Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS

Jordi Navarro, Adrian Curran Infectious Diseases Department, Hospital Universitari Vall d’Hebron, Universitat Autònoma de Barcelona, Barcelona, Spain Abstract: Efficacy is the main objective of antiretroviral treatment and adherence is one of the cornerstones to achiev...

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Autores principales:	Navarro J, Curran A
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	darunavir cobicistat fixed-dose combination HIV infection antiretroviral treatment. Immunologic diseases. Allergy RC581-607
Acceso en línea:	https://doaj.org/article/09a0768bc0c648c2b541b7d45621f610
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spelling	oai:doaj.org-article:09a0768bc0c648c2b541b7d45621f6102021-12-02T08:03:55ZProfile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS1179-1373https://doaj.org/article/09a0768bc0c648c2b541b7d45621f6102016-10-01T00:00:00Zhttps://www.dovepress.com/profile-of-once-daily-darunavircobicistat-fixed-dose-combination-for-t-peer-reviewed-article-HIVhttps://doaj.org/toc/1179-1373Jordi Navarro, Adrian Curran Infectious Diseases Department, Hospital Universitari Vall d’Hebron, Universitat Autònoma de Barcelona, Barcelona, Spain Abstract: Efficacy is the main objective of antiretroviral treatment and adherence is one of the cornerstones to achieve it. For this reason, treatment simplification is of key importance with regard to antiretroviral regimens. Rezolsta® (darunavir/cobicistat) is the first fixed-dose combination containing a protease inhibitor approved for HIV treatment. This coformulation includes darunavir, a protease inhibitor that has shown its efficacy and safety in naïve and treatment-experienced patients, and cobicistat, the new pharmacokinetic enhancer that is expected to replace ritonavir. Bioequivalence between ritonavir and cobicistat as darunavir boosters has been shown in studies involving healthy volunteers. Furthermore, efficacy and safety of darunavir/cobicistat observed in phase III studies, including naïve and pretreated patients without darunavir-associated resistance mutations, are comparable to historical data of darunavir/ritonavir 800/100 mg once-daily formulation. Adverse events with darunavir/cobicistat are scarce and mild, and basically include skin reactions and gastrointestinal disturbances. Although small increases in plasma creatinine are expected in patients receiving cobicistat due to the inhibition of creatinine transporters in kidney tubules, actual glomerular filtrate rate remains unaltered. Cobicistat does not have an inducer effect on metabolic pathways and shows much more selective inhibition than ritonavir. Therefore, isoenzyms different from CYP3A4 are supposed to be less affected by cobicistat, and thus fewer drug–drug interactions are expected. Keywords: darunavir, cobicistat, fixed-dose combination, HIV infection, antiretroviral treatmentNavarro JCurran ADove Medical Pressarticledarunavircobicistatfixed-dose combinationHIV infectionantiretroviral treatment.Immunologic diseases. AllergyRC581-607ENHIV/AIDS: Research and Palliative Care, Vol Volume 8, Pp 175-182 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	darunavir cobicistat fixed-dose combination HIV infection antiretroviral treatment. Immunologic diseases. Allergy RC581-607
spellingShingle	darunavir cobicistat fixed-dose combination HIV infection antiretroviral treatment. Immunologic diseases. Allergy RC581-607 Navarro J Curran A Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS
description	Jordi Navarro, Adrian Curran Infectious Diseases Department, Hospital Universitari Vall d’Hebron, Universitat Autònoma de Barcelona, Barcelona, Spain Abstract: Efficacy is the main objective of antiretroviral treatment and adherence is one of the cornerstones to achieve it. For this reason, treatment simplification is of key importance with regard to antiretroviral regimens. Rezolsta® (darunavir/cobicistat) is the first fixed-dose combination containing a protease inhibitor approved for HIV treatment. This coformulation includes darunavir, a protease inhibitor that has shown its efficacy and safety in naïve and treatment-experienced patients, and cobicistat, the new pharmacokinetic enhancer that is expected to replace ritonavir. Bioequivalence between ritonavir and cobicistat as darunavir boosters has been shown in studies involving healthy volunteers. Furthermore, efficacy and safety of darunavir/cobicistat observed in phase III studies, including naïve and pretreated patients without darunavir-associated resistance mutations, are comparable to historical data of darunavir/ritonavir 800/100 mg once-daily formulation. Adverse events with darunavir/cobicistat are scarce and mild, and basically include skin reactions and gastrointestinal disturbances. Although small increases in plasma creatinine are expected in patients receiving cobicistat due to the inhibition of creatinine transporters in kidney tubules, actual glomerular filtrate rate remains unaltered. Cobicistat does not have an inducer effect on metabolic pathways and shows much more selective inhibition than ritonavir. Therefore, isoenzyms different from CYP3A4 are supposed to be less affected by cobicistat, and thus fewer drug–drug interactions are expected. Keywords: darunavir, cobicistat, fixed-dose combination, HIV infection, antiretroviral treatment
format	article
author	Navarro J Curran A
author_facet	Navarro J Curran A
author_sort	Navarro J
title	Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS
title_short	Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS
title_full	Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS
title_fullStr	Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS
title_full_unstemmed	Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS
title_sort	profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of hiv/aids
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/09a0768bc0c648c2b541b7d45621f610
work_keys_str_mv	AT navarroj profileofoncedailydarunavircobicistatfixeddosecombinationforthetreatmentofhivaids AT currana profileofoncedailydarunavircobicistatfixeddosecombinationforthetreatmentofhivaids
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Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS

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