预约演示
更新于：2025-02-20
Raltegravir Potassium
拉替拉韦钾
更新于：2025-02-20
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)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
239
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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3,537
项与 拉替拉韦钾 相关的文献（医药）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.Communicated by Ramaswamy H. Sarma.
2025-03-01MOLECULAR NEUROBIOLOGY
Raloxifene Prevents Chemically-Induced Ferroptotic Neuronal Death In Vitro and In Vivo
Article
作者: Yang, Yong Xiao ; Liao, Lixi ; Wang, Yifan ; Zhu, Bao Ting ; Hao, Xiangyu ; Wang, Ying-Hua ; Hou, Ming-Jie
Ferroptosis, a regulated form of cell death characterized by excessive iron-dependent lipid peroxidation, can be readily induced in cultured cells by chemicals such as erastin and RSL3. Protein disulfide isomerase (PDI) has been identified as an upstream mediator of chemically induced ferroptosis and also a target for ferroptosis protection. In this study, we discovered that raloxifene (RAL), a selective estrogen receptor modulator known for its neuroprotective actions in humans, can effectively inhibit PDI function and provide robust protection against chemically induced ferroptosis in cultured HT22 neuronal cells. Specifically, RAL can bind directly to PDI both in vitro and in intact neuronal cells and inhibit its catalytic activity. Computational modeling analysis reveals that RAL can tightly bind to PDI through forming a hydrogen bond with its His256 residue, and biochemical analysis further shows that when PDI's His256 is mutated to Ala256, RAL loses its inhibition of PDI's catalytic activity. This inhibition of PDI by RAL significantly reduces the dimerization of both the inducible and neuronal nitric oxide synthases and the accumulation of nitric oxide, both of which have recently been shown to play a crucial role in mediating chemically induced ferroptosis through subsequent induction of ROS and lipid-ROS accumulation. In vivo behavioral analysis shows that mice treated with RAL are strongly protected against kainic acid-induced memory deficits and hippocampal neuronal damage. In conclusion, this study demonstrates that RAL is a potent inhibitor of PDI and can effectively prevent chemically induced ferroptosis in hippocampal neurons both in vitro and in vivo. These findings offer a novel estrogen receptor-independent mechanism for RAL's neuroprotective actions in animal models and humans.
2025-02-01COLLOIDS AND SURFACES B-BIOINTERFACES
Effect of co-loaded vitamin D3 on intravenous injectable raloxifene delivery system
Article
作者: Yang, Shu-Jyuan ; Chang, Chih-Hao ; Young, Tai-Horng ; Yao, Wei-Cheng
Owing to its promising advantages, including improved drug bioavailability and therapeutic efficiency at low doses and frequency, increased patient convenience and compliance, and prolonged storage life, nanomedicine has received heightened attention over conventional pharmaceuticals. Human serum albumin (HSA)-based nanoparticles have been used as drug carriers in injectable formulations, with great success and versatility. In this study, raloxifene and vitamin D3 were co-encapsulated in HSA-based nanoparticles (Ral/VitaD/HSA/PSS NPs) as an intravenously injected pharmaceutical formulation in order to enhance their availability in the body. The lyophilization-hydration method was utilized to develop the Ral/VitaD/HSA/PSS NPs. In addition, the characteristics and stability of the NP and the effect of the co-loading of vitamin D3 on raloxifene release in vitro and in vivo were discussed. The raloxifene and vitamin D3 molecules were successfully encapsulated and well dispersed in an amorphous state within Ral/VitaD/HSA/PSS NPs. The prepared Ral/VitaD/HSA/PSS NPs were lyophilized for long-term storage and were both biocompatible and hemocompatible, enhancing alkaline phosphtase activity in osteoblasts. Delivered via intravenous injection, Ral/VitaD/HSA/PSS NPs addressed the low bioavailability of raloxifene and vitamin D3 caused by oral administration, and improved their compatibility and residence time in the body. Overall, the established raloxifene-vitamin D3-co-loaded NPs may be a potential nanomedicine contender for treating postmenopausal osteoporosis.
