Antiviral activity of apricitabine in treatment-experienced HIV-1-infected patients with M184V who are failing combination therapy.
HIV Med
; 12(6): 334-42, 2011 Jul.
Article
em En
| MEDLINE
| ID: mdl-21054750
ABSTRACT
OBJECTIVES:
Apricitabine (ATC) is a novel deoxycytidine analogue nucleoside reverse transcriptase inhibitor (NRTI) with significant antiviral activity in vitro, including activity against HIV-1 with reverse transcriptase mutations that confer resistance to other NRTIs. ATC has shown promising antiviral activity and good tolerability when given as monotherapy for 10 days in treatment-naïve HIV-1-infected patients.METHODS:
In this Phase II randomized, double-blind study, 51 treatment-experienced HIV-1-infected patients with the reverse transcriptase mutation M184V who were failing therapy which included lamivudine (3TC) were randomized to receive twice-daily 600 mg ATC, 800 mg ATC or 150 mg 3TC for 21 days. Patients remained on their existing background regimen until day 21, when background therapy could be optimized according to genotype at screening.RESULTS:
At day 21, the mean change in viral load was -0.71 and -0.90 log(10) HIV-1 RNA copies/mL in the 600 and 800 mg ATC groups, respectively, compared with a -0.03 log(10) change in the 3TC group. In patients with at least three thymidine analogue mutations (TAMs) at baseline, greater reductions in viral load were observed in the 800 mg ATC group at day 21 than in the 600 mg ATC group. Few genotypic changes were detected at day 21 [two patients (600 mg ATC) lost and three patients (800 mg ATC) gained a TAM] and all patients with detectable virus retained the M184V mutation. The safety profiles of the two ATC doses were similar to that of 3TC.CONCLUSIONS:
Over the 21-day treatment period, ATC showed promising antiviral activity and was well tolerated in treatment-experienced patients with M184V, with or without additional TAMs.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Infecções por HIV
/
HIV-1
/
Fármacos Anti-HIV
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Farmacorresistência Viral
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Desoxicitidina
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Transcriptase Reversa do HIV
Tipo de estudo:
Clinical_trials
Limite:
Adult
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Female
/
Humans
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Male
/
Middle aged
País/Região como assunto:
America do sul
/
Argentina
/
Oceania
Idioma:
En
Revista:
HIV Med
Assunto da revista:
SINDROME DA IMUNODEFICIENCIA ADQUIRIDA (AIDS)
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Argentina