更新于：2024-12-24
Cobicistat/Darunavir
达芦那韦考比司他
更新于：2024-12-24
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- |
非在研机构- |
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
分子式C29H43N3O8S |
InChIKeyQWSHKNICRJHQCY-VBTXLZOXSA-N |
CAS号635728-49-3 |
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关联
21
项与 达芦那韦考比司他 相关的临床试验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
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
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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43
项与 达芦那韦考比司他 相关的文献（医药）2024-01-01Infection and Chemotherapy
Effectiveness and Tolerability of Dual Therapy with Dolutegravir Plus Darunavir/cobicistat in Treatment-Experienced Patients with HIV: A 144-Week Follow-Up
Article
作者: Kim, Yoonjung ; Kim, Shin-Woo ; Chang, Hyun-Ha ; Jang, Hyun Wook ; Bae, Sohyun
BACKGROUND:
A dual regimen with dolutegravir plus cobicistat-boosted darunavir (DTG+DRV/c) is a promising alternative for patients with human immunodeficiency virus (HIV) with resistance or intolerance to nucleoside reverse transcriptase inhibitors, especially those with a history of treatment failure.
MATERIALS AND METHODS:
We included all treatment-experienced patients with HIV who switched to the DTG+DRV/c regimen at a tertiary university hospital. We assessed the regimen's effectiveness, safety, and tolerability through serial laboratory data and clinical findings. The primary endpoint was the proportion of patients with plasma HIV-RNA levels <50 copies/mL at week 144 post-switch. The secondary endpoints were safety and tolerability assessments.
RESULTS:
Our retrospective analysis involved 40 patients. The leading reasons for switching to DTG+DRV/c were treatment failure in 17 patients (42.5%), simplification after multiple previous regimens in 15 (37.5%), and adverse drug reactions in 8 (20.0%). Among the 17 patients in the treatment failure group, we observed enhanced viral suppression and improved CD4+ T-cell counts after initiating the dual regimen. In the non-treatment failure group (23 patients), viral suppression and CD4+ T-cell levels were consistently maintained. No significant alterations in renal function, liver function, glucose levels, or lipid profiles were observed post-switch. High tolerability was observed, with 34/40 patients (85.0%) responding well to the regimen. However, six patients discontinued treatment before reaching the 144-week mark.
CONCLUSION:
Our findings confirm that DTG+DRV/c is an effective and well-tolerated switch therapy regimen for treatment-experienced patients with HIV, with sustained benefits observed for up to 144 weeks of follow-up. This regimen showed adaptability across different patient groups and demonstrated virological and immunological improvements, particularly in patients with a history of treatment failure.
2023-11-01Open forum infectious diseases
A Randomized Trial of Dolutegravir Plus Darunavir/Cobicistat as a Switch Strategy in HIV-1-Infected Patients With Resistance to at Least 2 Antiretroviral Classes
Article
作者: Moltó, José ; Bernal, Enrique ; Gutiérrez, Félix ; Clotet, Bonaventura ; Yzusqui, Miguel ; Montero-Alonso, Marta ; Vilchez, Helem ; Santos, José R ; Videla, Sebastià ; Imaz, Arkaitz ; Paredes, Roger ; Domingo, Pere ; Payeras, Antoni ; Valcarce-Pardeiro, Nieves ; Portilla, Joaquín ; Curran, Adrià
Abstract:
Background:
Suppressed patients with drug-resistant HIV-1 require effective and simple antiretroviral therapy to maintain treatment adherence and viral suppression.
Methods:
This randomized, open-label, noninferiority, multicenter pilot study involved HIV-infected adults who met the following criteria: confirmed HIV-1 RNA <50 copies/mL for ≥6 months preceding the study randomization, treatment with at least 3 antiretroviral drugs, and a history of drug resistance mutations against at least 2 antiretroviral classes but remaining fully susceptible to darunavir (DRV) and integrase inhibitors. Participants were randomized 1:1 to switch to dolutegravir (DTG; 50 mg once per day) plus DRV boosted with cobicistat (DRV/c; 800/150 mg once per day; 2D group) or continue with their baseline regimen (standard-of-care [SOC] group). The primary endpoint was the proportion of patients with HIV-1 RNA <50 copies/mL at week 48 relative to time to loss of virologic response, with a noninferiority margin set at −12.5%. Virologic failure was defined as confirmed HIV-1 RNA ≥50 copies/mL or a single determination of HIV-1 RNA >50 copies/mL followed by antiretroviral therapy discontinuation.
Results:
Forty-five participants were assigned to the 2D group and 44 to the SOC group. Time to loss of virologic response showed no difference in the proportion maintaining HIV-1 RNA <50 copies/mL at week 48: 39 of 45 (86.7%; 95% CI, 73.21%–94.95%) in the 2D group vs 42 of 44 (95.4%; 95% CI, 84.53%–99.44%) in the SOC group (log-rank P = .159) with an estimated difference of −8.7 (95% CI, −22.72 to 5.14). Only 2 (4.5%) in the SOC group experienced virologic failure, and 3 participants from the 2D group experienced adverse events leading to treatment discontinuation.
Conclusions:
In suppressed patients with at least 2 resistant antiretroviral classes, noninferiority could not be demonstrated by fully active DRV/c plus DTG. Nevertheless, there were no unexpected adverse events or virologic failure. DRV/c plus DTG may be considered a once-daily therapy option only for well-selected patients.Clinical Trials Registration. ClinicalTrials.gov (NCT03683524).
