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

Thibaut Gelé | Zendy; Hélène Gouget | Zendy; Valérie Furlan | Zendy; PierreHadrien Becker | Zendy; AnneMarie Taburet | Zendy; Olivier Lambotte | Zendy; Aurélie BarrailTran | Zendy

Open Access

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

Author(s) -

Thibaut Gelé,

Hélène Gouget,

Valérie Furlan,

PierreHadrien Becker,

AnneMarie Taburet,

Olivier Lambotte,

Aurélie BarrailTran

Publication year - 2020

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.00895-20

Subject(s) - dolutegravir , human serum albumin , plasma protein binding , chemistry , glycoprotein , in vitro , binding site , albumin , pharmacokinetics , serum albumin , in vivo , blood proteins , biochemistry , pharmacology , virology , biology , human immunodeficiency virus (hiv) , microbiology and biotechnology , viral load , antiretroviral therapy

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.

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