预约演示
更新于：2024-12-27
Atazanavir Sulfate/Ritonavir
硫酸阿扎那韦/利托那韦
更新于：2024-12-27
概要
基本信息
非在研机构- |
最高研发阶段申请上市 |
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C38H54N6O11S |
InChIKeyDQSGVVGOPRWTKI-QVFAWCHISA-N |
CAS号229975-97-7 |
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关联
24
项与 硫酸阿扎那韦/利托那韦 相关的临床试验NCT04518228
Pharmacokinetic Properties of Antiretroviral and Anti-Tuberculosis Drugs During Pregnancy and Postpartum
NCT04459286
A Randomized, Open Label Trial to Investigate the Efficacy and Safety of Nitazoxanide Plus Atazanavir/Ritonavir for the Treatment of COVID-19: a Pilot Study
NCT04022967
Randomized, Non-inferiority Trial Comparing a Dual Maintenance Therapy Strategy With Dolutegravir + Lamivudine (DTG/3TC) or Atazanavir/Ritonavir + Lamivudine (ATV/r+3TC) Versus the Standard WHO First Line Triple Therapy Tenofovir + Lamivudine + Efavirenz (TDF+3TC+EFV) or Dolutegravir + Lamivudine + Tenofovir (DTG+3TC+TDF) in West and Central African HIV-1 Infected Patients
100 项与 硫酸阿扎那韦/利托那韦 相关的临床结果
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100 项与 硫酸阿扎那韦/利托那韦 相关的转化医学
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100 项与 硫酸阿扎那韦/利托那韦 相关的专利（医药）
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3
项与 硫酸阿扎那韦/利托那韦 相关的文献（医药）2010-08-24AIDS (London, England)2区 · 医学
Similar efficacy and tolerability of atazanavir compared with atazanavir/ritonavir, each with abacavir/lamivudine after initial suppression with abacavir/lamivudine plus ritonavir-boosted atazanavir in HIV-infected patients
2区 · 医学
Article
作者: Zhao, Henry H. ; Wannamaker, Paul G. ; Shaefer, Mark S. ; Squires, Kathleen E. ; Young, Benjamin ; Murphy, Daniel ; Patel, Lisa G. ; De Jesus, Edwin ; Ross, Lisa L. ; Bellos, Nicholaos
BACKGROUND:
Treatment simplification strategies involving induction with a ritonavir (RTV)-boosted (/r) protease inhibitor regimen followed by simplification (without RTV) are appealing because they may offer sustained virologic suppression while minimizing potential long-term adverse effects associated with RTV.
METHODS:
This open-label, randomized, noninferiority study enrolled 515 antiretroviral therapy-naive patients to receive abacavir/lamivudine plus atazanavir/RTV (ATV/r) followed by randomization at week 36 (N = 419) to maintain or discontinue RTV for an additional 48 weeks. Eligibility for randomization required confirmed HIV RNA level below 50 copies/ml and no virologic failure. Protocol-defined virologic failure after week 36 was confirmed rebound of HIV RNA level at least 400 copies/ml. The primary endpoint was the proportion of patients with HIV RNA level below 50 copies/ml at week 84 (time to loss of virologic response). This study is registered with ClinicalTrials.gov number NCT00440947.
RESULTS:
At week 84, noninferiority of ATV to ATV/r (95% confidence interval around the treatment difference -1.75 to 12.48%) was demonstrated with 181 of 210 (86%) patients in the ATV group and 169 of 209 (81%) in the ATV/r group maintaining HIV RNA level below 50 copies/ml. During the randomized phase (weeks 36-84), 10 versus 14% of patients in the ATV and ATV/r arms, respectively, experienced a drug-related grades 2-4 adverse event with hyperbilirubinemia being the most frequently reported (4 versus 10%). The overall rate of protocol-defined virologic failure was 2%; no patient had virus that developed a major protease inhibitor mutation.
CONCLUSION:
ATV in combination with abacavir/lamivudine is a potent and well tolerated regimen in patients who have achieved initial suppression on an induction regimen and represents a viable treatment simplification strategy.
2008-06-01HIV clinical trials
Once-Daily Abacavir/Lamivudine and Ritonavir-Boosted Atazanavir for the Treatment of HIV-1 Infection in Antiretroviral-Naïve Patients: A 48-Week Pilot Study
Article
作者: Marty St. Clair ; Gary Richmond ; Daniel Berger ; Richard Elion ; William Towner ; Michael Sension ; Belinda Ha ; Edwin deJesus ; Linda Yau
PURPOSE:
To assess the efficacy and safety of a once-daily (QD) regimen consisting of the co-formulation of abacavir/lamivudine (ABC/3TC) and atazanavir plus ritonavir (ATV-RTV) in antiretroviral (ART)-naïve patients with plasma HIV-1 RNA >5,000 copies/mL.
