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更新于：2026-02-06
Danoprevir Sodium
达诺瑞韦钠
更新于：2026-02-06
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 中国 (2018-06-08), |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (中国)、特殊审批 (中国) |
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结构/序列
分子式C35H46FN5NaO9S |
InChIKeyPXTAHCFVHRHONT-HHGSPMIASA-N |
CAS号916826-48-7 |
关联
48
项与 达诺瑞韦钠 相关的临床试验NCT06263959
A Randomized, Double-blind, Placebo-controlled Phase IIa Clinical Study to Evaluate the Safety and Efficacy of GST-HG131 Tablets in Patients With Chronic Hepatitis B
CTR20201603
评价GST-HG131片在健康受试者中单中心、随机、双盲、安慰剂对照的多剂量、单次给药、多次给药的安全性、耐受性及药代动力学Ⅰa期临床试验
NCT04499443
To Evaluate the Safety, Tolerability and Pharmacokinetics of GST-HG131 Tablets in Single-center, Randomized, Double-blind, Placebo-controlled Multiple-dose, Single-dose, Multiple-dose Phase Ia Clinical Trials in Healthy Subjects
100 项与 达诺瑞韦钠 相关的临床结果
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100 项与 达诺瑞韦钠 相关的转化医学
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100 项与 达诺瑞韦钠 相关的专利（医药）
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186
项与 达诺瑞韦钠 相关的文献（医药）2025-08-04MOLECULAR PHARMACEUTICS
Drug Solubility in Human Colonic Fluids and Comparison to Small Intestinal and Simulated Fluids
Article
作者: Borde, Anders ; Karlsson, Eva M. ; Tannergren, Christer ; Brouwers, Joachim ; Olivefors, Astrid ; Augustijns, Patrick ; Steigert, Sebastian ; Vanuytsel, Tim
Colonic drug absorption is a prerequisite for a drug's suitability for colon-targeted and extended-release formulations. Since drug solubility is a key factor for uptake in the gastrointestinal tract, reliably estimating solubility in the human colon is essential for determining the feasibility of such formulation approaches. To date, our understanding of colonic drug solubility, how it compares to the proximal small intestine, and how it is linked to luminal fluid composition is limited by the scarcity of reference data available. Therefore, this study aimed to measure and compare the apparent solubility of eight drugs with varying physicochemical properties (apixaban, danoprevir, dexloxiglumide, febuxostat, fenofibrate, rofleponide, ticagrelor and tofacitinib) in pooled aspirates from the proximal human colon and small intestine, along with simulated media and buffers commonly used in solubility assessment. Additionally, the composition of the pooled luminal fluids was characterized. Whereas solubility in colonic and small intestinal fluids was comparable for most drugs, the small intestine's solubilizing capacity clearly exceeded that of the colon for the lipophilic drugs fenofibrate and ticagrelor. Extensive degradation of danoprevir was observed in both luminal fluids. Prediction of small intestinal solubility of the lipophilic compounds fenofibrate and ticagrelor was improved in fasted state simulated intestinal fluid compared to blank buffer, although the solubilizing capacity of the human fluids was only captured partially. Fasted state simulated colonic fluid solely improved the colonic solubility prediction of fenofibrate, while the prediction of ticagrelor remained outside the 2-fold prediction error threshold. Solubilities of all other drugs were predicted reasonably well in blank buffers and simulated media. The results generated in this study may serve as reference data for the validation of improved in vitro and in silico tools for colonic drug solubility prediction.
