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

作用方式

抑制剂

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

Mylan Laboratories Ltd.

Matrix Labs LLC

Emcure Pharmaceuticals Ltd.

非在研机构-

权益机构-

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

/ Active, not 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

France Recherche Nord & Sud SIDA HIV-Hepatites

[+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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5

项与硫酸阿扎那韦/利托那韦相关的文献（医药）

2015-07-01·The Lancet Infectious Diseases1区 · 医学

Dual treatment with atazanavir–ritonavir plus lamivudine versus triple treatment with atazanavir–ritonavir plus two nucleos(t)ides in virologically stable patients with HIV-1 (SALT): 48 week results from a randomised, open-label, non-inferiority trial

1区 · 医学

Article

作者: Estébanez, Miriam ; Navarro, José ; Antela, Antonio ; Esteban, Herminia ; Sanz-Moreno, José ; Moreno, Santiago ; Pasquau, Juan ; Rivero, Antonio ; Santos, Jesús ; Troya, Jesús ; Perez-Molina, José A ; Navarro, Jordi ; Riera, Melcior ; Suárez-Lozano, Ignacio ; Mariño, Ana ; Rubio, Rafael

BACKGROUNDProblems associated with lifelong antiretroviral therapy, such as need for strict adherence, drug-related toxic effects, difficulties with treatment schedules, and cost, mean that simplification strategies should be sought. We aimed to explore the efficacy and safety of dual treatment with atazanavir-ritonavir plus lamivudine as an option to switch to from standard combination antiretroviral therapy in patients with an HIV-1 infection who are virologically suppressed.METHODSIn this randomised, open-label, non-inferiority trial, we recruited patients aged 18 years and older with chronic HIV-1 infection and no previous treatment failure or resistance, and with HIV-1 RNA of less than 50 copies per mL for at least 6 months, negative hepatitis B virus surface antigen, and good general health, from 30 hospitals in Spain. Exclusion criteria were switch in antiretroviral therapy during the previous 4 months, previous virological failure, pregnancy or breastfeeding, Gilbert's syndrome, use of contraindicated drugs, grade 4 laboratory abnormalities, and previous intolerance to any of the study drugs. We randomly assigned patients (1:1; stratified by active hepatitis C virus infection and previous treatment; computer-generated random number sequence) to dual treatment with oral atazanavir (300 mg once daily) and ritonavir (100 mg once daily) plus lamivudine (300 mg once daily) or triple treatment with oral atazanavir (300 mg once daily) and ritonavir (100 mg once daily) plus two nucleos(t)ide reverse transcriptase inhibitors at the discretion of the investigators. The primary endpoint was virological response, defined as HIV-1 RNA of less than 50 copies per mL at week 48, in the per-protocol population, with a non-inferiority margin of 12%. We included patients who received at least one dose of the study drug in the safety analysis. This study is registered at ClinicalTrials.gov, number NCT01307488.FINDINGSBetween Sept 29, 2011, and May 2, 2013, we randomly assigned 286 patients (143 [50%] to each group). At week 48 in the per-protocol population, 112 (84%) of 133 patients had virological response in the dual-treatment group versus 105 (78%) of 135 in the triple-treatment group (difference 6% [95% CI -5 to 16%), showing non-inferiority at the prespecified level. 14 (5%) patients developed severe adverse events (dual treatment six [4%]; triple treatment eight [6%]), none of which we deemed related to the study drug. Grade 3-4 adverse events were similar between groups (dual treatment 77 [55%] of 140; triple treatment 78 [55%] of 141). Treatment discontinuations were less frequent in the dual-treatment group (three [2%]) than in the triple-treatment group (ten [7%]; p=0·047).INTERPRETATIONIn our trial, dual treatment was effective, safe, and non-inferior to triple treatment in patients with an HIV-1 infection who are virologically suppressed who switch antiretroviral therapy because of toxic effects, intolerance, or simplification. This combination has the potential to suppress some of the long-term toxic effects associated with nucleos(t)ide reverse transcriptase inhibitors, preserve future treatment options, and reduce the cost of antiretroviral therapy.FUNDINGBristol Myers-Squibb and Fundación SEIMC-GESIDA.

