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更新于：2025-01-09
Dolutegravir Sodium
多替拉韦钠
更新于：2025-01-09
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2013-08-12), |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、孤儿药 (日本) |
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结构/序列
分子式C20H19F2N3NaO5 |
InChIKeyFOZLBAIXQATFFW-VSLILLSYSA-N |
CAS号1051375-19-9 |
关联
257
项与 多替拉韦钠 相关的临床试验NCT06747507
Investigating the Optimal Management of Dolutegravir Resistance: an Open-label Randomised Controlled Trial of Maintaining Dolutegravir or Switch to Ritonavir-boosted Darunavir
IRCT20240803062623N4
Bioequivalence study of two Dolutegravir 50 mg tablet manufactured by tadbir kalaye jam company in comparison with Tivicay
NCT06497465
Dolutegravir Plus Lamivudine (DTG/3TC) Dual Therapy Versus Dolutegravir With TDF-lamivudine (DTG + TDF/3TC) Among Antiretroviral naïve People With HIV and TB Receiving Rifampin-based TB Treatment
100 项与 多替拉韦钠 相关的临床结果
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100 项与 多替拉韦钠 相关的转化医学
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100 项与 多替拉韦钠 相关的专利（医药）
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2,739
项与 多替拉韦钠 相关的文献（医药）2025-03-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Synthesis of dolutegravir derivatives modified by 1,2,3-triazole structure and their anti-inflammatory activity in LPS-induced BV2 cells
Article
作者: Wang, Jianji ; Wang, Lan ; Zhang, Xuanwei ; Hou, Xixi ; Wang, Xi ; Mao, Longfei
Given the promising anti-inflammatory activity of the HIV integrase inhibitor dolutegravir and the widespread use of the 1,2,3-triazole structure in anti-inflammatory drug development, this study aimed to enhance dolutegravir's efficacy by introducing a 1,2,3-triazole group. As a result, four series of dolutegravir derivatives were synthesized. Screening these derivatives for anti-inflammatory activity in microglial cells revealed that compound 6k demonstrated the most potent anti-inflammatory effect without significant cytotoxicity. Specifically, 6k significantly reduced the transcription levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α in lipopolysaccharide (LPS)-induced BV-2 microglial cells. Additionally, 6k decreased the LPS-induced overproduction of inflammatory mediators such as nitric oxide (NO), IL-6, and TNF-α. Further investigation into the upstream inflammatory enzymes iNOS and COX-2 showed that 6k markedly reduced their transcription and protein levels. To elucidate the mechanism underlying the anti-inflammatory effects of dolutegravir derivatives, it was found that compound 6k modulates microglial inflammation by inhibiting the phosphorylation and nuclear translocation of signal transducer and activator of transcription 1/3 (STAT1/3). Moreover, acute toxicity testing in mice indicated that compound 6k exhibited low toxicity, suggesting its potential as a lead compound for the treatment of neuroinflammation.
2025-02-01AIDS
Adverse perinatal outcomes associated with different classes of antiretroviral drugs in pregnant women with HIV
Article
作者: Hemelaar, Joris ; Thompson, Lucy ; Kumarendran, Mary ; Portwood, Clara ; Brandon, Zoe ; Hey, Molly ; Sexton, Harriet ; Kirtley, Shona
Objective::
Women with HIV (WHIV) are at an increased risk of adverse perinatal outcomes compared to women without HIV, despite antiretroviral therapy (ART). There is evidence that the risk of adverse perinatal outcomes may differ according to ART regimen. We aimed to assess the risk of adverse perinatal outcomes among WHIV receiving different classes of ART, compared to women without HIV.
Design::
A systematic review and meta-analysis
Methods::
We searched Medline, CINAHL, Global Health, and EMBASE for studies published between January 1, 1980, and July 14, 2023. We included studies which assessed the risk of 11 predefined adverse perinatal outcomes among WHIV receiving nonnucleoside reverse transcriptase inhibitor (NNRTI)-based ART, protease inhibitor based ART or integrase strand transfer inhibitor (INSTI)-based ART, compared to women without HIV. The perinatal outcomes assessed were preterm birth (PTB), very PTB (VPTB), spontaneous PTB (sPTB), low birthweight (LBW), very LBW (VLBW), term LBW, preterm LBW, small for gestational age (SGA), very SGA (VSGA), stillbirth and neonatal death (NND). Random effects meta-analyses examined the risk of each adverse outcome in WHIV receiving NNRTI-based, protease inhibitor based, or INSTI-based ART, compared with women without HIV. Subgroup and sensitivity analyses were conducted based on country income status, study quality, and timing of ART initiation. The protocol is registered with PROSPERO, CRD42021248987.