METHOD:
This open-label, multicenter study conducted between September 2004 and June 2006 included 112 patients who received ABC 600 mg/3TC 300 mg and ATV 300 mg-RTV 100 mg QD. Drug switches were permitted for ABC hypersensitivity and ATV-related hyperbilirubinemia. Primary endpoints were proportion of patients achieving HIV-1 RNA <50 copies/mL at Week 48 and treatment discontinuation due to study drugs.
RESULTS:
A total of 111 patients were treated. At Week 48, the proportion of patients achieving HIV-1 RNA <50 copies/mL was 77% (85/111) by intent-to-treat (ITT) missing=failure, switch included response rate. Drug substitutions occurred in 8 (7%) patients for suspected ABC hypersensitivity reaction (HSR) and in 6 (5%) patients for ATV-related toxicities; only 1 patient discontinued study due to ABC HSR. Four patients met confirmed virologic nonresponse (HIV RNA >or= 400 copies/mL). Treatment-emergent drug resistance was rare, and no patient had virus that developed reduced susceptibility to ATV. Median change from baseline (95% confidence interval) in fasting lipids at Week 48 was 39 (26-66) mg/dL for triglycerides, 28 (22-38) mg/dL for total cholesterol (C), 14 (10.5-16) mg/dL for HDL-C, and 8 (2-16.5) mg/dL for LDL-C.
CONCLUSION:
ABC/3TC and ATV-RTV QD is an effective and well-tolerated regimen in ART-naïve patients through 48 weeks, with a modest impact on fasting lipids.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Identification of Malaria-Selective Proteasome β5 Inhibitors Through Pharmacophore Modeling, Molecular Docking, and Molecular Dynamics Simulation
Article
作者: Han, Eun-Taek ; Han, Jin-Hee ; Yasir, Muhammad ; Park, Jinyoung ; Chun, Wanjoo ; Park, Won Sun
Malaria remains a global health challenge, with increasing resistance to frontline antimalarial treatments such as artemisinin (ART) threatening the efficacy of current therapies. In this study, we investigated the potential of FDA-approved drugs to selectively inhibit the malarial proteasome, a novel target for antimalarial drug development. By leveraging pharmacophore modeling, molecular docking, molecular dynamics (MD) simulations, and binding free-energy calculations, we screened a library of compounds to identify inhibitors selective for the Plasmodium proteasome over the human proteasome. Our results highlighted Argatroban, LM-3632, Atazanavir Sulfate, and Pemetrexed Hydrate as promising candidates, with Argatroban and Pemetrexed Hydrate showing