Long Dissociation of Bictegravir from HIV-1 Integrase-DNA Complexes-Reference-Cited by-同舟云学术

Long Dissociation of Bictegravir from HIV-1 Integrase-DNA Complexes

Published:2021-04-19 Issue:5 Volume:65 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

White Kirsten L.¹^ORCID,Osman Nathan²,Cuadra-Foy Ernesto²,Brenner Bluma G.²,Shivakumar Devleena¹,Campigotto Federico¹,Tsiang Manuel¹,Morganelli Philip A.¹,Novikov Nikolai¹,Lazerwith Scott E.¹,Jin Haolun¹,Niedziela-Majka Anita¹

Affiliation:

1. Gilead Sciences, Inc., Foster City, California, USA

2. McGill University AIDS Centre, Lady Davis Institute for Medical Research, Jewish General Hospital and Department of Microbiology and Immunology, McGill University, Montreal, Quebec, Canada

Abstract

The HIV integrase (IN) strand transfer inhibitor (INSTI) bictegravir (BIC) has a long dissociation half-life ( t 1/2 ) from wild-type IN-DNA complexes: BIC 163 h > dolutegravir (DTG) 96 h > raltegravir (RAL) 10 h > elvitegravir (EVG) 3.3 h. In cells, BIC had more durable antiviral activity against wild-type HIV after drug washout than RAL or EVG.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.02406-20

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