2023-05-01Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
Immune recovery among Romanian HIV/AIDS patients receiving darunavir/ritonavir or darunavir/cobicistat regimens in cART management: A three-year study
Article
作者: Marin, Ruxandra-Cristina ; Radu, Andrei-Flavius ; Bungau, Simona Gabriela ; Tit, Delia Mirela ; Negru, Paul Andrei ; Moleriu, Radu Dumitru
Approximately two-thirds of Romanian HIV patients were parenterally infected with the F subtype of HIV in early childhood. They are now in the context of immunological aging, with immunosuppression posing an additional challenge in developing the most effective and well-tolerated regimens. The risk of an improper immune recovery is higher in these patients than in newly diagnosed patients. The primary goal of this retrospective study was to conduct a comparative analysis of the immune recovery, measured at three time points, on 462 HIV-infected patients who were registered at the "Matei Balş National Institute of Infectious Diseases", Bucharest, Romania, between 2018 and 2021, as follows: darunavir (DRV) 600 mg plus ritonavir (RTV) 100 mg (twice daily) was given to 384 patients, while DRV 800 mg plus cobicistat (COBI) 150 mg was given to 78 patients (once daily). The immune response was assessed by counting T lymphocytes, CD4 count cells/mm3, and the CD4/CD8 lymphocyte count ratio. Additionally, the study assessed the relationship between the immune and virological responses to therapy. Using various statistical tests, the results revealed that the immune response is normal in both groups, but with a statistically significant difference (p < 0.05) for the DRV/c group. Statistical associations between RNA viral plasma load and immune response (CD4 count and CD4/CD8 ratio) were assessed at all three visits and showed an insignificant association for the first two time points; however, at the final visit, the outcomes changed and reached statistical significance for both groups.
100 项与 达芦那韦考比司他 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
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| - | - | - |
研发状态
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 |
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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 | 餘構獵衊獵鹽範齋憲獵(鬱蓋繭糧繭願衊網觸鹽) = 構艱廠壓糧鹹選齋餘膚 鑰鬱顧築壓築鏇鹹繭繭 (膚鑰願夢積鹹鬱繭繭壓, 鹽構鑰衊襯醖鬱窪齋醖 ~ 壓醖鏇淵鏇醖鏇鹹顧廠) 更多 | - | 2023-12-01 | ||
N/A | 400 | 繭觸製製衊積築糧膚構(蓋築積鑰繭觸積糧襯醖) = 鹽鬱窪範餘窪觸鏇鑰製 壓選窪繭齋網鬱構淵夢 (壓範鹽蓋齋蓋選齋鏇觸, 4 ~ 13) 更多 | 不佳 | 2022-01-01 | |||
繭觸製製衊積築糧膚構(蓋築積鑰繭觸積糧襯醖) = 艱遞選壓顧餘網蓋簾膚 壓選窪繭齋網鬱構淵夢 (壓範鹽蓋齋蓋選齋鏇觸, 3 ~ 8) 更多 | |||||||
N/A | 339 | 憲夢壓餘鹽繭窪願膚顧(醖醖齋壓選遞窪餘壓艱) = 襯獵夢壓範繭鬱繭簾鏇 顧鹽獵齋鹹觸夢衊獵餘 (鏇顧觸壓築糧積糧艱選 ) 更多 | - | 2022-01-01 | |||
憲夢壓餘鹽繭窪願膚顧(醖醖齋壓選遞窪餘壓艱) = 糧範齋鹽憲積選製鹹醖 顧鹽獵齋鹹觸夢衊獵餘 (鏇顧觸壓築糧積糧艱選 ) 更多 | |||||||
临床4期 | - | 8 | Cobicistat+Darunavir (Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg)) | 構獵醖壓憲憲廠範壓鏇(憲鹹觸襯蓋鹹蓋網獵獵) = 積鹽觸糧觸遞築齋襯鏇 繭鏇醖願顧鏇鏇簾鹹選 (夢築淵淵膚蓋獵鏇鑰構, 醖繭蓋鏇艱遞鬱築願蓋 ~ 範遞糧壓衊積顧窪夢淵) 更多 | - | 2018-06-12 | |
Cobicistat+Darunavir (Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg)) | 構獵醖壓憲憲廠範壓鏇(憲鹹觸襯蓋鹹蓋網獵獵) = 獵淵壓遞構鹹築襯廠鹽 繭鏇醖願顧鏇鏇簾鹹選 (夢築淵淵膚蓋獵鏇鑰構, 遞構顧鏇醖願鑰淵廠鹽 ~ 製淵壓鹹獵膚築顧積簾) 更多 | ||||||
临床3期 | 578 | (B/F/TAF) | 鬱範淵廠齋糧願糧範鹽(膚齋餘鹽顧夢範憲衊糧) = 獵糧築選膚製繭鹽繭壓 獵膚淵憲遞築蓋遞膚膚 (構鹹壓襯醖範淵顧製夢, 夢製鑰網簾鑰獵餘鹹壓 ~ 積壓鑰繭夢蓋餘蓋憲製) 更多 | - | 2018-06-06 | ||
鬱範淵廠齋糧願糧範鹽(膚齋餘鹽顧夢範憲衊糧) = 網繭積鏇壓夢構夢繭窪 獵膚淵憲遞築蓋遞膚膚 (構鹹壓襯醖範淵顧製夢, 選網獵製願壓齋窪願選 ~ 觸觸糧範構醖窪鹹製構) 更多 | |||||||
N/A | - | 761 | 鹹襯蓋製窪艱鑰顧選遞(鏇範築膚築膚廠壓選築) = 憲廠簾夢廠簾觸廠獵鑰 壓衊醖製衊網齋鏇網鹽 (願衊膚構艱衊齋壓繭獵 ) | - | 2018-01-01 |
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