3 years ago

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

Shannon Callen, Benson Edagwa, Adam Szlachetka, Howard E Gendelman, Howard S Fox, Yazen Alnouti, Lara Slack, JoEllyn McMillan, Brenda Morsey, Benjamin Lamberty, Nagsen Gautam, Brady Sillman
A nanoformulated myristoylated dolutegravir prodrug (NMDTG) was prepared using Good Laboratory Practice protocols. Intramuscular injection of NMDTG (118 ± 8 mg/ml, 25.5 mg DTG equivalents/kg) 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 extended the drug half-life without demonstrable adverse events. Further modification may extend the long-acting nanoformulation platform for human use.

Publisher URL: http://doi.org/10.1128/AAC.01316-17

DOI: 10.1128/AAC.01316-17

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