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Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques

A nanoformulated myristoylated dolutegravir prodrug (NMDTG) was prepared using good laboratory practice protocols. Intramuscular injection of NMDTG (118 ± 8 mg/ml, 25.5 mg of DTG equivalents/kg of body weight) to three rhesus macaques led to plasma DTG levels of 86 ± 12 and 28 ± 1 ng/ml on days 35 a...

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Autores principales: McMillan, JoEllyn, Szlachetka, Adam, Slack, Lara, Sillman, Brady, Lamberty, Benjamin, Morsey, Brenda, Callen, Shannon, Gautam, Nagsen, Alnouti, Yazen, Edagwa, Benson, Gendelman, Howard E., Fox, Howard S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Society for Microbiology 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5740312/
https://www.ncbi.nlm.nih.gov/pubmed/29061742
http://dx.doi.org/10.1128/AAC.01316-17
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author McMillan, JoEllyn
Szlachetka, Adam
Slack, Lara
Sillman, Brady
Lamberty, Benjamin
Morsey, Brenda
Callen, Shannon
Gautam, Nagsen
Alnouti, Yazen
Edagwa, Benson
Gendelman, Howard E.
Fox, Howard S.
author_facet McMillan, JoEllyn
Szlachetka, Adam
Slack, Lara
Sillman, Brady
Lamberty, Benjamin
Morsey, Brenda
Callen, Shannon
Gautam, Nagsen
Alnouti, Yazen
Edagwa, Benson
Gendelman, Howard E.
Fox, Howard S.
author_sort McMillan, JoEllyn
collection PubMed
description A nanoformulated myristoylated dolutegravir prodrug (NMDTG) was prepared using good laboratory practice protocols. Intramuscular injection of NMDTG (118 ± 8 mg/ml, 25.5 mg of DTG equivalents/kg of body weight) to three rhesus macaques led to plasma DTG levels of 86 ± 12 and 28 ± 1 ng/ml on days 35 and 91, respectively. The NMDTG platform showed no significant adverse events. Further modification may further extend the drug's apparent half-life for human use.
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spelling pubmed-57403122017-12-26 Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques McMillan, JoEllyn Szlachetka, Adam Slack, Lara Sillman, Brady Lamberty, Benjamin Morsey, Brenda Callen, Shannon Gautam, Nagsen Alnouti, Yazen Edagwa, Benson Gendelman, Howard E. Fox, Howard S. Antimicrob Agents Chemother Antiviral Agents A nanoformulated myristoylated dolutegravir prodrug (NMDTG) was prepared using good laboratory practice protocols. Intramuscular injection of NMDTG (118 ± 8 mg/ml, 25.5 mg of DTG equivalents/kg of body weight) to three rhesus macaques led to plasma DTG levels of 86 ± 12 and 28 ± 1 ng/ml on days 35 and 91, respectively. The NMDTG platform showed no significant adverse events. Further modification may further extend the drug's apparent half-life for human use. American Society for Microbiology 2017-12-21 /pmc/articles/PMC5740312/ /pubmed/29061742 http://dx.doi.org/10.1128/AAC.01316-17 Text en Copyright © 2017 McMillan et al. https://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution 4.0 International license (https://creativecommons.org/licenses/by/4.0/) .
spellingShingle Antiviral Agents
McMillan, JoEllyn
Szlachetka, Adam
Slack, Lara
Sillman, Brady
Lamberty, Benjamin
Morsey, Brenda
Callen, Shannon
Gautam, Nagsen
Alnouti, Yazen
Edagwa, Benson
Gendelman, Howard E.
Fox, Howard S.
Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques
title Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques
title_full Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques
title_fullStr Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques
title_full_unstemmed Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques
title_short Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques
title_sort pharmacokinetics of a long-acting nanoformulated dolutegravir prodrug in rhesus macaques
topic Antiviral Agents
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5740312/
https://www.ncbi.nlm.nih.gov/pubmed/29061742
http://dx.doi.org/10.1128/AAC.01316-17
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