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

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

This study aimed to characterize 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...

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Veröffentlicht in:Antimicrobial agents and chemotherapy 2020-10, Vol.64 (11)
Hauptverfasser: Gelé, Thibaut, Gouget, Hélène, Furlan, Valérie, Becker, Pierre-Hadrien, Taburet, Anne-Marie, Lambotte, Olivier, Barrail-Tran, Aurélie
Format: Artikel
Sprache:eng
Schlagworte:
Pharmacology
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Zusammenfassung:This study aimed to characterize 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.
ISSN:0066-4804
1098-6596
DOI:10.1128/AAC.00895-20