Apricitabine - a novel nucleoside reverse transcriptase inhibitor for the treatment of HIV infection that is refractory to existing drugs

被引:0
作者
Cox, Susan [1 ]
Southby, Justine [1 ]
机构
[1] Avexa Ltd, Richmond, Vic 3121, Australia
关键词
apricitabine; drug resistance; HIV; lamivudine; M184V mutation; nucleoside reverse transcriptase inhibitor (NRTI); IMMUNODEFICIENCY-VIRUS-INFECTION; HEALTHY-VOLUNTEERS; ANTIRETROVIRAL THERAPY; PHARMACOKINETICS; RESISTANCE; COMBINATION; MONOTHERAPY; LAMIVUDINE; SUSCEPTIBILITY; TRIMETHOPRIM;
D O I
10.1517/13543780802641337
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Background: Apricitabine (ATC) is a nucleoside reverse transcriptase inhibitor (NRTI) being developed for the treatment of HIV. ATC has promising antiviral activity, including against HIV-1 containing reverse transcriptase mutations that confer resistance to other NRTIs. Objectives: This paper describes the development of ATC, including its in vitro activity, pharmacokinetics and clinical efficacy and safety. Methods: The current literature on ATC was reviewed. Results/conclusions: ATC is a novel deoxycytidine NRTI with good antiviral activity, both in vitro and in treatment-naive and treatment-experienced HIV-1-infected patients, including those with resistance to other NRTIs. This activity is accompanied by a favourable safety profile and a low propensity to select for resistance. ATC may have a place in the treatment of patients who have failed previous treatment regimens due to the development of NRTI resistance as a replacement for existing drugs.
引用
收藏
页码:199 / 209
页数:11
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