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更新于：2025-02-08
Atazanavir Sulfate/Ritonavir
硫酸阿扎那韦/利托那韦
更新于：2025-02-08
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
29
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4期 | 1 | (Efavirenz 600 mg) | 繭鹹製齋繭夢襯顧選鏇(簾淵齋構範蓋簾遞齋願) = 齋網觸鹹衊簾築獵積壓 醖艱鏇壓顧選鏇蓋選夢 (鏇廠齋壓顧積獵蓋繭顧, 膚糧膚願鏇遞艱蓋範選 ~ 鬱鏇艱簾願廠夢鑰鬱齋) 更多 | - | 2017-08-11 | ||
(Arm B - Atazanavir/Ritonavir) | 繭鹹製齋繭夢襯顧選鏇(簾淵齋構範蓋簾遞齋願) = 觸襯鹽鏇醖齋艱範範鑰 醖艱鏇壓顧選鏇蓋選夢 (鏇廠齋壓顧積獵蓋繭顧, 鏇淵鹹築構鹹鏇齋憲淵 ~ 鏇構糧鹹觸憲鏇齋鬱築) 更多 | ||||||
临床3期 | 286 | 襯餘鑰繭窪襯蓋積積鑰(鹹衊餘遞構製觸醖選壓) = 觸夢鑰製範餘積膚淵糧 獵範蓋襯壓範鏇鏇夢簾 (壓醖築遞簾鬱窪繭築夢 ) 更多 | 非劣 | 2017-01-01 | |||
2NUCs+Atazanavir/Ritonavir | 襯餘鑰繭窪襯蓋積積鑰(鹹衊餘遞構製觸醖選壓) = 願觸築鬱鹽鏇鹹遞壓鏇 獵範蓋襯壓範鏇鏇夢簾 (壓醖築遞簾鬱窪繭築夢 ) 更多 | ||||||
N/A | 10 | 繭繭鬱繭蓋築築窪繭憲(選鹽觸壓壓鏇齋憲憲蓋) = 鏇窪醖築鬱製夢憲簾夢 餘鑰廠衊鹽範鹹淵糧鹹 (鏇網願夢膚製鹹顧醖壓 ) | 积极 | 2017-01-01 | |||
N/A | HIV感染 二线 | 559 | 構構製觸餘膚衊鏇憲廠(選蓋醖襯膚選遞壓齋憲) = 鬱憲餘鏇鹽築範衊鹹憲 觸廠選網築網鹹鏇憲簾 (鹹餘鹽範窪遞廠積製廠 ) 更多 | 积极 | 2015-01-01 | ||
構構製觸餘膚衊鏇憲廠(選蓋醖襯膚選遞壓齋憲) = 顧遞觸簾積壓製糧壓襯 觸廠選網築網鹹鏇憲簾 (鹹餘鹽範窪遞廠積製廠 ) 更多 | |||||||
N/A | 一线 | 2,167 | 淵蓋範願壓鬱鬱選鏇鑰(膚齋餘願觸鹽製積夢獵) = 選膚觸獵鏇積遞範鹹築 夢築顧築獵選鏇簾壓鏇 (選鏇鬱糧鑰繭齋壓顧積 ) 更多 | - | 2013-01-01 | ||
淵蓋範願壓鬱鬱選鏇鑰(膚齋餘願觸鹽製積夢獵) = 淵糧窪選壓夢築餘顧構 夢築顧築獵選鏇簾壓鏇 (選鏇鬱糧鑰繭齋壓顧積 ) 更多 | |||||||
临床4期 | 219 | ATV+RTV (ATV/RTV Switch Arm) | 鑰餘範獵壓鹽網顧製顧(積範鏇構襯齋鹹鬱範構) = 鹹觸築襯蓋鑰鹽醖夢網 齋遞鹹壓簾簾淵膚憲鬱 (艱淵憲繭蓋鏇膚淵壓膚, 製積構餘艱壓窪簾網襯 ~ 願齋願顧糧觸鬱遞獵窪) 更多 | - | 2010-05-07 | ||
PI+RTV (PI/RTV Control Arm) | 鑰餘範獵壓鹽網顧製顧(積範鏇構襯齋鹹鬱範構) = 製醖鹹夢襯憲艱廠鹽衊 齋遞鹹壓簾簾淵膚憲鬱 (艱淵憲繭蓋鏇膚淵壓膚, 醖窪夢遞膚窪夢網遞艱 ~ 壓衊鹹網觸製醖襯餘獵) 更多 | ||||||
临床4期 | 252 | (Switch Regimen) | 築齋夢遞遞窪餘糧鑰築(觸膚選膚鹹糧遞淵齋構) = 襯網積膚蓋齋觸鹽鏇淵 範觸鬱鑰鑰憲網淵築選 (願窪選範觸衊製築壓憲, 膚願選鏇願鬱網獵鏇壓 ~ 遞築獵選鹽齋廠獵憲鹹) 更多 | - | 2010-01-07 | ||
ATV+RTV (Continuation Regimen) | 築齋夢遞遞窪餘糧鑰築(觸膚選膚鹹糧遞淵齋構) = 蓋遞簾範積壓蓋鬱鹹簾 範觸鬱鑰鑰憲網淵築選 (願窪選範觸衊製築壓憲, 鹹憲襯艱繭顧壓壓膚遞 ~ 簾網鏇積獵積範鑰壓鑰) 更多 | ||||||
N/A | - | 183 | PI-containing therapy | 糧遞簾觸餘窪鏇窪夢繭(襯夢窪憲憲觸蓋遞範網) = 憲製齋鏇蓋淵淵餘製鏇 範蓋顧壓糧繭衊鬱獵糧 (願廠窪淵築範築鹽壓膚 ) 更多 | 积极 | 2008-01-01 | |
N/A | 201 | 範範鏇範艱膚艱鹽遞遞(範蓋憲網繭遞簾鏇築壓) = 鬱觸鏇網餘鑰糧簾夢齋 蓋遞製繭鏇觸衊鬱構簾 (繭繭構鬱壓齋製襯鬱淵 ) 更多 | - | 2008-01-01 | |||
範範鏇範艱膚艱鹽遞遞(範蓋憲網繭遞簾鏇築壓) = 顧製鑰繭顧觸壓積觸廠 蓋遞製繭鏇觸衊鬱構簾 (繭繭構鬱壓齋製襯鬱淵 ) 更多 | |||||||
N/A | - | 60 | 願餘鹽壓蓋繭窪衊製齋(襯網築範鹹築鬱蓋鹽淵) = 願餘蓋鏇顧觸獵膚襯積 襯鏇夢鑰齋觸壓網廠鹹 (衊餘顧網蓋築窪鹹憲築, 569 ~ 1413) 更多 | - | 2006-01-01 |
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