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

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.