Pharmacokinetic testing of a first-generation cabotegravir prodrug in rhesus macaques

JoEllyn M McMillan, Adam Szlachetka, Tian Zhou, Brenda Morsey, Benjamin Lamberty, Shannon Callen, Nagsen Gautam, Yazen Alnouti, Benson J Edagwa, Howard Eliot Gendelman, Howard S Fox

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

: Long-acting antiretrovirals can improve therapy and prevention for HIV-1 infection. Current long-acting cabotegravir (CAB LAP) can be administered every other month. Previously, we demonstrated that a myristoylated CAB prodrug encased in poloxamer 407 provided extended plasma drug concentrations. We now demonstrate that this first-generation nanoformulated prodrug can sustain plasma CAB concentrations above the protein-adjusted 90% inhibitory concentration for 4 months in rhesus macaques. A 2.5-fold extension in CAB half-life and a 1.6-fold increase in area under the concentration-time curve were observed compared with CAB LAP.

Original languageEnglish (US)
Pages (from-to)585-588
Number of pages4
JournalAIDS (London, England)
Volume33
Issue number3
DOIs
StatePublished - Mar 1 2019

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Prodrugs
Macaca mulatta
Pharmacokinetics
Poloxamer
HIV Infections
Half-Life
HIV-1
cellulose acetate-butyrate
Pharmaceutical Preparations
Proteins

ASJC Scopus subject areas

  • Immunology and Allergy
  • Immunology
  • Infectious Diseases

Cite this

Pharmacokinetic testing of a first-generation cabotegravir prodrug in rhesus macaques. / McMillan, JoEllyn M; Szlachetka, Adam; Zhou, Tian; Morsey, Brenda; Lamberty, Benjamin; Callen, Shannon; Gautam, Nagsen; Alnouti, Yazen; Edagwa, Benson J; Gendelman, Howard Eliot; Fox, Howard S.

In: AIDS (London, England), Vol. 33, No. 3, 01.03.2019, p. 585-588.

Research output: Contribution to journalArticle

McMillan, JoEllyn M ; Szlachetka, Adam ; Zhou, Tian ; Morsey, Brenda ; Lamberty, Benjamin ; Callen, Shannon ; Gautam, Nagsen ; Alnouti, Yazen ; Edagwa, Benson J ; Gendelman, Howard Eliot ; Fox, Howard S. / Pharmacokinetic testing of a first-generation cabotegravir prodrug in rhesus macaques. In: AIDS (London, England). 2019 ; Vol. 33, No. 3. pp. 585-588.
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AU - Callen, Shannon

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