乙醇达芦那韦/利托那韦(Darunavir Ethanolate/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

DARUNAVIR AND RITONAVIR、Darunavir/ritonavir、Virontar

+ [1]

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

Laboratorios Richmond SACIF

在研机构

Laboratorios Richmond SACIFMylan Pharmaceuticals, Inc.

非在研机构-

最高研发阶段批准上市

首次获批日期

阿根廷 (2015-01-01),

HIV感染

最高研发阶段(中国)-

特殊审评-

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结构

分子式C29H43N3O8S

InChIKeyQWSHKNICRJHQCY-VBTXLZOXSA-N

CAS号635728-49-3

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关联

34

项与乙醇达芦那韦/利托那韦相关的临床试验

NCT06139796 / Not yet recruiting临床1/2期IIT

Pharmacokinetics, Safety and Acceptability of a Solid Paediatric Fixed-dose Combination of Darunavir/ritonavir (DRV/r) 120/20 Mg for Children Living with HIV

The UNIVERSAL2 study is a research project designed to evaluate a newly developed formulation of an approved drug for children living with HIV aged over 3 years and weighing between 10 and 25 kg. The aim of UNIVERSAL2 is to determine the right dosage of this new formulation.

开始日期2024-12-01

申办/合作机构

Institut National de la Santé et de la Recherche Médicale

[+1]

NCT06338826 / Not yet recruiting临床2期IIT

Interventional, Multicenter, Open-label, Randomized, Non-comparative Trial Evaluating the Safety, in Terms of HBV Virological Control at 96 Weeks, of 2 Antiviral Treatment Relief Strategies, in Patients Co-infected With the HIV-1 and HBV Viruses

The main objective of this study is to evaluate at 96 weeks the safety with respect to hepatitis B control of 2 treatment reduction strategies for patients with previously controlled HIV-HBV co-infection on continuous triple therapy

开始日期2024-10-01

申办/合作机构

ANRS, Emerging Infectious Diseases

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]

100 项与乙醇达芦那韦/利托那韦相关的临床结果

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100 项与乙醇达芦那韦/利托那韦相关的转化医学

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100 项与乙醇达芦那韦/利托那韦相关的专利（医药）

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94

项与乙醇达芦那韦/利托那韦相关的文献（医药）

2024-01-01·HIV Medicine

Daily ritonavir‐boosted darunavir for viral suppression in pregnancy (DRV‐P)

Article

作者: Tkachuk, Stacey ; Tulloch, Karen ; Gacic, Nikolina ; Money, Deborah

AbstractBackgroundRitonavir‐boosted darunavir (DRV/r) is a preferred protease inhibitor in pregnant women living with HIV. Current practice at British Columbia's referral centre (the Oak Tree Clinic) is to dose DRV/r as 800/100 mg daily throughout pregnancy, although some guidelines recommend DRV/r 600/100 mg twice daily due to altered pharmacokinetics with once‐daily dosing.ObjectivesWe describe the effect of once‐daily DRV/r on viral suppression, vertical transmission, adverse drug effects and adherence in pregnant women living with HIV.MethodsThis was a retrospective analysis of pregnant women living with HIV in British Columbia. Eligible women gave birth between January 2015 and August 2021, and took DRV/r 800/100 mg daily at any time during pregnancy.ResultsThirty‐four women were included in this study. The mean (SD) age was 33 (5) years. Thirty (88%) women were diagnosed with HIV prior to pregnancy, with 22 (73%) having viral suppression at baseline. Four (12%) were diagnosed in pregnancy, with a median baseline viral load of 9616 copies/mL (range 8370–165 000). Viral suppression was achieved by 16 (100%), 24 (75%) and 26 (74%) women in the first, second and third trimesters, respectively. No vertical transmission occurred. This combination was well tolerated, with adverse drug effects that did not result in discontinuation or change in therapy. Most women maintained >75% adherence to once‐daily DRV/r at all times during pregnancy.ConclusionsRitonavir‐boosted darunavir 800/100 mg daily appears to be an appropriate dosing strategy for pregnant women living with HIV who are able to maintain optimal adherence.

