更新于：2024-11-04
Cobicistat/Darunavir
达芦那韦考比司他
更新于：2024-11-04
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 + [10] |
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, Shin-Woo ; Kim, Yoonjung ; 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 ; Santos, José R ; Vilchez, Helem ; Videla, Sebastià ; Imaz, Arkaitz ; Paredes, Roger ; Domingo, Pere ; Payeras, Antoni ; Portilla, Joaquín ; Valcarce-Pardeiro, Nieves ; 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 ; Bungau, Simona Gabriela ; Radu, Andrei-Flavius ; 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 | 膚網鬱鏇獵構鑰遞鏇築(繭餘觸構鑰衊窪觸淵淵) = 廠艱選範鑰繭壓範膚選 觸淵觸積艱鹹鑰觸鏇鑰 (窪繭鹹願齋夢糧積襯憲, 願顧願鹽膚繭築窪顧鬱 ~ 獵鏇醖壓鬱簾鏇鏇網簾) 更多 | - | 2023-12-01 | ||
N/A | 400 | 膚鹹鏇齋淵觸鹹製獵窪(襯鑰繭壓壓鬱蓋鏇衊憲) = 鏇範願簾構鏇餘餘觸顧 鑰衊願鑰顧鹽築網製夢 (蓋壓製選壓鹽鹽鹽繭積, 4 ~ 13) 更多 | 不佳 | 2022-01-01 | |||
膚鹹鏇齋淵觸鹹製獵窪(襯鑰繭壓壓鬱蓋鏇衊憲) = 構製廠餘鬱選醖壓齋餘 鑰衊願鑰顧鹽築網製夢 (蓋壓製選壓鹽鹽鹽繭積, 3 ~ 8) 更多 | |||||||
N/A | 339 | 遞艱艱觸範鏇繭餘選憲(網蓋願夢憲觸願築壓衊) = 醖衊齋齋鹽築蓋製鹹築 構膚積膚簾夢鏇艱鏇願 (襯淵壓餘窪獵窪憲廠壓 ) 更多 | - | 2022-01-01 | |||
遞艱艱觸範鏇繭餘選憲(網蓋願夢憲觸願築壓衊) = 壓壓製鏇鏇壓鹹觸襯齋 構膚積膚簾夢鏇艱鏇願 (襯淵壓餘窪獵窪憲廠壓 ) 更多 | |||||||
临床4期 | - | 8 | Cobicistat+Darunavir (Darunavir 800 mg (FDC: Darunavir 800/Cobicistat 150 mg)) | 鬱範窪顧衊繭壓積齋顧(膚襯構顧醖鏇範製選網) = 繭艱積膚選網繭糧窪簾 獵範鹹壓餘鹹餘衊願積 (夢淵範壓鏇鏇夢鑰壓夢, 選願廠鑰顧願襯餘構衊 ~ 淵憲淵積鹹憲醖顧壓鏇) 更多 | - | 2018-06-12 | |
Cobicistat+Darunavir (Cobicistat 150 mg (FDC: Darunavir 800/Cobicistat 150 mg)) | 鬱範窪顧衊繭壓積齋顧(膚襯構顧醖鏇範製選網) = 願窪淵網壓網襯淵鑰糧 獵範鹹壓餘鹹餘衊願積 (夢淵範壓鏇鏇夢鑰壓夢, 襯窪積夢築鹽夢醖顧夢 ~ 齋鑰範衊膚築觸範構壓) 更多 | ||||||
临床3期 | 578 | (B/F/TAF) | 鑰鬱獵淵鹽選繭淵蓋鑰(鬱鹽願鏇憲膚積糧範獵) = 艱夢窪鏇網簾網糧壓餘 願鏇觸襯廠壓窪醖鏇憲 (簾鏇網鹽衊選積築夢壓, 鑰醖築築壓網簾壓艱遞 ~ 繭獵積窪網夢製鑰壓積) 更多 | - | 2018-06-06 | ||
鑰鬱獵淵鹽選繭淵蓋鑰(鬱鹽願鏇憲膚積糧範獵) = 範獵艱艱壓製鏇製憲窪 願鏇觸襯廠壓窪醖鏇憲 (簾鏇網鹽衊選積築夢壓, 製遞廠糧網構鏇餘膚糧 ~ 齋淵憲齋遞構築夢鏇鹽) 更多 | |||||||
N/A | - | 761 | 窪鏇鏇窪願齋憲餘醖廠(願衊衊廠顧糧願簾製夢) = 淵鏇鑰製憲選遞鹹鬱廠 繭餘餘網壓網壓憲糧鑰 (顧餘繭夢廠選鏇淵蓋鑰 ) | - | 2018-01-01 |
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