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

Reference22 articles.

1. Panel on antiretroviral guidelines for adults and adolescents. 2019. Guidelines for the use of antiretroviral agents in adults and adolescents with HIV. Department of Health and Human Services, Washington, DC. https://aidsinfo.nih.gov/contentfiles/lvguidelines/adultandadolescentgl.pdf.

2. European AIDS Clinical Society. 2019. European guidelines for the treatment of HIV-positive adults in Europe. European AIDS Clinical Society, Brussels, Belgium.

3. Antiretroviral Drugs for Treatment and Prevention of HIV Infection in Adults

4. World Health Organization. 2019. WHO recommends dolutegravir as preferred HIV treatment option in all populations. World Health Organization, Geneva, Switzerland.

5. Persistent HIV-1 replication maintains the tissue reservoir during therapy

Cited by 5 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Predicting Factors of Plasma HIV RNA Undetectability after Switching to Co-Formulated Bictegravir, Emtricitabine, and Tenofovir Alafenamide in Experienced HIV-1 Patients: A Multicenter Study;Viruses;2023-08-12

2. Controversies in the Design of Strategies for the Cure of HIV Infection;Pathogens;2023-02-15

3. Pharmacokinetics and tissue distribution of tenofovir, emtricitabine and dolutegravir in mice;Journal of Antimicrobial Chemotherapy;2022-01-12

4. Dolutegravir Impairs Stem Cell-Based 3D Morphogenesis Models in a Manner Dependent on Dose and Timing of Exposure: An Implication for Its Developmental Toxicity;Toxicological Sciences;2021-09-13

5. Cerebrospinal fluid exposure to bictegravir/emtricitabine/tenofovir in HIV-1-infected patients with CNS impairment;Journal of Antimicrobial Chemotherapy;2021-09-11