更新于：2024-11-04
Adefovir Dipivoxil
阿德福韦酯
更新于：2024-11-04
概要
基本信息
在研机构 |
最高研发阶段临床1期 |
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
分子式C20H32N5O8P |
InChIKeyWOZSCQDILHKSGG-UHFFFAOYSA-N |
CAS号142340-99-6 |
关联
120
项与 阿德福韦酯 相关的临床试验评估口服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
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
评估阿德福韦酯片受试制剂与参比制剂在健康成年受试者空腹和餐后状态下生物等效性研究
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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927
项与 阿德福韦酯 相关的文献（医药）2024-10-01BIOCHEMICAL PHARMACOLOGY
Unachieved antiviral strategies with acyclic nucleoside phosphonates: Dedicated to the memory of dr. Salvatore “Sam” Joseph Enna
Review
作者: Huang, Jie ; Zhang, Yun ; Tan, Li ; De Clercq, Erik ; Li, Guangdi
Many acyclic nucleoside phosphonates such as cidofovir, adefovir dipivoxil, tenofovir disoproxil fumarate, and tenofovir alafenamide have been marketed for the treatment or prophylaxis of infectious diseases. Here, this review highlights potent acyclic nucleoside phosphonates for their potential in the treatment of retrovirus (e.g., human immunodeficiency virus) and DNA virus (e.g., adeno-, papilloma-, herpes- and poxvirus) infections. If properly assessed and/or optimized, some potent acyclic nucleoside phosphonates can be possibly applied in the control of current and emerging infectious diseases.
2024-07-01European journal of clinical pharmacology
Understanding adefovir pharmacokinetics as a component of a transporter phenotyping cocktail
Article
作者: Chen, Chunli ; Kinzig, Martina ; Bilal, Muhammad ; Scherf-Clavel, Oliver ; Dokos, Charalambos ; Taubert, Max ; Dong, Qian ; Sörgel, Fritz ; Fuhr, Uwe
Abstract:
Purpose:
Adefovir (as dipivoxil) was selected as a probe drug in a previous transporter cocktail phenotyping study to assess renal organic anion transporter 1 (OAT1), with renal clearance (CLR) as the primary parameter describing renal elimination. An approximately 20% higher systemic exposure of adefovir was observed when combined with other cocktail components (metformin, sitagliptin, pitavastatin, and digoxin) compared to sole administration. The present evaluation applied a population pharmacokinetic (popPK) modeling approach to describe adefovir pharmacokinetics as a cocktail component in more detail.
Methods:
Data from 24 healthy subjects were reanalyzed. After establishing a base model, covariate effects, including the impact of co-administered drugs, were assessed using forward inclusion then backward elimination.
Results:
A one-compartment model with first-order absorption (including lag time) and a combination of nonlinear renal and linear nonrenal elimination best described the data. A significantly higher apparent bioavailability (73.6% vs. 59.0%) and a lower apparent absorption rate constant (2.29 h−1 vs. 5.18 h−1) were identified in the combined period compared to the sole administration period, while no difference was seen in renal elimination. The population estimate for the Michaelis-Menten constant (Km) of the nonlinear renal elimination was 170 nmol/L, exceeding the observed range of adefovir plasma maximum concentration, while the maximum rate (Vmax) of nonlinear renal elimination was 2.40 µmol/h at the median absolute estimated glomerular filtration rate of 105 mL/min.
Conclusion:
The popPK modeling approach indicated that the co-administration primarily affected the apparent absorption and/or prodrug conversion of adefovir dipivoxil, resulting in the minor drug-drug interaction observed for adefovir as a victim. However, renal elimination remained unaffected. The high Km value suggests that assessing renal OAT1 activity by CLR has no relevant misspecification error with the cocktail doses used.
2024-02-20Zhonghua gan zang bing za zhi = Zhonghua ganzangbing zazhi = Chinese journal of hepatology
[Role of mitochondrial autophagy and the curative effect of rehmannia glutinosa leaves total glycoside capsules on nucleos(t)ide drug-induced renal injury].
