预约演示
更新于：2026-10-23
Emtricitabine
恩曲他滨
更新于：2026-10-23
概要
基本信息
药物类型 小分子化药 |
别名 (2R-cis)-4-amino-5-fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)-2(1H)-pyrimidinone、(−)-(2R,5S)-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine、(−)-2'-deoxy-5-fluoro-3'-thiacytidine + [18] |
靶点 |
作用方式 抑制剂 |
作用机制 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 (2003-07-02), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (日本) |
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结构/序列
分子式C8H10FN3O3S |
InChIKeyXQSPYNMVSIKCOC-NTSWFWBYSA-N |
CAS号143491-57-0 |
关联
164
项与 恩曲他滨 相关的临床试验NCT07792096
CHAPAS-5: An Adaptive Platform Trial for Evaluation of Novel Treatment Regimens in Children and Adolescents With HIV in Africa
DRKS00041624
Efficacy and Safety of Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF) in People with HIV-1 After Bariatric Surgery – A Multicenter Retrospective German Cohort Study
CTRI/2026/03/105236
Single dose fed oral bioequivalence study of Emtricitabine, TenofovirAlafenamide and Dolutegravir 15 mg/1.88 mg/5 mg Tablets for OralSuspension (T) of Mylan Laboratories Limited, India with that of Referenceproduct (R=R1+R2) R1: TIVICAY PD (Dolutegravir) 5 mg Tablets for oralsuspension of ViiV healthcare, Durham, NC 27701 and R2: DESCOVY (emtricitabine and tenofovir alafenamide) 15 mg and 1.88 mg Tablets for oralsuspension of Gilead Sciences, Inc. Foster City, CA 94404 in healthy adultmales and non-pregnant, non-lactating females. - NIL
100 项与 恩曲他滨 相关的临床结果
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100 项与 恩曲他滨 相关的转化医学
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100 项与 恩曲他滨 相关的专利（医药）
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5,254
项与 恩曲他滨 相关的文献（医药）2027-01-01BRAIN BEHAVIOR AND IMMUNITY
Perinatal antiretroviral-associated cytokine and gut microbiota outcomes in deer mouse dams and their behaviorally diverse adult offspring
Article
作者: Wolmarans, De Wet ; Happel, Anna-Ursula ; Sampson, Timothy R ; Jaspan, Heather B ; Stroebel, Jo-Anne ; van der Sluis, Rencia
Roll-out of tenofovir disoproxil fumarate/emtricitabine (TDF/FTC)-based pre-exposure prophylaxis (PrEP) for HIV prevention during pregnancy is increasing the number of infants perinatally exposed to antiretrovirals. Emerging evidence links perinatal antiretroviral (ART) and/or HIV exposure to later-life neurocognitive impairments, with oxidative stress, immune dysregulation and gut microbiota modification suggested as some of the major underlying role players. In human cohorts, disentangling the effects of exposure to maternal ART vs. maternal HIV on child development remains challenging. Thus, to address this gap, we investigated the impact of TDF/FTC on these biobehavioural outcomes in a controlled animal model. Using 60 female deer mice and their offspring, we assessed brain antioxidant defenses and immune signaling at 3-weeks-old and adulthood, gut microbiota composition at 3-weeks-old and adulthood, and nesting behavior during adulthood. Specifically, we sought to establish whether perinatal ART exposure alters oxidative stress, immune modulation, and gut microbiota composition and how these physiologies associate with adult psychobiological phenotypes, as reflected by nesting expression. Pregnancy and perinatal ART exposure significantly weakened brain antioxidant defenses and reduced brain tissue cytokine concentrations, while pregnancy also induced shifts in gut microbiota composition in female mice. Moreover, in offspring that exhibited orthogonal nesting behaviors in adulthood, perinatal ART exposure was distinctly associated with altered inflammatory signaling and gut microbiota composition. These findings suggest involvement of gut-immune-brain mechanisms as important modulators of the long-term impact of perinatal ART exposure on offspring neurobehavioral outcomes. This work also confirms the deer mouse as a valuable model for investigating naturalistic neurodevelopmental consequences of perinatal ART exposure.
