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


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.

SUBMITTER: McMillan J 

PROVIDER: S-EPMC5740312 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature

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

McMillan JoEllyn J   Szlachetka Adam A   Slack Lara L   Sillman Brady B   Lamberty Benjamin B   Morsey Brenda B   Callen Shannon S   Gautam Nagsen N   Alnouti Yazen Y   Edagwa Benson B   Gendelman Howard E HE   Fox Howard S HS  

Antimicrobial agents and chemotherapy 20171221 1


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. ...[more]

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