2023-06-01·eClinicalMedicine

Nucleoside/nucleotide reverse transcriptase inhibitor sparing regimen with once daily integrase inhibitor plus boosted darunavir is non-inferior to standard of care in virologically-suppressed children and adolescents living with HIV – Week 48 results of the randomised SMILE Penta-17-ANRS 152 clinical trial

Article

作者: Elenga, N. ; Gibb, Diana M. ; Tuna, J. ; Little, E. ; Ford, Deborah ; Blackstone, J. ; Fortuny Guasch, C. ; Van-Looy, N. ; Fernández, M. ; Puangmalai, P. ; Saidi, Y. ; Thapwai, T. ; Wachinger, T. ; Maduna, N. ; Silva Milhiero, T. ; Teixeira, C. ; Hirt, D. ; Doshi, S. ; Khusuwan, S. ; Khamjakkaew, W. ; Namuddu, R. ; Kiyimba, L. ; Sripaoraya, W. ; Paioni, Paolo ; Sampaio, A.C. ; Lawrence, L. ; Cotton, Mark ; Kyobutungi, P. ; Amuge, Pauline ; Slade, G. ; Pongprapass, S. ; Morkunaite, G. ; Prieto Tato, L. ; Turkova, A. ; Thewsoongnoen, J. ; Ford, D. ; Kalhert, C. ; Harper, L. ; Mbabazi, R. ; Saenjum, C. ; Babiker, Abdel ; Musiime, V. ; Srirompotong, U. ; Pouchain, H. ; Bbuye, D. ; Mendes, A.C. ; Ngampiyaskul, C. ; Khunene, M. ; Uyungrwoth, A. ; Dell’Orso, M. ; Maseko, L. ; Ferraz, I. ; Sibanda, N. ; Soria, A. ; Basiimwa, R. ; Lakha, R. ; Coto, M. ; Kaudha, E. ; Kekitiinwa, A.R. ; Niehues, T. ; Riault, Y. ; Fernandes, A. ; Nannungi, M. ; Liberty, Afaaf A. ; Townsend, S. ; Pavia Ruz, Noris ; Junkaew, R. ; Primak, N. ; Mespoulhe, P. ; Babu, E.L. ; Than-in-at, K. ; Tching Sin, M. ; Nascimento, H. ; Plonné, D. ; Ramos Amador, J.T. ; Navarro Gómez, M. ; Bilardi, D. ; Bologna, R. ; Ruklao, C. ; Barnabas, S. ; Morén, C. ; Gandhi, K. ; Vicentini, E. ; Wessels, M. ; Donngernl, D. ; Chan, Man K. ; Arulananthan, A. ; Agaba, G. ; Singh, U. ; Saegesser, C. ; Coelho, A. ; Raus, I. ; Pavia-Ruz, N. ; Vaughn-Gordon, Y. ; Nabwire, I. ; Muñoz Fernández, M.A. ; Manyi, F. ; Mulindwa, A. ; Chereau, N. ; Pinheiro, H. ; Namanda, S. ; Sukrakanchana, P. ; Neri-Macias, A. ; Groenewald, M. ; Saïdi, Yacine ; Moragas, M. ; Kitabalwa, J. ; Kamkoonmongkol, A. ; Nakabuye, S. ; Hamlyn, E. ; Torres Arauz, M. ; Cubells, M. ; Mostovenko, O. ; Nabalamba, M. ; Mur, A. ; Adebayo, A. ; Candeias, M.F. ; Nduna, N. ; Cagnot, C. ; Ategeka, J. ; Akoojee, N. ; Thungkham, K. ; Jourdain, G. ; Chalermpantmetagul, Suwalai ; Kekitiinwa, Adeodata R. ; Fedullo, A.G. ; Mulima, D. ; Weldon, S. ; Fourie, Y. ; Nalubwama, J. ; Welch, Steven B. ; Ahimbisibwe, G. ; Khamkon, J. ; Chinwong, D. ; Smuts, M. ; Groenewald, Marisa ; Torrent, R. ; Daniel, T. ; Petpranee, T. ; Inyakuwal, C. ; Ganger, L. ; Bologna, Rosa ; Giaquinto, C. ; Kanjanavanit, S. ; Taicz, M. ; Faria, C. ; Vergnano, S. ; Cardão, M. ; Theunissen, M. ; Musiime, Victor ; Tumusiime, J. ; Monteiro, F. ; Meeboon, C. ; Marques, Laura ; Epalza, C. ; Mangano, A. ; Daglish, J. ; Nardone, A. ; Léger, L. ; Gilmour, C. ; Hoorn, L. ; Mann, B. ; Flet, L. ; Hafner, S. ; Nsibuka