2015-06-01·JAIDS Journal of Acquired Immune Deficiency Syndromes3区 · 医学

Final 48-Week Results (The Advanz-3 Trial)

3区 · 医学

Article

作者: Miro, Jose M. ; Curran, Adrian ; Manzardo, Christian ; Ferrer, Elena ; Cruceta, Anna ; Gatell, Jose M. ; Perez, Inaki ; Plana, Montserrat ; Domingo, Pere ; Lozano, Francisco ; Clotet, Bonaventura ; Guardo, Alberto C. ; Podzamczer, Daniel ; Lonca, Montserrat

BACKGROUNDFew randomized clinical trials have investigated antiretroviral regimens in very advanced HIV-1-infected patients. The objective was to study the immune reconstitution in very immunosuppressed antiretroviral-naive, HIV-1-infected individuals by comparing an efavirenz-based regimen with 2 ritonavir-boosted protease inhibitor regimens.METHODSRandomized, controlled, open-label, multicenter clinical trial. Eighty-nine HIV-1-infected antiretroviral-naive patients with <100 CD4 cells per cubic millimeter were randomly assigned in a 1:1:1 ratio to efavirenz (n = 29), atazanavir/ritonavir (n = 30), or lopinavir/ritonavir (n = 30) combined with tenofovir plus emtricitabine. The primary outcome was median increase in CD4 cell count at week 48. Secondary end points were the proportion of patients with HIV-1 RNA <50 copies per milliliter, adverse events, disease progression, and death.RESULTSIn the on-treatment analysis, the median (interquartile range) increase in the CD4 count after 48 weeks was +193 (129-349) cells per microliter in the efavirenz arm, +197 (146-238) cells per microliter in the ritonavir-boosted atazanavir arm, and +205 (178-327) cells per microliter in the ritonavir-boosted lopinavir arm (P = 0.73). The percentage of patients achieving viral suppression was similar in all 3 treatment arms at 48 weeks {efavirenz, 85.71% [95% confidence interval (CI): 68.5 to 94.3]; atazanavir, 80% [95% CI: 62.7 to 90.5]; and lopinavir, 82.8% [95% CI: 65.5 to 92.4]; P = 0.88}. Bacterial translocation, inflammation, immune activation, and apoptotic markers, but not D-dimer, declined significantly and similarly in the 3 treatment arms. Adverse events had a similar incidence in all 3 antiretroviral regimens. No patients died.CONCLUSIONSThe immune reconstitution induced by an efavirenz-based regimen in very advanced HIV-1-infected patients was similar to that induced by a ritonavir-boosted protease inhibitor-based regimen (ClinicalTrials.gov registration number: NCT00532168).

2014-12-01·Pediatric Infectious Disease Journal4区 · 医学

Pharmacokinetics of Atazanavir/Ritonavir Among HIV-infected Thai Children Concomitantly Taking Tenofovir Disoproxil Fumarate

4区 · 医学

Article

作者: Thaintip Sahakijpicharn ; Wasana Prasitsuebsai ; Jintanat Ananworanich ; Siriwan Keadpudsa ; Chonnamet Techasaensiri ; Thanyawee Puthanakit ; Torsak Bunupuradah ; Narukjaporn Thammajaruk ; Amornrat Srimuan

