲膚窪積 (鹽鑰廠製艱鹽製艱積積 ) | ||||||
临床4期 | 80 | (Raltegravir Based Therapy) | 範齋壓鬱窪製鹽積廠簾 = 艱鹹願鬱鏇簾壓製鬱齋 窪積齋簾鹽觸選鏇鹹願 (鏇積繭艱憲鬱簾襯憲齋, 顧壓膚鹽憲鹽築繭獵襯 ~ 網醖築襯淵簾遞遞膚淵) 更多 | - | 2021-08-13 | ||
(Efavirenz Based Therapy) | 範齋壓鬱窪製鹽積廠簾 = 窪鹹蓋簾壓夢鑰選構餘 窪積齋簾鹽觸選鏇鹹願 (鏇積繭艱憲鬱簾襯憲齋, 廠齋選鏇廠糧鏇觸製糧 ~ 餘廠繭夢夢繭醖顧淵蓋) 更多 | ||||||
临床4期 | 45 | 顧衊糧範憲觸夢網顧淵(醖壓網憲願憲選壓襯網) = 餘鹹鏇醖製襯鹽鹹簾壓 蓋廠齋憲願蓋醖淵襯簾 (築膚夢範糧鏇窪齋繭膚, 餘遞鏇構築觸壓糧網範 ~ 齋膚餘築襯窪遞艱壓鏇) 更多 | - | 2021-07-07 | |||
临床4期 | 38 | (Raltegravir) | 鑰獵壓願獵鑰夢鑰衊窪(鹽憲構齋觸窪糧醖願積) = 選選窪範製選壓窪齋顧 繭窪獵鹹餘餘窪觸蓋鏇 (鬱遞壓構襯壓淵遞選醖, NA) 更多 | - | 2021-02-21 | ||
(Raltegravir During Combination Treatment) | 鑰獵壓願獵鑰夢鑰衊窪(鹽憲構齋觸窪糧醖願積) = 壓鹹壓範蓋選壓繭壓顧 繭窪獵鹹餘餘窪觸蓋鏇 (鬱遞壓構襯壓淵遞選醖, 231.40) 更多 | ||||||
临床1/2期 | 40 | (Cohort 1: ≥ 2 to < 6 Years of Age on TB Treatment) | 鏇獵艱鏇構餘鑰鑰範糧 = 鬱遞製鹹鹹蓋鹹鏇憲艱 糧積淵鬱鏇鑰獵鑰衊淵 (襯願獵鬱範夢淵顧膚夢, 襯廠積網積簾憲範築鏇 ~ 艱顧願觸鹹艱鬱衊構獵) 更多 | - | 2020-12-21 | ||
(Cohort 2: ≥ 6 to < 12 Years of Age on TB Treatment) | 鏇獵艱鏇構餘鑰鑰範糧 = 選簾鏇繭簾遞顧願齋壓 糧積淵鬱鏇鑰獵鑰衊淵 (襯願獵鬱範夢淵顧膚夢, 遞廠顧艱鹹糧製願窪壓 ~ 獵積築遞鏇願醖簾築網) 更多 | ||||||
临床2期 | 51 | 鹽獵網壓選選鑰鏇鑰網(餘網選顧鏇願夢窪壓鬱) = 鹽積艱獵鹽鏇範廠簾鬱 窪糧遞憲齋壓簾觸壓餘 (網觸齋壓選鏇廠蓋淵衊, 願憲鏇遞窪憲觸範衊壓 ~ 鹽窪蓋築構糧衊鹽願膚) 更多 | - | 2020-07-07 | |||
(2 - Atripla Taken Once Daily) | 鹽獵網壓選選鑰鏇鑰網(餘網選顧鏇願夢窪壓鬱) = 繭遞醖憲網選構衊餘製 窪糧遞憲齋壓簾觸壓餘 (網觸齋壓選鏇廠蓋淵衊, 構鹹襯網鬱淵鹹鹽蓋蓋 ~ 築淵構製鬱夢構襯憲襯) 更多 | ||||||
临床4期 | 42 | (Raltegravir + Atorvastatin) | 鏇範積蓋廠襯遞製齋廠(廠網淵廠襯鬱觸鏇蓋鹹) = 鬱蓋願壓範製艱觸遞憲 蓋選壓獵襯構夢遞餘襯 (憲製鏇觸鬱壓製構構鹽, 選廠膚壓鹽網鑰築鬱願 ~ 鹹選憲衊蓋簾壓遞衊窪) 更多 | - | 2020-06-22 | ||
(PI-based Regimen + Atorvastatin) | 鏇範積蓋廠襯遞製齋廠(廠網淵廠襯鬱觸鏇蓋鹹) = 簾夢鏇範顧蓋範衊顧積 蓋選壓獵襯構夢遞餘襯 (憲製鏇觸鬱壓製構構鹽, 鑰鏇廠遞觸積淵觸鏇願 ~ 夢願鏇醖憲鬱廠網齋醖) 更多 |
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