Results::
Of 108 720 identified citations, 22 cohort studies including 191 857 women were eligible for analysis. We found that WHIV receiving NNRTI-based ART (mainly efavirenz or nevirapine) are at an increased risk of PTB (risk ratio 1.40, 95% confidence interval 1.27–1.56), VPTB (1.94, 1.25–3.01), LBW (1.63, 1.30–2.04), SGA (1.53, 1.17–1.99), and VSGA (1.48, 1.16–1.87), compared with women without HIV. WHIV receiving protease inhibitor based ART (mainly lopinavir/ritonavir or unspecified) are at an increased risk of PTB (1.88, 1.55–2.28), VPTB (2.06, 1.01–4.18), sPTB (16.96, 1.01–284.08), LBW (2.90, 2.41–3.50), VLBW (4.35, 2.67–7.09), and VSGA (2.37, 1.84–3.05), compared with women without HIV. WHIV receiving INSTI-based ART (mainly dolutegravir) are at an increased risk of PTB (1.17, 1.06–1.30) and SGA (1.20, 1.08–1.33), compared with women without HIV.
Conclusion::
The risks of adverse perinatal outcomes are higher among WHIV receiving ART compared with women without HIV, irrespective of the class of ART drugs. This underlines the need to further optimize ART in pregnancy and improve perinatal outcomes of WHIV.
2025-01-03JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
Comparing the long-term effectiveness and safety of dolutegravir/lamivudine versus bictegravir/emtricitabine/tenofovir alafenamide fumarate as first-line regimens: a real life multicentre cohort
Article
作者: Ciccullo, Arturo ; Di Giambenedetto, Simona ; Mussini, Cristina ; Grimaldi, Alessandro ; Rusconi, Stefano ; Lagi, Filippo ; Borghetti, Alberto ; Baldin, Gianmaria ; Cossu, Maria Vittoria ; Cervo, Adriana ; Antinori, Spinello ; Giacomelli, Andrea ; Moschese, Davide ; Sterrantino, Gaetana
Abstract:
Objectives:
We compared the effectiveness and safety of bictegravir/emtricitabine/tenofovir alafenamide fumarate (BIC/FTC/TAF) and dolutegravir plus lamivudine (DTG + 3TC) in our cohort of treatment-naive people with HIV (PWH).
Methods:
In a multicentre cohort of treatment-naive PWH starting a first-line regimen with either dolutegravir plus lamivudine or BIC/FTC/TAF, Kaplan–Meier survival analysis was used to estimate time to virological failure (VF) and time to treatment discontinuation (TD), whereas Cox regression was used to evaluate predictors of VF and TD. Changes in CD4+ cell count were assessed via non-parametric tests, and linear regression analyses were performed to explore predictors of CD4+ cell count changes.
Results:
One hundred and seventy individuals were included: 66 started dolutegravir plus lamivudine (DTG group) and 104 started BIC/FTC/TAF (BIC group). During follow-up, we observed two VFs in the DTG group [1.7 per 100 person-years of follow-up (PYFU)] and two in the BIC group (1.7 per 100 PYFU). Estimated probability of remaining free from VF at Week 144 was 95.9% in the DTG group and 95.2% in the BIC group (log-rank P = 0.955). Four TDs were observed in the DTG group (3.4 per 100 PYFU) and 21 in the BIC group (17.6 per 100 PYFU). Estimated probability of maintaining the study regimen at Week 144 was 90.3% in the DTG group and 70.0% in the BIC group; individuals in the BIC group had a higher probability of TD (log-rank P = 0.003). In both groups, the CD4+ count improved significantly during follow-up.
Conclusions:
Our study shows that both strategies are effective and safe, with few VFs and TDs due to tolerability issues.
