Characteristics of Dolutegravir and Bictegravir Plasma Protein Binding: a First Approach for the Study of Pharmacologic Sanctuaries-Reference-Cited by-同舟云学术

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

Published:2020-10-20 Issue:11 Volume:64 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Gelé Thibaut¹²,Gouget Hélène²,Furlan Valérie³,Becker Pierre-Hadrien⁴,Taburet Anne-Marie²,Lambotte Olivier²⁵⁶,Barrail-Tran Aurélie¹²⁷^ORCID

Affiliation:

1. AP-HP, Université Paris-Saclay, Hôpital Bicêtre, Service de Pharmacie Clinique, Le Kremlin-Bicêtre, France

2. Université Paris-Saclay, Inserm, CEA, Immunologie des maladies virales, auto-immunes, hématologiques et bactériennes, Fontenay-aux-Roses, France

3. AP-HP, Université Paris-Saclay, Hôpital Bicêtre, Unité Fonctionnelle de Pharmacologie-Toxicologie, Le Kremlin-Bicêtre, France

4. AP-HP, Université Paris-Saclay, Hôpital Bicêtre, Service de Biochimie, Le Kremlin-Bicêtre, France

5. AP-HP, Université Paris-Saclay, Hôpital Bicêtre, Service de Médecine Interne - Immunologie, Le Kremlin-Bicêtre, France

6. Université Paris-Saclay, Faculté de Médecine, Le Kremlin-Bicêtre, France

7. Université Paris-Saclay, Faculté de Pharmacie, Châtenay-Malabry, France

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.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.00895-20

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