Kisekka, M. ; Niehues, Tim ; Augustin, S. ; Ngo Giang Huong, N. ; Rojo Conejo, P. ; Compagnucci, A. ; Mendes, D. ; Krueduangkam, N. ; Chamjamrat, W. ; Gao, L. ; Picault, L. ; Musiime, A. ; Srirojana, S. ; Prieto Tato, Luis ; Pieterse, S. ; Mamiane, A. ; Nambi, E. ; Kadhuba, R. ; Calvert, J. ; Baliruno, D. ; Reis Melo, A. ; Srisuk, W. ; Inshaw, J. ; Espinosa-Sotero, C. ; Isaacs, M. ; Williams, E.D. ; Ball, C. ; Oliveira, A. ; Phunkhum, P. ; Govender, S. ; Mwebaza, J. ; Meyer, L. ; Bhana, P. ; Rutebarika, D. ; Nalugo, A. ; Denjanta, S. ; Ribeiro, R. ; Tearsansern, P. ; Kongponoi, A. ; Matos, A.C. ; Liberty, A. ; Guillén Martin, S. ; Namusanje, J. ; Tikabibamu, J. ; Nolan, Aoife ; Boni, J. ; Kamboua, P. ; Blaise, N. ; Nyati, M. ; Rubanga, E. ; Nayagam, D. ; Widuch, K. ; Cotton, M. ; Hawkins, S. ; Nunes, R. ; Nabukeera Barung, N. ; Dollenmaier, G. ; Baita, A. ; Garcia, I. ; Gatto, M. ; Wohlwend, B. ; Gomes Neves, E. ; Estepa, C. ; Vadee, A. ; Ramos Amador, Jose Tomas ; Prucha, C. ; Coelho, Alexandra ; Reliquet, Véronique ; Mugarura, L. ; Cressey, T.R. ; Stepchenkova, T. ; Chalermpantmetagul, S. ; Compagnucci, Alexandra ; Sans, E. ; Ojok, M. ; Nolan, A. ; Sainz Costa, T. ; Giaquinto, Carlo ; Yingyong, P. ; Nazzinda, R. ; Violari, Avy ; Na Kalasin, N. ; Kaewbundit, A. ; Terrine, M.D. ; Volokha, A. ; Kaewmamueng, K. ; Kruenual, N. ; Corte-Real, R. ; Gibb, D.M. ; Noguera Julian, T. ; Amuge, P. ; Jarillo-Quijada, M.D. ; Limplertjareanwanich, J. ; Kaudha, Elizabeth ; Mellado Peña, M.J. ; Padrao, A. ; Caldeira, A. ; Chan, M. ; Coetzee, J. ; Duppenthaler, A. ; Tavares, M. ; Prieto, L. ; Ndiaye, M. ; Essack, Z. ; Noguera, T. ; Namuli, F. ; Kanjanavanit, Suparat ; Paioni, P. ; Arazi, S. ; Greetanukroh, P. ; Labeja Ocitti, S.P. ; Kityo, C.M. ; Muñoz- Hernández, R. ; Kongsuk, K. ; Nsirim, E. ; Babiker, A. ; Thrasyvoulou, L. ; Chanto, N. ; Correira, C. ; Morkunaite, Gabija ; Erasmus, J. ; Nanduudu, A. ; Khamduang, W. ; Khannak, P. ; Ross, M. ; Escosa García, L. ; Nunn, A. ; Reliquet, V. ; Kenny, J. ; Gilmour-White, S. ; Hemon, C. ; Barbani, M. ; Laomanit, L. ; Tupper, K. ; Gomez Salcedo, P. ; Peongjakta, R. ; Murciano Cabeza, A. ; Mujyambere, E. ; Morgado, M. ; Kisitu, G.P. ; Cweya, A. ; Nakalyango, A. ; Nakandi, L. ; Sudsaard, P. ; Bruno, E. ; Irvine, E. ; Moreno, M. ; Cressey, Tim R. ; Scott, K. ; Bamford, A. ; Paredes, E. ; Marques, L. ; Hudson, F. ; Chutima, D. ; Chankun, T. ; Ramsagar, N. ; Circosta, S. ; Callaghan, A. ; Ounchanum, P. ; Mendez García, P. ; Simanic, S. ; Klinprung, S. ; Fry, S. ; Bamford, Alasdair ; Oruk, S. ; Fuller, E. ; Smith, K. ; Makola, C. ; Thaweesombat, Y. ; Odoch, D. ; Fabiane, S. ; Kouakam, C. ; Welch, S. ; Rodallec, A. ; Violari, A. ; Saewtrakool, C. ; Katemba, C. ; Bagirigomwa, E. ; Signorell, R. ; Riault, Yoann ; Mkhize, S. ; Ahmad, M. ; Kirabira, A. ; Castro, C. ; Volokha, Alla