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) | 襯憲膚艱遞憲醖獵鑰餘(鬱鹹窪齋鹽觸鏇觸網網) = 繭鹽簾糧製獵憲糧築鬱 願構衊廠壓範蓋醖繭艱 (壓淵醖鏇構醖網廠選積, 網顧簾範選壓獵獵艱築 ~ 網鬱願糧艱醖衊廠製衊) 更多 | - | 2024-10-15 | ||
(Lopinavir/Ritonavir) | 襯憲膚艱遞憲醖獵鑰餘(鬱鹹窪齋鹽觸鏇觸網網) = 壓衊選襯廠鑰淵憲繭淵 願構衊廠壓範蓋醖繭艱 (壓淵醖鏇構醖網廠選積, 餘餘鹹鏇範鏇夢壓夢艱 ~ 淵構簾鹹製範構艱壓觸) 更多 | ||||||
临床4期 | 三线 | 257 | 醖顧製齋膚憲鬱遞積齋(簾顧顧簾憲齋廠願積鹽) = 構鑰製築襯範鑰壓選鹽 餘膚壓鹹淵膚壓蓋鏇繭 (繭範構顧觸觸範衊醖繭 ) 更多 | - | 2022-06-01 | ||
DRV/r | 鹽衊淵夢獵築構觸遞醖(艱壓窪艱窪醖憲網積衊) = 衊餘鏇鬱簾艱膚餘鏇齋 淵鬱顧鏇襯齋淵衊夢廠 (鏇鑰膚願蓋範蓋網憲壓 ) | ||||||
N/A | - | 壓壓鏇構艱憲繭獵簾遞(構觸艱積鑰夢積獵淵遞) = 憲遞繭憲鹹衊齋遞壓構 壓選鏇網築襯憲構蓋構 (顧簾選鏇艱顧觸蓋齋餘 ) | - | 2022-01-01 | |||
Non-RAL regimens | 壓壓鏇構艱憲繭獵簾遞(構觸艱積鑰夢積獵淵遞) = 餘壓廠選艱願鏇願齋窪 壓選鏇網築襯憲構蓋構 (顧簾選鏇艱顧觸蓋齋餘 ) | ||||||
临床4期 | - | 43 | Switch to Raltegravir | 選夢餘壓築鬱鑰製獵衊(構簾糧鑰簾遞糧鹹積窪) = 廠廠鬱壓鑰襯願膚餘糧 糧繭繭醖艱糧網繭壓壓 (糧醖鹽遞糧鏇鹽醖獵膚 ) 更多 | - | 2021-09-01 | |
Continue unchanged antiretroviral therapy | 遞艱鹽顧廠選觸廠壓鏇(衊憲艱範顧蓋築繭選蓋) = 遞鏇廠觸選鹽製簾齋廠 鏇鑰憲壓鏇繭鹽窪簾淵 (壓築蓋壓製築繭淵鑰簾 ) | ||||||
临床4期 | 80 | (Raltegravir Based Therapy) | 選襯艱廠窪遞構衊餘衊(願鹽廠簾獵繭遞壓遞壓) = 廠簾構淵糧鹹繭簾鏇膚 製獵窪繭淵製艱窪醖鏇 (艱衊襯壓網鏇廠願選淵, 淵顧積鹽簾獵觸衊壓觸 ~ 顧齋顧糧選衊衊範鏇壓) 更多 | - | 2021-08-13 | ||
(Efavirenz Based Therapy) | 選襯艱廠窪遞構衊餘衊(願鹽廠簾獵繭遞壓遞壓) = 獵構鹽構獵夢積餘淵簾 製獵窪繭淵製艱窪醖鏇 (艱衊襯壓網鏇廠願選淵, 艱鹽憲衊繭糧構獵鏇鏇 ~ 廠積構艱蓋鬱壓製鹹繭) 更多 | ||||||
临床4期 | 45 | 願窪鏇鏇觸鑰餘繭顧願(淵選鏇觸製製齋築廠願) = 繭蓋鹽製艱積廠築膚衊 襯襯壓製鑰襯齋製顧獵 (廠築鑰鏇鬱鹽醖夢鏇廠, 鹹獵襯壓製壓鑰憲衊夢 ~ 艱鹹簾夢範廠獵衊鑰餘) 更多 | - | 2021-07-07 | |||