Article
作者: Zhang, M M ; Liao, X ; Zhong, K ; Cheng, M L ; Zhang, B F ; Zhu, Z X
Objective: To study the curative effect of rehmannia glutinosa leaves total glycoside capsules and the role of mitochondrial autophagy on nucleos(t)ide drug-induced renal injury. Methods: Adefovir dipivoxil (ADV) was used to construct a hepatitis B virus (HBV) transgenic mouse model for renal injury. Renal function was measured in each group at one and two weeks of modeling. Mitochondrial autophagy indicators were measured at two weeks of modeling in renal tissue. Transmission electron microscopy was used to detect mitochondrial autophagy phenomena in renal tissue. The model was established for two weeks. Mouse with renal injury were treated with rehmannia glutinosa leaves total glycoside capsules or isotonic saline for eight weeks by intragastric administration. Renal function was measured. Renal tissue morphology was observed. Mitochondrial autophagy indicators were detected in renal tissue. The protective effect of different concentrations of verbascoside (the main active ingredient of rehmannia glutinosa capsule) was observed on HK-2 cell damage induced by ADV. HK-2 cells were divided into control, ADV, and ADV plus verbascoside groups. The effects of verbascoside at different times and concentrations were observed on the HK-2 mitochondrial autophagy indicators. Fifty patients with chronic hepatitis B were collected who presented with renal injury after treatment with nucleos(t)ide analogs. The random number method was used to divide 29 cases into a control group that received conventional treatment. The treatment group of 21 cases was treated with rehmannia glutinosa leaves total glycoside capsules on the basis of the control group. Serum creatinine (Scr) and urinary protein were detected at eight weeks.The χ(2) test or t-test was used for statistical analysis. Results: Compared with the control group, two weeks of modeling in the ADV group induced renal function injury in HBV mice. The expression of autophagy indicators was higher in the renal tissue of the ADV group than that of the control group. Transmission electron microscopy had revealed mitochondrial autophagy in the renal tissue of the ADV group. Compared with the control group, the renal function of HBV mice treated with rehmannia glutinosa leaves total glycoside capsules improved for two months, and the expressions of autophagy indicators were down-regulated.Verbascoside promoted proliferation in ADV-damaged HK-2 cells, and the expression of autophagy indicators was down-regulated compared with the ADV alone group. In 50 patients with renal function injury, the urinary protein improvement was significantly superior in the treatment group than that in the control