2024-06-01Drug metabolism and disposition: the biological fate of chemicals
HCV Antiviral Drugs Have the Potential to Adversely Perturb the Fetal-Maternal Communication Axis through Inhibition of CYP3A7 DHEA-S Oxidation
Article
作者: Hackett, John C ; Work, Hannah M ; Lampe, Jed N
The hepatitis C virus (HCV) poses a great risk to pregnant people and their developing fetus, yet no HCV antiviral treatment guidelines have been established. While there has been a substantial increase in the development of HCV antivirals, the effect they have on the developing fetus remains poorly defined. Many of these drugs are metabolized through the cytochrome P450 CYP3A pathway, which is mediated by cytochrome P450 3A7 (CYP3A7) in the fetus and developing infant. In this study, we sought to investigate the effect HCV antivirals have on CYP3A7 metabolism, as this CYP enzyme plays a vital role in proper fetal and neonatal development. Of the 13 HCV antivirals we investigated, 8 (∼62%) inhibited CYP3A7 metabolic activity by 50% or more at a concentration of 20 µM. Furthermore, paritaprevir, asunaprevir, simeprevir, danoprevir, and glecaprevir all had observed half-maximal inhibitory concentrations between the range of 10 and 20 µM, which is physiologically relevant in comparison with the Km of dehydroepiandrosterone-sulfate (DHEA-S) oxidation (reported to be between 5 and 20 µM). We also discovered that paritaprevir is a time-dependent inhibitor of CYP3A7, which shifts the IC50 ∼twofold from 11 µM to 5 µM. Upon further characterization, paritaprevir inactivates DHEA-S metabolism by CYP3A7, with KI and Kinact values of 4.66 µM and 0.00954 minute-1, respectively. Depending on treatment plan and off-label drug use, HCV treatment could adversely affect the fetal-maternal communication axis by blocking fetal CYP3A7 metabolism of important endogenous hormones. SIGNIFICANCE STATEMENT: The prevalence of HCV in pregnant people is estimated at between 1% and 8% of the global population, yet little to no information exists about the risk antiviral treatment poses to the developing fetus. There is a potential risk of drugs adversely affecting mother-fetal communication by inhibiting fetal hepatic CYP3A7, an integral enzyme for estriol production. We discovered that five HCV antivirals inhibited DHEA-S metabolism by CYP3A7, and paritaprevir inactivated the enzyme. Our studies demonstrate the potential threat these drugs pose to proper fetal development.
2024-03-12Boletin medico del Hospital Infantil de Mexico
Drugs and natural products for the treatment of COVID-19 during 2020, the first year of the pandemic
Article
作者: Arrieta-Cruz, Isabel ; Castillo-Arellano, Jorge I ; Magos-Guerrero, Gil A ; Jaimes-Castelán, Elia G ; Reyes-Chilpa, Ricardo ; Jiménez-Estrada, Manuel ; González-Espinosa, Claudia
This work aimed to show which treatments showed efficacy against coronavirus disease 2019 (COVID-19); therefore, the results of 37 clinical trials started in 2020 and completed in 2021 are reviewed and discussed here. These were selected from databases, excluding vaccines, computational studies, in silico, in vitro, and those with hyperimmune sera from recovered patients. We found 34 drugs, one vitamin, and one herbal remedy with pharmacological activity against symptomatic COVID-19. They reduced mortality, disease progression, or recovery time. For each treatment, the identifier and type of trial, the severity of the disease, the sponsor, the country where the trial was conducted, and the trial results are presented. The drugs were classified according to their mechanism of action. Several drugs that reduced mortality also reduced inflammation in the most severe cases. These include some that are not considered anti-inflammatory, such as Aviptadil, pyridostigmine bromide, anakinra, imatinib, baricitinib, and bevacizumab, as well as the combination of ivermectin, aspirin, dexamethasone, and enoxaparin. Nigella sativa seeds with honey have also been reported to have therapeutic activity. On the other hand, tofacitinib, novaferon with ritonavir, and lopinavir were also effective, as well as in combination with antiviral therapies such as danoprevir with ritonavir. The natural products colchicine and Vitamin D3 were only effective in patients with mild-to-moderate COVID-19, as was hydroxychloroquine. Drug repositioning has been the main tool in the search for effective therapies by expanding the pharmacological options available to patients.
