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

Author:

White Kirsten L.1ORCID,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

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