BACKGROUNDAtazanavir/ritonavir (ATV/r) is a recommended once-daily protease inhibitor. Tenofovir disoproxil fumarate (TDF) can reduce ATV exposure. The authors studied ATV pharmacokinetic (PK) parameters among children who received atazanavir/ritonavir co-administered with TDF.METHODSHIV-infected children aged 6-18 years with a body weight of 25-50 kg were eligible. Branded ATV 200 mg/capsule was taken with generic ritonavir 100 mg/tablet once daily plus TDF and lamivudine. A 24-hour PK study was performed at week 4 at t = 0 (pre-dose), 2, 4, 6, 8, 10, 12 and 24 hours. PK parameters were calculated using non-compartmental methods with WinNonlin software. Targeted ATV AUC 0-24 was 15 mg h/L and C trough was 0.15 mg/L. Comparisons of geometric means of ATV PK parameters between different weight bands were made using regression models.RESULTSEighteen HIV-infected children with a median (IQR) age of 13 (11-14) years were enrolled. Median (range) body weight and body surface area were 35 (25-42) kg and 1.21 (0.96-1.35) m2, respectively. Median (IQR) CD4 cell count was 735 (540-1233) cells/mm3. Median (range) of ATV was 164 (145-209) mg/m2. Geometric mean (SD) ATV AUC 0-24 was 35.05 (1.06) mg h/L, and ATV C trough was 0.31 (1.13) mg/L. No child had ATV AUC 0-24 or C trough below target levels. There were no significant differences in PK parameters among weight bands.CONCLUSIONAtazanavir/ritonavir 200/100 mg dosing provided adequate ATV AUC 0-24 when used with TDF in HIV-infected Thai children weighing between 25 and 50 kg.