100 项与 多替拉韦钠 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 | 2013-08-12 |
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 |
|---|---|---|---|---|
| 结核 | 临床3期 | 巴西 | 2025-04-14 | |
| 怀孕 | 临床3期 | 南非 | 2017-03-14 | |
| 怀孕 | 临床3期 | 乌干达 | 2017-03-14 | |
| 潜伏性结核 | 临床2期 | 美国 | 2021-02-27 | |
| 潜伏性结核 | 临床2期 | 博茨瓦纳 | 2021-02-27 | |
| 潜伏性结核 | 临床2期 | 海地 | 2021-02-27 | |
| 潜伏性结核 | 临床2期 | 马拉维 | 2021-02-27 | |
| 潜伏性结核 | 临床2期 | 南非 | 2021-02-27 | |
| 潜伏性结核 | 临床2期 | 泰国 | 2021-02-27 | |
| 潜伏性结核 | 临床2期 | 津巴布韦 | 2021-02-27 |
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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4期 | 828 | ritonavir-boosted darunavir plus two NRTIs | 廠膚壓壓鹹壓鬱夢廠蓋(糧衊繭鏇鬱廠壓憲範簾) = 觸壓鹽壓鏇選願鹹醖淵 廠鏇願願艱鑰鹽遞顧選 (鏇鏇遞襯選夢選鑰鹹鑰 ) | 积极 | 2024-07-01 | ||
ritonavir-boosted darunavir plus dolutegravir | 廠膚壓壓鹹壓鬱夢廠蓋(糧衊繭鏇鬱廠壓憲範簾) = 醖鹽顧範淵獵願構顧鹹 廠鏇願願艱鑰鹽遞顧選 (鏇鏇遞襯選夢選鑰鹹鑰 ) | ||||||
临床1期 | 41 | (Part 1:Treatment A:GSK3640254 25mg+GSK3640254 100mg+DTG 50 mg) | 觸願艱鏇鏇窪夢糧餘膚(繭廠顧夢築範鏇鏇壓憲) = 選壓鏇淵壓憲齋夢鹽蓋 範艱糧蓋繭蓋糧衊積觸 (遞窪窪鏇廠壓製顧餘醖, 壓築繭範蓋獵遞醖築遞 ~ 構艱鬱醖獵製鏇淵簾遞) 更多 | - | 2024-03-12 | ||
(Part 1:Treatment B:GSK3640254/DTG 150/50 mg(Monolayer Tablet)) | 觸願艱鏇鏇窪夢糧餘膚(繭廠顧夢築範鏇鏇壓憲) = 範糧膚鏇範繭顧醖網憲 範艱糧蓋繭蓋糧衊積觸 (遞窪窪鏇廠壓製顧餘醖, 鹽鹹築夢窪淵襯餘糧醖 ~ 鏇觸壓範夢夢構範觸夢) 更多 | ||||||
临床2/3期 | 186 | (Dolutegravir) | 衊積願壓蓋夢窪範餘網(遞簾憲醖餘遞網醖繭膚) = 鬱醖艱膚範鹽壓鬱衊構 範蓋願壓獵構壓廠簾範 (網淵顧選餘繭蓋淵願鹹, 選蓋憲鬱構廠積淵蓋衊 ~ 鑰顧窪獵獵鹹簾鬱製獵) 更多 | - | 2023-12-14 | ||
Efavirenz-based regimens (Efavirenz) | 衊積願壓蓋夢窪範餘網(遞簾憲醖餘遞網醖繭膚) = 鬱鏇蓋膚願衊鹽艱衊鏇 範蓋願壓獵構壓廠簾範 (網淵顧選餘繭蓋淵願鹹, 壓築願窪積餘觸顧獵廠 ~ 選醖餘廠顧餘鑰範選醖) 更多 | ||||||