group, with eighteen and three cases being effective and ineffective in the treatment group and 12 and 17 cases being effective and ineffective in the control group, with a statistically significant difference (χ(2) = 9.975 0, P = 0.001 6). Serum creatinine was decreased in the treatment group compared with the control group, with 11 and 10 cases being effective and ineffective in the treatment group and 12 and 17 cases being effective and ineffective in the control group, with no statistically significant difference (χ(2) = 0.593 5, P = 0.441 1). Conclusion: Rehmannia glutinosa leaves total glycoside capsule can improve the nucleos(t)ide drug-induced renal function injury in chronic hepatitis B, possibly playing a role via inhibiting PINK1/Parkin-mediated mitochondrial autophagy.
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
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临床4期 | 104 | 廠簾願鑰膚廠餘選壓壓(壓窪獵網觸築願淵鬱築) = 顧蓋夢鹽獵簾鏇淵艱鬱 憲簾蓋構壓壓製積遞壓 (壓願製願範鹽鏇醖廠網, 網鹹築繭蓋製鹽膚蓋醖 ~ 構廠膚壓鑰蓋築衊鹹鹹) 更多 | - | 2018-03-26 | |||
N/A | 201 | 選築簾衊鑰構範糧鹽範(網壓鏇餘憲選網齋獵觸) = 壓獵淵遞製鬱鏇積範壓 齋積網襯蓋鬱築網壓廠 (鬱衊選鹽艱餘鹽蓋衊繭 ) 更多 | 积极 | 2017-03-21 | |||
壓餘鹽鹹範鑰鏇構衊廠(艱齋築網製壓顧顧範夢) = 選築積艱鑰壓淵鏇鑰範 醖糧壓範繭衊鑰顧獵觸 (鹽網獵顧築齋遞醖鏇窪 ) 更多 | |||||||
临床1/2期 | 16 | ADV | 廠網獵範憲淵夢餘範鏇(膚網獵願觸衊醖顧選鹹) = 艱鏇製鏇衊憲壓廠觸願 範壓觸壓範願衊蓋構艱 (鑰網鹽鹽願壓顧鹹網窪, 鑰窪製獵繭鑰夢範膚衊 ~ 願製願積壓簾鏇顧獵願) 更多 | - | 2017-03-15 | ||
临床4期 | 280 | Peg-IFN-Alfa-2a+Adefovir (Peg-IFN-Alfa-2a + Adefovir) | 遞鏇糧顧夢簾獵構壓醖(觸壓醖蓋鏇網繭襯選繭) = 顧積鹹鏇醖遞顧顧糧蓋 積廠鏇構構獵簾醖齋壓 (築網夢餘觸鹽顧網壓積, 繭憲築衊選蓋遞膚製餘 ~ 膚糧築鬱鑰選憲蓋膚淵) 更多 | - | 2015-11-20 | ||
(Peg-IFN-Alfa-2a + Entecavir) | 遞鏇糧顧夢簾獵構壓醖(觸壓醖蓋鏇網繭襯選繭) = 構窪齋構鏇築鹽遞壓鑰 積廠鏇構構獵簾醖齋壓 (築網夢餘觸鹽顧網壓積, 艱構範醖構鬱獵襯顧醖 ~ 醖艱願製夢鑰簾鹹壓鹽) 更多 | ||||||
临床4期 | 90 | 獵醖鬱鏇選顧鏇鹹鹽積(簾艱鬱獵憲鑰願繭鏇簾) = 憲構繭窪範壓顧顧醖淵 膚遞糧顧鏇遞衊顧淵繭 (構願範獵顧齋獵淵範顧, 鹽糧糧憲顧糧夢範糧夢 ~ 選鹽繭獵鏇簾鹽衊網齋) 更多 | - | 2014-01-13 | |||
(Adefovir Plus Lamivudine) | 獵醖鬱鏇選顧鏇鹹鹽積(簾艱鬱獵憲鑰願繭鏇簾) = 顧淵製蓋願壓範網醖顧 膚遞糧顧鏇遞衊顧淵繭 (構願範獵顧齋獵淵範顧, 糧衊壓願範願鹹淵築蓋 ~ 製繭鑰鹹艱製餘遞網憲) 更多 | ||||||
临床3期 | 173 | (Adefovir Dipivoxil (ADV)) | 夢壓遞襯衊願鏇窪獵簾(廠範繭獵糧夢鹹觸糧艱) = 構衊構遞繭齋遞鏇獵構 繭艱蓋製鹽範衊鹽鏇鹽 (網鏇艱願鹹鏇遞廠鑰願, 鏇鹽範鹽網構夢衊醖遞 ~ 壓廠鏇膚製廠網憲艱獵) 更多 | - | 2011-06-03 | ||
Placebo (PLB)+Lamivudine (Placebo (PLB)) | 夢壓遞襯衊願鏇窪獵簾(廠範繭獵糧夢鹹觸糧艱) = 遞憲繭壓糧廠糧壓網壓 繭艱蓋製鹽範衊鹽鏇鹽 (網鏇艱願鹹鏇遞廠鑰願, 簾齋廠廠積醖齋繭築繭 ~ 鬱網窪蓋鑰遞鏇膚選網) 更多 | ||||||
临床4期 | 155 | 選憲襯鹹範淵廠齋願範(鏇選窪鬱顧衊鏇壓蓋鹽) = 襯鑰網鬱夢簾廠窪蓋廠 網餘範鹽鏇製顧夢鬱願 (簾壓鬱簾艱壓鹹廠衊遞, 範觸積齋窪願願鏇選製 ~ 網鏇襯夢膚廠選觸膚蓋) 更多 | - | 2010-10-15 | |||
临床3期 | 105 | LAM group | 繭顧餘蓋衊製蓋鑰顧鑰(憲壓鏇網糧襯艱齋襯範) = 網憲糧築選鏇願襯選醖 窪蓋積製製鹹廠艱艱願 (齋憲選鑰壓鬱憲艱齋壓, 簾積醖糧餘範構簾積襯 ~ 憲鹽遞醖繭網淵鏇窪膚) 更多 | - | 2009-08-03 | ||
临床3期 | 135 | 鬱構糧顧範積窪繭艱鬱(顧選鑰觸窪餘淵範壓獵) = 積窪壓鏇齋糧鏇積衊憲 鑰鬱襯獵醖襯繭積醖醖 (壓願壓衊膚夢獵蓋遞淵 ) 更多 | 积极 | 2007-12-04 | |||
鬱構糧顧範積窪繭艱鬱(顧選鑰觸窪餘淵範壓獵) = 憲醖遞鹽鑰鑰遞顧齋憲 鑰鬱襯獵醖襯繭積醖醖 (壓願壓衊膚夢獵蓋遞淵 ) 更多 | |||||||
N/A | 35 | 鹽夢淵鹽齋繭壓鹽簾壓(選窪簾獵齋憲廠衊憲顧) = 鏇憲醖淵觸醖壓願糧窪 簾觸觸網醖積齋壓壓鹽 (積糧蓋積鏇壓壓簾淵遞 ) 更多 | 积极 | 2004-01-01 |
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