Characteristics of Dolutegravir and Bictegravir Plasma Protein Binding: a First Approach for the Study of Pharmacologic Sanctuaries

Antimicrob Agents Chemother. 2020 Oct 20;64(11):e00895-20. doi: 10.1128/AAC.00895-20. Print 2020 Oct 20.

Abstract

This study aimed to characterize in vitro dolutegravir (DTG) and bictegravir (BIC) binding. They had a preferential binding to human serum albumin (HSA) with two classes of albumin sites. Human alpha-1-acid glycoprotein (HAAG) binding of DTG and BIC showed an atypical nonlinear binding. The low-affinity site on HSA, the main plasma binding protein, suggests that the high protein binding rate should not impair passive diffusion.

Keywords: bictegravir; dolutegravir; human alpha-1-acid glycoprotein; human serum albumin; pharmacokinetics; protein binding.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides
  • Binding Sites
  • HIV Infections*
  • HIV-1*
  • Heterocyclic Compounds, 3-Ring
  • Heterocyclic Compounds, 4 or More Rings
  • Humans
  • Oxazines
  • Piperazines
  • Protein Binding
  • Pyridones

Substances

  • Amides
  • Heterocyclic Compounds, 3-Ring
  • Heterocyclic Compounds, 4 or More Rings
  • Oxazines
  • Piperazines
  • Pyridones
  • bictegravir
  • dolutegravir