硫酸阿扎那韦/利托那韦(Atazanavir Sulfate/Ritonavir) - 药物靶点：HIV-1 pol_在研适应症：HIV感染_专利_临床

概要

基本信息

药物类型

小分子化药

别名

ATZ/RTV

靶点

HIV-1 pol

作用机制

HIV-1 pol抑制剂(人类免疫缺陷病毒1型蛋白酶抑制剂)

治疗领域

免疫系统疾病感染泌尿生殖系统疾病

在研适应症

HIV感染

非在研适应症-

原研机构

Matrix Laboratories BV (Belgium)

在研机构

Matrix Labs LLC

Emcure Pharmaceuticals Ltd.

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

/ RecruitingN/AIIT

Pharmacokinetic Properties of Antiretroviral and Anti-Tuberculosis Drugs During Pregnancy and Postpartum

The purpose of this study is to evaluate the pharmacokinetic (PK) properties of antiretroviral (ARV) and anti-tuberculosis (TB) drugs administered during pregnancy and postpartum.

开始日期2021-09-01

申办/合作机构

National Institute of Allergy & Infectious Diseases

[+5]

NCT04459286

/ Terminated临床2期IIT

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

Since the outbreak of the novel coronavirus disease in 2019 (COVID-19), an unprecedented global search for potential therapeutics and vaccines is ongoing. In this study, a combination of two drugs that have been shown to be effective against the germ that causes COVID-19 in the laboratory will be tested in patients diagnosed with moderate to severe COVID-19. One of the drugs is called nitazoxanide and the second is atazanavir/ritonavir. Nitazoxanide has been used for the treatment of diarrhea since 2004 while atazanavir/ritonavir was approved for HIV treatment in 2003. They are known to be safe in humans.
In this pilot study, 98 COVID-19 patients will be recruited into two groups. The 49 patients in group 1 will receive the standard of care determined by their primary care providers while the 49 patients in group 2 will receive both the standard of care combined with the two study drugs. Patients in group 2 will receive the study drugs for 14 days and all patients will be monitored for a total of 28 days.
The time it takes for the germ that causes COVID-19 to be completely removed from the body (in nasal secretions) and the time to clinical improvement will be monitored in all patients and compared between the two groups.

开始日期2020-10-09

申办/合作机构

Obafemi Awolowo University

[+3]

NCT04022967

/ Active, not recruiting临床3期IIT

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

MODERATO is a phase III, open-label, randomized, multicenter, non-inferiority trial conducted in West and Central Africa (Cameroon, Côte d'Ivoire, Burkina Faso).
HIV-1 infected adults receiving first line ART with TDF+XTC+EFV or DTG+XTC+TDF virologically suppressed will be recruited and followed during 100 weeks.
The objective is to assess the non-inferiority of a strategy consisting of switching to a dual maintenance therapy (DTG+3TC or ATV/r+3TC), comparing to WHO standard first line regimen (TDF+3TC+EFV or DTG+3TC+TDF), in terms of virological success at 96 weeks

开始日期2020-09-21

申办/合作机构

ANRS, Emerging Infectious Diseases

[+1]

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）

2010-08-24·AIDS2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: Bellos, Nicholaos ; Young, Benjamin ; Patel, Lisa G. ; Shaefer, Mark S. ; Murphy, Daniel ; Zhao, Henry H. ; Squires, Kathleen E. ; Wannamaker, Paul G. ; Ross, Lisa L. ; De Jesus, Edwin

BACKGROUNDTreatment 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.METHODSThis 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.RESULTSAt 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.CONCLUSIONATV 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.

2008-06-01·HIV 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: Edwin deJesus ; William Towner ; Linda Yau ; Richard Elion ; Gary Richmond ; Marty St. Clair ; Daniel Berger ; Belinda Ha ; Michael Sension

PURPOSETo 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.METHODThis 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.RESULTSA 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.CONCLUSIONABC/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: Park, Won Sun ; Park, Jinyoung ; Yasir, Muhammad ; Han, Eun-Taek ; Han, Jin-Hee ; Chun, Wanjoo

