替诺福韦磷酸酯(Tenofovir disoproxil phosphate) - 药物靶点：RT_在研适应症：乙型肝炎，慢性乙型肝炎，HIV感染_专利_临床

概要

基本信息

药物类型

小分子化药

别名

tenofovir disoproxil、Tefovir

靶点

RT

作用方式

抑制剂

作用机制

RT抑制剂(逆转录酶抑制剂)

治疗领域

免疫系统疾病感染消化系统疾病+ [1]

在研适应症

乙型肝炎慢性乙型肝炎HIV感染

非在研适应症-

原研机构

Hanmi Pharmaceutical Co., Ltd.

在研机构

Viatris Ltd. (New Zealand)Lupin Australia Pty Ltd.

Hanmi Pharmaceutical Co., Ltd.

非在研机构-

权益机构-

最高研发阶段批准上市

首次获批日期

欧盟 (2016-12-08),

慢性乙型肝炎乙型肝炎HIV感染

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C19H33N5O14P2

InChIKeyDJCLNKKHALBVLK-PFEQFJNWSA-N

CAS号1453166-76-1

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关联

20

项与替诺福韦磷酸酯相关的临床试验

NCT05005507

/ Terminated临床2期

A Phase 2, Open-label, Multicenter Study to Assess Efficacy, Safety, Tolerability, and Pharmacokinetics of Treatment With JNJ-73763989, Nucleos(t)Ide Analogs, and Pegylated Interferon Alpha-2a in Patients With Chronic Hepatitis B Virus Infection

The purpose of this study is to evaluate the efficacy in terms of hepatitis B surface antigen (HBsAg) changes from baseline for the treatment regimens of 24 weeks of JNJ-73763989 + 24 weeks of nucleos(t)ide analog (NA) + 12 or 24 weeks of pegylated interferon alpha-2a (PegIFN-alpha-2a) (with immediate or delayed start of PegIFN-alpha-2a treatment).

开始日期2021-11-03

申办/合作机构

Janssen Research & Development LLC

NCT04667104

/ Completed临床2期

A Phase 2, Open-label, Single-arm, Multicenter Study to Assess Efficacy, Safety, Tolerability, and Pharmacokinetics of Treatment With JNJ-73763989, JNJ-56136379, Nucleos(t)Ide Analogs, and Pegylated Interferon Alpha-2a in Virologically Suppressed Patients With Chronic Hepatitis B Virus Infection

The purpose of this study is to evaluate the efficacy in terms of hepatitis B surface antigen (HBsAg) levels of the study intervention (that is, JNJ-73763989 + JNJ-56136379 + nucleos[t]ide analog [NA] and pegylated interferon alpha-2a [PegIFN-alpha2a]).

开始日期2021-02-01

申办/合作机构

Janssen Research & Development LLC

NCT04453436

/ Unknown statusN/A

HIV Drug Resistance Profiles Among Individuals Failing Tenofovir/Lamivudine and Dolutegravir First Line Regimen in Brazil

Brazil was the first middle-income country to provide free and universal access to antiretroviral drugs to HIV infected individuals. Since 2014 local guidelines recommend that all HIV infected individuals be started on therapy regardless of CD4 count. Since January 2017, all patients are started on a DTG containing triple regimen. As of November 2018, 170,000 individuals were receiving DTG through the public health system. It is a public health priority to evaluate the risk of virologic failure and the subsequent development of INSTI resistance in these real-life settings. Our preliminary data from Brazil indicated a high virologic failure rate of 8% after 18 months of treatment TL+D. Our central hypothesis is that TDR may be associated and contribute to virologic failure with DTG in clinical practice. To test this central hypothesis, we will identify PLWH failing DTG containing regimens in Brazil. The insights generated with these studies will contribute to a more effective use of second generation INSTI in the future.

开始日期2020-09-01

申办/合作机构

Universidade Federal De Sao Paulo

[+1]

100 项与替诺福韦磷酸酯相关的临床结果

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100 项与替诺福韦磷酸酯相关的转化医学

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100 项与替诺福韦磷酸酯相关的专利（医药）

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253

项与替诺福韦磷酸酯相关的文献（医药）

2024-12-01·European Journal of Medicinal Chemistry

Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds

Article

作者: Šácha, Pavel ; Šimková, Adéla ; Konvalinka, Jan ; Staňurová, Jana ; Wichterle, Filip ; Čermáková, Kateřina ; Bušek, Petr ; Kryštůfek, Robin ; Vaníčková, Zdislava

