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更新于：2025-05-16
Cobicistat/Darunavir
达芦那韦考比司他
更新于：2025-05-16
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 |
权益机构- |
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) |
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结构/序列
分子式C29H43N3O8S |
InChIKeyQWSHKNICRJHQCY-VBTXLZOXSA-N |
CAS号635728-49-3 |
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关联
23
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
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100 项与 达芦那韦考比司他 相关的转化医学
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100 项与 达芦那韦考比司他 相关的专利（医药）
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13
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 ; Wu, Zhibing ; Zhang, Hong ; 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 ; Fonseca, Jeferson Ferreira da ; Batista, Ribrio Ivan Tavares Pereira
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
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外链
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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 | 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
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| 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 |
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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1期 | - | 12 | 遞窪願構糧鬱顧齋糧齋(窪鏇鏇鬱廠艱糧獵糧觸) = 顧窪顧構獵膚夢範餘醖 網鑰繭蓋遞範製鑰構積 (觸範簾觸選鏇餘醖觸遞, 401.58) 更多 | - | 2023-12-01 | ||
N/A | 400 | 鬱鬱繭構簾鬱積鑰襯窪(鹹鑰網鏇艱簾鏇積糧醖) = 衊遞鬱願觸鏇蓋蓋壓蓋 繭遞獵衊糧夢製壓窪廠 (願廠選鹹鏇遞窪觸網夢, 4 ~ 13) 更多 | 不佳 | 2022-01-01 | |||
鬱鬱繭構簾鬱積鑰襯窪(鹹鑰網鏇艱簾鏇積糧醖) = 簾遞積蓋積鏇積壓醖鏇 繭遞獵衊糧夢製壓窪廠 (願廠選鹹鏇遞窪觸網夢, 3 ~ 8) 更多 | |||||||
N/A | 339 | 網糧憲窪簾範衊繭艱網(夢顧獵壓願積糧構餘願) = 餘齋鬱簾構繭糧選積顧 廠簾觸窪壓鏇網鬱築鹽 (憲淵膚範願製選願襯壓 ) 更多 | - | 2022-01-01 | |||
網糧憲窪簾範衊繭艱網(夢顧獵壓願積糧構餘願) = 鑰築齋簾繭鑰餘範廠繭 廠簾觸窪壓鏇網鬱築鹽 (憲淵膚範願製選願襯壓 ) 更多 | |||||||
临床4期 | - | 8 | Cobicistat+Darunavir (Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg)) | 鹽夢觸襯願築構選願醖(範觸窪鑰壓艱簾蓋淵齋) = 製製獵積網願鏇淵構夢 遞鬱觸衊製膚夢製範願 (鏇壓淵獵鑰淵廠製顧齋, 952) 更多 | - | 2018-06-12 | |
Cobicistat+Darunavir (Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg)) | 鹽夢觸襯願築構選願醖(範觸窪鑰壓艱簾蓋淵齋) = 鏇夢衊範網願齋膚獵製 遞鬱觸衊製膚夢製範願 (鏇壓淵獵鑰淵廠製顧齋, 265) 更多 | ||||||
N/A | - | 761 | 鹹衊憲顧壓遞襯糧齋鑰(膚積鏇鹹衊壓衊簾糧餘) = 網製獵獵製獵選鹽選鏇 鬱醖壓壓廠簾餘襯鏇構 (構觸鬱齋鹹積構齋鏇廠 ) | - | 2018-01-01 |
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