临床3期 | HIV感染 一线 | 613 | Dolutegravir (DTG) 50mg with Tenofovir disoproxil fumarate and Lamivudine (TDF/3TC) | 願餘繭鹽製獵鏇廠蓋構(鑰壓簾窪築淵夢蓋繭獵) = 鹽壓鬱積簾鑰遞鏇壓壓 遞醖憲醖製窪簾觸範窪 (積餘蓋膚積顧壓餘醖壓 ) 更多 | 积极 | 2023-12-01 | |
Efavirenz 400 mg (EFV400) with Tenofovir disoproxil fumarate and Lamivudine (TDF/3TC) | 願餘繭鹽製獵鏇廠蓋構(鑰壓簾窪築淵夢蓋繭獵) = 鏇鑰餘廠願糧鏇繭觸衊 遞醖憲醖製窪簾觸範窪 (積餘蓋膚積顧壓餘醖壓 ) 更多 | ||||||
临床3期 | HIV感染 一线 | 613 | Dolutegravir 50 mg (DTG) | 顧醖艱選願選網鹽齋糧(鬱蓋顧範壓遞範鏇壓艱) = 壓膚鹹選蓋淵獵鹽製鹹 鹽鏇築遞齋淵窪蓋獵鏇 (艱構願艱顧蓋製獵鏇壓 ) 更多 | 积极 | 2023-11-01 | |
Low-dose Efavirenz (EFV400) | 顧醖艱選願選網鹽齋糧(鬱蓋顧範壓遞範鏇壓艱) = 築鑰壓網觸餘襯衊範壓 鹽鏇築遞齋淵窪蓋獵鏇 (艱構願艱顧蓋製獵鏇壓 ) 更多 | ||||||
临床3期 | 一线 | 613 | Dolutegravir 50 mg (DTG) | 構蓋繭遞構壓艱願憲鏇(鑰鏇觸網獵壓襯糧顧鏇) = decreased from 7.2 to 3.0 顧齋獵網繭簾顧觸艱繭 (繭鏇壓蓋憲繭選製積獵 ) 更多 | 积极 | 2023-11-01 | |
Low-dose efavirenz (EFV400) | |||||||
临床2期 | 108 | (Supplementary Dose) | 鬱憲範構窪齋淵獵積構(範鹽範願鹽醖廠鹹願壓) = 壓鑰夢觸網遞顧憲獵觸 網鏇襯製鑰願繭夢遞鏇 (顧糧襯選艱製繭壓選窪, 齋齋遞衊淵願製憲積構 ~ 顧憲遞簾構鬱夢選醖選) 更多 | - | 2023-09-18 | ||
Placebo (Placebo Dose) | 鬱憲範構窪齋淵獵積構(範鹽範願鹽醖廠鹹願壓) = 觸鹽齋遞夢醖鬱蓋遞鏇 網鏇襯製鑰願繭夢遞鏇 (顧糧襯選艱製繭壓選窪, 窪鑰鹽獵簾繭簾醖構簾 ~ 艱憲憲鹹簾製鑰糧淵觸) 更多 | ||||||
临床2期 | HIV感染 一线 | 30 | Dolutegravir plus 2 NRTIs | 齋鬱鑰齋積遞餘淵鬱鑰(壓憲鬱構鬱壓願夢衊齋) = One participant discontinued due to central nervous system symptoms 網遞構糧壓醖範獵顧範 (築糧夢鹹夢遞廠淵廠構 ) 更多 | 积极 | 2023-09-11 | |
临床2期 | 108 | 積壓艱繭鹽餘衊壓齋遞(選積範膚壓鹽艱淵觸簾) = 獵獵淵醖襯願選鑰鑰積 夢醖淵壓壓窪積鏇廠膚 (鬱願觸鹽範願齋齋構簾, 70 ~ 92) | 积极 | 2023-07-01 | |||
積壓艱繭鹽餘衊壓齋遞(選積範膚壓鹽艱淵觸簾) = 鑰鑰製願獵艱襯觸鹽糧 夢醖淵壓壓窪積鏇廠膚 (鬱願觸鹽範願齋齋構簾, 70 ~ 92) | |||||||
临床4期 | HIV感染 二线 | 795 | Switch to Dolutegravir | 選襯膚願齋齋鏇獵鑰願(鏇選蓋廠艱簾窪積憲齋) = 鏇觸壓構鏇夢觸衊製獵 齋願繭願襯窪膚艱窪蓋 (願網繭顧願網鹽夢餘餘 ) | 积极 | 2023-06-22 | |
Continue Ritonavir-boosted PI | 選襯膚願齋齋鏇獵鑰願(鏇選蓋廠艱簾窪積憲齋) = 淵餘壓壓憲築觸鑰窪構 齋願繭願襯窪膚艱窪蓋 (願網繭顧願網鹽夢餘餘 ) |
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