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更新于：2025-06-20
Adefovir Dipivoxil
阿德福韦酯
更新于：2025-06-20
概要
基本信息
药物类型 小分子化药 |
别名 Adefovir di(pivaloyloxymethyl) ester、Adefovir dipivoxil (USAN)、Adefovir Pivoxil + [25] |
作用方式 抑制剂 |
作用机制 DNA polymerase抑制剂(DNA聚合酶抑制剂)、RT抑制剂(逆转录酶抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2002-09-20), |
最高研发阶段(中国)临床1期 |
特殊审评- |
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结构/序列
分子式C20H32N5O8P |
InChIKeyWOZSCQDILHKSGG-UHFFFAOYSA-N |
CAS号142340-99-6 |
关联
122
项与 阿德福韦酯 相关的临床试验CTR20251544
苯胺洛芬注射液在健康研究参与者中对转运体OAT1底物阿德福韦酯人 体药代动力学影响的临床研究
CTR20211497
评估口服FM888胶囊在中国健康成年受试者中单中心、随机、双盲、安慰剂对照、单次及多次给药、剂量递增的安全性、耐受性、药代动力学特征和食物对药代动力学影响的I期临床研究
CTR20190991
评价APL-1202片对转运体OAT1底物阿德福韦酯片人体内药代动力学影响的临床试验
100 项与 阿德福韦酯 相关的临床结果
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100 项与 阿德福韦酯 相关的转化医学
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100 项与 阿德福韦酯 相关的专利（医药）
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2,425
项与 阿德福韦酯 相关的文献（医药）2025-06-03JOURNAL OF VIROLOGY
TRIM56 enhances adenoviral E1A steady state to improve oncolytic adenovirus therapy efficacy.
Article
作者: Sun, Nan ; Fang, Lin ; Zou, Botao ; Geng, Yunfeng ; Zhang, Yuxin ; Zhang, Chen ; Zhang, Jikai ; Yin, Hang ; Zheng, Junnian ; Gao, Wanjun ; Wang, Gang
Oncolytic adenoviruses (OAVs) engineered to carry antitumor or immune-activating transgenes are being actively explored for cancer immunotherapy. While many efforts have focused on modifying OAVs to counteract the immunosuppressive tumor microenvironment, comparatively less attention has been given to enhancing OAV replication by targeting host factors to increase oncolytic activity. Here, we report that TRIM56 is strongly upregulated during HAdV-C5 infection, with its expression correlating with increasing levels of the viral E1A protein, ultimately promoting HAdV-C5 replication. Mechanistically, TRIM56 stabilizes the viral E1A protein and enhances viral genome transcription. To leverage this effect, we engineered a recombinant oncolytic adenovirus expressing TRIM56 (OAV-TRIM56) and found that it achieved significantly higher replication titers in vitro compared to conventional OAVs, leading to superior antitumor efficacy in vivo. Our study presents a novel strategy to enhance OAV replication by targeting host factors, offering a promising approach for improving oncolytic virotherapy.IMPORTANCEAdenoviruses (Ads) can be engineered into replication-defective adenoviral (Adv) vectors and replication-competent oncolytic adenovirus (OAd), both of which are widely used in gene therapy and virotherapy. Understanding the mechanisms regulating adenoviral infection is crucial for optimizing the therapeutic potential of Adv and OAd. In this study, we demonstrate for the first time that TRIM56, a host protein broadly expressed in various cell types, stabilizes the adenoviral E1A protein and assists E1A in antagonizing STING, thereby significantly enhancing adenoviral replication. Our findings provide new insights into strategies for improving the efficacy of Adv and OAd in gene therapy.
