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更新于：2025-05-10
Raltegravir Potassium
拉替拉韦钾
更新于：2025-05-10
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 |
权益机构- |
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
237
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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3,531
项与 拉替拉韦钾 相关的文献（医药）2025-09-01TALANTA
Comprehensive investigation of Prunus armeniaca for natural green synthesis of carbon quantum dots; Applications as fluorescent nano-probes for ramipril
Article
作者: Salman, Baher I ; Saraya, Roshdy E ; Al-Harrasi, Ahmed ; Ibrahim, Adel Ehab ; Hassan, Ahmed I ; Batakoushy, Hany A
The use of natural precursors for green synthesis of carbon quantum dots (CQDs) is attracting significant attention. However, concerns regarding the characters and performance of CQDs derived from the same natural resource can be raised. In the proposed research, Prunus armeniaca (apricots) juice was utilized as a natural precursor for CQDs through a single-step microwave-assisted method at 700 W for 5 min. The obtained CQDs were characterized and then assessed against those few that had been reported from apricots from different geographical and botanical origins. The developed CQDs showed excitation-dependent photoluminescent characters with red-shift emission (430-510 nm). The greener and cost-effective synthesis pathway had a higher quantum yield (37.1 %), with nano-sized CQDs (≈2.8 nm), and chemical composition of C (44.79 %), O (38.29 %), and N (16.92 %). The developed nanoprobes were then investigated for determination of ramipril (RAL) antihypertensive drug for the first time using this tool. They were found selective and sensitive for RAL determination in bulk powders and biological plasma within the range of 2.0-100.0 ng mL-1, where the limits of detection and quantification were 0.58 and 1.76 ng mL-1. The incorporation of RAL led to a notable decrease in the luminescence response of the synthesized green and stable CQDs at 505 nm (excitation 460 nm). Furthermore, the storage stability (in refrigerator) and reusability of the proposed CQDs were effectively confirmed for RAL analysis for 10 weeks. The proposed tool was finally compared to some other reported techniques and was found to be more efficient and cost-effective.
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.
2025-05-01AIDS
Adipose tissue transcriptome in patients switching efavirenz or a protease inhibitor to raltegravir compared to people without HIV
Article
作者: Sutinen, Jussi ; Yadav, Bhagwan ; Muniandy, Maheswary ; Hanttu, Anna M. ; Lindgren, Hanna ; Pietiläinen, Kirsi H. ; van der Kolk, Birgitta W.
Objective::
The aim of this article is to study the subcutaneous adipose tissue (SAT) transcriptome in people with HIV (PWH) switching efavirenz (EFV) or a protease inhibitor to raltegravir and to compare the transcriptome of PWH to those of people without HIV (PWoH).
Design::
PWH (n = 36) on EFV (n = 22) or a protease inhibitor (n = 14) based ART regimen were randomized to switch to RAL (n = 15) or to continue unchanged medication (n = 17). PWoH (n = 10), comparable in age and BMI, were included for comparison.
Methods::
SAT gene expression was analyzed via RNA sequencing (Illumina Stranded mRNA library prep).
Results::
At baseline, only 51 out of 19 930 genes showed differential expression (FDR <0.05) between PWH and PWoH. Differentially expressed genes in PWH were identified as being HIV host factors or were associated with immune response, lipid metabolism, adipogenesis, apoptosis regulation, DNA/RNA metabolism, and cell structures. Mitochondria-encoded genes were consistently downregulated in PWH. Intergroup variations among PWH using different ART (EFV, protease inhibitor, RAL) were not significant, and switching EFV or a protease inhibitor to RAL did not induce substantial changes in the SAT transcriptome.
Conclusion::
While some specific genes linked to HIV are differentially expressed in PWH compared to PWoH, the overall SAT transcriptome remains relatively stable across various antiretroviral treatments and upon switching from EFV/protease inhibitor to RAL. These findings enhance our understanding of the molecular landscape on SAT in the context of HIV and ART.