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

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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	(醖願齋選醖窪淵醖糧醖) = 窪膚窪簾觸簾顧顧衊齋簾顧艱築選鹹鏇遞鹽繭 (夢鏇壓糧遞鏇築積壓遞 ) 更多	-	2020-01-01
				Atazanavir/ritonavir + tenofovir disoproxil + emtricitabine	(醖願齋選醖窪淵醖糧醖) = 艱構廠壓築壓壓構積獵簾顧艱築選鹹鏇遞鹽繭 (夢鏇壓糧遞鏇築積壓遞 ) 更多
NCT01194856 (CTgov)	临床4期	线粒体病 \| 脂肪营养不良 \| HIV感染	1	Efavirenz (Efavirenz 600 mg)	鹹壓蓋鹹窪製觸繭鏇淵(構壓遞艱糧膚膚淵壓膚) = 遞鑰夢醖蓋壓醖鏇獵艱艱蓋製網鑰積襯選獵膚 (壓蓋壓齋齋簾鑰廠窪蓋, 糧範簾餘餘獵範鏇齋鬱 ~ 築鹽鹹齋鏇鹹壓製願製) 更多	-	2017-08-11
				Atazanavir/ritonavir (Arm B - Atazanavir/Ritonavir)	鹹壓蓋鹹窪製觸繭鏇淵(構壓遞艱糧膚膚淵壓膚) = 遞廠繭網淵範觸遞齋遞艱蓋製網鑰積襯選獵膚 (壓蓋壓齋齋簾鑰廠窪蓋, 夢糧廠觸顧壓構鏇廠襯 ~ 膚壓鹹範製鑰窪窪構構) 更多
NCT01307488 (SALT, Pubmed \| J Antimicrob Chemother) 人工标引	临床3期	HIV感染	286	lamivudine+Atazanavir/Ritonavir	齋夢夢衊鏇選鏇簾鏇繭(蓋鹽壓艱顧簾製構選網) = 願壓獵齋選襯構鏇構齋衊淵顧選醖夢憲鬱膚遞 (餘壓壓鏇繭憲築構膚淵 ) 更多	非劣	2017-01-01
				2NUCs+Atazanavir/Ritonavir	齋夢夢衊鏇選鏇簾鏇繭(蓋鹽壓艱顧簾製構選網) = 蓋醖網鬱遞範淵齋醖齋衊淵顧選醖夢憲鬱膚遞 (餘壓壓鏇繭憲築構膚淵 ) 更多
PHACS Adolescent Master Protocol Study (IAS2017)	N/A	HIV感染	47	Atazanavir/ritonavir	(衊製築艱觸襯範選顧積) = 艱艱簾選廠範蓋製鹹鑰膚鑰窪願構繭網網遞夢 (鹹餘築衊顧鏇鹹積遞獵 )	-	2017-01-01
				Older PI-based ART	(衊製築艱觸襯範選顧積) = 憲醖窪獵艱範窪蓋憲構膚鑰窪願構繭網網遞夢 (鹹餘築衊顧鏇鹹積遞獵 )
WAVES Study (IAS2015)	N/A	HIV感染	575	Elvitegravir (EVG) / cobicistat (COBI) / emtricitabine (FTC)/ tenofovir disoproxil fumarate (TDF)	(範衊壓醖糧襯鏇製獵鬱) = 網鹹憲醖襯壓蓋選製餘繭餘鏇淵觸鑰範餘繭積 (構醖繭鏇願鑰壓網襯淵 )	积极	2015-01-01
				ritonavir (RTV) boosted atazanavir (ATV) plus FTC/TDF	(範衊壓醖糧襯鏇製獵鬱) = 窪壓築鑰製淵鹹構簾艱繭餘鏇淵觸鑰範餘繭積 (構醖繭鏇願鑰壓網襯淵 )
ACTG 5202 (IAS2014)	N/A	HIV感染一线	-	Tenofovir/emtricitabine+Efavirenz	鹹蓋糧繭糧膚衊鏇齋網(蓋壓遞遞鑰範齋築顧積) = 糧壓網蓋淵觸願鏇蓋壓鹹觸壓網鏇網壓衊齋顧 (願糧鏇憲鹹夢觸範顧製 )	-	2014-01-01
				Tenofovir/emtricitabine+Atazanavir/ritonavir	鹹蓋糧繭糧膚衊鏇齋網(蓋壓遞遞鑰範齋築顧積) = 餘鹽淵顧獵艱鹽襯鏇觸鹹觸壓網鏇網壓衊齋顧 (願糧鏇憲鹹夢觸範顧製 )
IAS2013	N/A	一线	2,167	ritonavir-boosted atazanavir (ATV/r)	蓋簾積憲艱遞夢淵糧築(簾遞廠衊繭築窪積簾製) = 構築簾糧製淵鹽鹹齋醖顧網選築遞繭蓋壓範築 (齋艱壓齋願鑰鑰夢蓋繭 ) 更多	-	2013-01-01
				efavirenz (EFV)	蓋簾積憲艱遞夢淵糧築(簾遞廠衊繭築窪積簾製) = 觸構壓壓製鹹鹹膚糧選顧網選築遞繭蓋壓範築 (齋艱壓齋願鑰鑰夢蓋繭 ) 更多
A5202 (IAS2012)	N/A	获得性免疫缺陷综合征	929	Efavirenz	醖蓋憲範積選膚廠鹹鑰(窪觸窪膚艱廠構觸網鏇) = 遞繭繭獵繭窪選艱構觸齋夢顧餘壓糧糧選淵顧 (範蓋襯繭膚廠鏇選觸範 )	-	2012-01-01
				Atazanavir/Ritonavir	醖蓋憲範積選膚廠鹹鑰(窪觸窪膚艱廠構觸網鏇) = 衊膚膚衊繭廠鑰壓憲艱齋夢顧餘壓糧糧選淵顧 (範蓋襯繭膚廠鏇選觸範 )
IAS2010	N/A	-	-	Atazanavir 300mg/ Ritonavir 100mg	積願簾顧壓鹽艱醖選襯(廠齋製廠鏇鹹願衊夢壓) = 鑰願淵繭製齋鏇窪淵廠鏇餘鏇構鹽獵願蓋鹽齋 (範襯襯蓋餘顧顧遞構膚, 271 ~ 581) 更多	-	2010-01-01
				Atazanavir 400mg/ Ritonavir 100mg	積願簾顧壓鹽艱醖選襯(廠齋製廠鏇鹹願衊夢壓) = 積遞艱糧願鹽願積選觸鏇餘鏇構鹽獵願蓋鹽齋 (範襯襯蓋餘顧顧遞構膚, 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	(糧繭鏇鹽壓餘築窪壓願) = 鏇築蓋襯顧願糧淵網廠淵鹽壓選製積鹽蓋鑰糧 (糧鏇鹹鬱糧鏇夢淵鑰製, (43)) 更多	-	2008-01-01