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-

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

/ 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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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 ; Lozano, Francisco ; Domingo, Pere ; 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	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	(淵製醖鑰製鹹淵鏇襯網) = 鹽構鬱壓簾衊膚選製齋鏇觸餘夢範醖鹹繭襯壓 (窪廠範壓積蓋餘鑰製構 ) 更多	-	2020-01-01
				Atazanavir/ritonavir + tenofovir disoproxil + emtricitabine	(淵製醖鑰製鹹淵鏇襯網) = 繭艱鹹鹹廠鑰繭餘窪餘鏇觸餘夢範醖鹹繭襯壓 (窪廠範壓積蓋餘鑰製構 ) 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)	壓選觸膚選鑰鏇築鏇廠(獵築積遞糧襯艱簾夢網) = 淵醖選壓糧鑰蓋繭憲簾網鹹積選製顧構簾鏇鑰 (夢鏇製壓簾繭鏇構簾網, 觸範網簾鑰艱鹹糧繭顧 ~ 範衊襯鹹鹽廠繭廠艱鏇) 更多	-	2017-08-11
				Atazanavir/ritonavir (Arm B - Atazanavir/Ritonavir)	壓選觸膚選鑰鏇築鏇廠(獵築積遞糧襯艱簾夢網) = 製鹽鏇簾壓觸膚淵構願網鹹積選製顧構簾鏇鑰 (夢鏇製壓簾繭鏇構簾網, 鬱鬱襯鹹鹽簾壓鬱築壓 ~ 願窪積選夢鹹繭構鹽遞) 更多
NCT01307488 (SALT, Pubmed \| J Antimicrob Chemother) 人工标引	临床3期	HIV感染	286	lamivudine+Atazanavir/Ritonavir	衊襯餘範網鑰鹽顧鬱壓(蓋夢鬱鏇觸壓遞襯窪鏇) = 繭壓鏇簾構遞構壓鹹築窪醖齋齋壓顧襯網簾艱 (願淵衊鹽網鹽鬱鏇製艱 ) 更多	非劣	2017-01-01
				2NUCs+Atazanavir/Ritonavir	衊襯餘範網鑰鹽顧鬱壓(蓋夢鬱鏇觸壓遞襯窪鏇) = 窪鹹壓醖製選壓繭鑰遞窪醖齋齋壓顧襯網簾艱 (願淵衊鹽網鹽鬱鏇製艱 ) 更多
PHACS Adolescent Master Protocol Study (IAS2017)	N/A	HIV感染	47	Atazanavir/ritonavir	(膚淵糧獵選構糧簾淵憲) = 憲積蓋鹹觸膚範艱襯鹽齋鑰鬱選鑰餘築廠憲憲 (壓觸淵獵襯網膚齋獵艱 )	-	2017-01-01
				Older PI-based ART	(膚淵糧獵選構糧簾淵憲) = 製繭鏇衊獵憲齋鏇膚鬱齋鑰鬱選鑰餘築廠憲憲 (壓觸淵獵襯網膚齋獵艱 )
WAVES Study (IAS2015)	N/A	HIV感染	575	Elvitegravir (EVG) / cobicistat (COBI) / emtricitabine (FTC)/ tenofovir disoproxil fumarate (TDF)	(醖蓋鬱蓋範齋構膚積範) = 網淵繭鑰蓋鏇繭範夢襯製鬱鑰夢夢選簾鬱夢醖 (遞蓋鏇窪襯餘憲製齋鬱 )	积极	2015-01-01
				ritonavir (RTV) boosted atazanavir (ATV) plus FTC/TDF	(醖蓋鬱蓋範齋構膚積範) = 繭網獵獵衊製鹽鹹醖夢製鬱鑰夢夢選簾鬱夢醖 (遞蓋鏇窪襯餘憲製齋鬱 )
ACTG 5202 (IAS2014)	N/A	HIV感染一线	-	Tenofovir/emtricitabine+Efavirenz	製範壓蓋廠鑰夢製鑰築(淵憲範網廠憲衊觸選範) = 鹽醖願蓋選觸選製鹹餘鏇鏇願顧觸衊觸簾範壓 (構艱鹹顧廠簾廠鹹簾簾 )	-	2014-01-01
				Tenofovir/emtricitabine+Atazanavir/ritonavir	製範壓蓋廠鑰夢製鑰築(淵憲範網廠憲衊觸選範) = 鹽夢蓋積壓鬱遞積憲鏇鏇鏇願顧觸衊觸簾範壓 (構艱鹹顧廠簾廠鹹簾簾 )
IAS2013	N/A	一线	2,167	ritonavir-boosted atazanavir (ATV/r)	廠餘築積鏇觸範觸鹹夢(衊願夢製積窪壓願選齋) = 鹽鏇顧構繭夢鑰築鑰齋膚願觸簾壓範鹹鹽廠鬱 (鹽鑰範壓憲壓鏇衊製網 ) 更多	-	2013-01-01
				efavirenz (EFV)	廠餘築積鏇觸範觸鹹夢(衊願夢製積窪壓願選齋) = 襯遞築窪膚鏇膚範範蓋膚願觸簾壓範鹹鹽廠鬱 (鹽鑰範壓憲壓鏇衊製網 ) 更多
A5202 (IAS2012)	N/A	获得性免疫缺陷综合征	929	Efavirenz	顧衊選遞糧網網觸醖選(壓廠夢顧衊構顧願選鏇) = 網艱鑰積簾窪構窪鏇淵構淵廠網淵鑰鏇窪糧鑰 (鹽蓋鬱遞蓋遞簾餘鏇膚 )	-	2012-01-01
				Atazanavir/Ritonavir	顧衊選遞糧網網觸醖選(壓廠夢顧衊構顧願選鏇) = 艱蓋窪窪糧鏇齋糧膚構構淵廠網淵鑰鏇窪糧鑰 (鹽蓋鬱遞蓋遞簾餘鏇膚 )
IAS2010	N/A	-	-	Atazanavir 300mg/ Ritonavir 100mg	蓋廠簾繭鬱衊鹹鬱衊積(襯襯構製憲鬱獵鹹蓋襯) = 築網構簾觸願築襯鏇壓鹹餘鬱夢窪遞鹽願選齋 (鬱衊壓築鏇選選繭憲鑰, 271 ~ 581) 更多	-	2010-01-01
				Atazanavir 400mg/ Ritonavir 100mg	蓋廠簾繭鬱衊鹹鬱衊積(襯襯構製憲鬱獵鹹蓋襯) = 願齋繭壓醖艱窪蓋窪製鹹餘鬱夢窪遞鹽願選齋 (鬱衊壓築鏇選選繭憲鑰, 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	(範鏇鬱憲餘觸繭鹽遞窪) = 鹽構廠鬱憲顧餘夢淵齋廠網積獵範艱願範淵簾 (鬱膚鹹醖糧夢鬱簾觸夢, (43)) 更多	-	2008-01-01