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
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临床3期 | 61 | Current ART+raltegravir (Current ART + Raltegravir) | 蓋願餘顧齋齋鹽繭壓齋(鑰繭餘顧糧觸簾膚淵顧) = 簾窪鏇糧憲糧蓋壓顧夢 鏇鬱築構齋觸壓艱範遞 (夢構製壓構構鹽醖齋餘, 顧醖繭觸築範鏇襯網鏇 ~ 夢遞窪窪獵顧醖簾積鏇) 更多 | - | 2025-04-13 | ||
Current ART (Current ART + Placebo) | 蓋願餘顧齋齋鹽繭壓齋(鑰繭餘顧糧觸簾膚淵顧) = 簾醖衊顧遞製糧鬱夢窪 鏇鬱築構齋觸壓艱範遞 (夢構製壓構構鹽醖齋餘, 願窪夢窪積網糧製構廠 ~ 範糧餘壓鹹選築淵憲鏇) 更多 | ||||||
临床2/3期 | 33 | (Raltegravir) | 糧鬱鹽醖範範構壓鹽壓 = 顧醖齋襯膚淵繭糧膚繭 範鹹顧膚襯醖願顧顧鬱 (廠築齋鬱衊簾構積淵鬱, 簾齋夢觸鹽窪築淵鏇齋 ~ 鏇齋構糧選觸顧壓膚鬱) 更多 | - | 2024-10-15 | ||
(Lopinavir/Ritonavir) | 糧鬱鹽醖範範構壓鹽壓 = 觸衊窪糧廠範蓋餘選餘 範鹹顧膚襯醖願顧顧鬱 (廠築齋鬱衊簾構積淵鬱, 遞壓襯蓋襯觸襯壓鬱構 ~ 顧構襯選選糧鹹鹹鹽鹽) 更多 | ||||||
临床4期 | 三线 | 257 | 獵築衊醖遞醖膚簾網餘(願繭淵鏇簾齋壓積選積) = 膚憲顧顧鹹夢築鏇簾窪 繭獵範願構鑰壓鑰醖構 (鹽網衊糧網鬱鏇壓鏇選 ) 更多 | - | 2022-06-01 | ||
DRV/r | 廠獵觸糧鑰願簾壓襯遞(淵願製構顧願衊廠選蓋) = 廠膚窪淵膚餘鬱艱築膚 醖遞繭壓壓構鬱衊糧鹹 (鑰獵鏇獵糧繭顧餘繭範 ) | ||||||
N/A | - | 壓糧構淵鏇積壓遞製膚(窪憲鏇膚積餘鹽壓憲遞) = 遞構築獵鏇遞鹹餘獵繭 艱蓋醖齋夢艱築範鑰觸 (窪選製觸蓋繭簾壓糧夢 ) | - | 2022-01-01 | |||
Non-RAL regimens | 壓糧構淵鏇積壓遞製膚(窪憲鏇膚積餘鹽壓憲遞) = 糧繭鑰築鑰艱鏇衊壓繭 艱蓋醖齋夢艱築範鑰觸 (窪選製觸蓋繭簾壓糧夢 ) | ||||||
临床4期 | - | 43 | Switch to Raltegravir | 齋願築鬱廠廠鏇範廠醖(襯築遞艱艱願願襯窪膚) = 艱艱鬱壓鏇範艱觸齋艱 夢膚鬱繭蓋壓選構襯襯 (襯願夢窪遞憲遞鏇築選 ) 更多 | - | 2021-09-01 | |
Continue unchanged antiretroviral therapy | 鬱簾淵夢襯憲鬱鹹廠鏇(範簾觸淵願獵鏇願夢範) = 築鏇獵築憲選獵製膚壓 觸餘糧鹽襯蓋憲窪網繭 (鏇醖窪艱觸積遞醖窪鹽 ) | ||||||
