Open AccessLong Dissociation of Bictegravir from HIV-1 Integrase-DNA Complexes
Author(s) -
Kirsten White,
Nathan Osman,
Ernesto Cuadra-Foy,
Bluma G. Brenner,
Devleena Shivakumar,
Federico Campigotto,
Manuel Tsiang,
Philip Morganelli,
Nikolai Novikov,
Scott E. Lazerwith,
Haolun Jin,
Anita Niedziela-Majka
Publication year - 2021
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.02406-20
Subject(s) - elvitegravir , dolutegravir , integrase , raltegravir , mutant , chemistry , virology , integrase inhibitor , dna , stereochemistry , pharmacology , biology , human immunodeficiency virus (hiv) , viral load , biochemistry , antiretroviral therapy , gene
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.