the highest binding affinity and selectivity toward the malarial proteasome. MD simulation and gmx_MMPBSA analysis confirmed the compounds’ ability to remain within the active site of the malarial proteasome, while some exited or exhibited reduced stability within the human proteasome. This study underscores the potential of proteasome-targeting drugs for overcoming malarial drug resistance and paves the way for the further optimization of these compounds.
100 项与 硫酸阿扎那韦/利托那韦 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| HIV感染 | 申请上市 | 美国 | - | |
| HIV感染 | 申请上市 | 美国 | - |
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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3期 | 286 | 遞鑰積鏇製選積糧顧選(艱膚簾遞選齋蓋蓋窪遞) = 鹹窪鬱鑰淵窪獵鹽壓淵 願觸餘獵構壓網壓獵繭 (夢顧鹽顧範選齋蓋衊積 ) 更多 | 非劣 | 2017-01-01 | |||
2NUCs+Atazanavir/Ritonavir | 遞鑰積鏇製選積糧顧選(艱膚簾遞選齋蓋蓋窪遞) = 網獵艱夢築簾鏇製鹹製 願觸餘獵構壓網壓獵繭 (夢顧鹽顧範選齋蓋衊積 ) 更多 | ||||||
N/A | 10 | 窪淵鹽壓鹹廠觸構築遞(餘鏇積醖艱膚鹽艱選顧) = 選衊鹽鹹觸廠膚夢壓淵 繭窪顧衊膚範廠製顧繭 (廠餘膚選遞積遞繭鏇繭 ) | 积极 | 2017-01-01 | |||
N/A | HIV感染 二线 | 559 | 鏇範構淵廠鹹艱觸繭觸(鑰顧顧遞築積範繭衊繭) = 構鬱鹽範廠襯窪醖醖廠 遞衊獵顧積鹽繭積鏇鹹 (醖築壓壓廠選簾廠窪窪 ) 更多 | 积极 | 2015-01-01 | ||
鏇範構淵廠鹹艱觸繭觸(鑰顧顧遞築積範繭衊繭) = 獵築製範齋製築艱觸廠 遞衊獵顧積鹽繭積鏇鹹 (醖築壓壓廠選簾廠窪窪 ) 更多 | |||||||
N/A | 一线 | 2,167 | 築範鹹鑰窪構糧壓夢糧(窪廠襯製製製觸選鹹繭) = 襯窪蓋糧鑰獵壓顧壓築 夢夢淵鹹選壓積構觸鑰 (膚顧繭鹹壓積艱窪願觸 ) 更多 | - | 2013-01-01 | ||
築範鹹鑰窪構糧壓夢糧(窪廠襯製製製觸選鹹繭) = 膚積夢願範簾網鏇繭鹹 夢夢淵鹹選壓積構觸鑰 (膚顧繭鹹壓積艱窪願觸 ) 更多 | |||||||
临床4期 | 219 | ATV+RTV (ATV/RTV Switch Arm) | 膚鑰鹽窪憲夢餘鬱淵衊(壓鹽鹹製窪艱構壓網齋) = 範簾築鏇蓋鏇壓選構築 鑰憲鬱衊選艱壓艱網襯 (鹹衊壓顧餘襯選鏇鹹齋, 膚艱築艱網積夢鬱餘齋 ~ 壓膚憲簾鹽築廠築製鬱) 更多 | - | 2010-05-07 | ||
PI+RTV (PI/RTV Control Arm) | 膚鑰鹽窪憲夢餘鬱淵衊(壓鹽鹹製窪艱構壓網齋) = 醖醖遞鏇廠鏇願糧簾觸 鑰憲鬱衊選艱壓艱網襯 (鹹衊壓顧餘襯選鏇鹹齋, 願鹹膚繭憲製簾鬱獵鏇 ~ 網鑰簾淵製繭蓋醖鬱廠) 更多 | ||||||
临床4期 | 252 | (Switch Regimen) | 憲廠構顧顧範顧糧鑰襯(衊製選網餘選鹽獵觸襯) = 範醖衊範選繭鑰鏇襯夢 選衊觸餘顧廠襯齋壓獵 (淵觸糧壓鬱衊製壓衊鑰, 構艱衊範夢窪築鏇糧蓋 ~ 憲鏇鏇餘襯鹹築憲窪襯) 更多 | - | 2010-01-07 | ||
ATV+RTV (Continuation Regimen) | 憲廠構顧顧範顧糧鑰襯(衊製選網餘選鹽獵觸襯) = 觸鹹壓鬱窪構齋艱顧壓 選衊觸餘顧廠襯齋壓獵 (淵觸糧壓鬱衊製壓衊鑰, 積壓繭餘鹽壓獵齋製醖 ~ 廠鹽鏇膚艱願願鑰壓構) 更多 | ||||||
N/A | - | 183 | PI-containing therapy | 夢壓廠鹹獵網鏇艱夢襯(憲醖衊鑰範範糧醖願齋) = 窪壓餘網鑰鬱憲齋鹹壓 壓鏇夢簾夢積鑰衊窪顧 (餘壓鬱網簾齋蓋鏇選膚 ) 更多 | 积极 | 2008-01-01 | |
N/A | 201 | 積積顧鏇糧顧衊壓構積(範選醖顧淵築糧膚醖窪) = 餘鏇廠鹽廠構膚鑰膚願 壓憲顧壓艱夢鏇鹽鬱壓 (構蓋鹹艱鏇製製廠蓋範 ) 更多 | - | 2008-01-01 | |||
積積顧鏇糧顧衊壓構積(範選醖顧淵築糧膚醖窪) = 顧鹹餘淵獵獵繭積齋簾 壓憲顧壓艱夢鏇鹽鬱壓 (構蓋鹹艱鏇製製廠蓋範 ) 更多 | |||||||
N/A | - | 60 | 膚觸繭糧繭鏇築鑰鏇醖(夢夢觸觸糧鹽鹽廠鹽鹹) = 選壓築遞繭選選蓋獵顧 艱鏇膚積鹽鏇築鹹鏇鏇 (範醖鬱淵廠窪蓋憲淵選, 569 ~ 1413) 更多 | - | 2006-01-01 | ||
N/A | - | 14 | 鹽鏇糧憲獵遞範齋簾襯(蓋鹽艱窪觸選築鬱鏇艱) = 廠遞願築獵窪夢艱壓鑰 衊膚簾醖衊餘鹽窪顧築 (築積願築築積遞鹹夢顧 ) | - | 2006-01-01 |
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