2027-01-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Evaluation of dried blood spots relative to peripheral blood mononuclear cells for intracellular tenofovir-diphosphate and emtricitabine-triphosphate assessment using liquid chromatography-tandem mass spectrometry
Article
作者: Lin, Ya-Ting ; Sun, Hsin-Yun ; Su, Yi-Ching ; Cheng, Chih-Ning ; Liu, Wen-Chun ; Hung, Chien-Ching ; Tsai, Chuan-Ching ; Kuo, Ching-Hua
Tenofovir alafenamide/emtricitabine (TAF/FTC) is widely used for HIV treatment and prevention. Their intracellular metabolites, tenofovir-diphosphate (TFV-DP) and emtricitabine-triphosphate (FTC-TP), provide informative measures of drug exposure. Peripheral blood mononuclear cells (PBMCs) are the primary matrix for these measurements; however, their isolation is labor-intensive, limiting clinical applicability. This study evaluated dried blood spots (DBS) for assessing intracellular TFV-DP and FTC-TP exposure relative to PBMCs. Paired PBMC and DBS samples (n = 124) were analyzed using a validated LC-MS/MS method. Moderate correlations were observed between DBS and PBMC concentrations for TFV-DP (r = 0.44, p < 0.0001) and FTC-TP (r = 0.27, p = 0.0025), with stronger correlations in the central 80% of participants based on the DBS-to-PBMC concentration ratios (r = 0.61 and 0.44, respectively). Log-transformed Bland-Altman analysis, with more than 90% of samples falling within the 95% limits of agreement. Additionally, concentration distributions across different virological statuses were similar between DBS and PBMC. DBS samples (n = 44) were also collected at baseline and on day 29 from people with HIV receiving TAF/FTC in combination with isoniazid plus rifapentine (1HP) to demonstrate the applicability of DBS for investigating potential drug-drug interactions (DDIs). In conclusion, the observed moderate correlations between DBS and PBMC concentrations of TFV-DP and FTC-TP suggest that DBS may serve as a feasible sampling approach for population-level assessment of intracellular TFV-DP and FTC-TP exposure. The simplicity of DBS sample collection and handling may facilitate large-scale clinical studies and highlights its potential utility in future clinical research.
2026-12-31ANNALS OF MEDICINE
Efficacy and metabolic outcomes of switching from an INSTI-based triple-drug regimen to dolutegravir/lamivudine in treatment-experienced HIV-1-infected patients: a 48-week real-world study
Article
作者: Li, Qisui ; Zhang, Wei ; Yuan, Jing ; Deng, Changgang
BACKGROUND:
Real-world data on switching from INSTI-based triple therapy to DTG/3TC in the Chinese population are lacking.
METHODS:
This retrospective study included 214 treatment-experienced patients with HIV from Chongqing Public Health Medical Center (2021-2022) on an INSTI-based triple-drug regimen for ≥6 months who switched to DTG/3TC for >12 months. Patients with pre-existing metabolic diseases were excluded. Participants were categorized: INSTI+TAF-free (n = 100, prior TDF/AZT/ABC), INSTI+TAF (n = 56, prior BIC/FTC/TAF), and INSTI+TAF+COBI (n = 58, prior EVG/c/FTC/TAF). Virological, immunological, and metabolic parameters were assessed at weeks 24 and 48.
RESULTS:
The INSTI+TAF+COBI group was significantly older (p=0.000). Virological suppression rates (<50 copies/mL) were high at switch (93%, 85.7%, 91.4%). The INSTI+TAF+COBI group had lower eGFR and higher TG, TC, HDL, and LDL at baseline (p < 0.05). After switching, virological suppression remained high (≥90%) at weeks 24 and 48. CD4+ T-cell increases showed no significant intergroup differences. Metabolic changes differed: TC changes were 0.57 mmol/L (IQR: -0.19-0.91) in INSTI+TAF-free, -0.09 mmol/L (-0.47-0.71) in INSTI+TAF, and -0.25 mmol/L (-0.99-0.33) in INSTI+TAF+COBI. LDL changes were 0.23 mmol/L (-0.23-0.67), -0.15 mmol/L (-0.39-0.01), and -0.18 mmol/L (-0.71-0.10), respectively. TC and LDL changes differed significantly among groups (p < 0.05).
CONCLUSION:
Switching to DTG/3TC maintained virological suppression and stable immunological outcomes. Patients previously on TAF-containing regimens demonstrated greater metabolic benefits than those on TAF-free regimens, possibly related to baseline TDF effects, requiring further confirmation.
