Bictegravir

V Spagnuolo, A Castagna, A Lazzarin

Research output: Contribution to journalArticle

Abstract

Purpose of review In this review, we will highlight and discuss the recent efficacy and safety data of bictegravir (BIC), a novel second-generation integrase strand transfer inhibitor (INSTI) that has been recently approved, in coformulation with emtricitabine and tenofovir alafenamide (B/F/TAF), for the treatment of HIV-1 infection in antiretroviral naïve subjects and in those with suppressed viremia. Recent findings Preclinical data showed that BIC has a genetic barrier that is higher than that of raltegravir and elvitegravir but is similar to that of dolutegravir (DTG), with retained activity in vitro against isolates containing substitutions associated with resistance against other INSTIs. Its pharmacokinetic interaction risks appear to be low. Results of the phase 3 GS-US-380-1489 and GS-US-380-1490 clinical trials showed that the coformulation B/F/TAF is not inferior to the recommended DTG-containing regimens in naïve subjects. Moreover, B/F/TAF exhibited excellent tolerability, and no treatment-emergent resistance to any component of the coformulation was observed. In addition, preliminary data support switching from DTG and emtricitabine/tenofovir alafenamide or boosted protease inhibitor-containing regimens to B/F/TAF in subjects with undetectable viremia. Summary The coformulation bictegravir/emtricitabine/tenofovir alafenamide is set to become a new option in the management of patients who are antiretroviral naïve and in those with suppressed viremia. © 2018 Wolters Kluwer Health, Inc. All rights reserved.
Original languageEnglish
Pages (from-to)326-333
Number of pages8
JournalCurrent Opinion in HIV and AIDS
Volume13
Issue number4
DOIs
Publication statusPublished - 2018

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Viremia
Integrases
Protease Inhibitors
HIV Infections
HIV-1
Pharmacokinetics
Clinical Trials
Safety
Health
Therapeutics
GS-7340
Emtricitabine
dolutegravir

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Bictegravir. / Spagnuolo, V; Castagna, A; Lazzarin, A.

In: Current Opinion in HIV and AIDS, Vol. 13, No. 4, 2018, p. 326-333.

Research output: Contribution to journalArticle

Spagnuolo, V, Castagna, A & Lazzarin, A 2018, 'Bictegravir', Current Opinion in HIV and AIDS, vol. 13, no. 4, pp. 326-333. https://doi.org/10.1097/COH.0000000000000468
Spagnuolo, V ; Castagna, A ; Lazzarin, A. / Bictegravir. In: Current Opinion in HIV and AIDS. 2018 ; Vol. 13, No. 4. pp. 326-333.
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