title: Formulation and pharmacology of long-acting cabotegravir.
abstract: OBJECTIVE
  Long-acting cabotegravir may provide a novel therapeutic option for both the treatment and prevention of HIV-1 infection that does not necessitate adherence to a daily regimen. The present review will highlight the unique formulation properties and pharmacologic attributes of long-acting cabotegravir nanosuspension.
  
  
  RESULTS
  Cabotegravir is a potent integrase strand transfer inhibitor that has been formulated as an oral tablet for daily administration and as a long-acting injectable nanosuspension. Long-acting cabotegravir is readily absorbed following intramuscular and subcutaneous administration and has an elimination half-life of approximately 40 days, allowing for administration on a monthly or less frequent schedule. Repeat-dose pharmacokinetic studies and population pharmacokinetic modeling indicate monthly and bi-monthly dosing achieves clinically relevant plasma concentrations considered effective for HIV maintenance therapy and that quarterly injections are appropriate for investigation as preexposure prophylaxis. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase 1A1 and is unlikely to be impacted by the cytochrome P450 metabolic pathway. In vitro and in vivo data suggest cabotegravir has a low propensity to cause, or be subject to, significant drug interactions.
  
  
  CONCLUSIONS
  The pharmacologic profile of long-acting cabotegravir supports its continued development for both treatment and prevention of HIV-1 infection.
authors.affiliation: aGlaxoSmithKline, Research Triangle Park, North Carolina bGlaxoSmithKline, Upper Providence, Pennsylvania, USA.
authors.forename: Christine
authors.initials: C
authors.lastname: Trezza
authors.forename: Susan L
authors.initials: SL
authors.lastname: Ford
authors.forename: William
authors.initials: W
authors.lastname: Spreen
authors.forename: Rennan
authors.initials: R
authors.lastname: Pan
authors.forename: Stephen
authors.initials: S
authors.lastname: Piscitelli
mesh_terms: D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D011728:Pyridones / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D054659:Diketopiperazines
chemical_list: D019380:Anti-HIV Agents; D011728:Pyridones; C584914:cabotegravir; D054659:Diketopiperazines