预约演示
更新于：2025-03-24
Cobicistat/Darunavir
达芦那韦考比司他
更新于：2025-03-24
概要
基本信息
药物类型 小分子化药 |
别名 Darunavir / Cobicistat、Darunavir and Cobicistat、Darunavir Ethanolate/Cobicistat + [11] |
作用方式 抑制剂 |
作用机制 CYP3A抑制剂(细胞色素P450家族成员3A家族抑制剂)、HIV-1 pol抑制剂(人类免疫缺陷病毒1型蛋白酶抑制剂) |
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 欧盟 (2014-11-19), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (韩国) |
登录后查看时间轴
结构/序列
分子式C29H43N3O8S |
InChIKeyQWSHKNICRJHQCY-VBTXLZOXSA-N |
CAS号635728-49-3 |
查看全部结构式(2)
关联
20
项与 达芦那韦考比司他 相关的临床试验NCT05197075
A Study to Assess the Acceptability of the Darunavir/Cobicistat (DRV/COBI) Fixed-dose Combination (FDC) Tablet in Human Immunodeficiency Virus (HIV)-1 Infected Children Aged >=3 Years and Weighing >=15 kg to <25 kg
NCT05378906
A Single-dose, Open-label, Randomized, Crossover Pivotal Bioequivalence Study in Healthy Participants to Assess the Bioequivalence of Darunavir 600 mg in the Presence of Cobicistat 90 mg When Administered as a Fixed Dose Combination Tablet (Darunavir/Cobicistat) Compared to the Co-administration of the Separate Available Formulations (Darunavir 100 mg/mL Suspension at a Dose of 600 mg and Cobicistat 90 mg Tablet), Under Fed Conditions
NCT04718805
A Single-dose, Open-label, Randomized, Crossover Pivotal Bioequivalence Study in Healthy Participants to Assess the Bioequivalence of Darunavir 675 mg in the Presence of 150 mg Cobicistat When Administered as a Fixed Dose Combination (Darunavir/Cobicistat) Compared to the Co-administration of the Separate Agents (Darunavir and Cobicistat) Under Fed Conditions
100 项与 达芦那韦考比司他 相关的临床结果
登录后查看更多信息
100 项与 达芦那韦考比司他 相关的转化医学
登录后查看更多信息
100 项与 达芦那韦考比司他 相关的专利（医药）
登录后查看更多信息
14
项与 达芦那韦考比司他 相关的文献（医药）2022-06-01Chemistry & biodiversity3区 · 化学
Design, Synthesis and in Vitro Antifungal Mechanism of Novel Phenylalanine Derivatives
3区 · 化学
Article
作者: Niu, Xue ; Zhang, Chengzhi ; Zhang, Hong ; Wu, Zhibing ; Dou, Li
Abstract:
To explore novel molecules with unique mechanisms against plant pathogenic fungi, a series of phenylalanine derivatives containing a 1,3,4‐oxadiazothioether moiety were designed and synthesized. Bioassays revealed that some target compounds at 100 μg/mL exhibited excellent antifungal activities against Thanatephorus cucumeris, such as G6 (92.1 %), G10 (94.3 %), G18 (99.1 %), and G19 (98.7 %), better than that of the commercial fungicide azoxystrobin (90.6 %), and the EC50 value of G10 against T. cucumeris was 31.9 μg/mL. Further mechanism studies of T. cucumeris treated with G10 demonstrated that this compound can affect the growth of mycelia by disrupting the integrity of the membrane, and the higher the concentration of the compound is, the greater the degree of membrane integrity damage, similar to the commercial fungicide azoxystrobin. These conclusions provide important information for further mechanism studies of this series of phenylalanine derivatives.
2020-10-01Theriogenology2区 · 农林科学
Embryo yield and quality are associated with progestogen treatment during superovulation protocol in lactating Lacaune ewes
2区 · 农林科学
Article
作者: Oliveira, Maria Emilia Franco ; Figueira, Lucas Machado ; Alves, Nadja Gomes ; Souza-Fabjan, Joanna Maria Gonçalves de ; Lima, Renato Ribeiro de ; Maia, Ana Lucia Rosa E Silva ; Morais, Maria Clara da Cruz ; Batista, Ribrio Ivan Tavares Pereira ; Fonseca, Jeferson Ferreira da
This study assessed the effect of progestogen treatment length on ovarian parameters and embryo yield in superovulated Lacaune ewes collected by nonsurgical embryo recovery. Twenty-three lactating ewes were superovulated 30 d apart using a cross-over design. All ewes received 60 mg of MAP intravaginal sponges for 6 (G-6 group) or 9 (G-9 group) d. A total dose of 133 mg pFSH was given in six decreasing doses (twice a day) starting at 60 h before device removal. Ultrasound examination of the ovaries was performed at the first pFSH injection and one day before embryo recovery, which was performed 6-7 d after the onset of estrus. Embryo recovery was conducted only in ewes that expressed estrus and were mated. There was no difference (P > 0.05) in the total number of follicles between G-6 (15.7 ± 1.0) and G-9 (15.6 ± 0.8) at the time of the first pFSH treatment. The percentage of responding donors with ≥3 corpora lutea (CL; 78.2% [18/23] vs 69.5% [16/23]), mean (±SEM) CL number (7.0 ± 1.2 vs 8.1 ± 1.6), transcervical passage rate (94.4% [17/18] vs 83.3% [15/18], and ova/embryo recovery rate (54.5% [60/110] vs 68.0% [83/122]) were not different (P > 0.05) between the G-6 and G-9 groups. However, the mean number of viable embryos was lower (P < 0.05) in the G-6 group (1.8 ± 0.7) than in the G-9 group. (3.5 ± 1.1). In conclusion, treatment with an intravaginal MAP sponge for 9 d during a superovulation protocol is beneficial for viable embryo yield in Lacaune ewes out of the breeding season.
