Cargando…

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

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Navarro, Jordi, Curran, Adrian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5098528/
https://www.ncbi.nlm.nih.gov/pubmed/27843352
http://dx.doi.org/10.2147/HIV.S56158
_version_ 1782465797490212864
author Navarro, Jordi
Curran, Adrian
author_facet Navarro, Jordi
Curran, Adrian
author_sort Navarro, Jordi
collection PubMed
description 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.
format Online
Article
Text
id pubmed-5098528
institution National Center for Biotechnology Information
language English
publishDate 2016
publisher Dove Medical Press
record_format MEDLINE/PubMed
spelling pubmed-50985282016-11-14 Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS Navarro, Jordi Curran, Adrian HIV AIDS (Auckl) Review 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. Dove Medical Press 2016-10-31 /pmc/articles/PMC5098528/ /pubmed/27843352 http://dx.doi.org/10.2147/HIV.S56158 Text en © 2016 Navarro and Curran. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Review
Navarro, Jordi
Curran, Adrian
Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS
title 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_short 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
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5098528/
https://www.ncbi.nlm.nih.gov/pubmed/27843352
http://dx.doi.org/10.2147/HIV.S56158
work_keys_str_mv AT navarrojordi profileofoncedailydarunavircobicistatfixeddosecombinationforthetreatmentofhivaids
AT curranadrian profileofoncedailydarunavircobicistatfixeddosecombinationforthetreatmentofhivaids