BackgroundIntegrase inhibitor (INSTI) with boosted darunavir (DRV/r), a regimen with a high-resistance barrier, avoiding NRTI toxicities, might be a switching option in children living with HIV (CLWHIV).MethodsSMILE is a randomised non-inferiority trial evaluating safety and antiviral efficacy of once-daily INSTI + DRV/r vs. continuing on current standard-of-care (SOC) triple ART (2NRTI + boosted PI/NNRTI) in virologically-suppressed CLWHIV aged 6-18 years. The primary outcome is the proportion with confirmed HIV-RNA ≥50 copies/mL by week 48, estimated by Kaplan-Meier method. Non-inferiority margin was 10%. Registration number for SMILE are: ISRCTN11193709, NCT #: NCT02383108.FindingsBetween 10th June 2016 and 30th August 2019, 318 participants were enrolled from Africa 53%, Europe 24%, Thailand 15% and Latin America 8%, 158 INSTI + DRV/r [153 Dolutegravir (DTG); 5 Elvitegravir (EVG)], 160 SOC. Median (range) age was 14.7 years (7.6-18.0); CD4 count 782 cells/mm³ (227-1647); 61% female. Median follow-up was 64.3 weeks with no loss to follow-up. By 48 weeks, 8 INSTI + DRV/r vs. 12 SOC had confirmed HIV-RNA ≥50 copies/mL; difference (INSTI + DRV/r-SOC) -2.5% (95% CI: -7.6, 2.5%), showing non-inferiority. No major PI or INSTI resistance mutations were observed. There were no differences in safety between arms. By week 48, difference (INSTI + DRV/r-SOC) in mean CD4 count change from baseline was -48.3 cells/mm³ (95% CI: -93.4, -3.2; p = 0.036). Difference (INSTI + DRV/r-SOC) in mean HDL change from baseline was -4.1 mg/dL (95% CI: -6.7, -1.4; p = 0.003). Weight and Body Mass Index (BMI) increased more in INSTI + DRV/r than SOC [difference: 1.97 kg (95% CI: 1.1, 2.9; p < 0.001), 0.66 kg/m² (95% CI: 0.3, 1.0; p < 0.001)].InterpretationIn virologically-suppressed children, switching to INSTI + DRV/r was non-inferior virologically, with similar safety profile, to continuing SOC. Small but significant differences in CD4, HDL-cholesterol, weight and BMI were observed between INSTI + DRV/r vs. SOC although clinical relevance needs further investigation. SMILE data corroborate adult findings and provide evidence for this NRTI-sparing regimen for children and adolescents.FundingFondazione Penta Onlus, Gilead, Janssen, INSERM/ANRS and UK MRC. ViiV-Healthcare provided Dolutegravir.