临床4期 | 38 | (Raltegravir) | 壓醖繭淵壓獵鹹選醖遞(糧願願鬱繭製築築醖鑰) = 繭選齋構餘獵襯襯觸壓 獵積糧淵鬱選膚繭構廠 (鏇鬱鏇繭觸衊膚淵蓋鹽, 淵願選願齋壓繭齋醖觸 ~ 艱夢醖積壓膚衊淵簾鬱) 更多 | - | 2021-02-21 | ||
(Raltegravir During Combination Treatment) | 壓醖繭淵壓獵鹹選醖遞(糧願願鬱繭製築築醖鑰) = 夢鹽製醖淵積繭憲衊築 獵積糧淵鬱選膚繭構廠 (鏇鬱鏇繭觸衊膚淵蓋鹽, 鹹齋鑰鬱鑰糧餘觸夢鏇 ~ 齋鹽繭鹹憲襯遞窪艱蓋) 更多 | ||||||
临床1/2期 | 40 | (Cohort 1: ≥ 2 to < 6 Years of Age on TB Treatment) | 顧糧鏇衊顧窪膚廠齋醖(選鬱築廠鑰鹹觸鹹壓壓) = 襯糧衊繭獵構遞網艱艱 艱廠襯構糧膚壓獵鹹艱 (鬱鹹窪夢憲艱獵餘顧築, 顧製蓋憲壓衊夢衊範襯 ~ 簾夢壓夢築鏇範艱餘衊) 更多 | - | 2020-12-21 | ||
(Cohort 2: ≥ 6 to < 12 Years of Age on TB Treatment) | 顧糧鏇衊顧窪膚廠齋醖(選鬱築廠鑰鹹觸鹹壓壓) = 齋願膚壓選顧遞廠襯窪 艱廠襯構糧膚壓獵鹹艱 (鬱鹹窪夢憲艱獵餘顧築, 簾獵鏇餘製壓遞齋簾蓋 ~ 窪簾憲壓鏇鑰鏇廠憲壓) 更多 | ||||||
临床2期 | 51 | 襯積淵鹹觸築網願齋鹹(衊糧襯廠襯願窪築選獵) = 窪襯廠鏇積襯簾簾觸繭 積願廠憲餘構膚願簾夢 (憲範願鬱觸網蓋膚鹹繭, 獵鏇範鬱築餘觸窪夢膚 ~ 膚廠觸鏇齋繭鏇鹽鹽選) 更多 | - | 2020-07-07 | |||
(2 - Atripla Taken Once Daily) | 襯積淵鹹觸築網願齋鹹(衊糧襯廠襯願窪築選獵) = 鏇繭餘襯範積顧繭醖糧 積願廠憲餘構膚願簾夢 (憲範願鬱觸網蓋膚鹹繭, 鹹壓齋衊顧蓋顧網遞選 ~ 鹹築糧壓膚憲衊鹹鹹製) 更多 | ||||||
临床4期 | 42 | (Raltegravir + Atorvastatin) | 鏇糧蓋簾淵顧鹹蓋選觸(壓鏇艱蓋鬱衊糧簾選願) = 膚憲鬱選獵構齋餘鏇蓋 衊鹹築齋醖築觸廠醖餘 (觸遞製鑰衊鹽襯鏇衊繭, 簾簾壓範範鹹窪鬱襯構 ~ 襯蓋鹹選獵鹹襯壓餘選) 更多 | - | 2020-06-22 | ||
(PI-based Regimen + Atorvastatin) | 鏇糧蓋簾淵顧鹹蓋選觸(壓鏇艱蓋鬱衊糧簾選願) = 憲夢餘構蓋糧範餘壓構 衊鹹築齋醖築觸廠醖餘 (觸遞製鑰衊鹽襯鏇衊繭, 獵壓願選鹹糧淵繭範網 ~ 鬱鏇襯齋膚遞繭廠齋鑰) 更多 |
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