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Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS

Dolutegravir (DTG) is a second-generation integrase strand transfer inhibitor (INSTI), which has now been licensed to be used in different countries including the UK. Earlier studies have demonstrated that DTG when used with nucleoside backbone in treatment-naïve and - experienced patients has been...

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Autores principales: Taha, Huda, Das, Archik, Das, Satyajit
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4598225/
https://www.ncbi.nlm.nih.gov/pubmed/26491363
http://dx.doi.org/10.2147/IDR.S68396
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author Taha, Huda
Das, Archik
Das, Satyajit
author_facet Taha, Huda
Das, Archik
Das, Satyajit
author_sort Taha, Huda
collection PubMed
description Dolutegravir (DTG) is a second-generation integrase strand transfer inhibitor (INSTI), which has now been licensed to be used in different countries including the UK. Earlier studies have demonstrated that DTG when used with nucleoside backbone in treatment-naïve and - experienced patients has been well tolerated and demonstrated virological suppression comparable to other INSTIs and superiority against other first-line agents, including efavirenz and boosted protease inhibitors. Like other INSTIs, DTG uses separate metabolic pathways compared to other antiretrovirals and is a minor substrate for CYP-450. It does not appear to have a significant interaction with drugs, which uses the CYP-450 system. Nonetheless, it uses renal solute transporters that may potentially inhibit the transport of other drugs and can have an effect on the elimination of other drugs. However, the impact of this mechanism appears to be very minimal and insignificant clinically. The side effect profiles of DTG are similar to raltegravir and have been found to be well tolerated. DTG has a long plasma half-life and is suitable for once daily use without the need for a boosting agent. DTG has all the potential to be used as a first-line drug in combination with other nucleoside backbones, especially in the form of a single tablet in combination with abacavir and lamivudine. The purpose of this review article is to present the summary of the available key information about the clinical usefulness of DTG in the treatment of HIV infection.
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spelling pubmed-45982252015-10-21 Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS Taha, Huda Das, Archik Das, Satyajit Infect Drug Resist Review Dolutegravir (DTG) is a second-generation integrase strand transfer inhibitor (INSTI), which has now been licensed to be used in different countries including the UK. Earlier studies have demonstrated that DTG when used with nucleoside backbone in treatment-naïve and - experienced patients has been well tolerated and demonstrated virological suppression comparable to other INSTIs and superiority against other first-line agents, including efavirenz and boosted protease inhibitors. Like other INSTIs, DTG uses separate metabolic pathways compared to other antiretrovirals and is a minor substrate for CYP-450. It does not appear to have a significant interaction with drugs, which uses the CYP-450 system. Nonetheless, it uses renal solute transporters that may potentially inhibit the transport of other drugs and can have an effect on the elimination of other drugs. However, the impact of this mechanism appears to be very minimal and insignificant clinically. The side effect profiles of DTG are similar to raltegravir and have been found to be well tolerated. DTG has a long plasma half-life and is suitable for once daily use without the need for a boosting agent. DTG has all the potential to be used as a first-line drug in combination with other nucleoside backbones, especially in the form of a single tablet in combination with abacavir and lamivudine. The purpose of this review article is to present the summary of the available key information about the clinical usefulness of DTG in the treatment of HIV infection. Dove Medical Press 2015-10-01 /pmc/articles/PMC4598225/ /pubmed/26491363 http://dx.doi.org/10.2147/IDR.S68396 Text en © 2015 Taha et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. 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
Taha, Huda
Das, Archik
Das, Satyajit
Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS
title Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS
title_full Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS
title_fullStr Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS
title_full_unstemmed Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS
title_short Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS
title_sort clinical effectiveness of dolutegravir in the treatment of hiv/aids
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4598225/
https://www.ncbi.nlm.nih.gov/pubmed/26491363
http://dx.doi.org/10.2147/IDR.S68396
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