2022-12-09·Medicine

Observational study to evaluate discontinuation of monotherapy with cobicistat-boosted darunavir in patients with human immunodeficiency virus

Article

作者: Montero, Marta ; Solana-Altabella, Antonio ; Salavert, Miguel ; Cuéllar-Monreal, Maria Jesús ; Monte-Boquet, Emilio ; Poveda-Andrés, José Luis ; Pérez-Huertas, Pablo

To evaluate the reasons for changing to monotherapy with protease inhibitors, together with the proportion and reasons for the interruption to treatment, in patients who have been treated at some point with cobicistat-boosted darunavir (DRV/c). Outpatients in a tertiary hospital. Observational retrospective study to evaluate monotherapy with DRV/c (800 mg/150 mg) in adult patients with human immunodeficiency virus infection, from December 2014 to July 2022. Demographic variables, viral load, cluster of differentiation 4 lymphocyte lymphocyte count, and antiretroviral therapy were assessed. 42 patients were included. 36% of the patients were undergoing monotherapy at the time of the analysis. The main reason for discontinuation was poor adherence. At time of analysis, 80% of the patients in monotherapy had an undetectable viral load. Antiretroviral therapy recommendations advise against exposing the patient to functional monotherapy with a single drug due to the high risk of virological failure and the onset of resistance to a single drug. Following the analysis of the results, DRV/c in monotherapy is not an effective strategy in the medium and long term due to factors such as lack of adherence or virological failure, although it can be maintained in specific circumstances. Therefore, patients undergoing monotherapy require close monitoring.

100 项与乙醇达芦那韦/利托那韦相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
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研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
HIV感染	阿根廷	Laboratorios Richmond SACIF	2015-01-01

未上市

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	Mylan Pharmaceuticals, Inc.	-

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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


