Dolutegravir maintains a durable effect against HIV replication in tissue culture even after drug washout | Zendy

Nathan Osman | Zendy; Thibault Mésplède | Zendy; Peter K. Quashie | Zendy; Maureen Oliveira | Zendy; Veronica Zanichelli | Zendy; Mark A. Wainberg | Zendy

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Dolutegravir maintains a durable effect against HIV replication in tissue culture even after drug washout

Author(s) -

Nathan Osman,

Thibault Mésplède,

Peter K. Quashie,

Maureen Oliveira,

Veronica Zanichelli,

Mark A. Wainberg

Publication year - 2015

Publication title -

journal of antimicrobial chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.124

H-Index - 194

eISSN - 1460-2091

pISSN - 0305-7453

DOI - 10.1093/jac/dkv176

Subject(s) - dolutegravir , raltegravir , integrase , integrase inhibitor , virology , pharmacology , reverse transcriptase , viral replication , drug , chemistry , medicine , virus , viral load , human immunodeficiency virus (hiv) , antiretroviral therapy , biochemistry , rna , gene

Of the currently approved HIV integrase strand transfer inhibitors (INSTIs), dolutegravir has shown greater efficacy than raltegravir at suppressing HIV-1 replication in treatment-experienced individuals. Biochemical experiments have also shown that dolutegravir has a longer dissociative half-life when bound to HIV integrase than does raltegravir. In order to study the intracellular efficacy of various INSTIs, we asked whether drug removal from INSTI-treated HIV-1-infected cells would result in different times to viral rebound. In addition, we assessed the role of the R263K substitution within the integrase ORF that is associated with low-level resistance to dolutegravir.

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