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


OBJECTIVE
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.


CONCLUSIONS
ATC is a novel deoxycytidine NRTI with good antiviral activity, both in vitro and in treatment-naïve 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.
Cox
Susan
S
Avexa Ltd, 576 Swan Street, Richmond, Victoria 3121, Australia. scox@avexa.com.au
Southby
Justine
J
D000818:Animals; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D003841:Deoxycytidine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D018894:Reverse Transcriptase Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*
D019380:Anti-HIV Agents; D018894:Reverse Transcriptase Inhibitors; D003841:Deoxycytidine; C508042:apricitabine