Fibroblast activation protein (FAP) has been extensively studied as a cancer biomarker for decades. Recently, small-molecule FAP inhibitors have been widely adopted as a targeting moiety of experimental theranostic radiotracers. Here we present a fast qPCR-based analytical method allowing FAP inhibition screening in a high-throughput regime. To identify clinically relevant compounds that might interfere with FAP-targeted approaches, we focused on a library of FDA-approved drugs. Using the DNA-linked Inhibitor Antibody Assay (DIANA), we tested a library of 2667 compounds within just a few hours and identified numerous FDA-approved drugs as novel FAP inhibitors. Among these, prodrugs of cephalosporin antibiotics and reverse transcriptase inhibitors, along with one elastase inhibitor, were the most potent FAP inhibitors in our dataset. In addition, by employing FAP DIANA in the quantification mode, we were able to determine FAP concentrations in human plasma samples. Together, our work expands the repertoire of FAP inhibitors, analyzes the potential interference of co-administered drugs with FAP-targeting strategies, and presents a sensitive and low-consumption ELISA alternative for FAP quantification with a detection limit of 50 pg/ml.

2024-09-01·International Journal of STD & AIDS

Acute hepatitis B in a hepatitis B vaccine non-responder

Article

作者: Cherif, Soumeya ; Seneviratne, Kanch ; Scott, Jane

Developing acute hepatitis B in immunocompetent non-responders to hepatitis B vaccination has been rarely reported. We report such a case in a 79 year old heterosexual male. There is evidence that tenofovir disoproxil/emtricitabine as primary prophylaxis can prevent acquisition of hepatitis B. In the current era of HIV pre-exposure prophylaxis (PrEP) with tenofovir disoproxil/emtricitabine, there is dual benefit of preventing HIV and hepatitis B. We discuss the importance of considering tenofovir disoproxil/emtricitabine pre-exposure prophylaxis in those hepatitis B vaccination non-responders at high risk of acquiring hepatitis B.

2024-09-01·Journal of Hepatology

Association between antiviral treatments and fracture in elderly patients with HBV needs further evaluation

Letter

作者: Jiang, Zai-Bo ; Wu, Jia-Lin ; Luo, Jun-Yang

This article is about long-term use of tenofovir disoproxil fumarate increases fracture risk in elderly patients with chronic hepatitis B which was published in a recent issue of the Journal of Hepatol.This topic is particularly intriguing as it explores the impact of entecavir (ETV) and tenofovir disoproxil (TDF) on the risk of bone fracture in patients with chronic hepatitis B based on a real-world territory-wide cohort.Their findings revealed that long-term TDF treatment for 2 years or more is associated with a higher incidence of bone fracture in older patients.Although this study was elegantly designed and inspiring, we believe that certain aspects warrant further discussion.Addnl., individuals with osteosarcopenia are significantly more likely to experience falls, fractures, and mortality than in non-osteosarcopenic groups.Therefore, this information is imperative for the readers knowledge, and baseline variables which should include bone mineral d. and sarcopenia index prior to the antiviral treatments are needed to draw a robust conclusion.Secondly, they noted that TDF-treated patients with a match were older and more likely to be female, as per the propensity score-matching.Here authors discovered that patients receiving TDF had a higher risk of developing incident fractures compared to those treated with ETV after 24 mo (weighted subdistribution hazard ratio 2.33, 95% CI 1.20 - 4.55, p = 0.014 for age > 65 years; weighted subdistribution hazard ratio 2.12, 95% CI 1.01 - 4.46, p = 0.047 for age > 70 years).Similarly, age and sex could both be risk factors for osteoporosis and fracture, which occur as part of the natural aging process, particularly in relation to menopause and the alterations in sex hormones that accompany advancing age.In order to further validate whether long-term use of TDF increases the risk of fractures in elderly patients with chronic hepatitis B, it is advisable to ensure consistency in terms of phys. activity intensity and diet composition between the two groups.In conclusion, while acknowledging the aforementioned points that merit careful consideration, we are genuinely grateful for the contribution of Yip et al. in their work, and their fi ndings support the current treatment guidelines, advocating for the customization of antiviral therapy based on age and comorbidities.