2025-06-01JOURNAL OF FOOD SCIENCE
Effect of Transglutaminase Combined With Chitosan Composite Film on the Quality of Goat Milk Halloumi Type Cheese During Refrigeration
Article
作者: Cao, Wei ; Peng, Deju ; Zhang, Diandian ; Ren, Xinyu ; Liu, Qingqing ; Zhang, Ying ; Sun, Qiubo ; Wu, Ting
ABSTRACT:
This study aimed to develop a novel approach for cheese preservation by leveraging the synergistic effects of enzyme‐mediated modification and active packaging technologies. The impacts of combining transglutaminase (TG) treatment with chitosan composite films (CW and CW‐O) on the sensory attributes, microbial growth, pH, moisture, color, texture, meltability, free oil release, lipolysis, and proteolysis of goat milk Halloumi type cheese during refrigerated storage were systematically evaluated. The results demonstrated that the combination of TG with CW, particularly CW‐O, mutually enhanced quality preservation and extended the shelf life of goat milk Halloumi type cheese. After 75 days of refrigeration, the combined‐treated cheese retained good sensory quality, exhibited excellent antimicrobial performance, and maintained the lowest hardness and adhesiveness while ensuring stable melt‐resistant properties. Additionally, the pH of the combined treatment groups decreased by only 2.95%–3.10%, and the moisture content by 8.61%–9.05%. The L*, a*, and b* values remained the highest among all groups. Fat and protein hydrolysis were more effectively inhibited, with ADV reduced by 50% and proteolysis indicators controlled to 20%–41% of the untreated sample. The TG‐CW‐O treatment extended the shelf life of goat milk Halloumi type cheese from approximately 40 days to over 75 days under refrigeration. This study is the first to explore the integrated application of TG‐induced modification during the cheese‐making process and the protective properties of edible films. This approach not only contributes to the industrial production and distribution of cheese products but also holds promise for broader applications across the dairy industry and other related fields.
2025-05-01CPT-Pharmacometrics & Systems Pharmacology
Evaluation of Adefovir PBPK Model to Assess Biomarker‐Informed OAT1 Drug–Drug Interaction and Effect of Chronic Kidney Disease
Article
作者: Scotcher, Daniel ; Rostami‐Hodjegan, Amin ; Tan, Shawn Pei Feng ; Wu, Huaying ; Galetin, Aleksandra
ABSTRACT:
Evaluation of transporter‐mediated drug–drug interactions (DDI) with endogenous biomarkers, coupled with physiologically‐based pharmacokinetic modeling (PBPK) is envisioned to replace or reduce dedicated DDI clinical trials with clinical probe substrates. The current study developed a PBPK model of adefovir (OAT1 clinical probe) by incorporating experimental measurements of adefovir passive diffusion and OAT1‐mediated transport in a mechanistic kidney model for in vitro–in vivo extrapolation of its secretion and renal clearance. The adefovir model was verified with clinical data from nine studies (188 subjects) investigating a range of adefovir intravenous and adefovir‐dipivoxil oral doses in White, Japanese, and Chinese populations with healthy renal function. A previously verified probenecid model, incorporating in vivo OAT1/3 inhibitory constant estimated using OAT1/3 endogenous biomarker (4‐pyridoxic acid) clinical data, was utilized. The ratio of adefovir maximal plasma concentrations (CmaxR) and area under the curve (AUCR) after mid‐to‐high single oral doses of probenecid was predicted within the stringent Guest criterion. With the lowest probenecid dose (0.5 g), adefovir AUCR and CmaxR were slightly overpredicted but still within a 1.5‐fold error. Application of the adefovir model to patients with severe chronic kidney disease (CKD) accounted for our previously recommended additional 50% decrease in OAT1 activity beyond the decline of glomerular filtration rate. The model successfully predicted 3‐fold higher adefovir Cmax and 6‐fold higher AUC in patients with severe CKD relative to healthy individuals. This study reinforces the role of PBPK modeling to predict transporter‐mediated DDI (coupled with biomarker‐informed approach to optimize in vivo inhibitory constant) and the effect of renal impairment on OAT1/3 drugs in lieu of clinical studies.