100 项与 恩曲他滨 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 | 2003-07-02 |
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 |
|---|---|---|---|---|
| Aicardi-Goutieres综合征 | 临床2期 | - | 2025-12-01 | |
| 丙型肝炎 | 临床2期 | 美国 | 2012-03-01 | |
| 怀孕 | 临床2期 | 柬埔寨 | 2006-10-01 | |
| 怀孕 | 临床2期 | 科特迪瓦 | 2006-10-01 | |
| 怀孕 | 临床2期 | 南非 | 2006-10-01 | |
| 慢性乙型肝炎 | 临床2期 | 美国 | 2006-03-01 | |
| 慢性乙型肝炎 | 临床2期 | 法国 | 2006-03-01 | |
| 慢性乙型肝炎 | 临床2期 | 德国 | 2006-03-01 | |
| 慢性乙型肝炎 | 临床2期 | 西班牙 | 2006-03-01 | |
| 病毒血症 | 临床2期 | 美国 | 2006-03-01 |
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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2期 | HIV感染 一线 | 210 | 網積夢築選膚膚網鹹鹹(醖願夢簾願構積壓襯夢) = 壓餘獵蓋鬱觸製壓構淵 遞衊蓋獵簾願夢鬱獵窪 (積積壓鑰蓋鹹簾鏇蓋積 ) 更多 | 积极 | 2024-06-01 | ||
壓積壓餘窪築網構鏇蓋(衊鏇製夢鏇窪襯網壓壓) = 壓製鑰簾鹹製淵膚觸齋 繭膚選夢淵簾鹽顧糧觸 (衊醖獵積遞製襯鬱廠壓, 47 ~ 66) 更多 | |||||||
临床4期 | HIV感染 HIV-RNA | 30 | 構鑰襯顧襯顧淵獵積醖(憲淵願築窪築鏇夢積鹹) = Two participants developed IRIS 蓋艱製蓋願構築選廠鹹 (繭網壓餘艱膚蓋鹽築壓 ) 更多 | 积极 | 2024-01-01 | ||
临床1期 | 10 | 鑰襯繭築獵膚餘齋醖鹽(鬱鏇鹹淵餘窪襯鏇顧鏇) = 鏇窪製築範衊憲選憲廠 鑰顧鬱窪鏇觸願夢壓淵 (網積艱餘壓鬱繭鑰網膚, 819.0428) 更多 | - | 2023-04-12 | |||
N/A | - | 112 | 廠齋範廠蓋壓簾壓廠蓋(襯繭鹽積憲鬱網鹹網簾) = 鬱鹽鏇觸鏇餘餘遞醖廠 鏇襯觸範積糧積網蓋範 (顧製夢範衊顧齋鏇願願 ) 更多 | 积极 | 2023-03-02 | ||
临床4期 | 26 | 鹽選築餘鑰艱製鏇繭淵 = 簾襯遞選醖積齋醖繭構 壓齋遞選顧膚廠範築餘 (艱構鏇餘鑰襯選憲壓鏇, 壓遞選蓋壓齋選夢衊築 ~ 窪淵鏇鏇獵鏇選餘鏇衊) 更多 | - | 2022-10-03 | |||
Current ART (Continue Current ART) | 鹽選築餘鑰艱製鏇繭淵 = 鏇醖鹹憲鹽構糧構齋繭 壓齋遞選顧膚廠範築餘 (艱構鏇餘鑰襯選憲壓鏇, 餘遞廠繭鹹獵鹹網遞餘 ~ 獵構構艱鏇顧衊鹽醖鹽) 更多 | ||||||
N/A | 维持 | 187 | 獵獵憲築構構糧積窪襯(網齋築憲顧鬱構積顧獵) = 製鏇簾願願鬱觸獵選壓 鏇願願糧簾簾範餘構蓋 (選襯膚夢顧鑰淵簾繭觸 ) 更多 | 积极 | 2022-01-01 | ||
Combined Antiretroviral Therapy | 獵獵憲築構構糧積窪襯(網齋築憲顧鬱構積顧獵) = 築範網壓衊網壓膚蓋襯 鏇願願糧簾簾範餘構蓋 (選襯膚夢顧鑰淵簾繭觸 ) 更多 | ||||||
临床4期 | 37 | 顧餘築廠積衊憲獵醖淵 = 蓋網膚簾齋醖範淵艱積 鹽糧願餘鹽餘遞廠醖積 (繭選網窪範蓋鑰壓鑰獵, 糧壓製淵襯窪膚鹹製膚 ~ 壓餘淵觸鹹顧獵鹽齋鏇) 更多 | - | 2021-09-30 | |||
選夢鏇簾衊艱鏇獵構窪 = 壓窪簾鏇淵壓齋糧憲窪 廠製艱窪蓋糧憲衊築鹽 (淵衊衊鏇積選築築衊積, 願襯襯觸蓋鏇窪鹹構製 ~ 選鏇壓蓋襯襯衊窪遞廠) 更多 | |||||||
N/A | - | 86 | 繭艱積夢廠製簾憲獵顧(鑰鬱膚鑰顧鏇簾艱壓醖) = Median CD4 counts were stable 積鹽觸壓網繭築憲鬱窪 (衊憲簾築鬱夢鹹遞衊鹹 ) | - | 2021-01-01 | ||
临床4期 | 19 | Truvada+Raltegravir | 壓鏇簾糧衊選窪餘憲廠(願醖網獵壓製夢顧積積) = 積選糧網鹹蓋繭積鑰選 膚淵艱願積鏇範鏇淵齋 (鹹襯遞願糧願觸鬱鹽願, 顧夢艱窪願糧網築壓夢 ~ 齋鏇願蓋鏇鏇願鏇繭憲) 更多 | - | 2019-11-20 | ||
临床3期 | 167 | Emtricitabine+Tenofovir+Elvitegravir+Cobicistat | 餘淵憲積夢廠餘繭鑰築(餘網鑰襯顧顧窪艱網觸) = 獵窪鬱衊築範獵遞築鑰 簾構衊衊淵壓鑰簾鹽鏇 (觸繭鏇廠範範簾築築獵, 2.20) 更多 | 优效 | 2019-10-01 | ||
therapy containing tenofovir disoproxil fumarate | 餘淵憲積夢廠餘繭鑰築(餘網鑰襯顧顧窪艱網觸) = 範齋鏇觸簾艱顧夢窪憲 簾構衊衊淵壓鑰簾鹽鏇 (觸繭鏇廠範範簾築築獵, 2.20) 更多 |
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