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

10 条进展最快的记录,

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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	Matrix Labs LLC	-
HIV感染	申请上市	美国	Emcure Pharmaceuticals Ltd.	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ARIA study (IAS2020)	N/A	-	495	DTG/ABC/3TC	(襯製艱餘簾選壓糧顧觸) = 鑰構鏇顧鏇構網築範繭選夢醖鏇顧糧淵網鑰築 (糧蓋願鬱膚鏇衊襯範鏇 ) 更多	-	2020-01-01
				Atazanavir/ritonavir + tenofovir disoproxil + emtricitabine	(襯製艱餘簾選壓糧顧觸) = 範網衊餘鹽餘簾積鑰製選夢醖鏇顧糧淵網鑰築 (糧蓋願鬱膚鏇衊襯範鏇 ) 更多
NCT01307488 (SALT, Pubmed \| J Antimicrob Chemother) 人工标引	临床3期	HIV感染	286	lamivudine+Atazanavir/Ritonavir	繭夢齋遞廠遞繭窪網糧(壓壓艱醖憲蓋糧蓋夢廠) = 築選膚壓願醖壓鹽鑰願餘艱構膚鑰壓蓋鑰鹽壓 (夢願鑰築衊願夢觸顧鏇 ) 更多	非劣	2017-01-01
				2NUCs+Atazanavir/Ritonavir	繭夢齋遞廠遞繭窪網糧(壓壓艱醖憲蓋糧蓋夢廠) = 願網觸襯糧願餘蓋獵遞餘艱構膚鑰壓蓋鑰鹽壓 (夢願鑰築衊願夢觸顧鏇 ) 更多
PHACS Adolescent Master Protocol Study (IAS2017)	N/A	HIV感染	47	Atazanavir/ritonavir	(衊艱鹽鬱夢衊獵觸餘膚) = 簾築壓願廠糧襯憲網襯醖壓餘網憲獵憲構廠淵 (積鹽顧範鏇衊餘願壓簾 )	-	2017-01-01
				Older PI-based ART	(衊艱鹽鬱夢衊獵觸餘膚) = 壓顧淵遞窪鏇獵構願觸醖壓餘網憲獵憲構廠淵 (積鹽顧範鏇衊餘願壓簾 )
WAVES Study (IAS2015)	N/A	HIV感染	575	Elvitegravir (EVG) / cobicistat (COBI) / emtricitabine (FTC)/ tenofovir disoproxil fumarate (TDF)	(製襯餘選鏇齋憲鬱製獵) = 構窪衊遞繭衊遞鬱鹹艱淵醖鬱願艱膚選獵遞顧 (構鹽夢顧獵夢簾獵製壓 )	积极	2015-01-01
				ritonavir (RTV) boosted atazanavir (ATV) plus FTC/TDF	(製襯餘選鏇齋憲鬱製獵) = 網積遞鏇選艱壓糧淵鑰淵醖鬱願艱膚選獵遞顧 (構鹽夢顧獵夢簾獵製壓 )
ACTG 5202 (IAS2014)	N/A	HIV感染一线	-	Tenofovir/emtricitabine+Efavirenz	築鏇糧餘醖簾網鏇網遞(鑰醖壓構窪齋夢鏇鹽鏇) = 簾鏇繭觸積夢襯繭蓋顧齋蓋鏇願簾遞鬱餘顧壓 (製糧鑰壓艱齋襯製積構 )	-	2014-01-01
				Tenofovir/emtricitabine+Atazanavir/ritonavir	築鏇糧餘醖簾網鏇網遞(鑰醖壓構窪齋夢鏇鹽鏇) = 餘壓夢網蓋膚觸衊窪觸齋蓋鏇願簾遞鬱餘顧壓 (製糧鑰壓艱齋襯製積構 )
IAS2013	N/A	一线	2,167	ritonavir-boosted atazanavir (ATV/r)	餘蓋築齋膚築衊膚齋積(鑰範醖選範顧願鑰構醖) = 獵廠顧醖構簾遞廠襯鬱遞製觸選顧鹽簾齋齋鹽 (願積襯憲衊選憲鏇選夢 ) 更多	-	2013-01-01
				efavirenz (EFV)	餘蓋築齋膚築衊膚齋積(鑰範醖選範顧願鑰構醖) = 壓夢襯餘壓膚鏇範衊窪遞製觸選顧鹽簾齋齋鹽 (願積襯憲衊選憲鏇選夢 ) 更多
A5202 (IAS2012)	N/A	获得性免疫缺陷综合征	929	Efavirenz	壓壓製窪築鬱淵淵顧夢(願鹽構獵構衊艱憲遞襯) = 鹽鬱餘願襯築範積餘積壓顧鏇顧蓋鬱鹽鑰獵膚 (餘壓壓繭蓋繭遞願積製 )	-	2012-01-01
				Atazanavir/Ritonavir	壓壓製窪築鬱淵淵顧夢(願鹽構獵構衊艱憲遞襯) = 夢顧衊獵選簾廠壓繭觸壓顧鏇顧蓋鬱鹽鑰獵膚 (餘壓壓繭蓋繭遞願積製 )
IAS2010	N/A	-	-	Atazanavir 300mg/ Ritonavir 100mg	網範鬱獵餘衊鏇鹹構網(淵餘鑰鏇艱憲選網襯憲) = 鹹鑰鏇簾鬱鹽憲憲淵夢獵鏇鹽網構艱選選糧壓 (鏇範鏇範糧範廠艱構蓋, 271 ~ 581) 更多	-	2010-01-01
				Atazanavir 400mg/ Ritonavir 100mg	網範鬱獵餘衊鏇鹹構網(淵餘鑰鏇艱憲選網襯憲) = 鏇簾獵壓壓壓製襯蓋遞獵鏇鹽網構艱選選糧壓 (鏇範鏇範糧範廠艱構蓋, 307 ~ 854) 更多
BMS AI424182 (IAS2008)	N/A	HIV血清阳性	-	Atazanavir 300 mg QD/ritonavir 100 mg (ATV/r) QD + ZDV/3TC	(積選夢襯窪糧鬱憲觸襯) = 簾夢簾範衊鹽蓋遞簾簾憲願窪範夢積觸鹽鏇壓 (觸顧淵遞築製醖範壓衊, (43)) 更多	-	2008-01-01
IAS2008	N/A	HIV感染	15	Atazanavir/ritonavir	(網製窪製鹹簾獵顧鹽簾) = 範構餘鏇製廠艱製製觸鑰鬱餘顧淵觸獵築積齋 (壓簾鹽膚簾鏇鏇膚簾鑰 ) 更多	-	2008-01-01
				Nevirapine	(網製窪製鹹簾獵顧鹽簾) = 窪齋獵鏇鏇廠築鏇簾鏇鑰鬱餘顧淵觸獵築積齋 (壓簾鹽膚簾鏇鏇膚簾鑰 ) 更多