天冬氨酸替诺福韦酯(Tenofovir Disoproxil Aspartate) - 药物靶点：RT_专利_临床

概要

基本信息

药物类型

小分子化药

别名

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

感染消化系统疾病

在研适应症-

非在研适应症

慢性乙型肝炎

原研机构

Chong Kun Dang Pharmaceutical Corp.

在研机构-

非在研机构

Chong Kun Dang Pharmaceutical Corp.

权益机构-

最高研发阶段无进展临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C23H37N6O14P

InChIKeyCCIDLBRRXVNEDK-KJTVYDLOSA-N

CAS号1571075-19-8

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关联

2

项与天冬氨酸替诺福韦酯相关的临床试验

NCT02805738

/ Unknown status临床3期

A Multicenter, Randomized, Double-blind, Parallel Design, Phase III Clinical Trial to Evaluate the Efficacy and Safety of CKD-390 Tablet and Viread® Tablet in Chronic Hepatitis B Patients

A Multicenter, Randomized, Double-blind, Parallel Design, Phase III Clinical Trial to Evaluate the Efficacy and Safety of CKD-390 tablet

开始日期2016-04-01

申办/合作机构

Chong Kun Dang Pharmaceutical Corp.

NCT02589457

/ Completed临床1期

A Randomized, Open-label, Single-dosing, 2x2 Crossover Study to Compare the Safety and Pharmacokinetics of CKD-390 Tablet (Tenofovir Disoproxil Aspartate) With Viread® Tablet (Tenofovir Disoproxil Fumarate) in Healthy Male Volunteers

The purpose of this study is to compare the safety and pharmacokinetics of CKD-390(Tenofovir Disoproxil Aspartate) and Viread® tablet(Tenofovir Disoproxil Fumarate) in healthy male volunteers.

开始日期2015-10-01

申办/合作机构

Chong Kun Dang Pharmaceutical Corp.

100 项与天冬氨酸替诺福韦酯相关的临床结果

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100 项与天冬氨酸替诺福韦酯相关的转化医学

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100 项与天冬氨酸替诺福韦酯相关的专利（医药）

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321

项与天冬氨酸替诺福韦酯相关的文献（医药）

2025-03-01·International Journal of STD & AIDS

Therapeutic drug monitoring of tenofovir disoproxil and emtricitabine in oral HIV pre-exposure prophylaxis (PrEP) users who have undergone gastrointestinal surgery

Article

作者: Jones, Rachael ; Tariq, Shema ; Coleman, Harry ; Ismail, Muhammad Azam ; Pool, Erica ; Stegmann, Katrina ; Teh, Yee Suh ; Loftus, Hannah ; Boffito, Marta ; Tyler, Stephanie ; Tittle, Victoria ; Nakamura, Anna ; Dosekun, Olamide ; Girometti, Nicolo

Objectives Oral HIV pre-exposure prophylaxis (PrEP) is highly effective in preventing HIV, but its efficacy depends on adequate absorption of drug, which may decrease following gastrointestinal surgery. Methods Clinicians across eight Genito-urinary Medicine clinics in the United Kingdom submitted data on PrEP users with history of gastrointestinal surgery who were referred to a national complex PrEP multi-disciplinary team between June 2021 and April 2023. Anonymised data were submitted on demographics, surgical history, PrEP regimen, and results of therapeutic drug monitoring (TDM) and HIV screening tests. Descriptive analyses were performed in SPSS version 29. Results Nine cases described cis-gender men-who-have-sex-with-men (MSM) with median age of 47.4 years (IQR = 43 – 56.5) taking tenofovir disoproxil (TDF)/emtricitabine (FTC) daily ( n = 8) or event-based ( n = 1) as PrEP. Median time between PrEP initiation and TDM was 53 days (IQR = 8.5–1705). The mean (±SD) trough concentration of tenofovir (TFV) and FTC were 90.2 ± 27.7 ng/mL and 76.0 ± 45.9 ng/mL, respectively. All patients had a negative HIV test at follow-up. Conclusions Plasma trough concentrations of TFV observed in our cohort taking TDF/FTC were above the expected concentrations associated with PrEP efficacy as previously described in the literature, suggesting that PrEP can be safely given in this population, with TDM used for reassurance.

2025-02-28·Open Forum Infectious Diseases

Preswitch Regimens Associated With Weight Gain Among Persons With HIV who Switch to Integrase Inhibitor–Containing Regimens

Article

作者: Okeke, Nwora Lance ; Cutshaw, Melissa Klein ; Harding, Mahmoud ; Davenport, Clemontina A

AbstractBackgroundWeight gain associated with integrase strand transfer inhibitors (INSTIs) is well documented. However, recent reports suggest that the observed weight gain among persons who switch to INSTIs may be associated with their preswitch regimen.MethodsWe conducted retrospective analyses of persons with HIV on antiretroviral therapy who switched to a second-generation INSTI–containing regimen (bictegravir/dolutegravir) at the Duke Adult Infectious Diseases Clinic (Durham, NC, USA) between 2014 and 2021. The outcome was weight change, operationalized as percent weight change, absolute weight change (kg), gaining ≥5% of preswitch weight, and gaining ≥10% of preswitch weight. The primary exposure was preswitch regimen.ResultsOur analysis included 750 persons. Cohort demographics were as follows: mean age (SD) 51 (11) years, 30% female at birth, 58% Black, 4% Hispanic ethnicity. At regimen switch, the mean CD4 count was 701 cells/mm3, and 68% had a viral load ≤20 copies/cc. Persons with preswitch regimens containing efavirenz had higher odds of gaining ≥5% body weight (odds ratio [OR], 1.62, 95% CI, 1.13–2.32) and ≥10% body weight (OR, 1.68; 95% CI, 1.02–2.73) after regimen switch, adjusted for age, sex, race, ethnicity, and preswitch body mass index. Persons with preswitch regimens containing tenofovir disoproxil (TDF) also had higher odds of gaining ≥5% body weight (OR, 1.64; 95% CI, 1.17–2.30).ConclusionsPreswitch regimens containing efavirenz and TDF were associated with significant weight gain after switching to INSTI-based regimens. Our findings support the hypothesis that the weight gain observed with switching to INSTI-based regimens could be driven by stopping medications with weight-suppressing properties.

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.

100 项与天冬氨酸替诺福韦酯相关的药物交易

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