2020-08-01International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases
Lack of antiviral activity of darunavir against SARS-CoV-2
Article
作者: Van Damme, Ellen ; Buyck, Christophe ; Ciesek, Sandra ; Woodfall, Brian ; Van Loock, Marnix ; Cinatl, Jindrich ; De Meyer, Sandra ; Bojkova, Denisa
OBJECTIVES:
Given the high need and the absence of specific antivirals for treatment of COVID-19 (the disease caused by severe acute respiratory syndrome-associated coronavirus-2 [SARS-CoV-2]), human immunodeficiency virus (HIV) protease inhibitors are being considered as therapeutic alternatives.
METHODS:
Prezcobix/Rezolsta is a fixed-dose combination of 800 mg of the HIV protease inhibitor darunavir (DRV) and 150 mg cobicistat, a CYP3A4 inhibitor, which is indicated in combination with other antiretroviral agents for the treatment of HIV infection. There are currently no definitive data on the safety and efficacy of DRV/cobicistat for the treatment of COVID-19. The in vitro antiviral activity of darunavir against a clinical isolate from a patient infected with SARS-CoV-2 was assessed.
RESULTS:
DRV showed no antiviral activity against SARS-CoV-2 at clinically relevant concentrations (EC50 > 100 μM). Remdesivir, used as a positive control, demonstrated potent antiviral activity (EC50 = 0.38 μM).
CONCLUSIONS:
Overall, the data do not support the use of DRV for the treatment of COVID-19.
100 项与 达芦那韦考比司他 相关的药物交易
登录后查看更多信息
外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| HIV感染 | 欧盟 | 2014-11-19 | |
| HIV感染 | 冰岛 | 2014-11-19 | |
| HIV感染 | 列支敦士登 | 2014-11-19 | |
| HIV感染 | 挪威 | 2014-11-19 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 获得性免疫缺陷综合征 | 临床3期 | 美国 | 2016-05-01 | |
| 怀孕 | 临床3期 | 美国 | 2009-04-09 | |
| 怀孕 | 临床3期 | 波多黎各 | 2009-04-09 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | - | 12 | 鑰構鹹憲範壓鬱窪艱積(衊願衊艱觸艱鹽衊鬱鹽) = 襯鏇願膚艱糧築醖齋觸 夢繭遞艱觸鏇範鏇獵齋 (蓋網蓋範蓋憲醖壓淵遞, 401.58) 更多 | - | 2023-12-01 | ||
N/A | 400 | 襯選餘簾襯廠製憲鏇遞(範鹹壓衊鬱構築製憲積) = 構齋餘願鑰顧憲夢衊顧 壓糧簾淵鹽繭艱淵遞鏇 (膚膚鬱糧顧選蓋觸製窪, 4 ~ 13) 更多 | 不佳 | 2022-01-01 | |||
襯選餘簾襯廠製憲鏇遞(範鹹壓衊鬱構築製憲積) = 廠艱觸鏇簾繭衊憲壓構 壓糧簾淵鹽繭艱淵遞鏇 (膚膚鬱糧顧選蓋觸製窪, 3 ~ 8) 更多 | |||||||
N/A | 339 | 選遞鹽餘窪積淵鹹糧獵(膚築鏇齋艱繭衊膚憲築) = 遞齋網窪淵築膚構願構 鹹獵願簾蓋憲積願齋艱 (簾鹹簾觸衊壓鏇鬱餘簾 ) 更多 | - | 2022-01-01 | |||
選遞鹽餘窪積淵鹹糧獵(膚築鏇齋艱繭衊膚憲築) = 衊夢網衊構網艱鹹襯顧 鹹獵願簾蓋憲積願齋艱 (簾鹹簾觸衊壓鏇鬱餘簾 ) 更多 | |||||||
临床4期 | - | 8 | Cobicistat+Darunavir (Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg)) | 網願範膚憲簾醖簾範網(構艱簾製繭製遞糧鑰築) = 餘獵夢觸鑰鹹觸選蓋製 壓願齋簾鑰構遞廠鬱窪 (鏇夢淵構醖鹹繭廠願膚, 952) 更多 | - | 2018-06-12 | |
Cobicistat+Darunavir (Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg)) | 網願範膚憲簾醖簾範網(構艱簾製繭製遞糧鑰築) = 築衊憲糧膚積鹽獵糧襯 壓願齋簾鑰構遞廠鬱窪 (鏇夢淵構醖鹹繭廠願膚, 265) 更多 | ||||||
N/A | - | 761 | 鑰簾齋膚繭憲艱簾襯壓(構壓築醖衊艱獵糧醖觸) = 顧願齋壓鑰遞糧顧壓窪 憲淵簾積衊鑰構憲蓋襯 (鏇鹽製廠膚廠鹹鹽簾糧 ) | - | 2018-01-01 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用