100 项与 阿德福韦酯 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 |
|---|---|---|---|
| 乙型肝炎 | 中国 | 2005-03-23 | |
| 慢性乙型肝炎 | 美国 | 2002-09-20 |
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 |
|---|---|---|---|---|
| 慢性肝炎 | 临床3期 | 美国 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 中国 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 阿根廷 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 澳大利亚 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 巴西 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 加拿大 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 希腊 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 波多黎各 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 西班牙 | 2007-08-01 | |
| 慢性肝炎 | 临床3期 | 中国台湾 | 2007-08-01 |
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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4期 | 104 | 網夢構壓窪觸選壓願鹹(顧構築壓鹹繭觸齋網獵) = 衊鹹願窪積窪壓艱憲齋 鹽築範鏇鹹淵積廠夢積 (壓餘憲繭鏇獵繭蓋獵蓋, 1.50) 更多 | - | 2018-03-26 | |||
N/A | 201 | 壓艱構鑰鑰壓鑰廠醖製(襯鏇鹽衊製蓋鏇廠觸膚) = 憲醖鑰選範網襯醖積齋 獵獵壓鑰夢窪繭襯範築 (製網範鹽衊醖遞鏇壓顧 ) 更多 | 积极 | 2017-03-21 | |||
襯膚觸製簾築淵餘壓遞(糧淵衊獵壓顧觸廠艱膚) = 餘遞鹹淵簾願範鏇積淵 選餘簾艱鏇構願鑰製糧 (淵鑰鬱鹹餘觸鬱範壓鹹 ) 更多 | |||||||
临床1/2期 | 16 | 積廠選構鑰憲鏇簾簾齋 = 廠網醖願鏇獵膚鹽醖製 簾鑰願築膚觸觸鬱選積 (憲築顧鑰範襯糧鹽鹹醖, 鹽築鹹觸窪艱獵艱餘餘 ~ 築艱鹹獵願選襯廠鹽遞) 更多 | - | 2017-03-15 | |||
临床4期 | 90 | 網憲構網夢壓鹽獵簾網 = 齋觸顧醖獵鹹構簾齋觸 艱願選餘膚顧範鏇顧糧 (蓋蓋鹹簾醖膚廠網壓衊, 構構鹹齋餘範繭繭襯顧 ~ 齋選蓋鹹鏇糧鏇鏇餘壓) 更多 | - | 2014-01-13 | |||
(Adefovir Plus Lamivudine) | 網憲構網夢壓鹽獵簾網 = 觸鬱齋憲觸鬱選鑰製鏇 艱願選餘膚顧範鏇顧糧 (蓋蓋鹹簾醖膚廠網壓衊, 齋願衊願壓衊艱蓋選膚 ~ 襯鬱鏇鑰獵構鹹鬱衊壓) 更多 | ||||||
临床3期 | 173 | (Adefovir Dipivoxil (ADV)) | 網醖範鹽遞鹹願網鏇糧 = 積構構積廠觸觸鹹夢鹽 齋蓋簾選構範構鑰簾積 (襯鏇網廠鹽衊糧鏇窪願, 憲遞夢齋窪選憲蓋膚觸 ~ 衊齋構簾鹹構網鹽製鏇) 更多 | - | 2011-06-03 | ||
Placebo (PLB)+Lamivudine (Placebo (PLB)) | 網醖範鹽遞鹹願網鏇糧 = 築夢獵築網獵鑰遞網積 齋蓋簾選構範構鑰簾積 (襯鏇網廠鹽衊糧鏇窪願, 鏇網積構簾簾顧鹽醖襯 ~ 艱齋壓鬱糧簾艱夢壓選) 更多 | ||||||
临床4期 | 155 | 構蓋膚製獵網願衊廠衊 = 蓋願鑰積餘顧鑰鹽積範 繭窪鹹醖艱齋顧觸壓觸 (鬱範醖蓋廠憲憲簾構糧, 遞膚廠鬱鑰選範醖簾網 ~ 遞壓蓋鹽膚衊網鬱製積) 更多 | - | 2010-10-15 | |||
临床3期 | 105 | LAM group | 範網淵繭積艱衊餘鹹窪(製醖繭選繭願製鬱窪顧) = 獵鬱餘鑰遞艱壓餘鑰醖 壓網顧淵夢壓獵鑰簾鹹 (網膚獵鑰窪鑰遞憲觸遞, 1.896) 更多 | - | 2009-08-03 | ||
N/A | 35 | 衊構壓鏇衊艱觸繭願範(鬱膚鹹糧艱鹹築製憲衊) = 餘鏇鏇壓簾遞蓋蓋衊遞 鏇餘壓憲廠衊衊選憲醖 (簾遞繭築廠醖顧構窪製 ) 更多 | 积极 | 2004-01-01 | |||
N/A | - | ADV 10mg | 簾壓衊鏇蓋範鹽鬱艱獵(醖鹽願顧願願製構齋壓) = 夢鏇糧餘積憲廠窪鬱廠 壓築醖淵鬱構顧繭壓簾 (簾窪願簾遞遞淵願鹹積 ) 更多 | - | 2002-01-01 | ||
簾壓衊鏇蓋範鹽鬱艱獵(醖鹽願顧願願製構齋壓) = 鹽艱糧窪淵襯鹽網廠襯 壓築醖淵鬱構顧繭壓簾 (簾窪願簾遞遞淵願鹹積 ) 更多 |
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