Pharmacokinetics of a long-acting nanoformulated dolutegravir prodrug in rhesus macaques

Jo Ellyn McMillan, Adam Szlachetka, Lara Slack, Brady Sillman, Benjamin Lamberty, Brenda Morsey, Shannon Callen, Nagsen Gautam, Yazen Alnouti, Benson Edagwa, Howard E. Gendelman, Howard S. Fox

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

Abstract

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.

Original languageEnglish (US)
Article numbere01316-17
JournalAntimicrobial Agents and Chemotherapy
Volume62
Issue number1
DOIs
StatePublished - Jan 2018

Keywords

  • Dolutegravir
  • Long-acting antiretrovirals
  • Monkeys
  • Nanoformulated antiretrovirals

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

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