100 项与 达诺瑞韦钠 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 |
|---|---|---|---|
| 慢性丙型肝炎 | 中国 | 2018-06-08 |
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 |
|---|---|---|---|---|
| 慢性丙型肝炎基因型 1 | 临床3期 | - | 2016-06-01 | |
| 假性高钾血症Cardiff型 | 临床3期 | - | 2016-06-01 | |
| 慢性乙型肝炎 | 临床2期 | 中国 | 2023-12-26 | |
| 血小板无力症 | 临床2期 | - | 2016-01-01 | |
| 代偿期肝硬化 | 临床2期 | 美国 | 2012-04-01 | |
| 代偿期肝硬化 | 临床2期 | 澳大利亚 | 2012-04-01 | |
| 代偿期肝硬化 | 临床2期 | 加拿大 | 2012-04-01 | |
| 代偿期肝硬化 | 临床2期 | 法国 | 2012-04-01 | |
| 代偿期肝硬化 | 临床2期 | 新西兰 | 2012-04-01 | |
| 代偿期肝硬化 | 临床2期 | 波兰 | 2012-04-01 |
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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期 | - | 獵鹹簾構鬱廠齋範構艱(積膚顧築襯構糧範構範) = 艱鑰製襯壓襯願淵鏇獵 簾遞築鑰繭範願淵齋餘 (淵餘範蓋襯齋鹽蓋憲鏇 ) | 积极 | 2025-07-11 | |||
临床1期 | - | - | (single-ascending-dose) | 遞鏇壓鑰選醖齋選艱餘(鑰鹽襯糧繭簾築遞窪鹹) = 窪襯顧網艱廠獵壓窪鹹 蓋築夢窪窪鏇遞選獵遞 (蓋窪遞窪網範糧鹽膚範 ) 更多 | 积极 | 2022-05-17 | |
(multiple-ascending-dose) | - | ||||||
临床3期 | 141 | 網憲遞糧獵衊鏇淵鏇壓 = 鹽遞夢簾蓋糧壓鑰築淵 鬱積鏇鑰簾壓積鑰顧網 (鑰願憲窪選簾顧廠鹹淵, 廠壓襯願鏇壓製襯製襯 ~ 獵鹽獵觸選構壓憲襯選) 更多 | - | 2021-03-23 | |||
临床2期 | 38 | 獵齋憲襯製鏇繭齋窪醖 = 鏇壓憲鹽鏇襯艱醖鹹夢 鏇蓋遞膚艱遞繭選夢製 (齋壓築鹽衊衊鏇夢製醖, 遞夢鏇繭選網繭構積衊 ~ 觸淵顧艱鬱醖糧鹹選願) 更多 | - | 2020-10-22 | |||
临床2/3期 | 424 | 夢鏇餘蓋糧選選鬱遞選(選鬱選憲鏇簾醖鏇窪範) = 鹽顧鑰構鬱膚範鹹鏇醖 憲鏇鏇觸鬱繭鬱鬱獵簾 (襯鏇簾製簾齋醖窪蓋艱, 97 ~ 100) 更多 | 积极 | 2019-09-28 | |||
临床3期 | 141 | 衊膚網顧遞鏇觸醖廠夢(窪淵艱餘願積糧憲艱膚) = 鬱壓簾廠餘繭壓築鹹壓 築遞鹽艱憲蓋選網鏇鑰 (築網築觸餘遞簾壓遞醖, 92.9 ~ 99.2) | 积极 | 2019-09-28 | |||
临床2期 | 38 | 觸艱蓋願鹽醖顧遞齋餘(夢憲鬱齋鑰餘餘製構窪) = 獵鏇選膚夢醖鏇願鑰襯 製獵製窪觸遞蓋築餘廠 (窪獵鹽觸網憲憲廠淵製 ) 更多 | 积极 | 2018-08-01 | |||
临床2期 | 70 | 鏇鏇簾鹽憲齋製憲夢艱 = 壓顧憲獵蓋願網餘鑰繭 鹽齋襯壓製繭膚網顧構 (壓襯憲獵獵遞衊築淵壓, 簾齋憲構願糧淵鏇廠觸 ~ 範夢鏇積鬱鏇積選憲遞) 更多 | - | 2018-02-07 | |||
临床1期 | 24 | Danoprevir-ritonavir | 壓遞範積願築觸衊築簾(廠糧範簾繭獵憲願襯醖) = 壓構蓋積簾鏇齋範鹽簾 壓糧窪鏇壓齋衊觸膚鹹 (鏇繭廠廠鑰鹽齋鹽鏇顧 ) | - | 2014-01-01 | ||
临床2期 | 237 | 簾獵鏇蓋網鑰襯鏇鏇築(蓋製壓選蓋艱蓋鏇餘憲) = Four patients given danoprevir (1 patient in the 600-mg group and 3 in the 900-mg group) had reversible, grade 4 increases in alanine aminotransferase, which led to early discontinuation of the 900-mg arm of the study 範憲醖壓範構夢餘艱憲 (膚艱餘憲壓獵醖選衊蓋 ) | - | 2013-10-01 | |||
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