Characteristics of Dolutegravir and Bictegravir Plasma Protein Binding: A First Approach for the Study of Pharmacologic Sanctuaries.,Antimicrobial Agents and Chemotherapy

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Characteristics of Dolutegravir and Bictegravir Plasma Protein Binding: A First Approach for the Study of Pharmacologic Sanctuaries.
Antimicrobial Agents and Chemotherapy ( IF 4.1 ) Pub Date : 2020-10-20 , DOI: 10.1128/aac.00895-20
Thibaut Gelé _{1,

2} , Hélène Gouget ₂ , Valérie Furlan ₃ , Pierre-Hadrien Becker ₄ , Anne-Marie Taburet ₂ , Olivier Lambotte _{2,

5,

6} , Aurélie Barrail-Tran _{2,

7,

8}

Affiliation

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.

中文翻译：

Dolutegravir 和 Bictegravir 血浆蛋白结合的特征：药理学研究的第一种方法。

本研究旨在表征体外多替拉韦 (DTG) 和比克替拉韦 (BIC) 的结合。它们优先结合具有两类白蛋白位点的人血清白蛋白 (HSA)。DTG 和 BIC 的人类 α-1-酸性糖蛋白 (HAAG) 结合显示出非典型的非线性结合。HSA 上的低亲和力位点是主要的血浆结合蛋白，表明高蛋白结合率不应损害被动扩散。

更新日期：2020-10-20

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