SMILE PENTA-17 TRIAL (IAS2021)	N/A	-	318	INSTI+Darunavir/r	(壓齋艱鏇製壓憲廠鏇醖): P-Value = 0.036 更多	-	2021-01-01
				boosted darunavir (Standard-of-care (SOC))
DRIVE-FORWARD, DRIVE-AHEAD (Pubmed \| Clin Infect Dis)	临床3期	HIV感染	-	Doravirine/lamivudine/tenofovir disoproxil fumarate	窪壓衊遞積繭範積夢醖(範選觸憲鹽繭遞網顧鏇) = 繭襯夢願衊鏇夢衊積範鹹膚襯顧獵衊繭構選製 (憲網廠遞窪憲齋選憲遞 ) 更多	积极	2020-03-17
				Darunavir plus ritonavir	窪壓衊遞積繭範積夢醖(範選觸憲鹽繭遞網顧鏇) = 獵醖齋淵範衊鏇壓鏇壓鹹膚襯顧獵衊繭構選製 (憲網廠遞窪憲齋選憲遞 ) 更多
DRIVE-FORWARD (IAS2018)	N/A	-	769	Doravirine (DOR)	(簾淵鏇醖廠糧選範醖繭) = DOR 17.0%, DRV+r 23.8% 膚醖齋艱窪憲壓衊鏇廠 (襯艱淵糧積觸醖鏇築範 ) 更多	积极	2018-01-01
				Ritonavir-boosted darunavir (DRV+r)
NCT02770508 (ANDES, IAS2017)	临床4期	HIV感染	145	Darunavir/ritonavir plus lamivudine	(壓窪淵簾膚壓遞鬱選鹽) = one patient was discontinued due to a drug-related grade 3 adverse event (rash) 範構構願選鏇遞襯築壓 (艱遞範鬱襯襯膚顧襯鑰 ) 更多	积极	2017-01-01
				Triple therapy with DRV/RTV plus TDF/3TC
ANRS 12269 (IAS2017)	N/A	HIV感染三线	201	Darunavir/r 600/100 mg BID + Raltegravir 400 mg BID	(艱餘鹽餘夢鏇鹹簾構築) = 膚壓糧夢鹹觸鬱鹽廠襯壓齋願餘築憲鹹蓋壓壓 (夢積願齋衊鏇糧鑰顧繭 ) 更多	积极	2017-01-01
NCT01516970 (PEPDar, CTgov)	临床3期	HIV感染	312	DRV/r+Ritonavir+Darunavir (Darunavir/Ritonavir Postexposure Prophylaxis (DRV/r PEP))	壓廠積願襯願鑰衊鏇鬱(鬱鏇鏇餘網觸繭壓膚鏇) = 觸醖醖鹹淵糧襯遞鬱鏇憲網鏇觸鹽廠繭遞夢艱 (鏇構淵鬱鏇顧膚餘繭齋, 範齋夢積鬱憲襯廠鑰選 ~ 淵鑰襯鏇窪淵夢醖廠蓋) 更多	-	2016-10-11
				SOCPEP (Standard of Care Postexposure Prophylaxis (SOCPEP))	壓廠積願襯願鑰衊鏇鬱(鬱鏇鏇餘網觸繭壓膚鏇) = 艱觸繭範構繭糧壓遞鹹憲網鏇觸鹽廠繭遞夢艱 (鏇構淵鬱鏇顧膚餘繭齋, 選鹽遞襯繭顧齋餘壓鹹 ~ 願繭積糧餘齋築築顧顧) 更多
NCT01066962 (NEAT001/ANRS143, Pubmed \| Lancet HIV)	临床3期	HIV感染	146	Darunavir-ritonavir + Raltegravir	窪齋鹽壓壓鹽繭蓋構蓋(顧鹹構襯觸觸淵構製窪) = 壓鹹醖鬱艱構選簾壓鑰築顧醖築選膚衊壓顧鏇 (齋夢製築範壓觸獵觸蓋 )	积极	2015-11-01
				Darunavir-ritonavir + Tenofovir-emtricitabine	窪齋鹽壓壓鹽繭蓋構蓋(顧鹹構襯觸觸淵構製窪) = 鹽觸窪艱壓憲獵齋襯觸築顧醖築選膚衊壓顧鏇 (齋夢製築範壓觸獵觸蓋 )
Pubmed \| HIV Med	N/A	-	-	etravirine plus darunavir/ritonavir	(憲蓋餘膚繭襯築鹹齋願) = 鹽餘繭製襯築糧積範鏇鹽齋淵積築獵網範鬱遞 (鏇鹽簾鏇壓糧製壓選構 ) 更多	-	2015-05-01
				etravirine plus an alternative boosted protease inhibitor	(憲蓋餘膚繭襯築鹹齋願) = 糧醖膚糧廠構艱醖鏇艱鹽齋淵積築獵網範鬱遞 (鏇鹽簾鏇壓糧製壓選構 ) 更多
MODERN (IAS2015)	N/A	-	-	Maraviroc (MVC) with darunavir/ritonavir (DRV/r)	(糧築範齋顧淵襯齋衊廠) = 鏇齋鹹齋築憲醖鑰齋醖夢選繭製觸齋餘網願糧 (壓網願鏇範願夢憲膚壓, 243) 更多	-	2015-01-01
				Tenofovir/emtricitabine (TDF/FTC) with DRV/r	(糧築範齋顧淵襯齋衊廠) = 廠構鬱鑰顧壓蓋範憲網夢選繭製觸齋餘網願糧 (壓網願鏇範願夢憲膚壓, 288) 更多
IAS2015	N/A	维生素D缺乏症	70	Atripla	糧積顧齋壓願製餘鏇窪(淵衊構範繭糧窪選壓餘): P-Value = 0.03 更多	-	2015-01-01
				Darunavir/Ritonavir monotherapy (DRV/r)