100 项与替诺福韦磷酸酯相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10834	-	J05AF07	DB00300

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
乙型肝炎	列支敦士登	Viatris Ltd. (New Zealand)	2016-12-08
乙型肝炎	冰岛	Viatris Ltd. (New Zealand)	2016-12-08
乙型肝炎	欧盟	Viatris Ltd. (New Zealand)	2016-12-08
乙型肝炎	挪威	Viatris Ltd. (New Zealand)	2016-12-08
慢性乙型肝炎	冰岛	Viatris Ltd. (New Zealand)	2016-12-08
慢性乙型肝炎	列支敦士登	Viatris Ltd. (New Zealand)	2016-12-08
慢性乙型肝炎	欧盟	Viatris Ltd. (New Zealand)	2016-12-08
慢性乙型肝炎	挪威	Viatris Ltd. (New Zealand)	2016-12-08
HIV感染	欧盟	Viatris Ltd. (New Zealand)	2016-12-08
HIV感染	挪威	Viatris Ltd. (New Zealand)	2016-12-08
HIV感染	列支敦士登	Viatris Ltd. (New Zealand)	2016-12-08
HIV感染	冰岛	Viatris Ltd. (New Zealand)	2016-12-08

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


AASLD2023	N/A	肝细胞癌	3,384	Tenofovir disoproxil (TDF)	(鹹製襯窪鑰醖遞顧簾願) = 憲鏇糧網廠築鬱鹹網壓顧鏇鏇觸餘選廠蓋獵網 (觸築鑰鏇齋鬱艱簾夢範 ) 更多	-	2023-11-10
				Entecavir (ETV)	(鹹製襯窪鑰醖遞顧簾願) = 鑰鏇築齋選鹹鹽獵蓋糧顧鏇鏇觸餘選廠蓋獵網 (觸築鑰鏇齋鬱艱簾夢範 ) 更多
ARIA study (IAS2020)	N/A	-	495	DTG/ABC/3TC	(顧淵願鬱積鹽膚膚襯築) = 襯窪願糧鏇齋選艱壓鹹齋蓋獵艱鑰醖願窪壓製 (選願簾積構鑰蓋壓糧蓋 ) 更多	-	2020-01-01
				Atazanavir/ritonavir + tenofovir disoproxil + emtricitabine	(顧淵願鬱積鹽膚膚襯築) = 憲選鑰鹹壓製選糧獵鑰齋蓋獵艱鑰醖願窪壓製 (選願簾積構鑰蓋壓糧蓋 ) 更多
NCT02577029 (MONARCH, CTgov)	临床2期	慢性乙型肝炎 \| 丁型肝炎	79	antihistamine+ARC-520 (Cohort 1)	築積繭齋願餘構餘遞衊(衊構繭鑰顧繭齋窪鏇糧) = 餘憲艱願鬱淵鏇蓋醖構餘觸廠鬱遞艱製艱繭積 (糧窪艱製觸衊蓋選築鹹, 糧簾網積範淵鹹範願齋 ~ 膚鏇顧壓淵製顧鏇鬱選) 更多	-	2019-04-12
				antihistamine+tenofovir disoproxil+ARC-520+pegylated interferon alpha 2a+entecavir (Cohort 2)	築積繭齋願餘構餘遞衊(衊構繭鑰顧繭齋窪鏇糧) = 鏇鏇蓋製築獵壓憲壓衊餘觸廠鬱遞艱製艱繭積 (糧窪艱製觸衊蓋選築鹹, 膚獵廠鹹窪鹹夢製築糧 ~ 網遞鏇齋製齋膚餘餘艱) 更多
NCT00734344 (CTgov)	N/A	HIV感染	18	Tenofovir disoproxil twice daily+Emtricitibine+Raltegravir (Arm 1)	遞夢襯積齋願窪壓築製(餘蓋艱襯餘網遞襯鹹餘) = 淵壓構鹹積範鬱襯獵鹹鬱鏇範鑰窪餘鹹廠壓窪 (淵淵壓醖憲鑰積壓齋憲, 獵積膚齋積製壓淵鑰襯 ~ 簾願鏇廠鬱醖鏇窪壓範) 更多	-	2016-05-30
				Tenofovir disoproxil once daily+Emtricitibine+Efavirenz (Arm 2)	遞夢襯積齋願窪壓築製(餘蓋艱襯餘網遞襯鹹餘) = 獵鏇廠襯鬱網鹹齋醖憲鬱鏇範鑰窪餘鹹廠壓窪 (淵淵壓醖憲鑰積壓齋憲, 範觸顧鑰齋構膚鑰淵淵 ~ 淵膚製製構繭蓋憲壓網) 更多
Pubmed \| Anesthesiology	N/A	早产	-	Oral Elixir	網窪膚憲蓋製鬱糧襯餘(鹽蓋觸製範鹹獵糧齋鑰) = These regimens may cause hepatotoxicity in some individuals if used for longer than 2-3 days 範夢鑰顧廠觸憲願鹽齋 (齋遞築鹹網築廠鑰簾築 )	-	2002-06-01
				Rectal Solution