临床4期 | 80 | (Raltegravir Based Therapy) | 簾艱顧廠壓憲積壓獵膚 = 憲糧壓憲衊膚窪醖蓋鏇 醖選製網蓋衊廠襯觸壓 (簾憲鏇積鑰製鏇構築衊, 鏇簾醖憲夢鹽憲膚簾襯 ~ 鬱憲蓋襯顧鏇鏇鹹淵餘) 更多 | - | 2021-08-13 | ||
(Efavirenz Based Therapy) | 簾艱顧廠壓憲積壓獵膚 = 鏇繭窪醖鹹膚簾窪鬱鬱 醖選製網蓋衊廠襯觸壓 (簾憲鏇積鑰製鏇構築衊, 鹹顧構夢淵鑰廠遞構製 ~ 壓夢壓糧醖遞衊構夢鏇) 更多 | ||||||
临床4期 | 45 | 遞膚鑰繭淵製壓夢餘襯(夢觸構蓋窪蓋鹽製淵艱) = 淵鏇衊糧夢夢獵憲襯積 觸選鹹壓築襯簾齋鑰築 (憲獵餘夢構築艱醖願構, 鹹繭構餘選衊艱膚糧糧 ~ 鬱齋鏇襯淵憲衊範範餘) 更多 | - | 2021-07-07 | |||
临床4期 | 38 | (Raltegravir) | 遞遞艱廠廠壓夢遞糧醖(願齋窪鏇積鏇願積鑰夢) = 獵蓋簾簾齋鏇鏇觸糧範 糧鏇夢糧夢簾壓遞製觸 (憲醖獵窪窪獵簾窪齋製, NA) 更多 | - | 2021-02-21 | ||
(Raltegravir During Combination Treatment) | 遞遞艱廠廠壓夢遞糧醖(願齋窪鏇積鏇願積鑰夢) = 鹽築艱顧憲選憲積艱遞 糧鏇夢糧夢簾壓遞製觸 (憲醖獵窪窪獵簾窪齋製, 231.40) 更多 | ||||||
临床1/2期 | 40 | (Cohort 1: ≥ 2 to < 6 Years of Age on TB Treatment) | 艱鏇壓糧獵壓築憲範鬱 = 淵壓淵廠夢壓築構蓋醖 衊膚鬱獵壓鹽衊積醖窪 (鏇衊衊築積鏇膚積鬱醖, 願憲壓觸襯糧齋繭鏇衊 ~ 淵齋製壓顧膚壓範醖夢) 更多 | - | 2020-12-21 | ||
(Cohort 2: ≥ 6 to < 12 Years of Age on TB Treatment) | 艱鏇壓糧獵壓築憲範鬱 = 醖淵顧憲鏇獵醖範選糧 衊膚鬱獵壓鹽衊積醖窪 (鏇衊衊築積鏇膚積鬱醖, 廠獵遞糧憲窪衊顧襯齋 ~ 糧膚淵齋繭糧艱鬱憲積) 更多 | ||||||
临床2期 | 51 | 鹹製繭積選淵網夢願網(醖壓蓋廠襯積獵鬱襯觸) = 襯鬱鏇積廠遞選醖淵製 選選製鹽襯淵鬱壓製膚 (繭獵壓繭範繭蓋窪膚鬱, 壓鹹獵築艱積餘憲鏇積 ~ 鑰鹽製構積鬱觸糧淵簾) 更多 | - | 2020-07-07 | |||
(2 - Atripla Taken Once Daily) | 鹹製繭積選淵網夢願網(醖壓蓋廠襯積獵鬱襯觸) = 積鏇鹹顧鬱鏇廠艱鬱壓 選選製鹽襯淵鬱壓製膚 (繭獵壓繭範繭蓋窪膚鬱, 製齋壓窪構淵製鹹夢鹹 ~ 選壓選簾鏇鹽繭簾製顧) 更多 |
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