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

Thibaut GeléHélène GougetValérie FurlanPierre-Hadrien BeckerAnne-Marie TaburetOlivier LambotteAurélie Barrail-Tran

Published in: Antimicrobial agents and chemotherapy (2020)

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.

Keyphrases

binding protein
dna binding
human serum albumin
hiv infected patients
antiretroviral therapy
protein protein
mass spectrometry